申请人:Gruppo Lepetit S.p.A.
公开号:US05786350A1
公开(公告)日:1998-07-28
Rifamycin antibiotic derivatives of formulae (I) and (Ia) bearing at the position 36 a substituent selected from (C.sub.1 -C.sub.8)alkyl, halo, hydroxy, (C.sub.1 -C.sub.4)acyloxy, (C.sub.1-C.sub.4)alkoxy, (C.sub.1 -C.sub.4)alkylthio, (C.sub.1 -C.sub.4)alkylamino, di(C.sub.1-C.sub.4)alkylamino and substituted 4-oxo-3-pyridinyl carbonyloxy of formula (1) obtained by reacting rifamycin with suitably substituted malonic acid. The compounds of the invention are antimicrobial agents mainly active against gram positive bacteria and fastidious gram negative bacteria showing the considerable antimicrobial activity against the rifamypicin resistant microbial strains.
公式(I)和(Ia)的利福霉素抗生素衍生物,在36号位置带有从(C.sub.1-C.sub.8)烷基,卤素,羟基,(C.sub.1-C.sub.4)酰氧基,(C.sub.1-C.sub.4)烷氧基,(C.sub.1-C.sub.4)烷基硫基,(C.sub.1-C.sub.4)烷基氨基,二(C.sub.1-C.sub.4)烷基氨基和公式(1)的取代4-氧代-3-吡啶基羰氧基。本发明化合物是主要对革兰氏阳性菌和难培养的革兰氏阴性菌具有抗微生物活性的抗菌剂,并对利福霉素耐药微生物菌株表现出相当的抗微生物活性。