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.Safety of tert-Butyl (4-hydroxycyclohexyl)carbamate 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, tert-Butyl (4-hydroxycyclohexyl)carbamate (cas: 224309-64-2Safety of tert-Butyl (4-hydroxycyclohexyl)carbamate).
tert-Butyl (4-hydroxycyclohexyl)carbamate (cas: 224309-64-2) belongs to alcohols. The oxygen atom of the strongly polarized O―H bond of an alcohol pulls electron density away from the hydrogen atom. This polarized hydrogen, which bears a partial positive charge, can form a hydrogen bond with a pair of nonbonding electrons on another oxygen atom. Alcohols may be oxidized to give ketones, aldehydes, and carboxylic acids. These functional groups are useful for further reactions. Oxidation of organic compounds generally increases the number of bonds from carbon to oxygen (or another electronegative element, such as a halogen), and it may decrease the number of bonds to hydrogen.Safety of tert-Butyl (4-hydroxycyclohexyl)carbamate
Referemce:
Alcohol – Wikipedia,
Alcohols – Chemistry LibreTexts