67608-58-6Relevant academic research and scientific papers
Discovery of meta-amido bromophenols as new antitubercular agents
Liang, Jie,Tang, Yun-xiang,Tang, Xiang-zheng,Liang, Hua-ju,Gao, Yamin,Fang, Cuiting,Zhang, Tian-yu,Yan, Ming
, p. 372 - 381 (2019/05/07)
A series of meta-amido bromophenol derivatives were designed and synthesized. The compounds were found to potently inhibit the growth of Mycobacterium tuberculosis H37Ra. They also exhibited moderate inhibitory activity against Mycobacterium tuberculosis H37Rv and multidrug-resistant strains. The compounds did not show inhibitory activity against normal Gram-positive and Gram-negative bacteria. Moderate cytotoxicities and good metabolic stability were observed for the selected compounds. The results demonstrated meta-amido bromophenols as a new class of antitubercular agents with good potentials.
Synthesis and biological properties of thiazole-analogues of pyochelin, a siderophore of Pseudomonas aeruginosa
No?l, Sabrina,Hoegy, Fran?oise,Rivault, Freddy,Rognan, Didier,Schalk, Isabelle J.,Mislin, Ga?tan L.A.
, p. 132 - 135 (2014/01/17)
Pyochelin is a siderophore common to all strains of Pseudomonas aeruginosa utilized by this Gram-negative bacterium to acquire iron(III). FptA is the outer membrane transporter responsible of ferric-pyochelin uptake in P. aeruginosa. We describe in this Letter the synthesis and the biological properties ( 55Fe uptake, binding to FptA) of several thiazole analogues of pyochelin. Among them we report in this Letter the two first pyochelin analogues able to bind FptA without promoting any iron uptake in P. aeruginosa.
COMPOUNDS AND METHODS FOR THE TREATMENT OF VIRUSES AND CANCER
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Page/Page column 24; 25, (2010/11/26)
The present invention relates to compounds according to the formula I: Where Ra is H or an optionally OH-substituted C1-C3 alkyl; R1 is OR1, an optionally substituted C4-12 carbocyclic group which may be saturated or unsaturated (including aromatic) or an optionally substituted heterocyclic group; R1 is an optionally substituted C1-C14 hydrocarbyl group or an optionally substituted heterocyclic group;; R2 , R3 and R4 are each independently H, an optionally substituted C1-C4 alkyl group (preferably CH3, CH2CH3 or CF3), halogen (preferably F, Cl, Br), OR, CN, NO2, a C1-C6 thioether, a C1-C6 thioester group, an optionally substituted CO2R group, an optionally substituted COR group or an optionally substituted OCOR group (preferably R4 is H); R is H or an optionally substituted C1-C6 alkyl group; RHET is an optionally substituted heterocyclic group; and pharmaceutically acceptable salts, solvates or polymorphs thereof.
Optimization of diarylamines as non-nucleoside inhibitors of HIV-1 reverse transcriptase
Ruiz-Caro, Juliana,Basavapathruni, Aravind,Kim, Joseph T.,Bailey, Christopher M.,Wang, Ligong,Anderson, Karen S.,Hamilton, Andrew D.,Jorgensen, William L.
, p. 668 - 671 (2007/10/03)
Following computational analyses, potential non-nucleoside inhibitors of HIV-1 reverse transcriptase have been pursued through synthesis and assaying for anti-viral activity. The general class Het-NH-Ph-U has been considered, where Het is an aromatic heterocycle and U is an unsaturated, hydrophobic group. Results for compounds with Het = 2-thiazoyl and 2-pyrimidinyl are the focus of this report.
N-(4-carb-amimidophenyl)glycineamide derivatives
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, (2008/06/13)
N-(4-carbamimidophenylamino) phenylglycineamide derivative compounds having the formula: in which E, g1, g2, Q, R and X1 to X4 are each as defined in the description, and hydrates or solvates and physiologically acceptable salts thereof can be used as inhibitors of the formation of the coagulation factors Xa, IXa and thrombin induced by the factor VIIa and by the tissue factor. These compounds can be used as medicaments for the treatment and/or prevention of thromboses, apoplexy, cardiac infarction, inflammation and arteriosclerosis or as antitumor agents.
