Application form Research Project Proposal

KINGDOM OF SAUDI ARABIA
National Science, Technology and Innovation Plan
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Sohda, T, Momose, Y, Meguro, K, Kawamatsu, Y, Sugiyama, Y, Ikeda, H, Arzneim-Forsch, 1990, 40, 37.

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CNPSTI RE-D1: APPLICATION FORM - RESEARCH PROJECT PROPOSAL
ITEM DESCRIPTION
PLAN
The First Five - Year Science, Technology and Innovation Plan
PROGRAM Strategic Technologies
SUB-PROGRAM /
TECHNOLOGY AREA1 Biotechnology
TRACK Medical and Health Research
SUB-TRACK Diabetics
PROJECT TITLE
(ENGLISH)
COMPUTRER BASED MOLECULAR MODELING, DRUG DESIGN,
SYNTHESIS AND ANTIDIABETIC EVALUATION OF NEW
POTENTIAL ANTIDIABETIC AGENTS
PROJECT TITLE
(ARABIC)
‫تصميم‬‫وتقييم‬ ‫وتشييد‬ ‫الحبسوبية‬ ‫الجزيئية‬ ‫النمذجة‬ ‫على‬ ‫مبنى‬ ‫دوائى‬.
PRINCIPAL
INVESTIGATOR
(ENGLISH)
Dr. Noman Shah
P. INVESTIGATOR
(ARABIC )
‫د‬.‫نعمبن‬
INSTITUTION Umm Al-Qura University
FOR OFFICIAL USE ONLY
SUBMITTED FOR THE
DEADLINE OF
30th
of MARCH 30th
of SEPTEMBER
DATE RECIEVED
PROJECT CODE
1
Applicants are advised to visit the following link for more information about technology areas, tracks and sub-
tracks http://www.kacst.edu.sa/en/research/Pages/default.aspx.

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CNPSTI RE -D1-1: PROJECT INFORMATION
ITEM DESCRIPTION
PROJECT TITLE
COMPUTRER BASED MOLECULAR MODELING, DRUG DESIGN,
SYNTHESIS AND ANTIDIABETIC EVALUATION OF NEW POTENTIAL
ANTIDIABETIC MEDICINE
TECHNOLOGY
AREA
Biotechnology
TRACK Medical and Health Research
SUB-TRACK Diabetics
PROJECT TYPE
(BASIC, APPLIED,
DEVELOPMENT)
Development
PROPOSED TOTAL
BUDGET (MAX.
TWO MILLIONS SR
)
Two millions
Saudi Riyals
ESTIMATED
DURATION ( MAX.
24 MONTHS)
24
Months
PROPOSED
STARTING DATE
January 2013
Month / Year
SENIOR PERSONNEL
PROJECT TEAM
No. Name Role
Area of
Specialization
1 Dr. Noman Shah P I Organic-Medicinal
Chemistry
2 Dr. Hassan Wadood CO- I Organic-Medicinal
Chemistry
3 Dr. Ahmed CO- I Biochemistry
OTHER PERSONNEL
6 Postdoctoral Associate
7 Ph.D. Student
8 Will be recruited M.S. Student
9 Will be recruited Technician
10 Will be recruited Project Manager
11 Will be recruited Other: Research Assistants
CONSULTANT*
12 Pr. Bill Gates Country: US
13 Pr. Stephon Hawking Country: US
*NOTE: a letter of approval from the consultant/s should be attached with the
application.
KEYWORDS
(MAX. 4)
1. Antidiabetic Type 2 agents 2.
3. 4.
IS THIS PROJECT
BEING SUBMITTED
TO ANY OTHER
FUNDING
INSTITUTION?
No
Yes, please specify
1.
2.
3.

