UNUSUAL TRANSFORMATION OF THE 3-HYDROXY-PICOLINOYL RESIDUE OF PRISTINAMYCIN I-A

被引:2
作者
PARIS, JM [1 ]
FRANCOIS, J [1 ]
MOLHERAT, C [1 ]
ALBANO, F [1 ]
ROBIN, M [1 ]
VUILHORGNE, M [1 ]
BARRIERE, JC [1 ]
机构
[1] RHONE POULENC RORER SA,CTR RECH VITRY ALFORTVILLE,F-94403 VITRY,FRANCE
关键词
D O I
10.7164/antibiotics.48.676
中图分类号
Q81 [生物工程学(生物技术)]; Q93 [微生物学];
学科分类号
071005 ; 0836 ; 090102 ; 100705 ;
摘要
Pristinamycin I-A was modified in a two-step procedure to give original derivatives possessing a tricyclic nucleus (8a, 8b, 8c) or a substituted pyrrole ring (10a, 10b) in place of the natural exocyclic 3-hydroxy-picolinoyl residue. This transformation involved firstly preparation of pyridinium betaines 5 from pristinamycin I-A and secondly a 1 similar to 3 dipolar cycloaddition between 5 and N-substituted maleimides or diethyl acetylenedicarboxylate. The compounds obtained were evaluated as antibacterial agents alone and in association with pristinamycin IIA.
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页码:676 / 682
页数:7
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