7537-09-9Relevant academic research and scientific papers
8-(4-Methoxyphenyl)pyrazolo[1,5-a]-1,3,5-triazines: Selective and centrally active corticotropin-releasing factor receptor-1 (CRF1) antagonists
Gilligan, Paul J.,He, Liqi,Clarke, Todd,Tivitmahaisoon, Parcharee,Lelas, Snjezana,Li, Yu-Wen,Heman, Karen,Fitzgerald, Lawrence,Miller, Keith,Zhang, Ge,Marshall, Anne,Krause, Carol,McElroy, John,Ward, Kathyrn,Shen, Helen,Wong, Harvey,Grossman, Scott,Nemeth, Gregory,Zaczek, Robert,Arneric, Stephen P.,Hartig, Paul,Robertson, David W.,Trainor, George
scheme or table, p. 3073 - 3083 (2010/01/16)
This report describes the syntheses and structure-activity relationships of 8-(4-methoxyphenyl)pyrazolo-[1,5-a]-1,3,5-triazine corticotropin releasing factor receptor-1 (CRF1) receptor antagonists. CRF1 receptor antagonists may be potential anxiolytic or antidepressant drugs. This research culminated in the discovery of analogue 12-3, which is a potent, selective CRF1 antagonist (hCRF1 IC50 ) 4.7 ± 2.0 nM) with weak affinity for the CRF-binding protein and biogenic amine receptors. This compound also has a good pharmacokinetic profile in dogs. Analogue 12-3 is orally effective in two rat models of anxiety: the defensive withdrawal (situational anxiety) model and the elevated plus maze test. Analogue 12-3 has been advanced to clinical trials.
PHOTOREACTION OF PHTHALIMIDES POSSESSING AN ORTHO-METHYLPHENYL GROUP IN THEIR N-SIDE CHAIN. SYNTHESIS OF TETRACYCLIC NITROGEN HETEROCYCLES
Machida, Minoru,Nakamura, Mayumi,Oda, Kazuaki,Takechi, Haruko,Ohno, Kosei,et al.
, p. 2683 - 2690 (2007/10/02)
Upon irradiation phthalimides (5 and 8) possesing o-methylphenyl group in their N-side chain gave mainly the tetracyclic ring systems (9 and 10).It was shown that the photocyclization occurs at ε- or ζ-position across the carbons of the benzene ring (B-ring).