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- Summary (English):
Type 2 diabetes is a common chronic disease, characterized by a progressive rise in blood glucose
and worsening insulin resistance that is a major cause of morbidity and mortality. Currently, it is
estimated that more than 16 million people suffering from diabetes live in the Eastern
Mediterranean Region. This staggering figure is expected to extend to almost 43 million by the
year 2025. In case no imperative action is undertaken, the proportion of people living with
diabetes is predicted to jump from 366 million in 2011 to 552 million by 2030, according to new
estimates. This corresponds to almost three new cases every ten seconds or about ten million per
year. Nearly 183 million people are unconscious that they have diabetes according to
International Diabetes Federation (IDF) estimates.
- Summary (Arabic):
‫تاندو‬ ‫انجهىجىس‬ ‫إرتفاع‬ ‫يزض‬(ٌ‫انسكز‬)‫انُىع‬ ٍ‫ي‬2‫عوا‬ ٍ‫يوشي‬ ‫يوزض‬ ‫هوى‬‫تود‬ ‫تارتفواع‬ ‫َتًُوش‬‫يسوتىي‬ ٍ‫فو‬ ٍ‫رَج‬
‫وانىفاج‬ ‫نهًزض‬ ٍ‫ُس‬ ‫ر‬ ‫سثة‬ ‫هى‬ ٌ‫انذ‬ ٍُ‫االَسىن‬ ‫يقاويح‬ ‫وتفاقى‬ ‫اندو‬ ٍ‫ف‬ ‫انسكز‬.ٌ‫ا‬ ً‫انو‬ ‫ا‬‫ا‬‫اانُو‬ ‫انتقودَزاخ‬ ‫وتشُز‬‫أكثوز‬
ٍ‫ي‬61ٌ‫َعُشى‬ ٌ‫انسكز‬ ٍ‫ي‬ ٌ‫َعاَى‬ ‫عخص‬ ٌ‫يهُى‬‫يُففوح‬ ٍ‫فو‬‫اووسو‬ ‫انشوز‬.‫انًوذهم‬ ‫انوزقى‬ ‫وهوذا‬ٌ‫أ‬ ‫انًتىقو‬ ٍ‫يو‬
‫َزتف‬ً‫إن‬ٍ‫ي‬ ‫َقزب‬ ‫يا‬34‫تحهى‬ ‫َسًح‬ ٌ‫يهُى‬‫ل‬‫عاو‬2222.‫عدو‬ ‫اال‬ ٍ‫وف‬‫إجوزا‬ ٌ‫أ‬ ‫اتخوا‬‫تقفوش‬ ٌ‫أ‬ ‫انًتىقو‬ ٍ‫فًو‬
ٌ‫َعُشى‬ ٍَ‫انذ‬ ٌ‫انسكا‬ ‫َسثح‬‫ي‬ٌ‫انسوكز‬ ‫يوزض‬ٍ‫يو‬411ٌ‫يهُوى‬ٍ‫فو‬2266ٍ‫اتو‬222ٌ‫يهُوى‬‫عواو‬ ‫تحهوىل‬2242
‫نتقدَزاخ‬ ‫وفقا‬‫جدَدج‬.‫ي‬ ‫َتىافق‬ ‫وهذا‬‫ثالث‬ ٍ‫ي‬ ‫َقزب‬ ‫يا‬‫جدَدج‬ ‫إصاتح‬ ‫ااالخ‬‫كوم‬ٌ‫ثوىا‬ ‫عشوز‬‫أو‬ٍُ‫يالَو‬ ‫عشوزج‬ ‫َحوى‬
‫سُىَا‬.‫هُاك‬ ٌ‫وأ‬ٍ‫ي‬ ‫َقزب‬ ‫يا‬684ٌ‫َعهًى‬ ‫ال‬ ‫َسًح‬ ٌ‫يهُى‬‫ندَهى‬ ٌ‫تأ‬ٌ‫انسكز‬ ‫يزض‬‫اال‬ ‫نتقدَزاخ‬ ‫وفقا‬ٍ‫انفودران‬ ‫تحا‬
ٌ‫نهسكز‬ ٍ‫اندون‬(IDF).
1. INTRODUCTION
Diabetes is one of the oldest known diseases. An Egyptian manuscript from 1550 BCE
asserts the sentence “the passing of too much urine” [1]. The great Indian physician
Sushruta (6th century BCE) differentiated the disease and classified it as Medhumeha [2].
The ancient Indians investigated for diabetes by contemplating if ants were tempted by a
person's urine, and designate the ailment "sweet urine disease" (Madhumeha). Presently,
diabetes is the world’s restless propagating chronic disease.
A UN Resolution 61/225 was voted on December 2006 recognizing diabetes as a major
health crisis encountered by all nations of the world. The Resolution baptized 14
November each year as the United Nations World Diabetes. The world Health
Organization recently warned that type II diabetes has become worldly pandemic [3]. In

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case no imperative action is taken, the proportion of people living with diabetes is
predicted to increment from 366 million in 2011 to 552 million by 2030, according to
new estimates. This corresponds to almost three new cases every ten seconds or about
ten million per year. Nearly 183 million people are unconscious that they have diabetes
according to International Diabetes Federation (IDF) estimates.
Diabetes mellitus is a chronic metabolic disease that originates when a person has high
blood sugar, either because the pancreatic cells do not produce enough insulin (because
the pancreas does not longer produce or not produce insulin in sufficient amounts), or
when the body cannot respond effectively to the insulin that is produced. Insulin is a
hormone generated by the pancreas that grants the uptake of glucose from the blood by
cells and converts it into energy.
Consequently, glucose present in food and consumed by diabetic people cannot be
converted into energy. Instead of being turned into energy the glucose stays in the blood.
Glucose gets entrapped in the bloodstream and spills into the urine when the muscles and
organs are starved for energy. For this reason blood glucose levels are higher in diabetic
people. The blood’s high sugar content damages the cells of many organs it flows
through. If the levels are very high, they can cause coma or death.
Defection in producing insulin, or of insulin to act properly, or both, generates increased
glucose (sugar) levels in the blood (hyperglycaemia). This is accompanied by long-term
damage to the body and deterioration of various organs and tissues.
Over time, diabetes engenders annihilation or invalidation throughout the body. It
disturbs the blood vessels and the heart, multiplying the risk of heart disease or stroke by
up to four times. Such complications are lethal to two-thirds of people who have diabetes.
By the time they are diagnosed, many people have already deteriorated the blood vessels
in their eyes and 90 percent of them have deterioration after 15 years with the illness; As
a result, almost 40,000 cases of blindness are engendered each year, making diabetes one
of the leading cause of adult-onset blindness [4]. When time passes, the high levels of
sugar in the blood damage the millions of tiny filtering units within each kidney. This
eventually leads to a major complication: kidney failure [5]. Amputations eventuate 10
times more frequently in people with diabetes than in sane people, and the illness also
invalidates the immune system, making people more receptive to serious infection.

