7-(Phenyl-substd cycloalkanoyl) penicillins - stable towards acids and penicillinase, and active against gram positive bacteria

摘要

New penicillins of formula (I) (R is H or opt. branched 1-4C alkoxy; X is a gp. n = 2,3 or 4; R1 = lower alkyl, aryl, halogen, NH2, NO2 or OH) are prepd. by reacting 6-APA with the corresp. acid. (I) and their salts are active against Gram positive bacteria including Stap-hylococci resistant to benzylpenicillin. They are stable towards both acids and penicillinase and are prepd. from readily available acylating agents. The alkoxy-substd. cpds. have very low toxicity e.g. single i.v. doses of 1.5-2.5g/kg are well-tolerated by white mice; the cpds. with R=H are relatively toxic.