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Molecules 2017, 22(3), 409; doi:10.3390/molecules22030409

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

1
Department of Biochemistry and Pharmacogenomics, Faculty of Pharmacy, Medical University of Warsaw, 02-097 Warsaw, Poland
2
Laboratory of Centre for Preclinical Research, Medical University of Warsaw, Banacha 1B, 02-097 Warsaw, Poland
3
Department of Biochemistry, Second Faculty of Medicine, Medical University of Warsaw, 02-097 Warsaw, Poland
4
Faculty of Chemistry, Maria Curie-Sklodowska University, 20-031 Lublin, Poland
5
Faculty of Chemistry, University of Wroclaw, 50-383 Wroclaw, Poland
6
Department of Life and Environmental Sciences, Section of Microbiology and Virology, University of Cagliari, 09042 Cittadella Universitaria Monserrato, Italy
7
Department of Molecular Medicine, Institute of Virology, Slovak Academy of Sciences, Dubravska cesta 9, 845 05 Bratislava, Slovak
*
Author to whom correspondence should be addressed.
Academic Editor: Diego Muñoz-Torrero
Received: 14 January 2017 / Revised: 16 February 2017 / Accepted: 1 March 2017 / Published: 6 March 2017
(This article belongs to the Section Medicinal Chemistry)
View Full-Text   |   Download PDF [819 KB, uploaded 6 March 2017]   |  

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 17), 1,2,4-triazole (compounds 1a7a), 1,3,4-thiadiazole (compounds 1b7b), and 1,3,4-oxadiazole (compounds 1f7f) moieties. The last group of compounds 1e7e involves the connection of a 2-pyridyl ring with 1,2,4-triazole and thiourea. 1H-NMR, 13C-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. View Full-Text
Keywords: 1,2,4-triazole; 1,3,4-thiadiazole; 1,3,4-oxadiazole; thiourea; X-ray crystal structure analysis; biological activity 1,2,4-triazole; 1,3,4-thiadiazole; 1,3,4-oxadiazole; thiourea; X-ray crystal structure analysis; biological activity
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This is an open access article distributed under the Creative Commons Attribution License which permits unrestricted use, distribution, and reproduction in any medium, provided the original work is properly cited. (CC BY 4.0).

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Szulczyk, D.; Tomaszewski, P.; Jóźwiak, M.; Kozioł, A.E.; Lis, T.; Collu, D.; Iuliano, F.; Struga, M. Synthesis and Biological Activities of Ethyl 2-(2-pyridylacetate) Derivatives Containing Thiourea, 1,2,4-triazole, Thiadiazole and Oxadiazole Moieties. Molecules 2017, 22, 409.

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