52651-15-7Relevant academic research and scientific papers
Small-molecule phosphodiesterase probes: Discovery of potent and selective CNS-penetrable quinazoline inhibitors of PDE1
Humphrey, John M.,Yang, Eddie,Ende, Christopher W. Am,Arnold, Eric P.,Head, Jenna L.,Jenkinson, Stephen,Lebel, Lorraine A.,Liras, Spiros,Pandit, Jayvardhan,Samas, Brian,Vajdos, Felix,Simons, Samuel P.,Evdokimov, Artem,Mansour, Mahmoud,Menniti, Frank S.
supporting information, p. 1290 - 1296 (2014/10/15)
PDE1 is a family of calcium-activated, dual substrate phosphodiesterases expressed in both the CNS and periphery that play a role in the integration of intracellular calcium and cyclic nucleotide signaling cascades. Exploration of the potential in targeting this family of enzymes to treat neuropsychiatric disorders has been hampered by a lack of potent, selective, and brain penetrable PDE1 inhibitors. To identify such compounds we used high-throughput screening, structure-based design, and targeted synthetic chemistry to discover the 4-aminoquinazoline 7a (PF-04471141) and the 4-indanylquinazoline 27 (PF-04822163) each of which are PDE1 inhibitors that readily cross the blood brain barrier. These quinazoline-based PDE1-selective inhibitors represent valuable new tools to study the biological processes regulated by PDE1 and to begin to determine the potential therapeutic utility of such compounds to treat neuropsychiatric disorders.
An improved synthesis of substituted indan-1-carboxylic acid
Gan, Zongjie,Zhang, Di,Cao, Zhe,Xu, Yungen
, p. 317 - 319 (2011/10/04)
Substituted indan-1-carboxylic acid compounds have been prepared by clyclisation of the phenyl succinic acid and reduction of the indanon-1-carboxylic acid with triethylsilane in trifluoracetic acid.
1,9-ALKANO-BRIDGED-2,3,4,5-TETRAHYDRO-1H-3-BENZAZEPINES
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, (2008/06/13)
1,9-Alkano-bridged-2,3,4,5-tetrahydro-1H-3-benzazepines and the derivatives thereof, i.e., the compounds of Formula I: STR1 wherein: R is selected from the group consisting of: hydrogen, cyano, lower alkyl, lower alkenyl, and aralkyl;each of R 1, R 2 and R 3 is independently selected from the group consisting of: hydrogen, hydroxy, halo, trifluoromethyl, nitro, amido, lower alkoxy, lower alkyl, and lower alkylthio; andY is lower alkylene having from two to four carbon atoms;and the pharmaceutically acceptable salts thereof, are useful as CNS agents, e.g., as antidepressants, anxiolytics and antihypertensives, and/or as precursors thereto.
