Aryloxy acetic acid diuretics with uricosuric activity. I. Polycyclic aryloxy acetic acids.
In order to obtain lead compounds for uricosuric diuretics, various polycyclic aryloxy acetic acids [isoindole derivative (7), quinazoline derivative (15), benzopyran derivative (20), xanthone derivative (24), benzofuran derivative (30) and indene derivative (36)] were prepared. These compounds were evaluated for diuretic activity in rats, uricosuric activity in rats and antihypertensive activity in 11-deoxycorticosterone acetate (DOCA)/salt hypertensive rats. Among the compounds, 20 showed potent diuretic, uricosuric and moderate antihypertensive activities. Therefore, we selected 20 as a lead compound for development of new uricosuric diuretics.
Kitagawa
M
M
Research Institute, Daiichi Pharmaceutical Co., Ltd., Tokyo, Japan.
Mimura
T
T
Tanaka
M
M
D000085:Acetates / Q000138:chemical synthesis* / Q000494:pharmacology; D000818:Animals; D004232:Diuretics / Q000138:chemical synthesis* / Q000494:pharmacology; D008297:Male; D051381:Rats; D011919:Rats, Inbred Strains; D014528:Uricosuric Agents / Q000138:chemical synthesis* / Q000494:pharmacology
D000085:Acetates; D004232:Diuretics; D014528:Uricosuric Agents