916765-70-3Relevant articles and documents
N-monoarylacetothioureas as potent urease inhibitors: synthesis, SAR, and biological evaluation
Fang, Hai-Lian,He, Jie-Ling,Li, Wei-Yi,Liu, Shan-Shan,Ni, Wei-Wei,Pan, Xing-Ming,Xiao, Zhu-Ping,Ye, Ya-Xi,Yi, Juan,Zhou, Mi,Zhou, Tian-Li,Zhu, Hai-Liang
, p. 404 - 413 (2020)
A urease inhibitor with good in vivo profile is considered as an alternative agent for treating infections caused by urease-producing bacteria such as Helicobacter pylori. Here, we report a series of N-monosubstituted thioureas, which act as effective urease inhibitors with very low cytotoxicity. One compound (b19) was evaluated in detail and shows promising features for further development as an agent to treat H. pylori caused diseases. Excellent values for the inhibition of b19 against both extracted urease and urease in intact cell were observed, which shows IC50 values of 0.16 ± 0.05 and 3.86 ± 0.10 μM, being 170- and 44-fold more potent than the clinically used drug AHA, respectively. Docking simulations suggested that the monosubstituted thiourea moiety penetrates urea binding site. In addition, b19 is a rapid and reversible urease inhibitor, and displays nM affinity to urease with very slow dissociation (koff=1.60 × 10?3 s?1) from the catalytic domain.
N-arylacetyl thiosemicarbazide urease inhibitor and preparation method and application thereof
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Paragraph 0028; 0029-0031; 0033; 0093, (2019/01/14)
N-arylacetyl thiosemicarbazide compounds have a structural formula as shown in the specification, have great inhibiting effects on urease and can be used for preparation of medicines for treating gastritis, gastric ulcer, lithangiuria and the like. The in
Design, Synthesis, and Structure-Activity Relationships of Pyridine-Based Rho Kinase (ROCK) Inhibitors
Green, Jeremy,Cao, Jingrong,Bandarage, Upul K.,Gao, Huai,Court, John,Marhefka, Craig,Jacobs, Marc,Taslimi, Paul,Newsome, David,Nakayama, Tomoko,Shah, Sundeep,Rodems, Steve
, p. 5028 - 5037 (2015/07/02)
The Rho kinases (ROCK1 and ROCK2) are highly homologous serine/threonine kinases that act on substrates associated with cellular motility, morphology, and contraction and are of therapeutic interest in diseases associated with cellular migration and contraction, such as hypertension, glaucoma, and erectile dysfunction. Beginning with compound 4, an inhibitor of ROCK1 identified through high-throughput screening, systematic exploration of SAR, and application of structure-based design, led to potent and selective ROCK inhibitors. Compound 37 represents significant improvements in inhibition potency, kinase selectivity, and CYP inhibition and possesses pharmacokinetics suitable for in vivo experimentation.
Selective inhibitors of rock protein kinase and uses thereof
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Page/Page column 35, (2008/06/13)
Described herein are compounds that are useful as ROCK inhibitors. These compounds, and pharmaceutically acceptable compositions thereof, are useful for treating or lessening the severity of a variety of disorders, including cardiovascular, inflammatory,
Convenient synthesis of N-(4-(2-aminopyridin-4-yl)thiazol-2-yl)-2-phenylacetamides
Bandarage, Upul K.,Come, Jon H.,Green, Jeremy
, p. 8079 - 8081 (2007/10/03)
We report a facile one-pot, three-step synthesis of N-(4-(2-aminopyridin-4-yl)thiazol-2-yl)-2-phenylacetamides via condensation of 2-p-methoxybenzylamino-4-acetylpyridine with phenylacetylthioureas.
