Journal of Medicinal Chemistry p. 2715 - 2720 (1990)
Update date:2022-08-02
Topics:
Rosen, Terry
Nagel, Arthur A.
Rizzi, James P.
Ives, Jeffrey L.
Daffeh, June B.
et al.
A novel structural class of highly potent and selective 5-HT3 receptor antagonists is described.The compounds in this new series contain a thiazole moiety linking an aromatic group and a nitrogen-containing basic region; the thiazole group appears to be acting as a carbonyl bioisostere in this system.An optimized member of this series, 4-(2-methoxyphenyl)-2-<<4(5)-methyl-5(4)-imidazolyl>methyl>thiazole (5), exhibits oral activity in the Bezold-Jarisch reflex paradigm comparable to or better than the standard agents ondansetron (1) and ICS-205-930 (2).Several of the structure-activity relationships are rationalized in terms of a computer pharmacophore model for 5-HT3 receptor binding.
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