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Your search keyword '"NOWAKOWSKI, J. T."' showing total 3 results
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3 results on '"NOWAKOWSKI, J. T."'

1. ChemInform Abstract: Thiazole as a Carbonyl Bioisostere. A Novel Class of Highly Potent and Selective 5‐HT3 Receptor Antagonists.

Author

ROSEN, T., primary, NAGEL, A. A., additional, RIZZI, J. P., additional, IVES, J. L., additional, DAFFEH, J. B., additional, GANONG, A. H., additional, GUARINO, K., additional, HEYM, J., additional, MCLEAN, S., additional, NOWAKOWSKI, J. T., additional, SCHMIDT, A. W., additional, SEEGER, T. F., additional, SIOK, C. J., additional, and VINCENT, L. A., additional

Published
1991
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3. Thiazole as a carbonyl bioisostere. A novel class of highly potent and selective 5-HT3 receptor antagonists.

Author

Rosen T, Nagel AA, Rizzi JP, Ives JL, Daffeh JB, Ganong AH, Guarino K, Heym J, McLean S, and Nowakowski JT

Subjects
Administration, Oral, Animals, Computer Graphics, In Vitro Techniques, Mice, Models, Molecular, Neurons metabolism, Radioligand Assay, Rats, Receptors, Serotonin classification, Serotonin Antagonists metabolism, Serotonin Antagonists pharmacology, Structure-Activity Relationship, Thiazoles administration & dosage, Thiazoles chemistry, Tumor Cells, Cultured, Receptors, Serotonin drug effects, Serotonin Antagonists chemical synthesis, Thiazoles pharmacology
Abstract

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.

Published
1990
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