36-DERIVATIVES OF RIFAMYCINS AND THEIR USE AS ANTIMICROBIAL AGENTS
申请人:GRUPPO LEPETIT S.P.A.
公开号:EP0700399A1
公开(公告)日:1996-03-13
US5786350A
申请人:——
公开号:US5786350A
公开(公告)日:1998-07-28
[EN] 36-DERIVATIVES OF RIFAMYCINS AND THEIR USE AS ANTIMICROBIAL AGENTS<br/>[FR] DERIVES-36 DE RIFAMYCINES ET LEUR UTILISATION COMME AGENTS ANTI-MICROBIENS
申请人:GRUPPO LEPETIT S.P.A.
公开号:WO1994028002A1
公开(公告)日:1994-12-08
(EN) Rifamycin antibiotic derivatives of formulae (I) and (Ia) bearing at the position 36 a substituent selected from (C1-C8)alkyl, halo, hydroxy, (C1-C4)acyloxy, (C1-C4)alkoxy, (C1-C4)alkylthio, (C1-C4)alkylamino, di(C1-C4)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 also considerable antimicrobial activity against the rifampicin resistant microbial strains.(FR) L'invention concerne des dérivés antibiotiques de rifamycine selon les formules (I) et (Ia) comportant à la position 36 un substituant sélectionné parmi alkyle(C1-C8), halo, hydroxy, acyloxy(C1-C4), alkoxy(C1-C4), alkylthio(C1-C4), alkylamino(C1-C4), dialkylamino(C1-C4) et 4-oxo-3-pyridinyle carbonyloxy subsitué de formule (1). Ces dérivés sont obtenus par réaction de la rifamycine avec un acide malonique adéquatement substitué. Les composés selon cette invention constituent des agents antimicrobiens principalement actifs contre les bactéries à Gram positif et les bactéries délicates à Gram négatif. Ils montrent également une activité anti-microbienne considérable contre les souches microbiennes résistant à la rifampicine.
36-derivatives of rifamycins and their use as antimicrobial agents
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.