The design of a novel class of potassium channel activating drugs, 2-(2,2-dimethylbenzopyran-4-yl)-pyridine-1-oxides.
The features of cromakalim responsible for its potassium channel activating property were investigated. A hypothesis relating three-dimensional structure to binding to a putative receptor was developed and used successfully to design the potent and structurally novel agents, 2-(2,2-dimethylbenzopyran-4-yl)-pyridine-1-oxides.
Attwood
M R
MR
Roche Products Limited, Welwyn Garden City, Herts, UK.
Jones
P S
PS
Kay
P B
PB
Paciorek
P M
PM
Redshaw
S
S
D000818:Animals; D001578:Benzopyrans / Q000494:pharmacology*; D001993:Bronchodilator Agents / Q000494:pharmacology; D055598:Chemical Phenomena; D002621:Chemistry; D019806:Cromakalim; D003497:Cyclic N-Oxides / Q000494:pharmacology*; D015195:Drug Design; D066298:In Vitro Techniques; D008297:Male; D015221:Potassium Channels / Q000187:drug effects*; D011725:Pyridines / Q000494:pharmacology*; D011758:Pyrroles / Q000494:pharmacology; D051381:Rats; D011919:Rats, Inbred Strains; D014665:Vasodilator Agents / Q000494:pharmacology
D001578:Benzopyrans; D001993:Bronchodilator Agents; D003497:Cyclic N-Oxides; D015221:Potassium Channels; D011725:Pyridines; D011758:Pyrroles; D014665:Vasodilator Agents; D019806:Cromakalim