1296202-60-2Relevant academic research and scientific papers
6-chlorine-N-(substituted benzyl)-1H-pyrrolo[2,3-b]pyridine-2-amide compound and preparation method as well as application thereof
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, (2016/10/10)
The invention discloses a 6-chlorine-N-(substituted benzyl)-1H-pyrrolo[2,3-b]pyridine-2-amide compound and a preparation method as well as application thereof, belonging to the field of HIV-1 integrase inhibitors. The compound is represented by a general formula (I), wherein R1 represents -F, -Me, -OMe and -H; R2 represents -H, -F, -Me, -OMe and -Cl; R3 represents -H, -F, -Me, -OMe, -Cl, -Br, -CF3 and -SO2Me. The preparation method of the compound comprises the steps of synthetising N-(6-chloropyridine-2-tertiary butyl) amide by using 6-chloropyridine-2-amine as a raw material and pivaloyl chloride, performing pyridine ring iodination, then hydrolyzing to obtain 6-chlorine-3-iodine pyridine-2-amine, cyclizing to obtain a compound with a carboxylic acid structure, and finally reacting with various substituted benzyls to obtain the compound disclosed by the invention.
Discovery and optimization of indole and 7-azaindoles as Rho kinase (ROCK) inhibitors (Part-II)
Sessions, E. Hampton,Chowdhury, Sarwat,Yin, Yan,Pocas, Jennifer R.,Grant, Wayne,Schr?ter, Thomas,Lin, Li,Ruiz, Claudia,Cameron, Michael D.,Lograsso, Philip,Bannister, Thomas D.,Feng, Yangbo
scheme or table, p. 7113 - 7118 (2012/01/05)
Therapeutic interventions with Rho kinase (ROCK) inhibitors may effectively treat several disorders such as hypertension, stroke, cancer, and glaucoma. Herein we disclose the optimization and biological evaluation of potent novel ROCK inhibitors based on substituted indole and 7-azaindole core scaffolds. Substitutions on the indole C3 position and on the indole NH and/or amide NH positions all yielded potent and selective ROCK inhibitors (25, 42, and 50). Improvement of aqueous solubility and tailoring of in vitro and in vivo DMPK properties could be achieved through these substitutions.
