Synthesis and structure-activity relationships in the cefpirome series. III. 7 Alpha-methoxy and 7 alpha-formamido analogues of cefpirome.
7 alpha-Methoxy and 7 alpha-formamido derivatives of cefpirome (HR 810) have been synthesized and tested in comparison with cefpirome and some analogues 1 against aerobic and anaerobic bacteria. Cefpirome and analogues 1 have good activity against Gram-positive and only limited activity against Gram-negative anaerobic bacteria. 7 alpha-Methoxy derivatives 2 show only a slight improvement of activity against Gram-negative anaerobes and are less active against all aerobes. Introduction of the 7 alpha-formamido group (compounds 3) results in an overall loss of activity towards both aerobic and anaerobic bacteria.
Lattrell
R
R
Hoechst AG, Pharma Forschung, Frankfurt/Main, FRG.
Duerckheimer
W
W
Limbert
M
M
D002511:Cephalosporins / Q000138:chemical synthesis* / Q000494:pharmacology; D055598:Chemical Phenomena; D002621:Chemistry; D006090:Gram-Negative Bacteria / Q000187:drug effects; D006094:Gram-Positive Bacteria / Q000187:drug effects; D009682:Magnetic Resonance Spectroscopy; D013329:Structure-Activity Relationship; D000097572:Cefpirome
D002511:Cephalosporins; D000097572:Cefpirome