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There are three main types of diabetes. First, type 1 diabetes accounts for about 10% of
all diabetes. It results from autoimmune mediated destruction of insulin-secreting β-cells
of the pancreas [6] and solicits daily insulin administration, also referred to as insulin-
dependent diabetes mellitus, IDDM for short, and juvenile diabetes.). Type 1 diabetes
amass alarming chemical substances in their blood from the burning of fat unless
controlled with daily injections of insulin. This can lead to a situation known as
ketoacidosis. This situation is potentially life threatening if not treated. Second, type 2, or
the most common form of diabetes that affects 85-90% of all diabetic people [7]. It is
mainly generated by insulin resistance, a condition in which cells fail to use insulin
properly, formerly referred to as non-insulin-dependent diabetes mellitus, NIDDM for
short, and adult-onset diabetes progressed to require injected insulin. This can develop to
type 1, or latent autoimmune diabetes of adults (or LADA or "type 1.5" diabetes) [8].
Type 2 diabetes can remain undetected for many years and the diagnosis is often made
from combined complications or fortuitously through an abnormal blood or urine glucose
analysis. It is often, but not always, in relation with obesity, which itself can cause insulin
resistance and induce elevated blood glucose levels.
Third gestational diabetes (GDM) [9] is another type of diabetes when pregnant women,
who have never had diabetes before, are subjected to high blood glucose levels during
pregnancy which may lead to the development of type 2 DM. It is associated with
complications in the period immediately before and after birth. Other causes of diabetes
include congenital, which is due to genetic defects of insulin secretion, cystic fibrosis-
related, steroid induced by high doses of glucocorticoids, and several forms of
monogenic.
Diabetes without adequate treatments can cause numerous complications. Disastrous
complications comprise diabetic ketoacidosis, or nonketotic hyperosmolar coma. Grave
long-term complications include cardiovascular disease, chronic renal failure, retinal
damage. According to estimations of 2010, there are 285 million people diabetes with
type 2 representing about 90% of the cases. [10]
Other types of diabetes as pre-diabetes illustrate a condition that takes place when a
person's blood glucose levels are more elevated than normal but not high enough for a
diagnosis of type 2 diabetes. Many people destined to develop type 2 diabetes spend

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many years in a state of pre-diabetes which has been designated by "largest healthcare
epidemic." [11].
The cause of diabetes relies on the type. Type 1 diabetes is partly inherited and then
triggered by certain infections, with some confirmation implicating Coxsackie B4 virus
[12]. Type 2 diabetes is due primarily to lifestyle factors and genetics [13]. There are
other causes of diabetes [14] including genetic defects of β-cell Function, genetic defects
in insulin processing or insulin action, exocrine pancreatic defects, infections or due to
some drugs.
While there is not yet a cure for diabetes, it can be controlled. The main goal of all
treatment is to control blood sugar levels, but the method varies depending on the type of
diabetes a person has.
The sustained, high plasma glucose levels results in a gradual progression of a number of
complications, including neuropathy, nephropathy, retinopathy, and premature
athereosclerosis [15]. Proper glycemic control is, most likely, necessary for the control of
diabetic complications in type 2 diabetes [16]. However, current therapies to reduce
plasma glucose levels have inherent problems including compliance, ineffectiveness, and
occurrence of hypoglycemic episodes with insulin and sulphonyl urea. Accordingly, there
is a need for more effective, orally administered agents, particularly ones that act as
insulin sensitizing antidiabetic agents in peripheral tissue in order to normalize both
glucose and insulin levels [17].
Therefore, it is crucial to control a convenient blood glucose level especially throughout
the primal phase of the disease [18]. The most commonly utilized oral hypoglycemics for
the disease are sulfonylureas. However these drugs produce severe hypoglycemia and
display primary or secondary failure, which is probably associated with their
particularities as insulin secretagogues [19]. Therefore, the need for nonsulfonylurea class
of hypoglycemic or insulin sensitizers, that does not raise insulin secretion but intensify
the action of insulin is urged [20].

