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Structure-activity relationships of penem antibiotics: Crystallographic structures and implications for their antimicrobial activities by Rie Tanaka; Yoshiaki Oyama; Seiichi Imajo; Shinsuke Matsuki; Masaji Ishiguro is a Biochemistry, Genetics and Molecular Biology article available to read on EtoBox.

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Twelve closely related crystal structures of the penem derivatives revealed a characteristic short contact of the oxygen atom in the C2 side-chains with the SI atom. The side-chain conformations of the crystal structures showed a good correlation with the antimicrobial activity. In particular, the penems which show high antimicrobial activity have similar torsion angles for S1-C2-C1'-C2', suggesting that the disposition of the C2' atom would be important for binding to penicillin-interacting enzymes. Two conformations of the C6 hydroxyethyl group were observed in the crystal structures. Of those two, the conformation with a larger torsion angle (8 = 179.2 °) is deduced to be the enzyme-bound conformation in the Michaelis complex. (~, 1997 Elsevier Science Ltd.

Who reads Structure-activity relationships of penem antibiotics: Crystallographic structures and implications for their antimicrobial activities?

Author

Rie Tanaka; Yoshiaki Oyama; Seiichi Imajo; Shinsuke Matsuki; Masaji Ishiguro

Publisher

Elsevier Science; Elsevier ; Elsevier Ltd.; Elsevier BV (ISSN 0968-0896)

Published

1997

Language

EN

Field

Biochemistry, Genetics and Molecular Biology (Life Sciences)