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- W1964989607 abstract "The anti-H. influenzae activity of meropenem (1a) was much higher than those of imipenem (4). panipenem (2b) and biapenem (7). To clarify the major structural features responsible for the anti-H. influenzae activity of carbapenem compounds, the structure-activity relationship to the anti-H. influenzae activity was investigated. The anti-H. influenzae activities of meropenem (1a) and 1 beta-methyl-panipenem (2a) were much higher than those of desmethyl-meropenem (1b) and panipenem (2b). respectively. Two carbapenems (5, 6) and imipenem (4), that have a strong basic C-2 side chain, showed lower anti-H. influenzae activity than meropenem (1a) having a weakly basic C-2 side chain and N-acetyl thienamycin (3) having a neutral C-2 side chain, respectively. As a result, we found that the introduction of the 1 beta-methyl group or the reduction of the basicity (cationic character) of the C-2 side chain increased the antimicrobial activity and bactericidal activity of carbapenems against H. influenzae due to their increased affinity for PBP-4 and PBP-5." @default.
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- W1964989607 date "1997-01-01" @default.
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- W1964989607 title "Structure-activity Relationships of Carbapenem Compounds to Anti-Haemophilus influenzae Activity and Affinity for Penicillin-binding Proteins Effect of 1.BETA.-Methyl Group and C-2 Side Chain." @default.
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- W1964989607 doi "https://doi.org/10.7164/antibiotics.50.162" @default.
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