Introduction of loviride, Introduction of zalcitabine

1. MEDICINAL CHEMISTRY III
Presented by : -
Prashant Ingawale
Prashant Jatkar
Yogesh Pawar
Gaurav Deshpande
1

2. Antiviral Drug
Loviride
Zalcitabine

3. LOVIRIDE
 Loviride (Loveride) was an antiviral drug
manafactured by Janssen that it active against HIV
 Loviride is a non nucleoside reverse transcriptase
inhibitor (NNRTI) that entered phase 3 trials in the
late 1990s but failed to get marketing approval because
of poor potency
 Molecular Formula C17H16Cl2N2O2

4. ZALCITABINE
 Zalcitabine, also called dideoxycytidine, is a
nucleoside analog reverse-transcriptase inhibitor.
 sold under the trade name Hivid.
 Zalcitabine was the third antiretroviral to be
approved by the Food and Drug Administration for the
treatment of HIV/AIDS.
 Chemical Formula :- C9H13N3O3

5. MoA Zalcitabine is a nucleoside reverse transcriptase inhibitor
(NRTI) with activity against Human Immunodeficiency Virus
Type 1 (HIV-1)
Within cells, zalcitabine is converted to its active metabolite,
dideoxycytidine 5'-triphosphate (ddCTP), by the sequential
action of cellular enzymes.
interferes with viral RNA-directed DNA polymerase (reverse
transcriptase) by competing for utilization of the natural
substrate deoxycytidine 5'-triphosphate (dCTP), as well as
incorpating into viral DNA.

6. .
 Due to it's lack of a 3'-OH group, the formation of a 5' to 3'
phosphodiester linkage that is necessary for DNA chain
elongation is inhibited, thus leading to the termination of
viral DNA growth.

7. pharmacokinetics
 Absorption :- 80% oral administration
 Distribution:- protein binding
 Metabolism :- Hepatic
 Elimination half-life :- 2 hr
 Excretion :- Renal

8. SIDE EFFECT
 inflammation of the pancreas (pancreatitis)
 liver failure,
 metabolic disturbance
 peripheral neuropathy
 headache, fever, abdominal
pain, nausea, vomiting, diarrhea, rash, mouth ulcers,
 painful swallowing, and difficulty sleeping.

9. USES
 Zalcitabine is an oral medication that is used for the
treatment of infections with the human
immunodeficiency virus (HIV
 It is used in treatment of retrovirus
 BRAND NAME:- Hivid

10. fundamental medicinal chemitry by Gareth Thomus
Text Book of Medicinal Chemistry by Anurekha Jain &
Harun M Patel
Guided By-: ms. Holkar madam

11. Thank You
!!!!