Chemical and pharmaceutical bulletin p. 2556 - 2564 (1994)
Update date:2022-08-04
Topics:
Kato
Nishino
Ito
Yamakuni
Takasugi
A series of pyrimido[1,6-alpha]indol-1(2H)-ones was prepared and evaluated for 5-HT3 receptor antagonist activity. The compounds in this series were regarded as bioisosters of the pyrido[1,2-alpha]indol-6(7H)-ones previously reported. High potency was found for compounds having 5-methyl substituents on both the pyrimido[1,6-alpha]indole ring and the imidazole ring. Optimized members of this series, 8b and (+)-26a, were potent 5-HT3 receptor antagonists as determined by measuring inhibition of the Bezold-Jarisch reflex in anesthetized rats (ED50 0.6 and 0.8 microgram/kg i.v., respectively), being equipotent to or more potent than FK 1052 (1) in the previous paper and 20- to 30-fold more potent than ondansetron (2).
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Doi:10.1016/0277-5387(94)00468-T
(1995)Doi:10.1002/jps.2600530918
(1964)Doi:10.1021/ja01583a044
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(1995)
