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Synthesis and Anticandidosic Activities of Some 3-Imidazo[1,2-a]Pyridinyl-1-Arylpropenone Derivatives

Synthesis and Anticandidosic Activities of Some 3-Imidazo[1,2-a]Pyridinyl-1-Arylpropenone Derivatives
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摘要 In this work, we show the synthesis of ten (10) new derivatives of 3-imidazo [1,2-a]pyridinyl-1-arylpropenone (10a - d). These new compounds were obtained by condensation of Claisen-Schmidt between derivatives of 2-substi- tuted-1H-imidazo[1,2-a]pyridine-3-carbaldehyde (3a - b and 7) and acetophenone derivatives (9a - e) in the presence of a base. The synthesized compounds were characterized by spectroscopic analyses <sup>1</sup>H and <sup>13</sup>C NMR. The antifungal activity of the ten (10) derivatives was determined on a resistant strain of Candida albicans by the microdilution method. The results showed that four (4) of them (10a, 10b, 10c and 10i) were active with minimum inhibitory concentrations (MICs) below 300 μmol/L. Of these four compounds, 10i was more potent than the others with a MIC of 41.98 μmol/L. In this work, we show the synthesis of ten (10) new derivatives of 3-imidazo [1,2-a]pyridinyl-1-arylpropenone (10a - d). These new compounds were obtained by condensation of Claisen-Schmidt between derivatives of 2-substi- tuted-1H-imidazo[1,2-a]pyridine-3-carbaldehyde (3a - b and 7) and acetophenone derivatives (9a - e) in the presence of a base. The synthesized compounds were characterized by spectroscopic analyses <sup>1</sup>H and <sup>13</sup>C NMR. The antifungal activity of the ten (10) derivatives was determined on a resistant strain of Candida albicans by the microdilution method. The results showed that four (4) of them (10a, 10b, 10c and 10i) were active with minimum inhibitory concentrations (MICs) below 300 μmol/L. Of these four compounds, 10i was more potent than the others with a MIC of 41.98 μmol/L.
作者 Kouassi Francesco Adingra Souleymane Coulibaly Kacou Alain Mahama Ouattara Drissa Sissouma Kouassi Francesco Adingra;Souleymane Coulibaly;Kacou Alain;Mahama Ouattara;Drissa Sissouma(Laboratoire de Constitution et Réaction de la Matière, UFR Sciences des Structures de la Matière et Technologie, Université Félix Houphou&euml;t Boigny, Abidjan, C&ocirc;te d’Ivoire;Département de Chimie Thérapeutique et Chimie organique, UFR Sciences Pharmaceutiques et Biologiques, Abidjan, C&ocirc;te d’Ivoire)
出处 《Advances in Biological Chemistry》 CAS 2022年第4期81-91,共11页 生物化学进展(英文)
关键词 Imidazo[1 2-a]Pyridine Arylpropenone Candida albicans ANTIFUNGAL Imidazo[1 2-a]Pyridine Arylpropenone Candida albicans Antifungal
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