10252-82-1Relevant academic research and scientific papers
Identification of thiophene-benzenesulfonamide derivatives for the treatment of multidrug-resistant tuberculosis
Batt, Sarah M.,Besra, Gurdyal S.,Fu, Lei,Huang, Haihong,Li, Gang,Lu, Yu,Qin, Rongfei,Wang, Bin,Wang, Pengxu,Wang, Yanan,Wu, Chengwei
, (2022/02/01)
A series of thiophene-benzenesulfonamide derivatives was designed and synthesized by exploring the structure-activity relationship of lead compounds 2,3-disubstituted thiophenes 25a and 297F as antituberculosis agents, which displayed potent antimycobacterial activity against drug-susceptible and clinically isolated drug-resistant tuberculosis. In particular, compound 17b, which had improved activity (minimum inhibitory concentration of 0.023 μg/mL) compared with the lead compounds, displayed good intracellular antimycobacterial activity in macrophages with a reduction of 1.29 log10 CFU. A druggability evaluation indicated that compound 17b had favorable hepatocyte stability, low cytotoxicity, and low hERG channel inhibition. Moreover, compound 17b exhibited modest in vivo efficacy in an acute mouse model of tuberculosis. In addition, the molecular docking study elucidated the binding mode of compound 17b in the active site of DprE1. Therefore, compound 17b may be a promising antituberculosis lead for further research.
Diaryl 2- amide-substituted thiophene imide ester compound as well as preparation method and application thereof (by machine translation)
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Paragraph 0357; 0361; 0364-0365; 0368; 0372; 0375-0376, (2020/02/17)
The invention also discloses a 2 - synthesis method thereof, and an application of the compound as an antibacterial agent, in the phthisis-caused by the bacterium, in particular to the, mycobacterium-induced infectious disease (especially (Tuberculosis,TB), mycobacterium- induced mycobacterium, tuberculosis), and (I) the invention, specifically relates to a pharmaceutical composition containing the compound of the present invention or, a R pharmaceutical composition comprising the compound of the present invention. 1 , R2 , R3 , R4 , R5 As described Y in the present invention. as described in the specification, the present invention is directed, to the preparation of novel compounds, having an anti-mycobacterial activity as potential, new drug (s) for the treatment (TB) or preventative treatment of infectious diseases, consisting of M. tuberculosis, in particular phthisis- caused by tubercular mycobacteria, while being useful in overcoming the problems associated with drug resistance. (by machine translation)
COMPOUNDS HAVING ANTIBACTERIAL ACTIVITY
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Page/Page column 106; 107, (2014/11/13)
The present invention relates to compounds of formula (I) and their uses. In particular, though not exclusively, it concerns heterocyclic compounds that inhibit the biogenesis of adhesive pili in Gram- negative bacteria, and their use in the prevention or
PYRIDYL INHIBITORS OF HEDGEHOG SIGNALLING
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Page/Page column 72; 101, (2009/11/29)
The invention provides novel inhibitors of hedgehog signaling that are useful as s therapeutic agent for treating malignancies where the compounds have the general formula (I): where A, X, Y R1, R2, R3, R4, m and n are as described herein.
HISTAMINE H3 RECEPTOR AGENTS, PREPARATION AND THERAPEUTIC USES
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Page/Page column 35, (2010/11/25)
The present invention discloses novel compounds of Formula I or pharmaceutically acceptable salts thereof which have histamine-H3 receptor antagonist or inverse agonist activity, as well as methods for preparing such compounds. In another embodiment, the
Pyridyl inhibitors of hedgehog signalling
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Page/Page column 78, (2010/10/20)
The invention provides novel inhibitors of hedgehog signaling that are useful as a therapeutic agents for treating malignancies where the compounds have the general formula I: wherein A, X, Y R1, R2, R3, R4, m and n are as described herein.
CHEMICAL COMPOUNDS
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Page 128, (2010/02/06)
Compounds of formula (I):wherein variable groups are as defined within; for use in the inhibition of 11betaHSD1 are described
Benzothiazole derivatives with activity as adenosine receptor ligands
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, (2008/06/13)
The present invention relates to substituted benzothiazole derivitives and to their pharmaceutically acceptable salts useful for the treatment of diseases related to the adenosine receptor.
Orally-active elastase inhibitors
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, (2008/06/13)
This invention relates to novel morpholinourea and related derivatives of pentafluoroethyl peptides which are orally active elastase inhibitors. These compounds are useful in the treatment of various inflammatory diseases and emphysema.
