Biaryl acids

Screening efforts at Merck have identified structurally novel biaryl acid analogues as PDF inhibitors (21, 22, 23) [102]. These compounds contain several aromatic rings and belong to a broad class of angiotensin II receptor antagonists. The analogues reported possess inhibitory activity versus E. coli PDF in the 1-50 mM range, with substitution at various regions of the molecule appearing feasible. All the inhibitors contain an acidic pharmacoph-ore, including tetrazole, carboxylate, acyl sulfonamide and carboxamide. Tetrazole and acyl sulfonamide appeared to provide the best potency, although the data set was small and the differences were not dramatic. The antibacterial activity of these compounds was not reported.

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