Wetzel B, Woitun E, Reuter W, Maier R, Lechner U
Arzneimittelforschung. 1985;35(1A):343-8. doi: 10.1002/chin.198528360.
The 6R-[(R)-2-[3-[5-pyrimidinyl]ureido]-2-(4-hydroxyphenyl) acetamido]-penicillanic acids (10), prepared by two synthetic routes, exhibit broad antimicrobial activity against Gram-positive and Gram-negative bacteria. Their structure activity relationships are discussed. 6R-[(R)-2-[3-[2-(p-Aminosulfonyl)anilino-4-hydroxy-5-pyrimidinyl] ureido]-2-(4-hydroxyphenyl)acetamido]-penicillanic acid, sodium salt (VX-VC 43, 10m), the most active compound, shows very low MIC (minimal inhibitory concentration) values against clinically important Gram-negative bacteria, primarily Pseudomonas aeruginosa.
通过两条合成路线制备的6R-[(R)-2-[3-[5-嘧啶基]脲基]-2-(4-羟基苯基)乙酰胺基]-青霉烷酸(10)，对革兰氏阳性菌和革兰氏阴性菌均表现出广泛的抗菌活性。讨论了它们的构效关系。最具活性的化合物6R-[(R)-2-[3-[2-(对氨基磺酰基)苯胺基-4-羟基-5-嘧啶基]脲基]-2-(4-羟基苯基)乙酰胺基]-青霉烷酸钠盐(VX-VC 43, 10m)，对临床上重要的革兰氏阴性菌，主要是铜绿假单胞菌，显示出非常低的最低抑菌浓度(MIC)值。
