Imidazothiazole derivatives. XI. Modulation of the CD2-receptor of human T trypsinized lymphocytes by several imidazothiazoles

Article abstract of DOI:10.1016/0223-5234(94)90101-5

About 40 substituted imidazo<2,1-b>thiazoles were obtained in order to study their in vitro immunological effect on the modulation of the expression of human T trypsinized lymphocytes by the CD₂ receptor.A synthetic program was developed to introduce either an oxygenated function, such as ester (11, 14), acid (12) and arylketonic groups (9, 13, 15), or two groups, such as an aryl and an ester (1, 6, 8), an acid (3, 7) or a hydrazide (2).These compounds were examined by an E-rosette-forming-cell test, and display a positive drug efficacity index, suggesting a regeneration effect on the expression of CD₂ receptors.The following structural parameters are favourable: an aryl moiety on the C-6 with a methoxy or nitro group: and an ethyl ester on the C-3, a double bond to the 2,3-position (the 5,6-position is ineffective).Acid and hydrazide functions or the loss of phenyl group on the C-6 decrease this activity.If the aryl group is on the C-3 or C-2 side chain, the activity is weaker and more so for the latter.However, the most interesting derivatives are less immunostimulating than levamisole hydrochloride. immunomodulator / imidazo<2,1-b>thiazole / human T lymphocyte / CD₂ receptor