Antiinflammatory activity of 5,6-diaryl-2,3-dihydroimidazo[2,1-b]thiazoles. Isomeric 4-pyridyl and 4-substituted-phenyl derivatives
- 1 January 1984
- journal article
- research article
- Published by American Chemical Society (ACS) in Journal of Medicinal Chemistry
- Vol. 27 (1) , 72-75
- https://doi.org/10.1021/jm00367a014
Abstract
Isomeric 5(6)-(4-pyridyl)- and 6(5)-(4-substituted-phenyl)-2,3-dihydroimidazo[2,1-b]thiazoles were prepared by a mixed benzoin-imidazothione route, and their structures were assigned by spectral comparison to compounds of established substitution pattern. The structural assignment was confirmed by X-ray analysis. Examination of the compounds for antiinflammatory activity by an adjuvant arthritic rat assay revealed strikingly higher potencies for 1 analogous series than for their isomers. This selectivity was paralleled in the ability to stimulate cell-mediated immunity, as refected in an oxazolone-induced contact sensitivity model. A drug-receptor complex is proposed that requires at lest 3 sites of interactions.This publication has 1 reference indexed in Scilit: