Dihydropyrimidinones--a new class of anti-staphylococcal antibiotics.
We report the synthesis and pharmacological evaluation of new derivatives of natural dipeptide antibiotic TAN-1057 A, B. In the course of this program, we identified novel analogues of the natural product that display similar antibacterial activity and showed improved tolerability.
Brands
Michael
M
BAYER AG, Business Group Pharma, Research, D-42096 Wuppertal, Germany.
Endermann
Rainer
R
Gahlmann
Reinhold
R
Krüger
Jochen
J
Raddatz
Siegfried
S
D000900:Anti-Bacterial Agents / Q000138:chemical synthesis* / Q000494:pharmacology*; D000970:Antineoplastic Agents / Q000138:chemical synthesis / Q000494:pharmacology; D004151:Dipeptides / Q000138:chemical synthesis / Q000737:chemistry / Q000494:pharmacology; D004354:Drug Screening Assays, Antitumor; D006801:Humans; D008264:Macrophages / Q000187:drug effects / Q000378:metabolism; D008826:Microbial Sensitivity Tests; D011500:Protein Synthesis Inhibitors / Q000138:chemical synthesis / Q000494:pharmacology; D011744:Pyrimidinones / Q000138:chemical synthesis* / Q000494:pharmacology*; D013210:Staphylococcus / Q000187:drug effects*; D013329:Structure-Activity Relationship; D014407:Tumor Cells, Cultured
D000900:Anti-Bacterial Agents; D000970:Antineoplastic Agents; D004151:Dipeptides; D011500:Protein Synthesis Inhibitors; D011744:Pyrimidinones; C081415:TAN 1057A