80166-00-3Relevant academic research and scientific papers
Discovery of a new class of multi-target heterocycle piperidine derivatives as potential antipsychotics with pro-cognitive effect
Gao, Lanchang,Hao, Chao,Chen, Jiali,Ma, Ru,Zheng, Lu,Wu, Qingkun,Liu, Xin,Liu, Bi-Feng,Zhang, Guisen,Chen, Yin,Jin, Jian
supporting information, (2021/03/19)
A series of benzoisoxazoleylpiperidine derivatives were synthesized by using the multi-target strategies and their potent affinities for dopamine (DA), serotonin (5-HT) and human histamine H3 receptors have been evaluated. Of these compounds, t
Synthesis and biological evaluation of a new class of multi-target heterocycle piperazine derivatives as potential antipsychotics
Gao, Lanchang,Hao, Chao,Ma, Ru,Chen, Jiali,Zhang, Guisen,Chen, Yin
, p. 16931 - 16941 (2021/05/25)
In this study, we designed and synthesized a novel series of multi-receptor ligands as polypharmacological antipsychotic agents by using a multi-receptor affinity strategy. Among them,3wcombines a multi-receptor mechanism with high mixed affinities for D
Discovery of (3-(4-(2-Oxa-6-azaspiro[3.3]heptan-6-ylmethyl)phenoxy)azetidin-1-yl)(5-(4-methoxyphenyl)-1,3,4-oxadiazol-2-yl)methanone (AZD1979), a Melanin Concentrating Hormone Receptor 1 (MCHr1) Antagonist with Favorable Physicochemical Properties
Johansson, Anders,L?fberg, Christian,Antonsson, Madeleine,Von Unge, Sverker,Hayes, Martin A.,Judkins, Robert,Ploj, Karolina,Benthem, Lambertus,Lindén, Daniel,Brodin, Peter,Wennerberg, Marie,Fredenwall, Marléne,Li, Lanna,Persson, Joachim,Bergman, Rolf,Pettersen, Anna,Gennemark, Peter,Hogner, Anders
, p. 2497 - 2511 (2016/04/10)
A novel series of melanin concentrating hormone receptor 1 (MCHr1) antagonists were the starting point for a drug discovery program that culminated in the discovery of 103 (AZD1979). The lead optimization program was conducted with a focus on reducing lipophilicity and understanding the physicochemical properties governing CNS exposure and undesired off-target pharmacology such as hERG interactions. An integrated approach was taken where the key assay was ex vivo receptor occupancy in mice. The candidate compound 103 displayed appropriate lipophilicity for a CNS indication and showed excellent permeability with no efflux. Preclinical GLP toxicology and safety pharmacology studies were without major findings and 103 was taken into clinical trials.
Structure-activity studies on a 1,2,3-triazole derivative, a potent in vitro inhibitor of prostaglandin synthesis: The role of the heterocyclic ring
Biagi,Dell'Omodarme,Ferretti,Giorgi,Livi,Scartoni
, p. 335 - 344 (2007/10/02)
This paper reports further structural modifications concerning the 1,2,3- triazole ring of the compound A, an effective in vitro inhibitor of prostaglandin synthesis. The introduction of different heterocyclic rings provided further information about of t
