54255-50-4Relevant academic research and scientific papers
ANTIBACTERIAL COMPOUNDS
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Page/Page column 88-89, (2019/05/22)
The present invention relates to compounds of general formula (II),to compositions comprising these compounds and to methods of treating Enterobacteriaceae bacterial diseases and infections using the compounds. The compounds find application in the treatment of infection with, and diseases caused by, Enterobacteriaceae.
Synthesis, protease inhibition, and antileishmanial activity of new benzoxazoles derived from acetophenone or benzophenone and synthetic precursors
Folquitto, Laís R. S.,Nogueira, Priscila F.,Espuri, Patrícia F.,Gontijo, Vanessa S.,de Souza, Thiago B.,Marques, Marcos J.,Carvalho, Diogo T.,Júdice, Wagner A. S.,Dias, Danielle F.
, p. 1149 - 1159 (2017/05/04)
Abstract: This work reports the synthesis, protease inhibition, and antileishmanial activity of ten benzoxazole derivatives, which were obtained in a three-step synthetic route from 4-hydroxy-acetophenone and 4-hydroxy-benzophenone. These benzoxazoles, the synthetic intermediates, and the starting ketones were evaluated for their inhibitory effect on the activity of cysteine (papain, rCPB2.8, and rCPB3.0) and serine (trypsin) proteases. All compounds showed significant values of IC50 against these enzymes (in the range of 0.0086–0.7612 μM for papain and 0.0075–0.5032 μM for trypsin), being more active than the standard inhibitors (1.7821 and 7.2318 μM, for E64 and TLCK, respectively). Following, all compounds were evaluated in vitro for their leishmanicidal activity against promastigote form of Leishmania amazonensis. The most active compounds were further evaluated against amastigote form and for its toxicity against murine macrophages. The benzoxazole 4d, a benzophenone derivative, and the intermediate 4-hydroxy-3-nitroacetophenone 2b showed significant antileishmanial activity (IC50 = 90.3 μM and IC50 = 130.9 μM, respectively) with selectivity indexes (5.22 and 18.09, respectively) compared to or better than those of two established leishmanicidal drugs, pentamidine (0.58) and amphotericin B (5.31). Graphical Abstract: [InlineMediaObject not available: see fulltext.].
New heterocyclic chalcones. Part 6. Synthesis and cytotoxic activities of 5- or 6-(3-aryl- 2-propenoyl)-2(3H)-benzoxazolones
Ivanova, Yordanka B.,Momekov, Georgi T.,Petrov, Ognyan I.
, p. 23 - 28 (2013/05/22)
A number of chalcones bearing an oxazole cycle were synthesized by Claisen-Schmidt condensation of 5-acetyl-2(3 H )-benzoxazolone or 6-acetyl-2(3 H )-benzoxazolone and the appropriate aldehydes. The chalcones were evaluated for cytotoxic activity against several tumor cell lines - BV-173 (human B cell precursor leukemia), MCF-7 and MDA-MB-231 (human breast adenocarcinoma) using the MTT-dye reduction assay. The tested compounds exhibit concentration- dependent cytotoxic effects at micromolar concentrations. Exposure of the BV-173 tumor cell line to compound 3f results in strong monoand oligonucleosomal fragmentation of genomic DNA, as evidenced by a 'cell death detection' ELISA kit, which unambiguously indicates that the induction of apoptosis is implicated in the cytotoxic mode of action of the tested compound.
Regulatory molecules for the 5-HT3 receptor ion channel gating system
Yoshida, Satoshi,Watanabe, Takashi,Sato, Yasuo
, p. 3515 - 3523 (2008/02/07)
Substituted benzoxazole derivatives which possess a nitrogen-containing heterocycle at C2 are selective partial agonists of the 5-HT3 receptor. Alteration of substituents on the benzoxazole nucleus affords both agonist-like and antagonist-like compounds, and uniquely modifies the function of the 5-HT3 receptor ion channel gating system. SAR and corroborative computational docking study for these partial agonists successfully explained structure and function of the 5-HT3 receptor.
Liquid crystal composition, liquid crystal device, display apparatus and display method
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, (2008/06/13)
A mesomorphic compound represented by the following formula (I): STR1 wherein R1 and R2 respectively denote an alkyl group or alkoxy group each having 4-16 carbon atoms optionally substituted, halogen, --CN or --CF3. The mesomorphic compound is effective for providing a ferroelectric liquid crystal composition showing an improved low-temperature operation characteristic and a decreased temperature-dependence of response speed.
Mesomorphic compound for use in liquid crystal composition and liquid crystal device and display apparatus using same
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, (2008/06/13)
A mesomorphic compound represented by the following formula [I]: STR1 wherein R1 and R2 independently denote an alkyl group having 1-16 carbon atoms capable of having a substituent; X1, X2, X3 and X4 independently denote a single bond STR2 A1, A2 and A3 independently denote STR3 X5 and X6 independently denote hydrogen atom, fluorine, chlorine, bromine, CH3, CN or CF3 ; n1 and n2 are 0 or 1, with provisos that (1) X2 cannot be a single bond when n1 is 0, (2) X3 cannot be a single bond when N2 is 1 and (3) at least one of X2 and X3 denotes STR4 when both n1 and n2 is O and A2 denote STR5
Unequivocal Preparation of 4- and 5-Acyl-2-aminophenols
Aichaoui, Hocine,Lesieur, Isabelle,Henichart, Jean-Pierre
, p. 679 - 680 (2007/10/02)
Unequivocal methods for the specific preparation of 4- or 5-acyl-2-aminophenols are reported. 5-Acyl-2-aminophenols are obtained by ring opening with dilute sodium hydroxide of 2(3H)-benzoxazolinones acylated at position 6. 4-Acyl-2-aminophenols are obtai
