19202-27-8Relevant articles and documents
Design, synthesis and activity evaluation of N-(pyridin-4-yl) salicylamides as antimycobacterial agents
Dian, He,Zhou, De-Bin,Mou, Jian-Ping,Yang, Zhu-Qing,Zhong, Jia,Ding, Xiao-Quan,Li, Chong,Wang, Xiao-Hong,Zhang, Jian-Gang
, p. 7269 - 7275 (2015/04/22)
A series of N-(pyridin-4-yl) salicylamides derivatives were prepared through acylation of the corresponding acetylsalicyloyl chlorides with substituted 4-amino-pyridines. These compounds were evaluated in vitro for antimycobacterial activities against Myc
Design and synthesis of an orally active metabotropic glutamate receptor subtype-2 (mGluR2) positive allosteric modulator (PAM) that decreases cocaine self-administration in rats
Dhanya, Raveendra-Panickar,Sidique, Shyama,Sheffler, Douglas J.,Nickols, Hilary Highfield,Herath, Ananda,Yang, Li,Dahl, Russell,Ardecky, Robert,Semenova, Svetlana,Markou, Athina,Conn, P. Jeffrey,Cosford, Nicholas D. P.
experimental part, p. 342 - 353 (2011/03/18)
The modification of 3′-((2-cyclopentyl-6,7-dimethyl-1-oxo-2,3- dihydro-1H-inden-5-yloxy)methyl)biphenyl-4-carboxylic acid (BINA, 1) by incorporating heteroatoms into the structure and replacing the cyclopentyl moiety led to the development of new mGluR2 positive allosteric modulators (PAMs) with optimized potency and superior druglike properties. These analogues are more potent than 1 in vitro and are highly selective for mGluR2 vs other mGluR subtypes. They have significantly improved pharmacokinetic (PK) properties, with excellent oral bioavailability and brain penetration. The benzisothiazol-3-one derivative 14 decreased cocaine self-administration in rats, providing proof-of-concept for the use of mGluR2 PAMs for the treatment of cocaine dependence.
Structure-activity relationships of non-peptide vasopressin V(1a) antagonists: 1-(1-multi-substituted benzoyl 4-piperidyl)-3,4-dihydro-2(1H)- quinolinones
Kondo,Ogawa,Nakaya,Tominaga,Yabuuchi
, p. 725 - 733 (2007/10/03)
During our systematic studies on the arginine vasopressin receptor V(1a)- antagonistic activity of 1-(1-benzoyl substituted 4-piperidyl)-3,4-dihydro- 2(1H)-quinolinones, we found a general substituent effect on the benzene ring. Hydrogen-bonding ability a