3rd Pharm D medicinal chemistry

1. Medicinal chemistry
Prodrug topic

2. Medicinal chemistry
• Two Structure of carrier linked prodrug?
• Answer:

6. Electronic parameter

12. Mention stearic parameters

13. What are lead compounds, how they are helpful
In drug discovery ❓
• Answer: A lead compound is generally defined as a new
chemical entity that could potentially be developed into a
new drug by optimizing its beneficial effects and minimizing
its side effects (see Chapter 9 for a more detailed discussion
of the criteria). From: Drug
Discovery and Development (Second Edition), 2013

14. Applications of QSAR In drug design
•Answer: QSAR are being applied in many
disciplines, for example: risk assessment,
toxicity prediction, and regulatory decisions
in addition to drug discovery and lead
optimization.

15. What is CADD, Enumerate the application
•Computer-aided design (CAD) is the use of
computers (or workstations) to aid in the creation,
modification, analysis, or optimization of a design.
... CAD may be used to design curves and figures in
two-dimensional (2D) space; or curves, surfaces, and
solids in three-dimensional (3D) space.

16. Anti hypertension
• Uses and structure of propranolol
• Answer:Propranolol is a synthetic, nonselective beta-adrenergic receptor
blocker with antianginal, antiarrhythmic, antihypertensive
properties. Propranolol competitively antagonizes beta-adrenergic receptors,
thereby causing negative chronotropic and inotropic effects leading to a reduction
in cardiac output.

17. • Structure and uses of Amiodarone and Diltiazem
• Answer:This medication is used to treat certain types of serious (possibly fatal)
irregular heartbeat (such as persistent ventricular fibrillation/tachycardia). It is used
to restore normal heart rhythm and maintain a regular, steady
heartbeat. Amiodarone is known as an anti-arrhythmic drug.

18. • Use and structure of diltiazem
• Answer:Diltiazem is used to prevent chest pain (angina). It may help to increase
your ability to exercise and decrease how often you may get angina
attacks. Diltiazem is called a calcium channel blocker. It works by relaxing blood
vessels in the body and heart and lowers the heart rate.

19. • Q.3 What are ACE inhibitors, give two examples
• Answer . Angiotensin-converting-enzyme inhibitors are a class of medication used
primarily for the treatment of high blood pressure and heart failure. They work by causing
relaxation of blood vessels as well as a decrease in blood volume, which leads to lower
blood pressure and decreased oxygen demand from the heart.
• Examples. Benazepril (Lotensin)
• Captopril.
• Enalapril (Vasotec)
• Fosinopril.

20. • Q.4 Name any two calcium Channel blockers and their uses
• Answer. Calcium channel blockers are prescription medications that relax
blood vessels and increase the supply of blood and oxygen to the heart while also
reducing the heart's workload. Examples of calcium channel blockers include:
Amlodipine (Norvasc) Bepridil (Vascor)
• Use. High blood pressure (hypertension)
• Heart arrhythmia
• Cluster headaches

21. • Q.5 Structure and uses of minoxidil.
• Answer. Uses. Minoxidil is used with other medications to treat high blood
pressure (hypertension). Lowering high blood pressure helps prevent strokes,
heart attacks, and kidney problems. Minoxidil works by relaxing blood vessels so
blood can flow more easily.

22. • Q.6 Structure and uses of felodipine
• Answer:Felodipine is used to treat high blood pressure (hypertension). Lowering
high blood pressure helps prevent strokes, heart attacks, and kidney
problems. Felodipine is known as a calcium channel blocker. By blocking calcium,
this medication relaxes and widens blood vessels so blood can flow more easily

23. • Q.7 Structure and uses of nefidipine
• Answer:Nifedipine is a first generation calcium channel blocker used to treat
hypertension and angina pectoris.

24. • Q.8 Structure and uses of isosorbIde dinitrate
• Answer: Uses.Isosorbide dinitrate is used to treat or prevent attacks of chest
pain (angina)

25. • Q.9 What are vasodilator and two examples
• Answer:Vasodilators are medicines that dilate (widen) blood vessels, allowing
blood to flow more easily through. Some act directly on the smooth muscle cells
lining the blood vessels
• Examples. Oxygen.
• Nitric oxide.
• Nitroprusside (Nipride, Nitropress)
• Sildenafil (Revatio, Viagra)
• Tadalafil (Adcirca, Cialis)

26. • Q.10 Structure and uses of captopril
• Answer :Captopril is used to treat high blood pressure (hypertension),
congestive heart failure, kidney problems caused by diabetes, and to improve
survival after a heart attack

27. Anti hypertension
• Q.11 Structure and uses propranolol and phenytoin
• Answer:Phenytoin is an anti-epileptic drug, also called an anticonvulsant.
Phenytoin works by slowing down impulses in the brain that cause seizures.
Phenytoin is used to control seizures

28. • Q.12 structure and specific uses of Amyl nitrate
• Answer:employed medically to treat heart diseases such as angina and to treat
cyanide poisoning. Its use as a prescription medicine comes from its ability to
lower blood pressure.

29. • Q.13 Write the synthesis of warfarin
• Answer:

30. • Q.14 Any two anticoagulants with their MOA
• Answer: