Results 51 to 60 of about 24,259 (231)

Identification of a novel class of autotaxin inhibitors through cross-screening [PDF]

, 2015
Three novel series were generated in order to mimic the pharmacophoric features displayed by lead compound AM095, a Lysophosphatidic acid (LPA1) receptor antagonist. Biological evaluation of this array of putative LPA1 antagonists led us to the discovery
Budd, David C., Castagna, Diana, Duffy, Emma L., Jamieson, Craig, Macdonald, Simon J. F., Pritchard, John M., Semaan, Dima, Watson, Allan J. B., Young, Louise C.   +8 more
core   +1 more source

Syntheses and Characterizations of Some New N-alkyl, Isoxazole and Dioxazole Derivatives of 5-Chloroisatin [PDF]

, 2017
N-alkyl and cycloadducts derivatives of 5-Chloroisatin were synthesized in good to excellent yields. The method evidences a selective N-alkylation when using 1,2-bis (2-chloroethoxy) ethane as efficient spacer at room temperature on the 5-Chloroisatin ...
Rodi, Y. K. (Y), Senhaji, O. (O), Skalli, M. K. (M), Tribak, Z. (Z)   +3 more
core   +1 more source

A Synergistic Inhibitor Development Strategy Against Human UDP‐Galactose‐4‐Epimerase

Angewandte Chemie International Edition, EarlyView.
The epimerase GalE is crucial for the biosynthesis of cancer‐relevant O‐GalNAc glycans. Here, we employ orthogonal, structurally enabled small molecule fragment screens to yield both covalent and non‐covalent inhibitors against GalE within no more than 22 elaborated compounds.
William M. Browne, Jonathan Pettinger, Teresa Weckwerth, Andrew Purkiss, Sing Hei Lok, Louisa Penicaut, Roksana Ogrodowicz, Raveena Prema, Simone Kunzelmann, Chloe Roustan, Ganka Bineva‐Todd, Saskia Pieters, Francesca Zappacosta, Alfred E. Doherty, Isobel Oram, Christelle Soudy, Robert Quinlan, Joanna Redmond, Svend Kjaer, David House, Stephane Mouilleron, Jacob T. Bush, Benjamin Schumann   +22 more
wiley   +1 more source

2,10-Bis(3-bromophenyl)-3,7,11,15-tetraoxa-8,16-diazatricyclo[12.2.1.16,9]octadeca-1(16),6(18),8,14(17)-tetraene

Acta Crystallographica Section E, 2010
The title compound, C24H20Br2N2O4, is an 18-membered tricycle including two isoxazole rings. The asymmetric unit contains one half of the formula unit; a centre of inversion is located at the centroid of the compound.
Kwang Ha, Sae Byul Park, Young Ju Lee, Hyung Jin Kim   +3 more
doaj   +1 more source

SYNTHESIS OF UNSYMMETRICALLY SUBSTITUTED ISOXAZOLES AS INTERMEDIATES FOR BENT-CORE MESOGENS

Studia Universitatis Babes-Bolyai Chemia, 2016
3,5-Disubstituted isoxazoles have been designed and synthesized to be used as central units for bent-core mesogens. The substituents at position 3 of the isoxazole ring are either hydroxymethyl or carboxyl, while alkenyl-terminated substituents have ...
Gheorghe ROMAN
doaj  

4-(4-Fluorophenyl)-2-methyl-3-(1-oxy-4-pyridyl)isoxazol-5(2H)-one

Acta Crystallographica Section E, 2008
The crystal structure of the title compound, C15H11FN2O3, was determined as part of a study on the biological activity of isoxazolone derivatives as p38 mitogen-activated protein kinase (MAPK) inhibitors.
Stefan Laufer, Dieter Schollmeyer, Simona Margutti   +2 more
doaj   +1 more source

Synthesis and Structure of Unsymmetrical Anthracenyl-Isoxazole Antitumor Agents Via the Diastereoselective Bromination of 3-(9′-Anthryl)-Isoxazole Esters

Crystals
In pursuit of unsymmetrical precursors for the novel series of anthracenyl-isoxazole amide (AIM) antitumor agents, a series of substituted anthracenes were subjected to bromination and re-aromatization in our study, during which we solved four single ...
Michael J. Campbell, Daniel A. Decato, Chun Li, Matthew J. Weaver, Nicholas R. Natale   +4 more
doaj   +1 more source

1-Methyl-3-p-tolyl-3,3a,4,9b-tetrahydro-1H-chromeno[4,3-c]isoxazole-3a-carbonitrile

Acta Crystallographica Section E, 2011
In the title compound, C19H18N2O2, the dihedral angle between the mean planes of the fused chromeno and isoxazole units is 43.71 (7)°. The isoxazole and pyran rings exhibit envelope and half chair conformations, respectively.
Rajeswari Gangadharan, K. Sethusankar, Gandhi Murugan, Manickam Bakthadoss   +3 more
doaj   +1 more source

Sterically Facilitated Intramolecular Nucleophilic NMe₂ Group Substitution in the Synthesis of Fused Isoxazoles: Theoretical Study

Molecules, 2020
The influence of steric repulsion between the NMe2 group and a second ortho-(peri-)substituent in the series of 1-dimethylaminonaphthalene and N,N-dimethylanilene ortho-oximes on the ease of the NMe2 group’s intramolecular nucleophilic substitution is ...
Alexander S. Antonov, Elena Yu Tupikina, Valerii V. Karpov, Valeriia V. Mulloyarova, Victor G. Bardakov   +4 more
doaj   +1 more source

Neuronal circuitry for pain processing in the dorsal horn [PDF]

, 2010
Neurons in the spinal dorsal horn process sensory information, which is then transmitted to several brain regions, including those responsible for pain perception.
A Dhaka, A Ribeiro-da-Silva, A Ribeiro-da-Silva, AF Keller, AG Brown, AH Watson, AJ Todd, AJ Todd, AJ Todd, AJ Todd, AJ Todd, AJ Todd, AJ Todd, AJ Todd, AJ Todd, AJ Todd, AJ Todd, AL Bailey, AM Taylor, Andrew J. Todd, AR Light, AW Hantman, AW Hantman, B Lynn, B Rexed, BA Graham, C Albuquerque, C Gauriau, C Gauriau, C Gauriau, C Torsney, CJ Woodbury, CJ Woodbury, CJ Woolf, D Andrew, D Lima, D Lima, D Lima, D Lima, D Schoffnegger, D Schoffnegger, D Uta, DI Hughes, DI Hughes, DI Hughes, DJ Cavanaugh, DJ Maxwell, DL Bennett, DS Bredt, E Polgár, E Polgár, E Polgár, E Polgár, E Polgár, E Polgár, E Polgár, E Polgár, E Polgár, E Polgár, E Polgár, ET Zhang, ET Zhang, G Kato, GG Nagy, GJ Bennett, GJ Michael, GT Whiteside, H Baba, H Bester, H Ikeda, H Ikeda, H Sakamoto, HJ Hu, HY Huang, I Decosterd, I Laing, J Sandkuhler, J Scholz, J Zheng, JA Coull, JA Esteban, JF Bernard, JH Hwang, JJ Azkue, JL Hylden, JM Castro-Lopes, K Abe, K Feil, K Noguchi, KA Moore, KM Al-Khater, KM Al-Khater, KS Al Ghamdi, L Almarestani, L Sivilotti, LE Lorenzo, M Antal, M Antal, M Gassner, M Larsson, M Malcangio, M Mori, M Naim, M Okamoto, M Randic, M Rethelyi, M Zoli, MB Plenderleith, MJ Eaton, MJ Perry, MJ Zylka, ML Nichols, MM Heinricher, MM Naim, MW Salter, NK Littlewood, P Boscan, P Brumovsky, P Shortland, PD Wall, PW Mantyh, PW Mantyh, Q Liu, R Burstein, R Ruscheweyh, R Ruscheweyh, RC Spike, RC Spike, RM Slugg, RP Seal, RR Ji, S Neumann, S Neumann, SA Prescott, SA Shehab, SF Santos, SH Kim, SN Lawson, SP Schneider, T Ibuki, T Kemp, T Kohno, T Yasaka, T Yasaka, TJ Grudt, TL Yaksh, TP Malan, VS Seybold, WD Snider, WD Willis, X Zhang, X Zhang, XH Yu, Y Lu, Y Lu, Y Lu, YG Tong, YQ Ding, Z Puskár, ZS Han   +159 more
core   +1 more source