Title:Synthesis, Crystal Structure and Anti-HIV Activity of 2- Adamantyl/adamantylmethyl-5-aryl-1,3,4-oxadiazoles
Volume: 8
Issue: 6
Author(s): Mahmood-ul-Hassan Khan, Tashfeen Akhtar, Najim A. Al-Masoudi, Helen Stoeckli-Evans and Shahid Hameed
Affiliation:
Keywords:
Adamantyl derivatives, Anti-HIV activity, Hydrazide cyclization, 1, 3, 4-Oxadiazoles
Abstract: Two series of 2-adamantyl/adamantylmethyl-5-aryl-1,3,4-oxadiazoles (4a-l and 5a-l) were synthesized by
cyclodehydration of adamantan-1-carboxylic acid/adamantylacetic acid with various aryl hydrazides (3a-l) in the presence
of POCl3. The synthesis was supported by spectroanalytical techniques and verified further by crystal structure determination
of compounds 4e and 5k. The synthesized compounds were screened for their inhibitory activity against HIV-1 and
HIV-2 in MT-4 cells. Compound 5b exhibited a moderate activity in vitro for the replication of both virus types, suggesting
for further structural modification as a new lead in the development of an antiviral agent.
