Category: 142253-56-3

Discovery of IACS-9779 and IACS-70465 as Potent Inhibitors Targeting Indoleamine 2,3-Dioxygenase 1 (IDO1) Apoenzyme was written by Hamilton, Matthew M.;Mseeh, Faika;McAfoos, Timothy J.;Leonard, Paul G.;Reyna, Naphtali J.;Harris, Angela L.;Xu, Alan;Han, Michelle;Soth, Michael J.;Czako, Barbara;Theroff, Jay P.;Mandal, Pijus K.;Burke, Jason P.;Virgin-Downey, Brett;Petrocchi, Alessia;Pfaffinger, Dana;Rogers, Norma E.;Parker, Connor A.;Yu, Simon S.;Jiang, Yongying;Krapp, Stephan;Lammens, Alfred;Trevitt, Graham;Tremblay, Martin R.;Mikule, Keith;Wilcoxen, Keith;Cross, Jason B.;Jones, Philip;Marszalek, Joseph R.;Lewis, Richard T.. And the article was included in Journal of Medicinal Chemistry in 2021.Electric Literature of C9H17NO3 This article mentions the following:

Indoleamine 2,3-dioxygenase 1 (IDO1), a heme-containing enzyme that mediates the rate-limiting step in the metabolism of L-tryptophan to kynurenine, has been widely explored as a potential immunotherapeutic target in oncol. The authors have developed a class of inhibitors with a conformationally constrained bicyclo[3.1.0]hexane core. These potently inhibited IDO1 in a cellular context by binding to the apoenzyme, as elucidated by biochem. characterization and X-ray crystallog. A SKOV3 tumor model was instrumental in differentiating compounds, leading to the identification of I (IACS-9779) and II (IACS-70465). IACS-70465 has excellent cellular potency, a robust pharmacodynamic response, and in a human whole blood assay was more potent than linrodostat (BMS-986205). IACS-9779 with a predicted human efficacious once-daily dose below 1 mg/kg to sustain >90% inhibition of IDO1 displayed an acceptable safety margin in rodent toxicol. and dog cardiovascular studies to support advancement into preclin. safety evaluation for human development. In the experiment, the researchers used many compounds, for example, 1-Boc-Azetidine-3-yl-methanol (cas: 142253-56-3Electric Literature of C9H17NO3).

1-Boc-Azetidine-3-yl-methanol (cas: 142253-56-3) belongs to alcohols. Alkyl halides are often synthesized from alcohols, in effect substituting a halogen atom for the hydroxyl group. Converting an alcohol to an alkene requires removal of the hydroxyl group and a hydrogen atom on the neighbouring carbon atom. Dehydrations are most commonly carried out by warming the alcohol in the presence of a strong dehydrating acid, such as concentrated sulfuric acid.Electric Literature of C9H17NO3

Referemce:
Alcohol – Wikipedia,
Alcohols – Chemistry LibreTexts

Direct Conversion of Primary Alcohols to 1,2-Amino Alcohols: Enantioselective Iridium-Catalyzed Carbonyl Reductive Coupling of Phthalimido-Allene via Hydrogen Auto-Transfer was written by Spielmann, Kim;Xiang, Ming;Schwartz, Leyah A.;Krische, Michael J.. And the article was included in Journal of the American Chemical Society in 2019.HPLC of Formula: 142253-56-3 This article mentions the following:

The first catalytic enantioselective carbonyl (α-amino)allylations are described. Phthalimido-allene and primary alcs. engage in hydrogen auto-transfer-mediated carbonyl reductive coupling by way of (α-amino)allyliridium-aldehyde pairs to form vicinal amino alcs. with high levels of regio-, anti-diastereo-, and enantioselectivity. Reaction progress kinetic anal. and isotopic labeling studies corroborate a catalytic cycle involving turnover-limiting alc. dehydrogenation followed by rapid allene hydrometalation. In the experiment, the researchers used many compounds, for example, 1-Boc-Azetidine-3-yl-methanol (cas: 142253-56-3HPLC of Formula: 142253-56-3).

1-Boc-Azetidine-3-yl-methanol (cas: 142253-56-3) belongs to alcohols. Alkyl halides are often synthesized from alcohols, in effect substituting a halogen atom for the hydroxyl group. Tertiary alcohols cannot be oxidized at all without breaking carbon-carbon bonds, whereas primary alcohols can be oxidized to aldehydes or further oxidized to carboxylic acids.HPLC of Formula: 142253-56-3

Referemce:
Alcohol – Wikipedia,
Alcohols – Chemistry LibreTexts

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