56824-22-7Relevant articles and documents
Design, synthesis, and biological evaluation of 3,4-dihydroquinolin-2(1 H)-one and 1,2,3,4-tetrahydroquinoline-based selective human neuronal nitric oxide synthase (nNOS) inhibitors
Ramnauth, Jailall,Speed, Joanne,Maddaford, Shawn P.,Dove, Peter,Annedi, Subhash C.,Renton, Paul,Rakhit, Suman,Andrews, John,Silverman, Sarah,Mladenova, Gabriela,Zinghini, Salvatore,Nair, Sheela,Catalano, Concettina,Lee, David K.H.,De Felice, Milena,Porreca, Frank
, p. 5562 - 5575 (2011)
Neuronal nitric oxide synthase (nNOS) inhibitors are effective in preclinical models of many neurological disorders. In this study, two related series of compounds, 3,4-dihydroquinolin-2(1H)-one and 1,2,3,4- tetrahydroquinoline, containing a 6-substituted thiophene amidine group were synthesized and evaluated as inhibitors of human nitric oxide synthase (NOS). A structure-activity relationship (SAR) study led to the identification of a number of potent and selective nNOS inhibitors. Furthermore, a few representative compounds were shown to possess druglike properties, features that are often difficult to achieve when designing nNOS inhibitors. Compound (S)-35, with excellent potency and selectivity for nNOS, was shown to fully reverse thermal hyperalgesia when given to rats at a dose of 30 mg/kg intraperitonieally (ip) in the L5/L6 spinal nerve ligation model of neuropathic pain (Chung model). In addition, this compound reduced tactile hyperesthesia (allodynia) after oral administration (30 mg/kg) in a rat model of dural inflammation relevant to migraine pain.
Asymmetric synthesis of H1 receptor antagonist (R,R)-clemastine
Lee, Sun Young,Jung, Jung Wha,Kim, Tae-Hyun,Kim, Hee-Doo
, p. 2131 - 2136 (2015/12/08)
The first asymmetric synthesis of (R,R)-clemastine (1) has been accomplished by the coupling of (R)-tertiary alcohol 2 and (R)-chloroethylpyrrolidine 3 via O-alkylation. (R)-Tertiary alcohol 2 was synthesized by stereoselective alkylation of chiral α-benz
SUBSTITUTED BENZHYDRYLETHERS
-
Page/Page column 34, (2009/08/18)
Disclosed herein are substituted benzhydrylethers of Formula I, processes of preparation thereof, pharmaceutical compositions thereof, and methods of their use thereof.