77924-06-2Relevant academic research and scientific papers
Identification of a novel neuropeptide s receptor antagonist scaffold based on the sha-68 core
Bool, Heather,Clark, Stewart D.,Gay, Elaine,Jahan, Rajwana,Jewula, Gabriel,McElhinny, Charles,Runyon, Scott,Snyder, Rodney,Uprety, Rajendra,Zarkin, Allison,Zhang, Yanan
, (2021/10/20)
Activation of the neuropeptide S receptor (NPSR) system has been shown to produce an-xiolytic-like actions, arousal, and enhance memory consolidation, whereas blockade of the NPSR has been shown to reduce relapse to substances of abuse and duration of anesthetics. We report here the discovery of a novel core scaffold (+) N-benzyl-3-(2-methylpropyl)-1-oxo-3-phenyl-1H,3H,4H,5H,6H,7H-furo[3,4-c]pyridine-5-carboxamide with potent NPSR antagonist activity in vitro. Pharmacokinetic parameters demonstrate that 14b reaches pharmacologically relevant levels in plasma and the brain following intraperitoneal (i.p.) administration, but is cleared rapidly from plasma. Compound 14b was able to block NPS (0.3 nmol)-stimulated locomotor activity in C57/Bl6 mice at 3 mg/kg (i.p.), indicating potent in vivo activity for the structural class. This suggests that 14b can serve as a useful tool for continued mapping of the pharmacological functions of the NPS receptor system.
APPLICATIONS of ORGANOLITHIUM and RELATED REAGENTS in SYNTHESIS. Part IV. A General Study of the Reaction of N,N-Dialkylpyridinecarboxamides with Lithium Diisopropylamide
Epsztajn, Jan,Brzezinski, Jacek Z.,Jozwiak, Andrzej
, p. 401 - 441 (2007/10/02)
The reactions of the N,N-dialkylpyridinecarboxamides (1), (2) and (3) derived from picolinic, nicotinic and isonicotinic acids with lithium diisopropylamides have been examied.It is shown that in contrast with N,N-diethylpyridinecarboxamides (1a), (2a) an
REACTIONS OF THE N,N-DIALKYLPYRIDYLCARBOXYLIC AMIDES WITH LITHIUM AMIDES. REGIOSELECTIVE LITHIATION OF N,N-DIISOPROPYLPYRIDYLCARBOXYLIC AMIDES, A USEFUL METHOD FOR SYNTHESIS OF 2,3- AND 3,4-DISUBSTITUTED PYRIDINES
Epsztajn, Jan,Berski, Zbigniew,Brzezinski, Jacek Z.,Jozwiak, Andrzej
, p. 4739 - 4742 (2007/10/02)
The behaviour of the N,N-dimethyl-, N,N-diethyl- and N,N,-diisopropylpyridylcarboxylic amides in the reactions with Et2NLi and iPr2NLi, and a convenient way of synthesis of 2,3- and 3,4-disubstituted pyridines, by the direct lithiation of N,N-diisopropylamides leading subsequently to the ortho new C-C bonds formation, are described.
