New fatty monoesters of erythromycin A.
作者:Michel PHILIPPE、Alain CAMPOS、Henri SEBAG、Andre ROUGIER、Didier DUPUIS、Didier SAINT-LEGER、Guy VANLERBERGHE
DOI:10.1248/cpb.38.1672
日期:——
New fatty polynic (linoleic, linolenic, arachidonic, linoelaidic) mono esters of erythromycin A have been synthesized by using various reagents such as acyl chloride, carboxylic acid anhydride, and mixed carbonic anhydride. These different ways of activating the fatty acid allowed a regioselectivity of esterification at position 2' of the desosamine ring or position 4" of the cladinose ring of erythromycin A. The in vitro antibacterial properties of these new esters against members of the resident flora of the human skin were determined and compared with those of erythromycin A. The number and the stereochemistry of the double bonds seem to play a crucial role in the expression of thei n vitro antibacterial activity.
通过使用各种试剂(如酰基氯、羧酸酐和混合碳酐)合成了新的红霉素 A 脂肪多炔(亚油酸、亚麻酸、花生四烯酸和亚麻酸)单酯。测定了这些新酯对人体皮肤常住菌群的体外抗菌特性,并将其与红霉素 A 的抗菌特性进行了比较。双键的数量和立体化学似乎在体外抗菌活性的表现中起着至关重要的作用。