657424-79-8Relevant academic research and scientific papers
Design, synthesis and structure-based optimization of novel isoxazole-containing benzamide derivatives as FtsZ modulators
Bi, Fangchao,Song, Di,Zhang, Nan,Liu, Zhiyang,Gu, Xinjie,Hu, Chaoyu,Cai, Xiaokang,Venter, Henrietta,Ma, Shutao
, p. 90 - 103 (2018/10/04)
Antibiotic resistance among clinically significant bacterial pathogens is becoming a prevalent threat to public health, and new antibacterial agents with novel mechanisms of action hence are in an urgent need. Utilizing computational docking method and structure-based optimization strategy, we rationally designed and synthesized two series of isoxazol-3-yl- and isoxazol-5-yl-containing benzamide derivatives that targeted the bacterial cell division protein FtsZ. Evaluation of their activity against a panel of Gram-positive and -negative pathogens revealed that compounds B14 and B16 that possessed the isoxazol-5-yl group showed strong antibacterial activity against various testing strains, including methicillin-resistant Staphylococcus aureus and penicillin-resistant S. aureus. Further molecular biological studies and docking analyses proved that the compound functioned as an effective inhibitor to alter the dynamics of FtsZ self-polymerization via a stimulatory mechanism, which finally terminated the cell division and caused cell death. Taken together, these results could suggest a promising chemotype for development of new FtsZ-targeting bactericidal agent.
Design, synthesis and biological evaluation of stilbene derivatives as novel inhibitors of protein tyrosine phosphatase 1B
He, Haibing,Ge, Yinghua,Dai, Hong,Cui, Song,Ye, Fei,Jin, Jia,Shi, Yujun
, (2016/12/30)
By imitating the scaffold of lithocholic acid (LCA), a natural steroidal compound displaying Protein Tyrosine Phosphatase 1B (PTP1B) inhibitory activity, a series of stilbene derivatives containing phenyl-substituted isoxazoles were designed and synthesized. The structures of the title compounds were confirmed by 1H-NMR, 13C-NMR and HRMS. Activities of the title compounds were evaluated on PTP1B and the homologous enzyme TCPTP by using a colorimetric assay. Most of the target compounds had good activities against PTP1B. Among them, compound 29 (IC50 = 0.91 ± 0.33 μM), characterized by a 5-(2,3-dichlorophenyl) isoxazole moiety, exhibited an activity about 14-fold higher than the lead compound LCA and a 4.2-fold selectivity over TCPTP. Compound 29 was identified as a competitive inhibitor of PTP1B with a Ki value of 0.78 μM in enzyme kinetic studies.
Biarylmethoxy isonipecotanilides as potent and selective inhibitors of blood coagulation factor Xa
Lopopolo, Gianfranco,Fiorella, Filomena,De Candia, Modesto,Nicolotti, Orazio,Martel, Sophie,Carrupt, Pierre-Alain,Altomare, Cosimo
experimental part, p. 180 - 191 (2012/01/05)
New chloro-substituted biarylmethoxyphenyl piperidine-4-carboxamides were synthesized and assayed in vitro as inhibitors of the blood coagulation enzymes factor Xa (fXa) and thrombin. An investigation of effects of the amidine and isopropyl groups attache
MGLUR5 MODULATORS
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, (2008/06/13)
The present invention is directed to compounds of formula (I) Wherein R1 to R5, X and Z are further defined in the description. The invention also relates to processes for the preparation of the compounds and to intermediates used in
Substituted piperazines as metabotropic glutamate receptor antagonists
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Page/Page column 18, (2008/06/13)
The invention relates to compounds of formula I or pharmaceutically acceptable salts or solvates thereof: where Ar1, Ar2, Hy, L, R1, m and n are as defined in the description. The invention also includes pharmaceutical compositions and uses thereof, processes for making the compounds, as well as methods for the medical treatment of mGluR5-mediated disorders.
MGluR5 modulators V
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Page/Page column 14; 15, (2008/06/13)
The present invention is directed to novel compounds, to a process for their preparation, their use in therapy and pharmaceutical compositions comprising the novel compounds.
5- (PHENYLISOXAZOLYLETHOXY) -TRIAZOL- 3 -YL SUBSTITUTED PYRIDINE COMPOUNDS FOR THE TREATMENT OF NEUROLOGICAL, PSYCHIATRIC OR PAIN DISORDERS
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Page/Page column 13; 18, (2008/06/13)
The present invention is directed to novel compounds of formula (I) / (I1) / (III), their use in therapy and pharmaceutical compositions comprising said novel compounds.
MGluR5 modulators VI
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Page/Page column 9, (2008/06/13)
The present invention is directed to novel compounds, to a process for their preparation, their use in therapy and pharmaceutical compositions comprising the novel compounds.
FUSED HETEROCYCLIC COMPOUNDS AND THEIR USE AS METABOTROPIC GLUTAMATE RECEPTOR ANTAGONISTS
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Page/Page column 49-50, (2008/06/13)
The present invention is directed to compounds of formula (I): Wherein X1, X2, X3, X4, X5, X6, X7, X8, X9, X10, R1, R2, Rs
NEW COMPOUNDS
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Page 159, (2010/02/06)
The present invention relates to new compounds of formula I, (I) a process for their preparation and new intermediates prepared therein, pharmaceutical formulations containing said compounds and to the use of said compounds in therapy.
