cas 189250-15-5, CHEMBRDG-BB 5101460 | Articles data

Articles about 189250-15-5Total 3 be found

Design, Synthesis, and Characterization of Ogerin-Based Positive Allosteric Modulators for G Protein-Coupled Receptor 68 (GPR68)
G protein-coupled receptor 68 (GPR68) is an understudied orphan G protein-coupled receptor (GPCR). It is expressed most abundantly in the brain, potentially playing important roles in learning and memory. Pharmacological studies with GPR68 have been hinde
Yu, Xufen,Huang, Xi-Ping,Kenakin, Terry P.,Slocum, Samuel T.,Chen, Xin,Martini, Michael L.,Liu, Jing,Jin, Jian
p. 7557 - 7574
(2019/09/09)

Substituted 3-(4-(1,3,5-triazin-2-yl)-phenyl)-2-aminopropanoic acids as novel tryptophan hydroxylase inhibitors
Tryptophan hydroxylase (TPH) is a key enzyme in the synthesis of serotonin. As a neurotransmitter, serotonin plays important physiological roles both peripherally and centrally. Here we describe the discovery of substituted triazines as a novel class of tryptophan hydroxylase inhibitors. This class of TPH inhibitors can selectively reduce serotonin levels in murine intestine after oral administration without affecting levels in the brain. These TPH inhibitors may provide novel treatments for gastrointestinal disorders associated with dysregulation of the serotonergic system, such as chemotherapy-induced emesis and irritable bowel syndrome.
Jin, Haihong,Cianchetta, Giovanni,Devasagayaraj, Arokiasamy,Gu, Kunjian,Marinelli, Brett,Samala, Lakshman,Scott, Sheldon,Stouch, Terry,Tunoori, Ashok,Wang, Ying,Zang, Yi,Zhang, Chengmin,David Kimball,Main, Alan J.,Ding, Zhi-Ming,Sun, Weimei,Yang, Qi,Yu, Xiang-Qing,Powell, David R.,Wilson, Alan,Liu, Qingyun,Shi, Zhi-Cai
scheme or table
p. 5229 - 5232
(2010/03/31)

Screening for novel antimicrobials from encoded combinatorial libraries by using a two-dimensional agar format
A sensitive lawn-based format has been developed to screen bead-tethered combinatorial chemical libraries for antimicrobial activity. This method has been validated with beads linked to penicillin V via a photocleavable chemical linker in several analyses including a spike-and-recover experiment. The lawn-based screen sensitivity was modified to detect antibacterial compounds of modest potency, and a demonstration experiment with a naive combinatorial library of over 46,000 individual triazines was evaluated for antibacterial activity. Numerous hits were identified, and both active and inactive compounds were resynthesized and confirmed in traditional broth assays. This demonstration experiment suggests that novel antimicrobial compounds can be easily identified from very large combinatorial libraries of small, nonpeptidic compounds.
Silen, Joy L.,Lu, Amy T.,Solas, Dennis W.,Gore, Medini A.,Maclean, Derek,Shah, Nikil H.,Coffin, Jill M.,Bhinderwala, Naseema S.,Wang, Yongwen,Tsutsui, Ken T.,Look, Gary C.,Campbell, David A.,Hale, Ron L.,Navre, Marc,Deluca-Flaherty, Camille R.
p. 1447 - 1453
(2007/10/03)