339370-45-5Relevant articles and documents
CHEMICAL COMPOUNDS
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Paragraph 0170-0172, (2021/04/02)
The present disclosure describes novel compounds, or their pharmaceutically acceptable salts, pharmaceutical compositions containing them, and their medical uses. The compounds of the disclosure have activity as Janus kinase (JAK) inhibitors and are useful in the treatment or control of inflammation, auto-immune diseases, cancer, and other disorders and indications where modulation of JAK would be desirable. Also described herein are methods of treating inflammation, auto-immune diseases, cancer, and other conditions susceptible to inhibition of JAK by administering a compound herein described.
Synthesis, biological evaluation, and enzyme assay of some 5-N-substituted-2-N-(arylsulphonyl)-L(+)glutamines as potential anticancer agents
Jha, Tarun,Samanta, Soma,Halder, Amit Kumar,Adhikari, Nilanjan,Abdul Amin,Sanyal, Arpita,Mukherjee, Tanmoy
, p. 1259 - 1264 (2020/12/04)
Thirty 5-N-substituted-2-N-(arylsulphonyl)-L(+)glutamines were synthesized and evaluated biologically for their anticancer activities. The best active compound of this series showed 92.92% inhibition of tumor weight against Ehrlich Ascites Carcinoma cells. The most active compound was proved to be a competitive inhibitor of glutaminase in the enzyme assay. The best active compound may be a starting point to generate 'lead' for further exploration.
Possible anticancer agents: synthesis, pharmacological activity, and molecular modeling studies on some 5-N -Substituted-2-N-(substituted benzenesulphonyl)-L(+)Glutamines
Jha, Tarun,Basu, Soumya,Halder, Amit Kumar,Adhikari, Nilanjan,Samanta, Soma
, p. 1437 - 1458 (2017/06/05)
On the basis of our earlier work, fortyone 5-N-substituted-2N-(substituted benzenesulphonyl)-L(+)glutamines were synthesized and screened for cancer cell inhibitory activity. The best active compounds showed 91% tumor cell inhibition, whereas other three compounds showed more than 80% inhibition. Two-dimensional quantitative structure–activity relationship modeling and three-dimensional quantitative structure–activity relationship k-nearest neighbor molecular field analysis studies were done to get an insight into structural requirements toward further improved anticancer activity. Considering the fact that these compounds are competitive inhibitors of glutaminase, a molecular docking study followed by molecular dynamic simulation analysis were performed. The work may help to develop new anticancer agents.
Design, synthesis, and biological evaluation of 1,2,4-triazole bearing 5-substituted biphenyl-2-sulfonamide derivatives as potential antihypertensive candidates
Liu, Jie,Liu, Qin,Yang, Xue,Xu, Shengtao,Zhang, Hengyuan,Bai, Renren,Yao, Hequan,Jiang, Jieyun,Shen, Mingqin,Wu, Xiaoming,Xu, Jinyi
, p. 7742 - 7751 (2014/01/06)
A series of novel 1,2,4-triazole bearing 5-substituted biphenyl-2- sulfonamide derivatives were designed and synthesized to develop new angiotensin II subtype 2 (AT2) receptor agonists as novel antihypertensive candidates. It was found that 14f (IC50 = 0.4 nM) and 15e (IC 50 = 5.0 nM) displayed potent AT2 receptor affinity and selectivity in binding assays. Biological evaluation in vivo suggested that 14f is obviously superior to that of reference drug losartan in RHRs, and meanwhile, 14f has no significant impact on heart rate. The interesting activities of these compounds may make them promising candidates as antihypertensive agents.
NOVEL MALONIC ACID SULFONAMIDE DERIVATIVE AND PHARMACEUTICAL USE THEREOF
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Page/Page column 75, (2010/04/25)
The present invention provides a novel compound having an agonist action at AT2 receptor and expected as a pharmaceutical product, and also provides a method of treating or preventing various diseases. The novel sulfonyl malonamide derivative,
Selective angiotensin II AT2 receptor agonists: Arylbenzylimidazole structure-activity relationships
Wu, Xiongyu,Wan, Yiqian,Mahalingam,Murugaiah,Plouffe, Bianca,Botros, Milad,Karlén, Anders,Hallberg, Mathias,Gallo-Payet, Nicole,Alterman, Mathias
, p. 7160 - 7168 (2008/04/18)
Structural alterations in the 2- and 5-positions of the first drug-like selective angiotensin II AT2 receptor agonist (1) have been performed. The imidazole ring system was proven to be a strong determinant for the AT2 selectivity, and with few exceptions all variations gave good AT2 receptor affinities and with retained high AT 2/AT1 selectivities. On the contrary to the findings with AT1 receptor agonists, the impact of structural modifications in the 5-position of the AT2 selective compounds were less pronounced regarding activation of the AT2 receptor. The butyloxyphenyl (56) and the propylthienyl (50) derivatives were found to exert a high agonistic effect as deduced from their capacity to induce neurite elongation in neuronal cells, as does angiotensin II.
Catalytic Properties of Carbonyl Reductase from Rabbit Kidney for Acetohexamide and Its Analogs
Imamura, Yorishige,Higuchi, Toshiyuki,Otagiri, Masaki,Nagumo, Shinji,Akita, Hiroyuki
, p. 387 - 394 (2007/10/02)
Analogs submitted by ethyl, n-propyl, n-butyl, and isopropyl groups instead of methyl group adjacent to a ketone group of acetohexamide were synthesized and the structural requirements of carbonyl reductase from rabbit kidney for these analogs were kineti
