SYNTHESIS AND ANTIMICROBIAL ACTIVITY OF PYRIMIDINYLUREIDOCEPHALOSPORINS

The synthesis of a series of 7R-[(R)-2-[3-[5-pyrimidinyl]ureido]-2-(aryl)acetamido]-3-cephem-4-carboxylates is described. Variation of the substituents at the 3-position in the cephem nucleus, at the 2-position of the pyrimidine ring, and of the phenyl residue in the acyl side chain is carried out....

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Veröffentlicht in:	Journal of antibiotics 1985, Vol.38(6), pp.740-745
Hauptverfasser:	WETZEL, B., WOITUN, E., MAIER, R., REUTER, W., LECHNER, U.
Format:	Artikel
Sprache:	eng
Schlagworte:	Bacteria - drug effects Cephalosporins - chemical synthesis Cephalosporins - pharmacology Chemical Phenomena Chemistry Exact sciences and technology Heterocyclic compounds Heterocyclic compounds with n hetero atom and also o and/or s, se, te hetero atoms Organic chemistry Preparations and properties Structure-Activity Relationship
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Beschreibung
Zusammenfassung:	The synthesis of a series of 7R-[(R)-2-[3-[5-pyrimidinyl]ureido]-2-(aryl)acetamido]-3-cephem-4-carboxylates is described. Variation of the substituents at the 3-position in the cephem nucleus, at the 2-position of the pyrimidine ring, and of the phenyl residue in the acyl side chain is carried out. Qualitative structure-activity relationships in this series are discussed. VX-VD 2, the most interesting compound, exhibits broad antimicrobial activity against Gram-negative bacteria, including Pseudomonas aeruginosa.
ISSN:	0021-8820 1881-1469
DOI:	10.7164/antibiotics.38.740