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2. PROJECT OBJECTIVES
Three main project objectives are stated below:
1- Design, docking and synthesis of novel diabetic medicine.
2- Pharmacological activity evaluation of the medicine.
3- Search for more potent molecules to be used in clinical development for diabetic
treatment
3. LITERATURE REVIEW
Diabetes mellitus type 2, NIDDM, is a chronic and progressive metabolic disorder of
carbohydrate and lipid metabolism and accounts for the remaining 90 % of diabetes
mellitus [23]. Type 2 diabetes is a metabolic disorder caused, in part, by insulin
resistance in peripheral tissues and/or impaired insulin secretion by the pancreas. In turn,
glucose metabolism is decreased in muscle and thus, fat and glucose output by liver rises.
The resultant high blood glucose level usually generates many dramatic complications
[3]. At the molecular level, the mechanism of insulin resistance in type II diabetes
appears to implicate defects in post-receptor signal transduction [24]. The sustained, high
plasma glucose levels results in a gradual progression of a number of complications,
including neuropathy, nephropathy, retinopathy, and premature athereosclerosis [25].
Therefore, proper glycemic control is, most likely, necessary for the control of diabetic
complications in type 2 diabetes during the early stages of the disease [18, 26]. The
treatment generally prescribed for type 2 diabetes has been a combination of diet,
exercise, and oral hypoglycemic agents such as sulfonylureas and biguanides.
Sulfonylureas, which are insulin secretagogues, stimulate insulin secretion from
pancreatic -cells and are often recognized to generate severe hypoglycemia [27] and
weight gain [28]. In addition, both primary and secondary treatment failure rates with
sulfonylureas are high, causing complications [29]. Therefore, drugs that inverse the
insulin resistance without activating insulin release from cells achieve a major medical

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need in the therapy of type II diabetes and hence the potentials to decrease long-term
complications of NIDDM. However, current therapies to reduce plasma glucose levels
have inherent problems including compliance, ineffectiveness, and occurrence of
hypoglycemic episodes with insulin and sulphonyl urea.

Page 10 of 25
1. DESCRIPTION OF THE PROPOSED WORK
4.1 Approach, tasks and phases:
Form RE -D1-2:APPROACH UTILIZED FOR ACHIEVING OBJECTIVES
OBJECTIVE APPROACH OF ACHIEVING THE OBJECTIVE
1
Design, Docking
and Synthesis of
novel medicine
Here, chemistry will be used to accomplish efficiently the synthesis of intermediates and
final products, and the structural identification of compounds through spectroscopic
analysis.
2
Pharmacological
activity evaluation of
the medicine
The second objective will be achieved by providing an in-depth pre-clinical assessment of
the novel medicine.
3
Search for more
potent medicine
The structure-activity relationship will be established for the most potent medicine. This
study will provide insight into the observed diabetic effects and supply evidence for
further development of these compounds for antidiabetic therapy.
Form RE -D1-3: MAPPING OF PHASES AND TASKS TO ACHIEVE OBJECTIVES
OBJECTIVES PHASES TASKS
1
Design, Docking and
Synthesis of novel
medicine
Phase 1: Preparation for launching
the research project
Phase 2: Molecular modelling
docking study)
Phase 3: Synthesis, purification and
characterisation of medicine.
1. Setting-up research lab and purchasing
chemicals, reagents, solvents, glassware, gas
supplies, instruments.
2. Literature review.
1. Construct data base of the 3D structures of
medicine.
2. Molecular modelling fitting studies
between generate common feature.
1. Investigating, developing, performing and
monitoring chemical reactions.
2. Optimization the yield and reaction time
using the microwave irradiation instrument.
3. Training students/technicians
4. Evaluation and discussion of the results
and writing reports.
2
Pharmacological activity
evaluation of the medicine
Phase 4: Preparing materials and
equipment
Acquiring instruments.
1. Tissue culture medicines from insulin
action studies and lipid accumulation.

Page 11 of 25
Phase 5: Assay development and
optimisation
Phase 6: Biological evaluation
2. RNA extraction
1. Evaluation of compound.
2. Evaluation of compounds for their effects
on covalent modification.
3. Evaluation of compounds in cytotoxicity.
4. Evaluation and discussion of the results;
final reporting.
3
Search for more
potent medicine to be used
in clinical development for
diabetic treatment
Phase 7: Preparation of libraries of
medicine for further bio- testing.
1. Acquiring materials.
2. Repeat tasks from objectives 1 and.
3. In vivo evaluation
4. - Writing and submission of a patent
- Writing papers in reputable peer reviewed
journals.
- Participation in conferences to present the
findings
- Write the progress and final report
4.2 Research methodology
Methodology is the systematic, theoretical analysis of the methods applied to a field of study, or
the theoretical analysis of the body of methods and principles associated with a branch of
knowledge. It, typically, encompasses concepts such as paradigm, theoretical model, phases and
quantitative or qualitative techniques.[1]
A Methodology does not set out to provide solutions but offers the theoretical underpinning for
understanding which method, set of methods or so called “best practices” can be applied to a
specific case.

