Francisco Gerardo D, Li Zhong, Albright J Donald, Eudy Nancy H, Katz Alan H, Petersen Peter J, Labthavikul Pornpen, Singh Guy, Yang Youjun, Rasmussen Beth A, Lin Yang-I, Mansour Tarek S
Chemical Sciences and Infectious Diseases, Wyeth Research, Pearl River, NY 10965, USA.
Bioorg Med Chem Lett. 2004 Jan 5;14(1):235-8. doi: 10.1016/j.bmcl.2003.09.082.
Over 50 phenyl thiazolyl urea and carbamate derivatives were synthesized for evaluation as new inhibitors of bacterial cell-wall biosynthesis. Many of them demonstrated good activity against MurA and MurB and gram-positive bacteria including MRSA, VRE and PRSP. 3,4-Difluorophenyl 5-cyanothiazolylurea (3p) with clog P of 2.64 demonstrated antibacterial activity against both gram-positive and gram-negative bacteria.
合成了50多种苯基噻唑基脲和氨基甲酸酯衍生物，以评估其作为细菌细胞壁生物合成新抑制剂的性能。其中许多化合物对MurA和MurB以及包括耐甲氧西林金黄色葡萄球菌（MRSA）、耐万古霉素肠球菌（VRE）和耐青霉素肺炎链球菌（PRSP）在内的革兰氏阳性菌表现出良好的活性。脂水分配系数（clog P）为2.64的3,4-二氟苯基5-氰基噻唑基脲（3p）对革兰氏阳性菌和革兰氏阴性菌均表现出抗菌活性。
