- A novel series of 6-methoxy-1H-benzotriazole-5-carboxamide derivatives with dual antiemetic and gastroprokinetic activities
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A novel series of 6-methoxy-1H-benzotriazole-5-carboxamide derivatives with a medium perhydroazacycle ring in the amine moiety were prepared, and their antiemetic and gastroprokinetic activities were evaluated. Among them, N-(1-ethylhexahydroazepin-3-yl)-, N-(1-ethyloctahydroazocin-3-yl)- and N-(1- ethyloctahydroazonin-3-yl)-6-methoxy-1H-benzotriazole-5-carboxamides (24, 36, 37) showed a potent antiemetic activity (inhibition of apomorphine-induced emesis in dogs) along with gastroprokinetic activity (gastric emptying in rats).
- Hirokawa, Yoshimi,Yamazaki, Hiroshi,Yoshida, Naoyuki,Kato, Shiro
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p. 1973 - 1978
(2007/10/03)
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- Method for enhancing memory or correcting memory deficiency with arylamidopyrazolidines and arylamidodiazabicycloalkanes
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A pharmaceutical method for improving memory or correcting memory deficiency is disclosed, utilizing compounds having the formula: STR1 wherein m and n are zero and one and when m is zero, the dotted line represents a double bond; X is oxygen or sulfur; R1 and R2 are hydrogen, loweralkyl, phenyl or phenylloweralkyl, or R1 and R2 taken together may form a fused second ring with the nitrogen atoms having three or four methylene groups to which may be attached at any second ring carbon atom thereof, a loweralkyl or phenyl radical; R3 is hydrogen or loweralkyl; Ar is phenyl, pyridyl, furanyl, thienyl, methoxy-1H-benzotriazolyl, indolinyl, methoxyindolinyl, methoxypyrimidinyl, aminomethoxypyrimidinyl, 1,3-benzodioxolyl or naphthalenyl, the active optical isomers; and the pharmaceutically acceptable acid addition salts thereof.
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- Hydrolysis of the antiemetic drug alizapride
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First order rate constants of the hydrolysis of N-[(1-allyl-2-pyrrolidinyl)-methyl]-6-methoxy-1H-benzotriazole-5-carboxami de (alizapride, Vergentan) in acid and alkaline medium were determined. The activation energy observed in alkaline solution was 60.3 kJ.mol-1. The substance was not hydrolized in vitro by esterase, liver homogenate or plasma.
- Hoffmann,Jacobi
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p. 1714 - 1715
(2007/10/02)
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