80526-44-9Relevant articles and documents
SYNTHESIS OF 2-AMINOBENZOXAZOLE COMPOUNDS
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Page/Page column 7, (2010/05/13)
A method for forming an optionally substituted 2-aminobenzoxazole compound includes: contacting an optionally substituted 2-aminophenol compound with (1) an amine of the formula NHR2R3, wherein R2 and R3 are each independently selected from H, an optionally substituted alkyl group or an optionally substituted aryl group, or R2 and R3, taken together with the nitrogen atom to which they are attached, form an optionally substituted heterocyclic ring; and (2) a reactant selected from the group consisting of: (a) C(OR)4, wherein R represents an alkyl group; (b) C(OAr)4, wherein Ar represents an aryl group; and (c) CCl2(OAr)2, wherein Ar represents an aryl group, in combination with a base; thereby forming the optionally substituted 2-aminobenzoxazole compound.
Regulatory molecules for the 5-HT3 receptor ion channel gating system
Yoshida, Satoshi,Watanabe, Takashi,Sato, Yasuo
, p. 3515 - 3523 (2008/02/07)
Substituted benzoxazole derivatives which possess a nitrogen-containing heterocycle at C2 are selective partial agonists of the 5-HT3 receptor. Alteration of substituents on the benzoxazole nucleus affords both agonist-like and antagonist-like compounds, and uniquely modifies the function of the 5-HT3 receptor ion channel gating system. SAR and corroborative computational docking study for these partial agonists successfully explained structure and function of the 5-HT3 receptor.
Orally active benzoxazole derivative as 5-HT3 receptor partial agonist for treatment of diarrhea-predominant irritable bowel syndrome
Yoshida, Satoshi,Shiokawa, Sojiro,Kawano, Ken-Ichi,Ito, Tomoko,Murakami, Hiroshi,Suzuki, Hisashi,Sato, Yasuo
, p. 7075 - 7079 (2007/10/03)
During our search for therapeutic agents to treat diarrhea-predominant IBS, we found that 2-substituted benzoxazole derivatives have a characteristic 5-HT3 receptor partial agonist activity with high affinity. Some of these compounds showed high in vitro metabolical stability, and 6g showed marked antidiarrhetic activity with little side effect of constipation in in vivo tests. Our results indicate that 5-HT3 receptor partial agonists might be superior as therapeutic agents to the drugs currently used for IBS treatment.