14446-24-3Relevant academic research and scientific papers
Light-Driven Intramolecular C?N Cross-Coupling via a Long-Lived Photoactive Photoisomer Complex
Jing, Dong,Lu, Cong,Chen, Zhuo,Jin, Songyang,Xie, Lijuan,Meng, Ziyi,Su, Zhishan,Zheng, Ke
, p. 14666 - 14672 (2019/09/06)
Reported herein is a visible-light-driven intramolecular C?N cross-coupling reaction under mild reaction conditions (metal- and photocatalyst-free, at room temperature) via a long-lived photoactive photoisomer complex. This strategy was used to rapidly prepare the N-substituted polycyclic quinazolinone derivatives with a broad substrate scope (>50 examples) and further exploited to synthesize the natural products tryptanthrin, rutaecarpine, and their analogues. The success of gram-scale synthesis and solar-driven transformation, as well as promising tumor-suppressing biological activity, proves the potential of this strategy for practical applications. Mechanistic investigations, including control experiments, DFT calculations, UV-vis spectroscopy, EPR, and X-ray single-crystal structure of the key intermediate, provides insight into the mechanism.
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.
COMPOUNDS AND COMPOSITIONS AS MODULATORS OF GPR119 ACTIVITY
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Page/Page column 24-25, (2009/10/18)
The invention provides compounds, pharmaceutical compositions comprising such compounds and methods of using such compounds to treat or prevent diseases or disorders associated with the activity of GPR119.
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.
Structure activity relationship studies of carboxamido-biaryl ethers as opioid receptor antagonists (OpRAs). Part 2
Takeuchi, Kumiko,Holloway, William G.,Mitch, Charles H.,Quimby, Steven J.,McKinzie, Jamie H.,Suter, Todd M.,Statnick, Michael A.,Surface, Peggy L.,Emmerson, Paul J.,Thomas, Elizabeth M.,Siegel, Miles G.
, p. 6841 - 6846 (2008/09/17)
A series of 6-bicycloaryloxynicotinamides were identified as opioid receptor antagonists at mu, kappa, and delta receptors. Compounds in the 6-(2,3,4,5-tetrahydro-1H-benzo[c]azepin-7-yloxy)nicotinamide scaffold exhibited potent in vitro functional antagonism at all three receptors.
Naphthamidine urokinase inhibitors
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, (2008/06/13)
Compounds having the formula: are inhibitors of urokinase and are useful in the treatment of diseases in which urokinase plays a role. Also disclosed are urokinase-inhibiting compositions, methods for the preparation of urokinase-inhibitors, and a method of inhibiting urokinase in a mammal.
Naphthamidine urokinase inhibitors
-
, (2008/06/13)
Compounds having the formula are inhibitors of urokinase and are useful in the treatment of diseases in which urokinase plays a role. Also disclosed are urokinase-inhibiting compositions, methods for the preparation of urokinase-inhibitors, and a method of inhibiting urokinase in a mammal.