Page 12 of 25
It has been defined also as follows:
1."the analysis of the principles of methods, rules, and postulates employed by a discipline";[2]
2."the systematic study of methods that are, can be, or have been applied within a discipline";[2]
3."the study or description of methods".[3]
In recent years, the word methodology has become a "pretentious substitute for the word method".[4]
Many recent uses of the word methodology mistakenly treat it a synonym for method or body of methods.
Doing this shifts it away from its true epistemological meaning and reduces it to being the procedure
itself, the set of tools or the instruments that should have been its outcome. A methodology is the design
process for carrying out research or the development of a procedure and is not in itself an instrument for
doing those things. Using it as a synonym for method or set of methods, leads to misinterpretation and
undermines the proper analysis that should go into designing research. Generally for any research study
both primary and secondary research are done which facilitates in the better understanding of the entire
study. Primary research helps garner relevant and adequate data of the current state of affairs pertaining to
any subject and provides an insight into the exact nature of the problem. Owing to the broad and complex
nature of this research topic which would require delving into many aspects of the study including an
ethnographic study which would in turn include a longitudinal time horizon which cannot be possibly
encompassed within this research as it goes well beyond the possibilities of an academic research.The use
of pre-packaged, 'ready-to-go' methods do not constitute a methodology and are no substitute for the
necessary scientific search for the most appropriate method to approach a problem".[
4.3 Management Plan
The Form RE -D1-4: ROLE AND INVOLVEMENT DURATION OF PROJECT TEAM
TEAM MEMBERS ROLE
DURATION
(MONTHS)
SENIOR PERSONNEL:
Dr. Noman Shah -Supervising and managing the project.
-Coordination of the progress work between the two sites
-Responsible for administrative, reporting and purchasing
requirements.
-Conducting all experiments to test the feasibility.
-Optimizing yield and reaction time with microwave instrument.
-Training staff in synthesis, purification, spectroscopic analysis
and microwave instrument.
-Following-up the practical work of staff
-Interpretation of results
-Communicate findings through reports, publications and
presentation in international congress.
24
Dr. Hassan Wadood -Designing, docking and performing medicine.
-Conducting all experiments to test the feasibility of the
approach.
20

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-Optimizing yield and reaction time with microwave instrument.
-Training staff in synthesis, purification, spectroscopic analysis
and microwave instrument.
-Following-up the practical work of staff
-Interpretation of results.
-Writing reports to PI.
-Contribution in writing and submitting paper for publication
Dr. Ahmed -Setting up of the cell culture laboratory
-Acquiring materials for cell culture, RNA analysis, insulin
action and bioassays.
--Analysing and reporting of results.
-Training students and staff in bio-testing.
-Writing of reports,
-Contribution in writing and submitting paper for publication.
20
OTHER PERSONNEL:
Project Manager - Conducting quotations, purchasing, following up materials
-Performing and following up all administrative work
-Budgeting
- Ticketing
20
Research Assistant
M.S. Student
Technicians
-Conducting chemical reactions, purification
-Performing the technical task in the lab, operation instruments
and characterization of products
-Conducting biological assays
-Reporting and evaluating results
-Writing first draft report
20
7
14
CONSULTANT:
Pr. Bill Gates Providing technical assistance for conducting bio-tests 2
Pr. Stephen Hawking Providing technical assistance for molecular modelling 2

Page 14 of 25

Page 15 of 25
FormRE- D1-5: WORK PLAN AND TIME SCHEDUAL
242322212019181716151413121110987654321
INVOLVEMENT
DURATION
PHASES & TASKS
ParticipationPHASE I
xxNSTask 1.1: Setting-up research lab and
purchasing chemicals, reagents,
solvents, glassware, gas supplies,
instruments.
xxxxxxxNS, HWTask 1.2: Literature review
PHASE 2
xxxxxxxNS, HW
Task 2.1: Construct data
PHASE 3
xxxxxxxxxxxxxxxxxxxNS, HWTask 3.1: Investigating, developing,
performing and monitoring chemical
reactions.
xxxxxxxxxxxxxxxxNS, HWTask 3.2: Optimization the yield and
reaction time using the microwave
irradiation instrument.
xxxxxxxxxxxxxxxxxxxNS, HWTask 3.3: Employing crystallisation,
distillation and separation
chromatographic techniques.
xxxNS, HW, AMTask 3.5: Training
students/technicians
xxxTask 3.6: Evaluation and discussion
of the results and writing reports
PHASE 4
Noman Shah (NS), Hassan Wadood (HW), Ahmad (AM)

