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  • Title: Synthesis and anti-HIV activity of some isatin derivatives.
    Author: Sridhar SK, Pandeya SN, De Clercq E.
    Journal: Boll Chim Farm; 2001; 140(5):302-5. PubMed ID: 11680082.
    Abstract:
    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.
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