Sato, Masanori; Kondo, Takekazu; Kohno, Yasushi; Seto, Shigeki published their research in Bioorganic & Medicinal Chemistry in 2021. The article was titled 《Discovery of benzo[f]pyrido[4,3-b][1,4]oxazepin-10-one derivatives as orally available bromodomain and extra-terminal domain (BET) inhibitors with efficacy in an in vivo psoriatic animal model》.Electric Literature of C6H13NO The article contains the following contents:
Several compounds I (R1 = H, F; R2 = H, F, Cl, OMe; X = O, S) starting from previously reported pyrido-benzodiazepinone derivative II were designed and synthesized to enhance BRD4 inhibitory activity while avoiding hERG inhibition. Mol. docking studies and structure-activity relationship studies led to the identification of 9-fluorobenzo[f]pyrido[4,3-b][1,4]oxazepin-10-one derivative I (X = O; R1 = F; R2 = H), which exhibited potent BRD4 inhibitory activity with excellent potency in imiquimod-induced psoriasis model mice.trans-4-Aminocyclohexanol(cas: 27489-62-9Electric Literature of C6H13NO) was used in this study.
trans-4-Aminocyclohexanol(cas: 27489-62-9) belongs to anime. The reaction of alkyl halides, R―X, where X is a halogen, or analogous reagents with ammonia (or amines) is useful with certain compounds. Not all alkyl halides are effective reagents; the reaction is sluggish with secondary alkyl groups and fails with tertiary ones. Its usefulness is largely confined to primary alkyl halides (those having two hydrogen atoms on the reacting site).Electric Literature of C6H13NO
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