| Literature DB >> 8978844 |
S E Draheim1, N J Bach, R D Dillard, D R Berry, D G Carlson, N Y Chirgadze, D K Clawson, L W Hartley, L M Johnson, N D Jones, E R McKinney, E D Mihelich, J L Olkowski, R W Schevitz, A C Smith, D W Snyder, C D Sommers, J P Wery.
Abstract
The preceding papers of this series detail the development of functionalized indole-3-acetamides as inhibitors of hnps-PLA2. We describe here the extension of the structure-activity relationship to include a series of indole-3-glyoxamide derivatives. Functionalized indole-3-glyoxamides with an acidic substituent appended to the 4- or 5-position of the indole ring were prepared and tested as inhibitors of hnps-PLA2. It was found that the indole-3-glyoxamides with a 4-oxyacetic acid substituent had optimal inhibitory activity. These inhibitors exhibited an improvement in potency over the best of the indole-3-acetamides, and LY315920 (6m) was selected for evaluation clinically as an hnps-PLA2 inhibitor.Entities:
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Year: 1996 PMID： 8978844 DOI： 10.1021/jm960487f
Source DB: PubMed Journal: J Med Chem ISSN： 0022-2623 Impact factor: 7.446