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Synthesis and Biological Activities of Ethyl 2-(2-pyridylacetate) Derivatives Containing Thiourea, 1,2,4-triazole, Thiadiazole and Oxadiazole Moieties.

Synthesis and Biological Activities of Ethyl 2-(2-pyridylacetate) Derivatives Containing Thiourea, 1,2,4-triazole, Thiadiazole and Oxadiazole Moieties.
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Szulczyk D, Tomaszewski P, Jóźwiak M, Kozioł AE, Lis T, Collu D, Iuliano F, Struga M,


Szulczyk D, Tomaszewski P, Jóźwiak M, Kozioł AE, Lis T, Collu D, Iuliano F, Struga M, (click to view)

Szulczyk D, Tomaszewski P, Jóźwiak M, Kozioł AE, Lis T, Collu D, Iuliano F, Struga M,

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Molecules (Basel, Switzerland) 2017 03 0622(3) pii 10.3390/molecules22030409

Abstract

Thirty six novel heterocyclic derivatives of ethyl 2-(2-pyridylacetate) were efficiently synthesized. The new compounds involve the linkage of a 2-pyridyl ring with thiosemicarbazide (compounds 1-7), 1,2,4-triazole (compounds 1a-7a), 1,3,4-thiadiazole (compounds 1b-7b), and 1,3,4-oxadiazole (compounds 1f-7f) moieties. The last group of compounds 1e-7e involves the connection of a 2-pyridyl ring with 1,2,4-triazole and thiourea. ¹H-NMR, (13)C-NMR and MS methods were used to confirm the structures of the obtained derivatives. The molecular structures of 3, 3b, 7a and 7f were further confirmed by X-ray crystallography. All obtained compounds were tested in vitro against a number of microorganisms, including Gram-positive cocci, Gram-negative rods and Candida albicans. In addition, the obtained compounds were tested for cytotoxicity and antiviral activity against HIV-1.

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