Page 16 of 25
4.4 Project Deliverables:
FormRE- D1-6: RELATIONSHIP TO STRATEGIC FRAMEWORK2
PROJECT
EXPECTED
OUTCOMES
STRATEGIC TECHNOLOGY PROGRAM GOALS PROJECT
OBJECTIVES
ACHIEVED
GOAL 1 GOAL 2 GOAL3
Development of
novel
MEDICINE
Develop
undergraduate and
vocation training
programs and on-the-
job training
opportunities to create
a pool of technically
skilled support staff
and technicians who
are committed to good
laboratories practices
Increase national
scientific discovery
and productivity
through
dissemination of
findings via
publications in peer-
reviewed and
reputed journals
1
Design docking and
synthesis of novel
medicine
Identification of
leads as
potential potent
medicine
Develop postgraduate
training to create a
locally competent
talent capable of
conducting novel
medical and health
sciences research
Develop
mechanism for
private fund-
raising for
research through
industry
partnerships
Establishing national
mechanisms for
capturing intellectual
properties and
accelerating their
commercialization
2
Pharmacological
activity evaluation
of the medicine
Identify
potential drug
candidates for
diabetic therapy
Prepare competitive
recruitment package
in order to attract,
retain and nurture
first-class researchers
Establish
infrastructure to
facilitate and
expedite
acquisition of
resources
Develop mechanism
to encourage
research
partnerships and
create new industries
&
Promote
performance of basic
and translational
interdisciplinary
research for better
understanding and
treatment of diseases
pertinent to the KSA
3
Search for more
potent medicine

Page 17 of 25
The three expected outcomes of this research project allow the achievement of many goals of the
Strategic Technology Program Goals (Strategic Priorities for Medical and Health program in Saudi
Arabia) described in the form RE-D-1-6. In this section we develop the relationships of the
outcomes of the project to the objectives and the linkages with the related goals.
OUTCOME 1 (Development of novel medicine)) will be the achievement outcome of the first
objective Design, docking and synthesis of novel medicine
GOAL 1: Develop undergraduate and vocation training programs and on-the-job training
opportunities to create a pool of technically skilled support staff and technicians who are
committed to good laboratories practices
GOAL 3: Increase national scientific discovery and productivity through dissemination of
findings via publications in peer-reviewed and reputed journals
OUTCOME 2 (Identification of leads as potential potent medicine) will be the achievement of the
second objective: Pharmacological activity evaluation of the medicine systems.
GOAL 1: Develop postgraduate training to create a locally competent talent capable of
conducting novel medical and health sciences research
GOAL 2: Develop mechanism for private fund-raising for research through industry
partnerships
GOAL 3: Establishing national mechanisms for capturing intellectual properties and
accelerating their commercialization
OUTCOME 3 (Identify potential drug candidates for diabetic therapy) will be the achievement of
the third objective: Search for more potent molecules to be used in clinical development for
diabetic treatment.
GOAL 1: Prepare competitive recruitment package in order to attract, retain and nurture
first-class researchers
GOAL 2: Establish infrastructure to facilitate and expedite acquisition of resources
GOAL 3: Develop mechanism to encourage research partnerships and create new industries
&: Promote performance of basic and translational interdisciplinary research for better
understanding and treatment of diseases pertinent to the KSA

Page 18 of 25
5. VALUE TO THE KINGDOM
This research project will be conducted in the field of medicinal chemistry, at the cutting edge of
diabetes research. The focus on development of new synthetic drug compounds ended up in
amalgamating many other disciplines such as biochemistry, pharmacology, molecular biology and
medicine into medicinal chemistry.
Umm Al-Qura University, ranked as one of the foremost biotechnology universities in KSA, is
committed to providing an exceptional platform in which both researchers and students can excel,
and achieve their professional and personal goals.
Accordingly, this research project creates foundations for university-based research and its valuable
beneficial impact on different levels namely: academia, industry society and economy in KSA.
At the academic level, the project will:
- provide a multidisciplinary environment that encourages creativity and scientific investment in the
field of pharmaceutical technology; working in teams is essential for drug discovery because many
different aspects of a molecule (preparation, isolation, characterization, biological and
pharmacological studies..) must be identified for a clinical studies candidate.
- exploit the research capacity in the Faculty of Pharmacy and the Faculty of Medicine at Umm Al-
Qura university for the aim of creating novel knowledge which can be exploited by supporting
continuous educational improvement and implementation of new undergraduate and graduate
(Master, Ph.D.) curricula.
- encourage inter-universities interactions (King Saud University KSA, Newcastle University UK) to
generate constructive alliances and synergy between local and/or international researchers and to
build affiliations and partnerships with renowned international universities.
- offer pharmaceutical industry focused programs as specialized programs to form graduates for
career focus tracks in real-world pharmaceutical industry.
- train Saudi students to master a wide range of synthetic methods, analytical techniques, medicinal
chemistry skills and biological testing methods. Students are placed in a competitive position as they
are developed, for a challenging and rewarding professional career in chemical and pharmaceutical
research to design, synthesize and identify chemical leads for drug discovery.
- facilitate placements of Saudi graduates in pharmaceutical and chemical industry sectors as well as
laboratories, research centers, universities and institutes of technology since they may be involved in
pharmaceutical research, biological/therapeutic evaluation of medicinal products and
production/manufacture, quality control, quality assurance and process development.
- offer short courses, workshops, and support seminars for undergraduates and graduates students.

