- 作者: 林和盛 ; Rampersaud, Ashraff A. ; Flokowitsch, Jane E. 等
- 作者服務機構: Lilly Research Laboratories, Eli Lilly and Co., Indianapolis, Indiana, U.S.A.
- 中文摘要: The preparation and biological evaluation of 7.beta.- [ [ 2-(phenyl)thiazol-4-yl ] acetamido ] cephalosporins and 7.beta.- [ [ 2-(pyridin-2-yl)thiazol-4-yl ] acetamido ] cephalosporins, 9a-o, substituted at the 3-position with acetyloxymethyl, chlorine, hydrogen, and methyl are described. Hantzsch's thiazole synthesis is employed to provide thiazoleacetic acids (5a-e), subsequently followed by Morpho CDI-assisted amidation to complete the synthesis of target cephalosporins 9a-o. These compounds display activity selectively against Gram-positive bacteria, but are inactive against most Gram-negative bacteria tested. Those with acetyloxymethyl at the 3-position, i.e., 9a, 9e, 9i, 9m, and 9o, exhibit activity with minimal inhibitory concentrations of 16.mu.g/mL or lower against four strains of methicillin-resistant staphylococci, namely Staphylococcus aureus X400 and S13E and Staphylococcus epidermidis 270 and 222. Notably, 9a displays an activity profile similar to that of vancomycin regarding its spectrum and potency.
- 英文摘要: --
- 中文關鍵字: Gram-Positive Bacteria; Methicillin-Resistant Staphylococci; Cephalosporin; Thiazole Synthesis; Amidation
- 英文關鍵字: 革蘭陽性菌;抗二甲氧苯青黴素葡萄球菌;頭芽胞菌素;唑合成;醯胺化