Yildiz-Oren Ilkay, Yalcin Ismail, Aki-Sener Esin, Ucarturk Nejat
Department of Pharmaceutical Chemistry, Faculty of Pharmacy, Ankara University, Tandogan, 06100 Ankara, Turkey.
Eur J Med Chem. 2004 Mar;39(3):291-8. doi: 10.1016/j.ejmech.2003.11.014.
A series of multisubstituted benzoxazoles, benzimidazoles, and benzothiazoles (5-7) as non-nucleoside fused isosteric heterocyclic compounds was synthesized and tested for their antibacterial activities against various Gram-positive and Gram-negative bacteria and antifungal activity against the fungus Candida albicans. Microbiological results indicated that the synthesized compounds possessed a broad spectrum of activity against the tested microorganisms at MIC values between 100 and 3.12 microg/ml. Structure-activity relationships (SAR) studies revealed that benzothiazole ring system enhanced the antimicrobial activity against Staphylococcus aureus. In these sets of non-nucleoside fused heterocyclic compounds electron withdrawing groups at position 5 of the benzazoles increased the activity against C. albicans.
合成了一系列多取代苯并恶唑、苯并咪唑和苯并噻唑（5 - 7）作为非核苷稠合等排杂环化合物，并测试了它们对各种革兰氏阳性菌和革兰氏阴性菌的抗菌活性以及对白色念珠菌的抗真菌活性。微生物学结果表明，合成的化合物在100至3.12微克/毫升的最低抑菌浓度（MIC）值下对测试微生物具有广谱活性。构效关系（SAR）研究表明，苯并噻唑环系统增强了对金黄色葡萄球菌的抗菌活性。在这些非核苷稠合杂环化合物组中，苯并唑5位的吸电子基团增加了对白色念珠菌的活性。
