Temiz-Arpaci Ozlem, Yildiz Ilkay, Ozkan Semiha, Kaynak Fatma, Aki-Sener Esin, Yalçin Ismail
Ankara University, Faculty of Pharmacy, Department of Pharmaceutical Chemistry, Degol Str Tandoğan, Tandoğan, Ankara, Turkey.
Eur J Med Chem. 2008 Jul;43(7):1423-31. doi: 10.1016/j.ejmech.2007.09.023. Epub 2007 Oct 5.
The synthesis and antimicrobial activity of a new series of 5-ethylsulphonyl-2-(substituted-phenyl/substituted-benzyl and/or phenylethyl)benzoxazole derivatives (3a-3t) except 3a, 3g, 3h, 3k [R.S. Pottorf, N.K. Chadha, M. Katkevies, V. Ozola, E. Suna, H. Ghane, T. Regberg, M.R. Player, Tetrahedron Lett. 44 (1) (2003) 175] were described. The in vitro antimicrobial activity of the compounds was determined against some Gram-positive, Gram-negative bacteria, a fungi Candida albicans and their drug-resistant isolates in comparison with standard drugs. Antimicrobial results indicated that the synthesized compounds possessed a broad spectrum of activity with MIC values 250-7.81 microg/ml. While all compounds are less potent than fluconazole against C. albicans, most of them are more potent than fluconazole against C. albicans isolate.
除3a、3g、3h、3k外，一系列新的5-乙基磺酰基-2-（取代苯基/取代苄基和/或苯乙基）苯并恶唑衍生物（3a-3t）的合成及其抗菌活性已被描述[R.S. Pottorf，N.K. Chadha，M. Katkevies，V. Ozola，E. Suna，H. Ghane，T. Regberg，M.R. Player，《四面体快报》44 (1) (2003) 175]。与标准药物相比，测定了这些化合物对一些革兰氏阳性菌、革兰氏阴性菌、白色念珠菌及其耐药菌株的体外抗菌活性。抗菌结果表明，合成的化合物具有广泛的活性，最低抑菌浓度（MIC）值为250-7.81微克/毫升。虽然所有化合物对白色念珠菌的效力均低于氟康唑，但它们中的大多数对白色念珠菌分离株的效力高于氟康唑。