Page 19 of 25
- generate conferences which can provide a forum for local and international researchers, students,
entrepreneurs and industry leaders to deliberate innovation in diabetes therapy.
- use the current research center which embodies a highly integrated basic and translational
multidisciplinary environment for better understanding and annihilating of diseases pertinent to the
KSA. The key to success is converting the latest scientific achievements generated by research into
innovative therapeutic treatments able to significantly improve the cure rates for cancer with
simultaneous elimination of side effects. The center will extend the spectrum of research interests to
cover other areas focused on development of cardiovascular, anticancer and other therapies, with a
particular emphasis on understanding the individual's quality of life of the Saudi society.
At the industrial, social and economic levels, the interest of developing new local anitdiabetic agents
will:
- achieve the effective transfer and implementation of research results and technology to medical local
institutions in the private and public sectors in KSA and raises their ability to take advantage of the
scientific knowledge generated by academia.
- bridge the gap between cutting edge academic research and industrial development of diabetes
therapeutics and diagnostics.
- maximize diabetic patient cost-benefit from publicly funded research in an attempt to tackle
concerns about care costs.
- ensure the foundations of a modern economy and a modern society in KSA which rely on advanced
technology.
- deliver better health incomes to diabetic patients by ameliorating their quality and length of life.
- improve the access to higher clinical therapeutic quality for Saudi diabetic patients concomitant with
the decrease of the costs and deficits of the national health insurance of KSA in the care of patients
with chronic diseases.
Consequently, this project could pave the way for advancements and betterments in many strategic
sectors of the Kingdom.

Page 20 of 25
6. PROJECT EXECUTION
In preamble, we found it necessary to introduce the main researchers of the multi-disciplinary group
and the consultancy team who will be involved in the proper execution of this research project.
6.1 Current Resources:
This research proposal has not been submitted to any other sources of funding.
The physical location of the research at the Faculty of Pharmacy is in dedicated areas for drug discovery and
development specifically designated for that purpose. The research center, approx. 80 square meters, is
located in the basement of the building of the faculty. It is a modern facility providing all infrastructures
essential for general lab operation, including vacuum, compressed gas. The space accommodates 4 fume
hoods and 10 benches.
The equipments available at Umm Al-Qura University in the Faculty of Pharmacy that will be helpful for
the realization of the project are:
1- Infra-Red Spectroscopy (Nicolet 200 from Thermo Company) which will be used for examining the
functional group present or absent in the compound.
2- Discovery Studio 3.1 software which will be used to perform molecular modeling of compounds
The equipment’s available at Umm Al-Qura University in the Faculty of Medicine that will be helpful for
the realization of the project are:
1- Safety cabinet and CO2 incubator will be used for tissue culture of tumor cell lines.
2- UV-Visible spectroscopy from Thermo which will be used for studying the DNA binding and for
determining the growth inhibition concentration of molecules using MTT assay.
The science library at the Umm Al-Qura University provides an extensive range of chemistry and biology
reference texts and major journals. The library also subscribes to a data base in chemistry (Sci-Finder) and to
the online journals database Science Direct and ACS which provide access to a worldwide range of
scientific research publications.
6.2 Requested Resources:
1] Human resources:

Page 21 of 25
The proposed project will be conducted in two sites of Umm Al-Qura University (Mecca): College of
Pharmacy and College of Medicine.
The research team involved in this project will consist of researchers with different fields of expertise: two
medicinal chemists and a biochemist (see in preamble of this section).
Two research assistants (part-time), one MS student and two technicians will be hired for the project. Many
undergraduate students enrolled in pharmacy and chemistry curriculum will have the opportunity to be
engaged in this research project at the chemistry-biology interface. They will perform the experiments,
measurements, biological tests, and result analyses.
A project manager will be recruited to facilitate the administrative work for the realization of the project.
2] Equipments, materials and consumables:
Taking into account the nature and complexity of the research proposal, the following resources are
necessary for the proper execution of the project:
Year 1 Year 2
Supplies:
Chemicals, Reagents for synthetic chemistry 60000 30000
Solvents, Chromatography supplies,
NMR consumables and amalysis
60000 60000
Elemental analysis for C, H and N 40000 40000
consumables 20000 20000
Service and maintenance of NMR, GC/MS 20000 30000
Tissue culture supplies 100000 20000
Chemicals, reagents, supplies for cell-free experiments 50000 30000
Mice 80000
consumables 30000 30000
Supplies Total: 460000 260000
Instrument
CEM Discover focused microwave synthesis instrument 210000
water bath, rotavapor 65000
Total Direct Costs: 735000 260000
SEE INSTRUCTIONS
BEFORE COMPLETING FORM RE- D1-7: PROPOSED BUDGET (in Saudi Riyals)
PROJECT TITLE: COMPUTRER BASED MOLECULAR MODELING, DRUG DESIGN, SYNTHESIS AND
ANTIDIABETIC EVALUATION OF CERTAIN NEW THIAZOLIDINEDIONE (TZD)
ANALOGUES FOR DEVELOPING NEW POTENTIAL ANTIDIABETIC TYPE 2
AGENTS
DURATION: (24) MONTHS
ITEM: CATEGORY NO. COMPENSATION
FIRST YEAR SECOND YEAR
TOTAL
Months Budget Months Budget
Manpower
Consultants 2 10000 2 40000 2 40000 80000
Principal investigator 1 6000 12 72000 12 72000 144000
Co-investigator 2 5000 10 100000 10 100000 200000

