79889-86-4Relevant academic research and scientific papers
Inhibitors of apoptosis in lymphocytes: Synthesis and biological evaluation of compounds related to pifithrin-α
Barchéchath, Sylvie D.,Tawatao, Rommel I.,Corr, Maripat,Carson, Dennis A.,Cottam, Howard B.
, p. 6409 - 6422 (2007/10/03)
The chemoprotection of cells from apoptosis induced by toxins or ionizing radiation could be important for biodefense and in the treatment of acute injuries. We describe a series of small heterocycles, including fused benzothiazoles, benzimidazoles, and related compounds, that abrogate thymocyte apoptosis induced by dexamethasone and γ-irradiation. To optimize the protective activity of the previously reported pifithrin-α (PFT-α, 1), various derivatives and analogues of this and the corresponding ring-closed imidazobenzothiazole (IBT, 39) were synthesized. The aromatic analogues of 39 were more protective than 39, while the aromatic analogues of 1 were not active. Compound 19 containing a pyrrolidinyl substituent on the phenyl ring provided potent antiapoptotic activity (EC50 of 1.31 μM compared to 4.16 μM for 1). Modification of aromatic 39 with a pyrrolidinyl para substituent (compound 60) enhanced the activity, lowering the EC50 to 0.35 μM. Also, 60 provided significant protection against γ-irradiation-induced apoptosis, as expected. Compounds 19 and 60 may be promising for potential clinical development.
DIHYDRO-5,6 IMIDAZOTHIAZOLES, DIHYDRO-2,3 IMIDAZOBENZOTHIAZOLES, ANALOGUES DU LEVAMISOLE
Amarouch, H.,Loiseau, P. R.,Bonnafous, M.,Caujolle, R.,Payard, M.,et al.
, p. 421 - 438 (2007/10/02)
New compounds containing 5,6-dihydro imidazothiazole 2,3,5,6-tetrahydro imidazothiazole and 2,3-dihydro imidazobenzothiazole rings, substituted by heterocycles analogue to chromones, were synthesized and screened against three nematodes, in vitro.The results indicate moderate anthelmintic properties, compared to levamisole; nevertheless, some products exhibit a significant degree of activity.
Imidazobenzothiazoles. 2. New Immunosuppressive Agents
Mase, Toshiyasu,Arima, Hideki,Tomioka, Kenichi,Yamada, Toshimitsu,Murase, Kiyoshi
, p. 386 - 394 (2007/10/02)
A series of 2-phenylimidazobenzothiazole 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)imidazobenzothiazole (20).
