Synthesis and optimization of novel α-phenylglycinamides as selective TRPM8 antagonists was written by Kobayashi, Jun-ichi;Hirasawa, Hideaki;Ozawa, Tetsuji;Ozawa, Tomonaga;Takeda, Hiroo;Fujimori, Yoshikazu;Nakanishi, Osamu;Kamada, Noboru;Ikeda, Tetsuya. And the article was included in Bioorganic & Medicinal Chemistry in 2017.Category: chlorides-buliding-blocks The following contents are mentioned in the article:
Transient receptor potential melastatin 8 (TRPM8) is activated by innocuous cold and chem. substances, and antagonists of this channel have been considered to be effective for pain and urinary diseases. N-(3-aminopropyl)-2-{[(3-methylphenyl)methyl]oxy}-N-(2-thienylmethyl)benzamide hydrochloride (AMTB), a TRPM8 antagonist, was proposed to be effective for overactive bladder and painful bladder syndrome; however, there is a potential risk of low blood pressure. We report herein the synthesis and structure-activity relationships of novel phenylglycine derivatives that led to the identification of KPR-2579 (20l), a TRPM8 selective antagonist. KPR-2579 reduced the number of icilin-induced wet-dog shakes and rhythmic bladder contraction in rats, with no neg. cardiovascular effects at the ED. This study involved multiple reactions and reactants, such as (R)-1-(3-Chloro-5-fluorophenyl)ethanamine hydrochloride (cas: 1820574-01-3Category: chlorides-buliding-blocks).
(R)-1-(3-Chloro-5-fluorophenyl)ethanamine hydrochloride (cas: 1820574-01-3) belongs to organic chlorides. Chlorination modifies the physical properties of hydrocarbons in several ways. These compounds are typically denser than water due to the higher atomic weight of chlorine versus hydrogen. Alkyl chlorides are versatile building blocks in organic chemistry. While alkyl bromides and iodides are more reactive, alkyl chlorides tend to be less expensive and more readily available.Category: chlorides-buliding-blocks
Referemce:
Chloride – Wikipedia,
Chlorides – an overview | ScienceDirect Topics