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Chemical modification of nodulisporic acid A: preliminary structure-activity relationships
P T Meinke1, M B Ayer, S L Colletti
1Department of Medicinal Chemistry, Merck Research Laboratories, Rahway, NJ 07065-0900, USA. peter_meinke@merck.com
Bioorganic & Medicinal Chemistry Letters
|October 31, 2000
Abstract:
Medicinal chemistry efforts were initiated to identify the key constituents of the nodulisporic acid A (1) pharmacophore that are integral to its potent insecticidal activity. New semisynthetic derivatives delineated 1 into 'permissive' and 'nonpermissive' regions and led to the discovery of new nodulisporamides with significantly improved flea efficacy.