New Aryl-1,3-thiazole-4-carbohydrazides, Their 1,3,4-Oxadiazole-2-thione, 1,2,4-Triazole, Isatin-3-ylidene and Carboxamide Derivatives. Synthesis and Anti-HIV Activity

作者：Zia Mehwash; Akhtar Tashfeen; Hameed Shahid^*; Al Masoudi Najim A

来源：Zeitschrift Fur Naturforschung Section B-a Journal of Chemical Sciences, 2012, 67(7): 747-758.

DOI：10.5560/ZNB.2012-0095

• anti-HIV Activity
• Amino Acids
• Imine Derivatives
• Oxadiazoles
• Thiazoles

A series of isatin-3-ylidene (6a-i) and arylthiazolyl-1,3,4-oxadiazole-2-thione derivatives 7a-i derived from arylthiazolyl carbohydrazide analogs 4a-i were synthesized. Analogously, coupling of 4f with various amino acid methyl esters in the presence of HOBt/DCC reagents afforded the carboxamide derivatives 9a-d. The newly synthesized compounds were assayed against HIV-1 and HIV-2 in MT-4 cells. All compounds are inactive, except compounds 9b and 9c which showed inhibition of HIV-1 with EC50 = 2.34 mu g mL(-1), and 1.12 mu g mL(-1) with therapeutic indexes (SI) of 9 and %26lt;1, respectively.

• 出版日期2012-7