Effect of YM-11124 on cell-mediated immune responses, type I to type III allergic reactions and inflammatory reaction was determined in mice, rats and guinea pigs. YM-11124 inhibited picryl chloride- and methylated bovine serum albumin-induced delayed-type hypersensitivity reactions by the treatment during both the sensitization and the elicitation phases in mice. Bilateral adrenalectomy did not prevent the suppression of DTH response by YM-11124. YM-11124 significantly prolonged the survival time of allogenic skin grafts in mice. Furthermore, YM-11124 inhibited the passive Arthus reaction in guinea pigs and the reversed passive Arthus reaction in rats. However, YM-11124 did not affect the passive cutaneous anaphylaxis reaction in rats, Forssman shock in guinea pigs and paw edema in rats. These results indicate that YM-11124 suppresses not only cell-mediated immune responses (type IV allergic reactions) but also type III allergic reactions without influence on types I and II allergic reactions as well as acute inflammation.

01 Jul 1988·EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY

Imidazo[2,1-b]benzothiazoles 3: syntheses and immunosuppressive activities of 2-(m-acyloxyphenyl)imidazo[2,1-b]benzothiazoles

Author: Hideki Arima ; Kenichi Tomioka ; Kiyoshi Murase ; Toshiyasu Mase ; Toshimitsu Yamada

A series of acyl derivatives e.g., I [R = Me, Et, CO₂H (CH₂)_nCO₂H, CH:CHCO₂R¹, CH₂NH₂, CH₂NMe₂, (CH₂)₂NH₂; n = 1-3; R¹ = H, Et] of 2-(m-hydroxyphenyl)imidazo[2,1-b]benzothiazole (II), a selective immunosuppressive agent for delayed type hypersensitivity (DTH), was prepared and tested for its suppressive activity of DTH in mice after oral administration.Six compounds were more potent immunosuppressive agents than II but they showed no effect on humoral immunity as in the case of II.

01 Mar 1986·Journal of medicinal chemistryQ1 · MEDICINE

Imidazo[2,1-b]benzothiazoles. 2. New immunosuppressive agents

Q1 · MEDICINE

Article

Author: Arima, Hideki ; Mase, Toshiyasu ; Murase, Kiyoshi ; Tomioka, Kenichi ; Yamada, Toshimitsu

A series of 2-phenylimidazo[2,1-b]benzothiazole derivatives was prepared and tested for immunological activities. Some of the compounds showed significant suppressive activity of delayed type hypersensitivity (DTH) without inhibition of humoral immunity in mice by oral administration. The most active compound was 2-(m-hydroxyphenyl)imidazo[2,1-b]benzothiazole (20).

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Indication	Highest Phase	Country/Location	Organization	Date
Anaphylaxis	Preclinical	Japan	Yamanouchi Pharmaceutical Co., Ltd.	-

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