Literature DB >> 12110331

Synthesis and anti-inflammatory activity of phthalimide derivatives, designed as new thalidomide analogues.

Lídia M Lima1, Paulo Castro, Alexandre L Machado, Carlos Alberto M Fraga, Claire Lugnier, Vera Lúcia Gonçalves de Moraes, Eliezer J Barreiro.   

Abstract

This paper describes the synthesis and anti-inflammatory activity of new N-phenyl-phthalimide sulfonamides (3a-e) and the isosters N-phenyl-phthalimide amides (4a-e), designed as hybrids of thalidomide (1) and aryl sulfonamide phosphodiesterase inhibitor (2). In these series, compound 3e (LASSBio 468), having a sulfonyl-thiomorpholine moiety, showed potent inhibitory activity on LPS-induced neutrophil recruitment with ED(50)=2.5mg kg(-1), which was correlated with its inhibitory effect on TNF-alpha level.

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Year:  2002        PMID： 12110331     DOI： 10.1016/s0968-0896(02)00152-9

Source DB:  PubMed          Journal:  Bioorg Med Chem        ISSN： 0968-0896            Impact factor:   3.641


  26 in total

1.  Synthesis and cross-coupling reactions of imidomethyltrifluoroborates with aryl chlorides.

Authors:  Rammohan Devulapally; Nicolas Fleury-Brégeot; Gary A Molander; Dave G Seapy
Journal:  Tetrahedron Lett       Date:  2012-02-29       Impact factor: 2.415

2.  Mutagenicity of new lead compounds to treat sickle cell disease symptoms in a Salmonella/microsome assay.

Authors:  Jean Leandro dos Santos; Eliana A Varanda; Lídia Moreira Lima; Chung Man Chin
Journal:  Int J Mol Sci       Date:  2010-02-25       Impact factor: 5.923

3.  Palladium-catalyzed one-step synthesis of isoindole-1,3-diones by carbonylative cyclization of o-halobenzoates and primary amines.

Authors:  Shilpa A Worlikar; Richard C Larock
Journal:  J Org Chem       Date:  2008-08-20       Impact factor: 4.354

Review 4.  Biomarkers in acute lung injury: insights into the pathogenesis of acute lung injury.

Authors:  L J Mark Cross; Michael A Matthay
Journal:  Crit Care Clin       Date:  2011-04       Impact factor: 3.598

5.  LASSBio-596: a New Pre-clinical Candidate for Rheumatoid Arthritis?

Authors:  Max Denisson Maurício Viana; Alyne Almeida de Lima; Geraldo José da Silva Neto; Suellen Maria Albuquerque da Silva; Anderson Brandão Leite; Elane Conceição Dos Santos; Ênio José Bassi; Eliane Aparecida Campesatto; Aline Cavalcanti de Queiroz; Eliezer Jesus Barreiro; Lidia Moreira Lima; Magna Suzana Alexandre-Moreira
Journal:  Inflammation       Date:  2021-10-25       Impact factor: 4.092

6.  Nitric oxide rescues thalidomide mediated teratogenicity.

Authors:  Jamila H Siamwala; Vimal Veeriah; M Krishna Priya; Saranya Rajendran; Uttara Saran; Swaraj Sinha; Shunmugam Nagarajan; T Pradeep; Suvro Chatterjee
Journal:  Sci Rep       Date:  2012-09-20       Impact factor: 4.379

7.  Butane-1,4-diaminium 2-(meth-oxy-carbon-yl)benzoate dihydrate.

Authors:  Jian Li
Journal:  Acta Crystallogr Sect E Struct Rep Online       Date:  2011-02-09

8.  2-[4-tert-Butyl-5-(2-chloro-benz-yl)-1,3-thia-zol-2-yl]isoindoline-1,3-dione.

Authors:  Zhi-Gang Yao; Jun-Mei Peng; Su-Fang Huo; Ai-Xi Hu
Journal:  Acta Crystallogr Sect E Struct Rep Online       Date:  2010-10-23

9.  Polyunsaturated fatty acids synergize with lipid droplet binding thalidomide analogs to induce oxidative stress in cancer cells.

Authors:  László G Puskás; Liliána Z Fehér; Csaba Vizler; Ferhan Ayaydin; Erzsébet Rásó; Eszter Molnár; István Magyary; Iván Kanizsai; Márió Gyuris; Ramóna Madácsi; Gabriella Fábián; Klaudia Farkas; Péter Hegyi; Ferenc Baska; Béla Ozsvári; Klára Kitajka
Journal:  Lipids Health Dis       Date:  2010-06-02       Impact factor: 3.876

10.  2-(2-Iodo-phen-yl)isoindoline-1,3-dione.

Authors:  Güneş Demirtaş; Necmi Dege; Ayşen Alaman Ağar; Orhan Büyükgüngör
Journal:  Acta Crystallogr Sect E Struct Rep Online       Date:  2011-03-12
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