The Chemistry of Pseudomonic Acid Part 14 Synthesis and <i>In Vivo</i> Biological Activity of Heterocyclyl Substituted Oxazole Derivatives

N. J. P. BROOM; J. S. ELDER; P. C. T. HANNAN; J. E. PONS; P. J. O'HANLON; G. WALKER; J. WILSON; P. WOODALL

doi:10.7164/antibiotics.48.1336

The Chemistry of Pseudomonic Acid Part 14

Synthesis and In Vivo Biological Activity of Heterocyclyl Substituted Oxazole Derivatives

N. J. P. BROOM, J. S. ELDER, P. C. T. HANNAN, J. E. PONS, P. J. O'HANLON, G. WALKER, J. WILSON, P. WOODALL

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JOURNAL FREE ACCESS

1995 Volume 48 Issue 11 Pages 1336-1344

DOI https://doi.org/10.7164/antibiotics.48.1336

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Abstract

Semisynthetic analogues of pseudomonic acid A have been prepared containing a heterocyclyl substituted oxazole. Derivatives in which the heterocycle was thiophene, furan, pyridine, or isoxazole showed good antibacterial potency and were further evaluated in vivo. Both pharmacokinetic parameters and oral activity against an experimental intraperitoneal sepsis were superior to results obtained from previously described pseudomonic acid A derivatives.

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