Study of the structure-activity relationships of new dihydropyridine derivatives.
The effects of structure around the 3- and 5-alkoxycarbonyl groups and the 2-carbamate groups of 4-(2,3-dichlorophenyl)-2-carbamoyloxymethyl dihydropyridine derivatives were investigated, concerning their vasodilating action, plasma level, hypotensive action and acute toxicity. High negative linear correlation was found between the plasma levels and the number of C atoms in esterifying alkyl groups in 3- and 5-positions of the dihydropyridine ring. High plasma levels and effective hypotensive action were found in compounds having lower alkyls as esterifying groups of 3- and 5-carboxyl groups, among 2-unsubstituted derivatives.
Suzuki
K
K
Central Research Laboratories, Banyu Pharmaceutical Co., Ltd., Tokyo, Japan.
Nagura
J
J
Shiratori
K
K
Murayama
B
B
Harada
N
N
Miyano
T
T
Takeya
K
K
D000818:Animals; D000959:Antihypertensive Agents; D001794:Blood Pressure / Q000187:drug effects; D002121:Calcium Channel Blockers / Q000097:blood / Q000494:pharmacology*; D003326:Coronary Circulation / Q000187:drug effects; D004095:Dihydropyridines / Q000097:blood / Q000494:pharmacology*; D066298:In Vitro Techniques; D007928:Lethal Dose 50; D008297:Male; D011817:Rabbits; D051381:Rats; D011918:Rats, Inbred SHR; D013329:Structure-Activity Relationship
D000959:Antihypertensive Agents; D002121:Calcium Channel Blockers; D004095:Dihydropyridines; C048962:NPK 1886