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A Structure-Activity Relationship Study of Novel Phenylacetamides Which Are Sodium Channel Blockers

A Structure-Activity Relationship Study of Novel Phenylacetamides Which Are Sodium Channel Blockers

I Roufos, S Hays, R D Schwarz

J Med Chem. 1996 Mar 29;39(7):1514-20.

PMID: 8691482

Abstract:

A structure-activity relationship study of a series of novel Na(+) channel blockers, structurally related to N-[3-(2,6-dimethyl-1-piperidinyl)propyl]-alpha-phenylbenzeneacetamide (1, PD85639) is described. The diphenylacetic acid portion of the molecule was left unchanged throughout the study, while structural features in the amine portion and the amide alkyl linkage of the molecule were modified. The compounds were tested for inhibition of veratridine-stimulated Na(+) influx in CHO cells expressing type IIA Na(+) channels. Several derivatives show a trend toward more potent Na+ channel blockade activity with increasing lipophilicity of the amine portion of the molecule. The presence of a phenyl ring near the amine increases inhibitory potency. A three-carbon spacer between the amide and amine is optimal, and a secondary amide linkage is preferred.

Chemicals Related in the Paper:

Catalog Number	Product Name	Structure	CAS Number	Price
AP149838211	PD-85639		149838-21-1	Price

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