Nabata Hiroyuki

Design of potent K+ channel openers by pharmacophore model

Abstract A pharmacophore model which explains rationally structure-activity relationships of chemically diverse potent K + channel openers, has been constructed. Potent benzopyran derivatives with thioamide, amide, and ( N -cyano)amidine groupa at the 4-position have been designed using the model.

N,N-disubstituted benzopyran-4-(N′-cyano)carboxamidines, cromakalim analogs with selective activity for guinea pig trachealis

N-Cyano-2,2-dimethyl-6-nitro-2H-1-benzopyran-4-carboxamidines have been synthesized. Some of these compounds exhibited selective activity for guinea pig trachealis.

Substituent effects of benzopyran-4-(N-cyano)-carboxamidine potassium channel openers for selectivity to guinea pig trachealis

Abstract 6-Substituted benzopyran-4-(N-cyano)amidines 1 and their analogs have been synthesized. Some of these compounds, 1a, 1e, and 1f exhibited selective activity for guinea pig trachealis.