- I2/TBHP-Mediated tandem cyclization and oxidation reaction: Facile access to 2-substituted thiazoles and benzothiazoles
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The efficient synthesis of 2-substituted thiazoles and benzothiazoles has been accomplished employing readily available cysteine esters and 2-aminobenzenethiols as N and S sources. The reaction proceeds under an I2/TBHP system and involves a on
- Liu, Li,Tan, Chen,Fan, Rong,Wang, Zihan,Du, Hongguang,Xu, Kun,Tan, Jiajing
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- 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
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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 μgmL-1, and 1.12 μgmL-1 with therapeutic indexes (SI) of 9 and 1, respectively.
- Zia, Mehwash,Akhtar, Tashfeen,Hameed, Shahid,Al-Masoudi, Najim A.
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p. 747 - 758
(2012/11/13)
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