Synthesis and Biological Activities of Ethyl 2-(2-pyridylacetate) Derivatives Containing Thiourea, 1,2,4-triazole, Thiadiazole and Oxadiazole Moieties
| Autor: | Anna E. Koziol, David Collu, Filippo Iuliano, Piotr Tomaszewski, Michał Jóźwiak, Daniel Szulczyk, Tadeusz Lis, Marta Struga |
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| Jazyk: | angličtina |
| Rok vydání: | 2017 |
| Předmět: |
Models
Molecular Pharmaceutical Science Oxadiazole biological activity Microbial Sensitivity Tests 010402 general chemistry Ring (chemistry) Crystallography X-Ray 01 natural sciences Article Analytical Chemistry X-ray crystal structure analysis Cell Line lcsh:QD241-441 chemistry.chemical_compound Structure-Activity Relationship 1 2 4-triazole lcsh:Organic chemistry Anti-Infective Agents Drug Discovery Thiadiazoles 1 3 4-oxadiazole Organic chemistry Humans Physical and Theoretical Chemistry Candida albicans Cytotoxicity Heterocyclic derivatives Cells Cultured 1 3 4-thiadiazole Oxadiazoles biology Bacteria Molecular Structure 010405 organic chemistry Organic Chemistry Fungi Thiourea 1 2 4-Triazole thiourea Triazoles biology.organism_classification In vitro 0104 chemical sciences chemistry Chemistry (miscellaneous) HIV-1 Molecular Medicine |
| Zdroj: | Molecules : A Journal of Synthetic Chemistry and Natural Product Chemistry Molecules; Volume 22; Issue 3; Pages: 409 Molecules, Vol 22, Iss 3, p 409 (2017) |
| ISSN: | 1420-3049 |
| Popis: | 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, 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. |
| Databáze: | OpenAIRE |
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