14446-24-3Relevant articles and documents
Effect of pH on the Regioselectivity of Pictet-Spengler Reactions of 3-Hydroxyphenethylamines with Formaldehyde and Acetaldehyde
Bates, Hans A.,Bagheri, Kourosh,Vertino, Paula M.
, p. 3061 - 3063 (1986)
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Discovery of tetrahydroisoquinoline (THIQ) derivatives as potent and orally bioavailable LFA-1/ICAM-1 antagonists
Zhong, Min,Shen, Wang,Barr, Kenneth J.,Arbitrario, Jennifer P.,Arkin, Michelle R.,Bui, Minna,Chen, Teresa,Cunningham, Brian C.,Evanchik, Marc J.,Hanan, Emily J.,Hoch, Ute,Huen, Karen,Hyde, Jennifer,Kumer, Jeffery L.,Lac, Teresa,Lawrence, Chris E.,Martell, Jose R.,Oslob, Johan D.,Paulvannan, Kumar,Prabhu, Saileta,Silverman, Jeffrey A.,Wright, Jasmin,Yu, Chul H.,Zhu, Jiang,Flanagan, W. Mike
scheme or table, p. 5269 - 5273 (2010/10/18)
This letter describes the discovery of a novel series of tetrahydroisoquinoline (THIQ)-derived small molecules that potently inhibit both human T-cell migration and super-antigen induced T-cell activation through disruption of the binding of integrin LFA-1 to its receptor, ICAM-1. In addition to excellent in vitro potency, 6q shows good pharmacokinetic properties and its ethyl ester (6t) demonstrates good oral bioavailability in both mouse and rat. Either intravenous administration of 6q or oral administration of its ethyl ester (6t) produced a significant reduction of neutrophil migration in a thioglycollate-induced murine peritonitis model.
Carbon-11 labeled indolylpropylamine analog as a new potential PET agent for imaging of the serotonin transporter
Ben-Daniel,Deuther-Conrad,Scheunemann,Steinbach,Brust,Mishani
, p. 6364 - 6370 (2008/12/21)
The synthesis and structure-activity relationship of a new class of indole derivatives with low-nanomolar affinity for the SERT and high selectivity versus the 5-HT1A receptor were recently reported. Based on their chemical structure, four new indolylpropylamine derivatives which contain atoms to afford future labeling with PET isotopes, were synthesized and evaluated as SERT ligands. The chemistry of these novel derivatives, their biological evaluation, the general method of preparing the precursor indole for labeling, and the C-11 labeling of the most promising indole derivative, are described herein.