The Journal of Antibiotics
Online ISSN : 1881-1469
Print ISSN : 0021-8820
ISSN-L : 0021-8820
SYNTHESIS AND STRUCTURE-ACTIVITY RELATIONSHIPS OF SOME 6β-ACRYLAMIDO PENICILLINS
RICHARD K. ANDERSON, PAULINE C. CHAPMAN, SUZANNE C. COSHAM, J. SYDNEY DAVIES, TREVOR J. GRINTER, MICHAEL A. HARRIS, DAVID J. MERRIKIN, CHRISTINA A. MITCHELL, ROGER J. PONSFORD, CAROL F. SMITH, ANDREW V. STACHULSKI
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1993 Volume 46 Issue 2 Pages 331-342

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Abstract

Syntheses are described for penicillins (4b-4i, 5a and 5b) which possess a 6β-(2-heteroaryl-3-substituted)-propenamido side-chain of fixed geometry. In vitro results for these compounds against a range of Gram-positive and Gram-negative bacteria showed in most cases good stability against both penicillinase and TEM-1 β-lactamase; analogues (4b-4i) bearing a 2-(2-aminothiazol-4-yl) unit showed the best intrinsic activity, the cyclohexyl compound (4b) being the most promising. The 1-acetoxyethyl ester (6) of 4b was also prepared; in experimental animal studies the in vivo properties of this compound compared favourably with cefuroxime axetil and are reported together with selected in vivo data for the other compounds.

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The Journal of Antibiotics, Series A

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