Page 22 of 25
Co-investigator
Research assistants
(MS holder)
2 5000 10 100000 10 100000 200000
PhD students
Ms students 1 6000 7 42000 42000
Undergrads students
Project manager 1 3000 10 30000 10 30000 60000
Technicians 2 2000 7 28000 7 28000 56000
Secretarial- clerical
Other
Summer
compens.
Compensation 1
Compensation 2
Total (including summer compensation) 370000 412000 782000
Equipment
&
materials
major equipment ( <= 100.000) 210000 210000
Equipment (> 100,000) 65000 65000
Materials & supplies 460000 260000 720000
Item total 735000 260000 995000
Travel
Conferences 10000 10000
Training
Field trips
Tickets 15000 15000 30000
Item total 15000 25000 40000
Others
Patent registration 15000 15000
Publications 10000 10000
Workshop
Other expenses 8000 10000 18000
Item total 8000 35000 43000
7% for SCIENCE AND TECHNOLOGY UNIT 84903 55097 140000
Grand total 1212903 787097 2000000
Compensations (including summer compensation) 39.1% 782000
Equipment& materials 49.75% 995000
Travel 2.0% 40000
Others 2.15% 43000
SCIENCE AND TECHNOLOGY UNIT 7 % 140000
Grand total 100% 2000000
6.4 Budget Justification:
The proposal entitled “COMPUTRER BASED MOLECULAR MODELING, DRUG DESIGN,
SYNTHESIS AND ANTIDIABETIC EVALUATION OF MEDICINE” promises for the Kingdom
of Saudi Arabia to achieve all the objectives mentioned in section 2.
Consultant:
Bill Gates will be approached regarding the biological activity of medicine.

Page 23 of 25
Their respectively field of expertise will be highly valued for the execution of the project.
The participation of research assistants (MS holder, part-time), graduate (MS student),
technicians as well as undergraduate students is essential for the execution of the project. They
will acquire a variety of techniques and skills from the synthesis to the biological testing. The
research team will dedicate maximum time to achieve the goals of this proposal
The remuneration of man power is set at 39.1% of the total proposed budget. 49.75% of the total
budget is devoted to cover expenses in equipment and material for the proper execution of the
project. 2% of the funds will be utilized to enhance knowledge in terms of attending conferences
and symposiums in order to execute the project in successfully. 2.15% will be used for patent
registration, publications and preparation of the project reports. Finally, 7% of the budget will
cover the administrative work of the Science and Technology Unit.
Budget justification for acquiring the following instrument:
CEM Discovery microwave irradiation instrument will be purchased using the requested funds.
The acquisition of this instrument will be beneficial for research activities. It has found many
applications in chemical synthesis particularly in the pharmaceutical industry for developing
compounds in the lead optimization phase of drug development. The acquisition of such an
instrument will enhance the research potential of faculty members, and provide the solid and
necessary support for the medicinal chemistry curriculum. The involvement in research activities
is necessary for providing training projects to undergraduate and graduate students in the faculty
of pharmacy of Umm Al-Qura University in the field of medicinal chemistry.

Page 24 of 25
8. UNDERTAKING OF THE PROJECT TEAM
Form RE- D1-8: UNDERTAKING OF THE PROJECT TEAM
The project team undertakes that this project or any part of it, is:
1- Prepared in full conformity with the SCIENTIFIC INTEGRITY RULES.
2- Original work of the signatories or individuals working under their supervision, including the text, graphics,
publications, and documents, unless otherwise indicated.
3- Not funded by any other sources.
4- Not submitted to any other funding institution during the evaluation process.
5- Not sought fund from any other sources if it is funded by the NSTIP.
SIGNATUREID NUMBER3
NAMEROLE
2321234567
Dr. Noman ShahPI
2321234568
Dr. Hassan Wadood
COI. 1
2321234569
Dr. Ahmad
COI. 2
3
ID number includes National ID for citizens and Iqama for non-citizens team members.

Page 25 of 25
9. REFERENCES:
^ Irny, S.I. and Rose, A.A. (2005) “Designing a Strategic Information Systems Planning Methodology
for Malaysian Institutes of Higher Learning (isp- ipta), Issues in Information System, Volume VI, No. 1,
2005.
2.^ Jump up to: a b Methodology Usage Notes, entry at Merriam–Webster
3.Jump up ^ Baskerville, R. (2009). 35. "Computer and Information Security Handbook aha". Computers
& Security. Morgan Kaufmann Publications (ᾘ ed.) (Elsevier Inc) 10 (8): 605 Extra |pages= or |at=
(help). ISBN 978-0-12-374354-1
4.^ Jump up to: a b misuse of the word Methodology in technical contexts
5.Jump up ^ See, for example, Thomas Kuhn, The Structure of Scientific Revolutions (University of
Chicago, 1970, 2nd ed.)
10. RESUMES:

Application form Research Project Proposal

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Application form Research Project Proposal