7254-19-5Relevant articles and documents
Synthesis, structure-activity relationship and antiviral activity of indole-containing inhibitors of Flavivirus NS2B-NS3 protease
Kneubehl, Alexander R.,Li, Xin,Lin, Yi-Lun,Nie, Shenyou,Rico-Hesse, Rebecca,Song, Yongcheng,Vogt, Megan B.,Wu, Fangrui,Wu, Xiaowei,Yao, Yuan,Zhao, Jidong
, (2021/08/26)
Zika virus belongs to the Flavivirus family of RNA viruses, which include other important human pathogens such as dengue and West Nile virus. There are no approved antiviral drugs for these viruses. The highly conserved NS2B-NS3 protease of Flavivirus is essential for the replication of these viruses and it is therefore a drug target. Compound screen followed by medicinal chemistry optimization yielded a novel series of 2,6-disubstituted indole compounds that are potent inhibitors of Zika virus protease (ZVpro) with IC50 values as low as 320 nM. The structure-activity relationships of these and related compounds are discussed. Enzyme kinetics studies show the inhibitor 66 most likely exhibited a non-competitive mode of inhibition. In addition, this series of ZVpro inhibitors also inhibit the NS2B-NS3 protease of dengue and West Nile virus with reduced potencies. The most potent compounds 66 and 67 strongly inhibited Zika virus replication in cells with EC68 values of 1–3 μM. These compounds are novel pharmacological leads for further drug development targeting Zika virus.
Substituted indole - 2 - formic acid (by machine translation)
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, (2017/10/28)
This invention relates to a substituted indole - 2 - carboxylic acid synthesis method, is to replace the phenyl hydrazine hydrochloride or arylhydrazines as raw materials, through with pyruvic acid ethyl ester cheng zong, Fischer indole synthesis by reaction of substituted indole - 2 - carboxylic acid ethyl ester, hydrolysis to obtain the substituted - 2 - carboxylic acid. Product purity is greater than 97%, the reaction yield is 64%. Synthesis method of the invention with non-harsh conditions, the operation is simple, and environmental friendliness, it has certain economic benefits. It is a kind of raw materials are easy, simple operation, three wastes, high yield of indole - 2 - carboxylic acid synthesis method. (by machine translation)
Cathepsin K inhibitor and application thereof
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Paragraph 0219; 0220; 0221; 0276; 0277; 0278, (2017/08/28)
The invention relates to a cathepsin K inhibitor and an application thereof, in particular to compounds (as shown in formula (I) in the specification) for treating or preventing cathepsin-dependent diseases. The compounds comprise but not limited to the cathepsin K inhibitor. The compounds and pharmaceutical composition of the compounds can be used as a bone resorption inhibitor in the treatment of related diseases.
Synthesis of 3,3-Dihalo-2-oxindoles from 2-Substituted Indoles via Halogenation–Decarboxylation/Desulfonamidation–Oxidation Process
Jiang, Xiaojian,Zhang, Feng,Yang, Junjie,Yu, Pei,Yi, Peng,Sun, Yewei,Wang, Yuqiang
supporting information, p. 3938 - 3942 (2016/12/30)
A novel one-pot reaction which combines halogenation, decarboxylation/desulfonamidation with oxidation has been developed. Diverse valuable 3,3-dihalo-2-oxindole compounds can be produced rapidly and safely with isolated yields of up to 98% under mild conditions. (Figure presented.).
New arylthioindoles and related bioisosteres at the sulfur bridging group. 4. Synthesis, tubulin polymerization, cell growth inhibition, and molecular modeling studies
La Regina, Giuseppe,Sarkar, Taradas,Bai, Ruoli,Edler, Michael C.,Saletti, Roberto,Coluccia, Antonio,Piscitelli, Francesco,Minelli, Lara,Gatti, Valerio,Mazzoccoli, Carmela,Palermo, Vanessa,Mazzoni, Cristina,Falcone, Claudio,Scovassi, Anna Ivana,Giansanti, Vincenzo,Campiglia, Pietro,Porta, Amalia,Maresca, Bruno,Hamel, Ernest,Brancale, Andrea,Novellino, Ettore,Silvestri, Romano
experimental part, p. 7512 - 7527 (2010/05/18)
New arylthioindoles along with the corresponding ketone and methylene compounds were potent tubulin assembly inhibitors. As growth inhibitors of MCF-7 cells, sulfur derivatives were superior or sometimes equivalent to the ketones, while methylene derivatives were substantially less effective. Esters 24, 27-29, 36, 39, and 41 showed ～50% of inhibition on human HeLa and HCT116/chr3 cells at 0.5 μM, and these compounds inhibited the growth of HEK, M14, and U937 cells with IC50's in the 78-220 nM range. While murine macrophage J744.1 cell growth was significantly less affected (20% at higher concentrations), four other nontransformed cell lines remained sensitive to these esters. The effect of drug treatment on cell morphology was examined by time-lapse microscopy. In a protocol set up to evaluate toxicity on the Saccharomyces cerevisiae BY4741 wild type strain, compounds 24 and 54 strongly reduced cell growth, and 29, 36, and 39 also showed significant inhibition. 2009 American Chemical Society.
PHARMACEUTICALLY ACTIVE BENZOXAZOLE, BENZTHIAZOLE AND BENZIMIDAZOLE ACID DERIVATIVES
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Page 29, (2010/02/07)
Compounds of formula (I): wherein R1, R2 and R3 are independently, hydrogen, halogen, CF3, OR6, NR7R8, NR8COR10, NR8SO2R10 or C1-6 alkyl optionally substituted by hydroxy, C1-6 alkoxy or NR7R8; R4 is NR8CONR8R9, NR8COR9, NR8SO2R9, or W-CONR8R9, where W is a bond, C1-6 alkylene, C2-6 alkenylene or C2-6 alkynylene; and R5 is Formula (A) methods for their synthesis, pharmaceutical compositions comprising them and their use in medicine, in particular for the treatment of cancer.
Novel 3,4-Dihydroquinolin-2(1H)-one inhibitors of human glycogen phosphorylase a
Rosauer, Keith G.,Ogawa, Anthony K.,Willoughby, Chris A.,Ellsworth, Kenneth P.,Geissler, Wayne M.,Myers, Robert W.,Deng, Qiaolin,Chapman, Kevin T.,Harris, Georgianna,Moller, David E.
, p. 4385 - 4388 (2007/10/03)
The preparation of a series of substituted indoles coupled to six- and seven-membered cyclic lactams is described and their role as human glycogen phosphorylase a inhibitors discussed. The SAR of the indole moiety and lactam ring are presented.
