2-Amino-4-arylthiazole Derivatives as Anti-giardial Agents: Synthesis, Biological Evaluation and QSAR Studies
Abstract: A series of seven 2-amino-4-arylthiazoles were prepared following Hantzsch’s modified method under microwave irradiation. A set of 50 derivatives was obtained and the in vitro activity against Giardia intestinalis was evaluated. The results on the biological activity revealed that, in general, the N-(5-bromo-4-aryl-thiazol-2-yl)-acetamide scaffold showed high bioactivity. In particular, compounds 6e (IC50 = 0.39 μM) and 6b (IC50 = 0.87 μM) were found to be more potent than the positive control metronidazole. Citoxicity and acute toxicity tests performed showed low toxicity and high selectivity of the most active compounds (6e SI = 139, 6b SI = 52.3). A QSAR analysis was applied to a data set of 37 obtained 2-amino-4-arylthiazoles derivatives and the best model described a strongly correlation between the anti-giardiasic activity and molecular descriptors as E2M, RDF115m, F10, MATS6v, and Hypnotic-80, with high statistical quality. This finding indicates that N-substituted aminothiazole scaffold should be investigated for the development of highly selective anti-giardial agent.
- Location
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Deutsche Nationalbibliothek Frankfurt am Main
- Extent
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Online-Ressource
- Language
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Englisch
- Bibliographic citation
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2-Amino-4-arylthiazole Derivatives as Anti-giardial Agents: Synthesis, Biological Evaluation and QSAR Studies ; volume:13 ; number:1 ; year:2015 ; extent:10
Open chemistry ; 13, Heft 1 (2015) (gesamt 10)
- Creator
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Mocelo-Castell, Raul
Villanueva-Novelo, Carlos
Cáceres-Castillo, David
Carballo, Ruben M.
Quijano-Quiñones, Ramiro F.
Quesadas-Rojas, Mariana
Cantillo-Ciau, Zulema
Cedillo-Rivera, Roberto
Moo-Puc, Rosa E.
Moujir, Laila M.
Mena-Rejón, Gonzalo J.
- DOI
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10.1515/chem-2015-0127
- URN
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urn:nbn:de:101:1-2410161541134.217373583078
- Rights
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Open Access; Der Zugriff auf das Objekt ist unbeschränkt möglich.
- Last update
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15.08.2025, 7:35 AM CEST
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Associated
- Mocelo-Castell, Raul
- Villanueva-Novelo, Carlos
- Cáceres-Castillo, David
- Carballo, Ruben M.
- Quijano-Quiñones, Ramiro F.
- Quesadas-Rojas, Mariana
- Cantillo-Ciau, Zulema
- Cedillo-Rivera, Roberto
- Moo-Puc, Rosa E.
- Moujir, Laila M.
- Mena-Rejón, Gonzalo J.
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