Pyrimidinone antibiotics--heterocyclic analogues with improved antibacterial spectrum.
We report the synthesis and pharmacological evaluation of new derivatives of the natural dipeptide antibiotic TAN 1057 A,B containing heterocycles either in the beta-amino acid side chain or as mimics of the urea function. In the course of this program, we identified novel analogues that display activity towards a broader panel of Gram-positive bacteriae.
Brands
Michael
M
BAYER AG, Business Group Pharma, Research, D-42096, Wuppertal, Germany. michael.brands.b@nayer.com
Grande
Yolanda Cancho
YC
Endermann
Rainer
R
Gahlmann
Reinhold
R
Krüger
Jochen
J
Raddatz
Siegfried
S
D000596:Amino Acids / Q000737:chemistry; D000900:Anti-Bacterial Agents / Q000138:chemical synthesis* / Q000494:pharmacology; D004151:Dipeptides / Q000138:chemical synthesis* / Q000494:pharmacology; D006094:Gram-Positive Bacteria / Q000187:drug effects; D006571:Heterocyclic Compounds / Q000138:chemical synthesis* / Q000494:pharmacology; D008826:Microbial Sensitivity Tests; D015394:Molecular Structure; D011744:Pyrimidinones / Q000138:chemical synthesis* / Q000494:pharmacology; D013237:Stereoisomerism; D014508:Urea / Q000737:chemistry
D000596:Amino Acids; D000900:Anti-Bacterial Agents; D004151:Dipeptides; D006571:Heterocyclic Compounds; D011744:Pyrimidinones; C081415:TAN 1057A; C081416:TAN 1057B; D014508:Urea