Recommanded Product: 1193-21-1In 2021 ,《Design, synthesis, and structure-activity relationships study of N-pyrimidyl/pyridyl-2-thiazolamine analogues as novel positive allosteric modulators of M3 muscarinic acetylcholine receptor》 appeared in Chemical & Pharmaceutical Bulletin. The author of the article were Tanaka, Hiroaki; Akaiwa, Michinori; Negoro, Kenji; Kawaminami, Eiji; Mihara, Hisashi; Fuji, Hideyoshi; Okimoto, Risa; Ino, Katsutoshi; Ishizu, Kenichiro; Takahashi, Taisuke. The article conveys some information:
The M3 muscarinic acetylcholine receptor (mAChR) plays an essential pharmacol. role in mediating a broad range of actions of acetylcholine (ACh) released throughout the periphery and central nerve system (CNS). Nevertheless, its agonistic functions remain unclear due to the lack of available subtype-selective agonists or pos. allosteric modulators (PAMs). Based on the extended structure-activity relationships (SARs) study on a previously reported PAM of the M3 mAChR, 2-acylaminothiazole I, aa series of N-azinyl-2-thiazolamine analogs II (X = pyridine-2,6-diyl, pyrimidine-2,4-diyl, 5-fluoropyrimidine-4,6-diyl, pyrazine-3,6-diyl, etc.) were identified as new scaffolds. The SARs study was rationalized using conformational analyses based on intramol. interactions. A comprehensive study of a series of analogs described in this paper suggests that a unique sulfur-nitrogen nonbonding interaction in the N-azinyl-2-thiazolamine moiety enables conformations that are essential for activity. Further, a SARs study around the N-pyrimidyl/pyridyl-2-thiazolamine core culminated in the discovery of the compound II (X = 5-fluoro-2-methylpyrimidine-4,6-diyl), which showed potent in vitro PAM activity for the M3 mAChR with excellent subtype selectivity. Compound II (X = 5-fluoro-2-methylpyrimidine-4,6-diyl) also showed a distinct pharmacol. effect on isolated smooth muscle tissue from rat bladder and favorable pharmacokinetics profiles, suggesting its potential as a chem. tool for probing the M3 mAChR in further research. In addition to this study using 4,6-Dichloropyrimidine, there are many other studies that have used 4,6-Dichloropyrimidine(cas: 1193-21-1Recommanded Product: 1193-21-1) was used in this study.
4,6-Dichloropyrimidine(cas: 1193-21-1) is a member of organic chlorides. Organic chlorides are compounds containing a carbon-chlorine bond, which are widely used in the oil field as a wax dissolver. They are generally not present in crude oils and are typically the result of additives, cleaning solutions or chemicals used for oil recovery.Recommanded Product: 1193-21-1
Referemce:
Pyrimidine | C4H4N2 – PubChem,
Pyrimidine – Wikipedia