Nakajima, Yutaka; Tojo, Takashi; Morita, Masataka; Hatanaka, Keiko; Shirakami, Shohei; Tanaka, Akira; Sasaki, Hiroshi; Nakai, Kazuo; Mukoyoshi, Koichiro; Hamaguchi, Hisao; Takahashi, Fumie; Moritomo, Ayako; Higashi, Yasuyuki; Inoue, Takayuki published the artcile< Synthesis and evaluation of 1H-pyrrolo[2,3-b]pyridine derivatives as novel immunomodulators targeting Janus kinase 3>, COA of Formula: C8H5ClN2O2, the main research area is pyrrolopyridine preparation Janus kinase inhibitor lipophilicity mol docking pharmacokinetics.
A series of 1H-pyrrolo[2,3-b]pyridine derivatives I [R = H, Me, c-Hex, Ph; R1 = NHCH(CH2CH3)2, piperidin-1-yl, ((1S,2R)-2-methylcyclohexyl)aminyl, cyclohexylaminyl, etc.] as novel immunomodulators targeting JAK3 for use in treating immune diseases such as organ transplantation has been described. In the chem. modification of N-cyclohexyl-N-methyl-1H-pyrrolo[2,3-b]pyridin-4-amine, the introduction of a carbamoyl group to the C5-position and substitution of a cyclohexylamino group at the C4-position of the 1H-pyrrolo[2,3-b]pyridine ring led to a large increase in JAK3 inhibitory activity. Compound I [R = H, R1 = ((1S,2R)-2-methylcyclohexyl)aminyl] was identified as a potent, moderately selective JAK3 inhibitor, and the immunomodulating effect of I [R = H, R1 = ((1S,2R)-2-methylcyclohexyl)aminyl] on interleukin-2-stimulated T cell proliferation was shown. Docking calculations and WaterMap anal. of the 1H-pyrrolo[2,3-b]pyridine-5-carboxamide derivatives I were conducted to confirm the substituent effects on JAK3 inhibitory activity.
Chemical & Pharmaceutical Bulletin published new progress about Amines Role: RCT (Reactant), RACT (Reactant or Reagent). 920966-03-6 belongs to class pyridine-derivatives, and the molecular formula is C8H5ClN2O2, COA of Formula: C8H5ClN2O2.