3557-22-0Relevant academic research and scientific papers
Design, synthesis, and biological evaluation of novel 4H-chromen-4-one derivatives as antituberculosis agents against multidrug-resistant tuberculosis
Fu, Lei,Liu, Yuke,Lu, Yu,Sheng, Li,Wang, Bin,Zhang, Dongfeng,Zhao, Hongyi,Zhao, Wenting
, (2020/01/28)
A series of 4H-chromen-4-one derivatives obtained by scaffold morphing of the benzofuran compound, TAM16, were tested for antitubercular activity. Compound 8d was active against drug-sensitive and multidrug-resistant tuberculosis. A preliminary druggability evaluation showed that compound 8d displayed favorable mouse and human microsomal stability, low cytotoxicity, and acceptable oral bioavailability. An in vivo study indicated that compound 8d exhibited modest efficacy in an acute mouse model of TB after 3 weeks of treatment. Thus, 8d is a promising antituberculosis lead compound.
Synthesis, antimycobacterial evaluation and pharmacophore modeling of analogues of the natural product formononetin
Mutai, Peggoty,Pavadai, Elumalai,Wiid, Ian,Ngwane, Andile,Baker, Bienyameen,Chibale, Kelly
supporting information, p. 2510 - 2513 (2015/06/02)
Abstract The synthesis and antimycobacterial activity of formononetin analogues is hereby reported. Formononetin and its analogue 11E showed 88% and 95% growth inhibition, respectively, against the H37Rv strain of Mycobacterium tuberculosis. Pharmacophore modeling studies indicated that the presence of a hydroxyl group in formononetin and its analogues, is crucial for maintaining activity.
ESTROGEN RECEPTOR MODULATORS AND USES THEREOF
-
Paragraph 00380; 00440, (2013/07/05)
Described herein are compounds that are estrogen receptor modulators. Also described are pharmaceutical compositions and medicaments that include the compounds described herein, as well as methods of using such estrogen receptor modulators, alone and in c
BENZISOXAZOLE COMPOUND
-
Page/Page column 185, (2009/02/10)
Disclosed is a compound represented by the general formula (I) or a salt thereof: wherein any one of R1, R2 and R3 represents a group represented by the formula: -(CH2)m-NR11R12 (wherein m is 1 or 2; and R11 and R12 independently represent a hydrogen atom or a C1-6 alkyl group or may, together with a nitrogen atom to which R11 and R12 are bound, form a 4- or 5-membered cyclic group); the remaining two or R1, R2 and R3 independently represent a group represented by the formula: -(O)n-R21 (wherein n is 0 or 1; and R21 represents a hydrogen atom, a C1-6 alkyl group, a C2-6 alkenyl group, a C2-6 alkynyl group, or the like); and R4 represents a C1-6 alkyl group which may have a substituent or the like.
Flavonol based ruthenium acetylides as fluorescent chemosensors for lead ions
Fillaut, Jean-Luc,Andriès, Julien,Marwaha, Ripu Daman,Lano?, Pierre-Henri,Lohio, Olivier,Toupet, Loic,Gareth Williams
, p. 228 - 234 (2008/03/14)
Flavonol based alkynyl ruthenium complexes devoted to the detection of metal traces in solution are described. The sensitivity of both absorption and emission properties of the 3-hydroxyflavone unit as a receptor for the metal cations, and of an alkynyl ruthenium moiety as an extended π-conjugated system, provides an efficient molecular sensor for rapid, sensitive and selective detection of lead(II) cations.
Synthesis and description of chalcone-like compounds, inhibitors of aldose reductase
Severi,Costantino,Benvenuti,Vampa,Mucci
, p. 128 - 136 (2007/10/03)
A series of hydroxy- and hydroxy-methoxychalcones was synthesized and the inhibitory activity and selectivity of the compounds towards bovine lens aldose reductase (AR) were tested. All the compounds display affinity for AR. The most active proved to be 1-(2,4-dihydroxyphenyl)-3-(4-hydroxyphenyl)propen-1-one (isoliquiritigenin, IC50= 7.60 μM). The selectivity of this compound was also tested, its inhibitory activity being assayed against glutathione reductase and sorbitol dehydrogenase.
QUINOLINYL-BENZOPYRAN DERIVATIVES AS ANTAGONISTS OF LEUKOTRIENE D4
-
, (2008/06/13)
This invention relates to certain quinolinyl-benzopyran compounds and their use as valuable pharmaceutical agents, particularly as lipoxygenase inhibitors and/or leukotriene antagonists and/or mediator release inhibitors possessing anti-inflammatory and anti-allergic properties.
QUINOLINYL-CHROMONE DERIVATIVES AND USE FOR TREATMENT OF HYPERSENSITIVE AILMENTS
-
, (2008/06/13)
This invention relates to certain quinolinyl-chromone compounds and their use as valuable pharmaceutical agents, particularly as lipoxygenase inhibitors and/or leukotriene antagonists possessing anti-inflammatory and anti-allergic properties.
N-Vinylimidazoles and -triazoles and pharmaceutical compositions containing them
-
, (2008/06/13)
Described are N-vinylazoles of the general formula: (wherein R is hydrogen, hydroxy, halogen, C1-C5 alkoxy, C2-C5 alkenyloxy, optionally substituted benzyloxy, tetrahydropyranyl-oxy, difluoromethoxy, 2-(2,4-dich
SYNTHESES OF PHENOLIC METABOLITES OF AN ANTIFUNGAL IMIDAZOLE DERIVATIVE (CLOCONAZOLE HYDROCHLORIDE)
Takahashi, Kimio,Shimizu, Sumio,Ogata, Masaru
, p. 1483 - 1491 (2007/10/02)
Syntheses of phenolic metabolites of antifungal vinylimidazole derivative 6*HCl (Cloconazole hydrochloride) are described.Phenolic compound 8 was prepared from 2 using selective mono THP protection, followed by imidazolation and deprotection. 10 was synth
