Discovery and SAR Studies of Orally Active Somatostatin Receptor Subtype-2 (SSTR2) Agonists for the Treatment of Acromegaly was written by Ishida, Akiharu;Tajima, Yohei;Okabe, Yasuyuki;Matsushita, Takeshi;Sekiguchi, Tetsuya;Imaide, Satomi;Nomura, Yoshinori;Tanaka, Motoyuki;Nojima, Shoji;Yoshida, Atsushi;Iyoda, Yoko;Aoki, Shohei;Nishio, Takuya;Komagata, Tatsuya;Iwaki, Masanori;Shono, Tomoyuki;Naganawa, Atsushi;Imagawa, Akira. And the article was included in ACS Chemical Neuroscience in 2020.Recommanded Product: 142253-56-3 This article mentions the following:
Acromegaly is a disease caused by the oversecretion of growth hormone. It is currently treated by i.v. injection with cyclic peptide drugs that activate somatostatin receptor subtype 2 (SSTR2). Here, novel nonpeptidic, small-mol., and orally active SSTR2 agonists were identified from a hit compound (13). Pharmacophore studies enabled scaffold hopping to obtain a unique 3,4,5-trisubstituted pyridine motif. Further optimization conferred potent SSTR2 agonistic activity and metabolic stability. Several compounds were evaluated and these showed good oral pharmacokinetic profiles in rats, and one representative compound (25)(I) showed highly potent inhibition of growth hormone secretion induced by growth hormone-releasing hormone in rats. Based on these results, 25 was identified as a promising lead for further optimization. A structure-activity relationship (SAR) study and the metabolic stability data for this compound are also described. In the experiment, the researchers used many compounds, for example, 1-Boc-Azetidine-3-yl-methanol (cas: 142253-56-3Recommanded Product: 142253-56-3).
1-Boc-Azetidine-3-yl-methanol (cas: 142253-56-3) belongs to alcohols. Alcohols are weak acids. The most acidic simple alcohols (methanol and ethanol) are about as acidic as water, and most other alcohols are somewhat less acidic. The most common reactions of alcohols can be classified as oxidation, dehydration, substitution, esterification, and reactions of alkoxides.Recommanded Product: 142253-56-3
Referemce:
Alcohol – Wikipedia,
Alcohols – Chemistry LibreTexts