Synthesis and anti-HIV activity of some isatin derivatives.
Isatin/5-substituted Isatin was reacted with 2-aminothiazole, 2-aminopyridine, 4-methoxyaniline to form Schiff bases and the N-Mannich bases of the above Schiff bases were synthesized by reacting with formaldehyde and piperidine. The chemical structures of the synthesized compounds were confirmed by means of IR, 1H-NMR data and elemental analysis. Investigation of Anti-HIV activity was done against replication of HIV-1 (III B) and HIV-2 (ROD) in MT-4 cells. Azidothymidine (AZT) was used as the reference standard. The most active compound of the series was 3-(2-thiazolylimino)-5-bromo-1,3-dihydro-indol-2-one (VI) which demonstrated 28% and 10% protection against HIV-1 and HIV-2 respectively.
Sridhar
S K
SK
Department of Pharmaceutical Chemistry, Vel's College of Pharmacy, Old Pallavaram, Chennai, India.
Pandeya
S N
SN
De Clercq
E
E
D019380:Anti-HIV Agents / Q000138:chemical synthesis* / Q000494:pharmacology*; D002478:Cells, Cultured; D055598:Chemical Phenomena; D002627:Chemistry, Physical; D006801:Humans; D007202:Indicators and Reagents; D007510:Isatin / Q000031:analogs & derivatives* / Q000138:chemical synthesis / Q000494:pharmacology*; D013778:Tetrazolium Salts; D013844:Thiazoles
D019380:Anti-HIV Agents; D007202:Indicators and Reagents; D013778:Tetrazolium Salts; D013844:Thiazoles; D007510:Isatin; C022616:thiazolyl blue