21816-42-2Relevant articles and documents
6-(Azaindol-2-yl)pyridine-3-sulfonamides as potent and selective inhibitors targeting hepatitis C virus NS4B
Chen, Guangming,Ren, Hongyu,Zhang, Nanjing,Lennox, William,Turpoff, Anthony,Paget, Steven,Li, Chunshi,Almstead, Neil,Njoroge, F. George,Gu, Zhengxian,Graci, Jason,Jung, Stephen P.,Colacino, Joseph,Lahser, Fred,Zhao, Xin,Weetall, Marla,Nomeir, Amin,Karp, Gary M.
, p. 781 - 786 (2015)
A structure-activity relationship investigation of various 6-(azaindol-2-yl)pyridine-3-sulfonamides using the HCV replicon cell culture assay led to the identification of a potent series of 7-azaindoles that target the hepatitis C virus NS4B. Compound 2ac, identified via further optimization of the series, has excellent potency against the HCV 1b replicon with an EC50 of 2 nM and a selectivity index of >5000 with respect to cellular GAPDH RNA. Compound 2ac also has excellent oral plasma exposure levels in rats, dogs and monkeys and has a favorable liver to plasma distribution profile in rats.
Discovery and crystallography of bicyclic arylaminoazines as potent inhibitors of HIV-1 reverse transcriptase
Lee, Won-Gil,Frey, Kathleen M.,Gallardo-Macias, Ricardo,Spasov, Krasimir A.,Chan, Albert H.,Anderson, Karen S.,Jorgensen, William L.
, p. 4824 - 4827 (2015/10/28)
Non-nucleoside inhibitors of HIV-1 reverse transcriptase (HIV-RT) are reported that incorporate a 7-indolizinylamino or 2-naphthylamino substituent on a pyrimidine or 1,3,5-triazine core. The most potent compounds show below 10 nanomolar activity towards wild-type HIV-1 and variants bearing Tyr181Cys and Lys103Asn/Tyr181Cys resistance mutations. The compounds also feature good aqueous solubility. Crystal structures for two complexes enhance the analysis of the structure-activity data.
Syntheses of five potential heterocyclic amine food mutagens
Tanga,Bupp,Tochimoto
, p. 717 - 727 (2007/10/03)
The syntheses of the potential heterocyclic amine food mutagens, 3,5,7- trimethyl-2-aminoimidazo[4,5-b]pyridine, 1,4,7-trimethyl-2-aminoimidazo[4,5- c]pyridine, 1,6,7-trimethyl-2-aminoimidazo[4,5-c]-pyridine, 3,4,6-trimethyl- 2-aminoimidazo[4,5-c]pyridine, and 1,4,6-trimethyl-7-aminoimidazo[4,5-c]- pyridine are described.