Prasad Davinder, Kumar Awanit, Shukla Praveen Kumar, Nath Mahendra
Department of Chemistry, University of Delhi, Delhi 110 007, India.
Org Med Chem Lett. 2011 Aug 3;1(1):4. doi: 10.1186/2191-2858-1-4.
Novel 2-arylthiazolidin-4-one derivatives (8a-q and 11) have been synthesized in good-to-excellent yields (70-96%) by one-pot three-component condensation-cyclization reaction of aromatic or aliphatic primary amines, aromatic aldehydes, and thioglycolic acid in polypropylene glycol at 110°C temperature. The in vitro antimicrobial activity of the synthesized 2-arylthiazolidin-4-ones was investigated against a panel of six pathogenic fungal strains, a Gram-positive and three Gram-negative bacteria. Results revealed that the compounds (8a-d) bearing 3-(4-(1H-imidazolylmethyl)phenyl)-substituent displayed significant antibacterial efficacy specifically against Klebsiella pneumoniae (minimum inhibitory concentration 12.5 μg/mL). In addition, some of the synthesized compounds have also shown antimicotic activity against Sporothrix schenckii, Trichophyton mentagrophytes, and Aspergillus fumigatus at the concentration of 50 μg/mL.
通过在110°C温度下，使芳香族或脂肪族伯胺、芳香醛和巯基乙酸在聚丙二醇中进行一锅三组分缩合环化反应，已以良好至优异的产率（70 - 96%）合成了新型2-芳基噻唑烷-4-酮衍生物（8a - q和11）。研究了合成的2-芳基噻唑烷-4-酮对一组六种致病真菌菌株、一种革兰氏阳性菌和三种革兰氏阴性菌的体外抗菌活性。结果表明，带有3-(4-(1H-咪唑基甲基)phenyl)-取代基的化合物（8a - d）对肺炎克雷伯菌显示出显著的抗菌效果（最低抑菌浓度为12.5 μg/mL）。此外，一些合成化合物在50 μg/mL的浓度下对申克孢子丝菌、须癣毛癣菌和烟曲霉也表现出抗真菌活性。
