Department of Pharmaceutical Chemistry of Aristotle University of Thessaloniki, School of Pharmacy, Thessaloniki 54124, Greece.
Bioorg Med Chem. 2013 Jan 15;21(2):532-9. doi: 10.1016/j.bmc.2012.10.046. Epub 2012 Nov 17.
As a part of our ongoing studies in developing new derivatives as dual antimicrobial/anti-inflammatory agents we describe the synthesis of novel 5-arylidene-2-(1,3-thiazol-2-ylimino)-1,3-thiazolidin-4-ones. All newly synthesized compounds were tested for their anti-inflammatory activity using carrageenan mouse paw edema bioassay. Their COX-1/LOX inhibitory activities were also determined. Moreover, all compounds were evaluated for their antimicrobial and antifungal activities against a panel of Gram positive, Gram negative bacteria and moulds. All tested compounds exhibited better antimicrobial activity than commercial drugs, bifonazole, ketoconazole, ampicillin and streptomycin.
作为我们正在进行的开发新的双重抗菌/抗炎衍生物的研究的一部分，我们描述了新型 5-亚芳基-2-(1,3-噻唑-2-基亚氨基)-1,3-噻唑烷-4-酮的合成。所有新合成的化合物都通过角叉菜胶小鼠足跖肿胀生物测定法测试其抗炎活性。还测定了它们对 COX-1/LOX 的抑制活性。此外，还评估了所有化合物对革兰氏阳性、革兰氏阴性细菌和霉菌的抗菌和抗真菌活性。所有测试的化合物都表现出比商业药物比呋唑酮、酮康唑、氨苄西林和链霉素更好的抗菌活性。
