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Amidoalkylation of heterocyclic amines by N-[5-(alkylsulfanyl)-1,3,4-thiadiazol-2-yl]- 2'-chloroacetamide and antimicrobial activity of derivatives

T. T. ToshmurodovInstitute of the Chemistry of Plant Substances, Academy of Sciences of the Republic of Uzbekistan, Mirzo Ulugbek Str. 77, 100170, Tashkent, UzbekistanA. A. ZiyaevInstitute of the Chemistry of Plant Substances, Academy of Sciences of the Republic of Uzbekistan, Mirzo Ulugbek Str. 77, 100170, Tashkent, UzbekistanС. А. СасмаковInstitute of the Chemistry of Plant Substances, Academy of Sciences of the Republic of Uzbekistan, Mirzo Ulugbek Str. 77, 100170, Tashkent, UzbekistanJaloliddin AbdurakhmanovInstitute of the Chemistry of Plant Substances, Academy of Sciences of the Republic of Uzbekistan, Mirzo Ulugbek Str. 77, 100170, Tashkent, UzbekistanMavluda A. ZiyaevaTashkent state Technical University named after I. Karimov, Universitetskaya-2 Str., 100095, Tashkent, UzbekistanД. С. ИсмаиловаInstitute of the Chemistry of Plant Substances, Academy of Sciences of the Republic of Uzbekistan, Mirzo Ulugbek Str. 77, 100170, Tashkent, UzbekistanShakhnoza S. AzimovaInstitute of the Chemistry of Plant Substances, Academy of Sciences of the Republic of Uzbekistan, Mirzo Ulugbek Str. 77, 100170, Tashkent, Uzbekistan
Current Chemistry Lettersjournal2021en
ABI

Abstract

Amidoalkylation of secondary heterocyclic amines by N-[5-(alkylsulfanyl)-1,3,4-thiadiazol-2-yl]-2'-chloroacetamide resulted the new compounds 5-10 that contain 1,3,4-thiadiazole-5-thione moiety alongside pyperidine, morpholine, and cytisine fragments. In vitro screening of antimicrobial activity of synthesized compounds showed that N-[5-(amylsulfanyl)-1,3,4-thiadiazol-2-yl]-2'-morpholinacetamide exhibited an appreciable antibacterial activity against gram-negative bacteria of Escherichia coli (inhibition zone diameter of 16 mm) and gram-positive bacteria of Staphylococcus aureus and Bacillus subtilis (10-13 mm).

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