Literature DB >> 15203134

Synthesis and pharmacological evaluation of amide conjugates of NSAIDs with L-cysteine ethyl ester, combining potent antiinflammatory and antioxidant properties with significantly reduced gastrointestinal toxicity.

Dimitrios Galanakis1, Angeliki P Kourounakis, Karyophyllis C Tsiakitzis, Christos Doulgkeris, Eleni A Rekka, Antonios Gavalas, Constantina Kravaritou, Christos Charitos, Panos N Kourounakis.   

Abstract

The synthesis and pharmacological evaluation of a series of amide derivatives of NSAIDs with L-cysteine ethyl ester is described. The novel derivatives are potent antiinflammatory, antioxidant and hypocholesterolemic-hypolipidemic agents, while they demonstrate considerably reduced gastrointestinal toxicity. This molecular modification may offer a general route to safer antiinflammatory agents, potentially suitable for chronic use in conditions such as neurodegenerative disorders.

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Year:  2004        PMID: 15203134     DOI: 10.1016/j.bmcl.2004.05.025

Source DB:  PubMed          Journal:  Bioorg Med Chem Lett        ISSN: 0960-894X            Impact factor:   2.823


  14 in total

1.  Synthesis of tert-butyl (substituted benzamido)phenylcarbamate derivatives: anti-inflammatory activity and docking studies.

Authors:  Shankar Bhookya; Jalapathi Pochampally; Anil Valeru; Vianala Sunitha; Saikrishna Balabadra; Vijjulatha Manga; Karunakar Rao Kudle
Journal:  J Chem Biol       Date:  2017-04-05

2.  2-[2-(2,6-Dichloro-anilino)phen-yl]-N-[(2S)-2-methyl-3-oxo-8-phenyl-1-thia-4-aza-spiro-[4.5]dec-4-yl]acetamide.

Authors:  Mehmet Akkurt; Mebble Nassozi; Ayşe Kocabalkanlı; Islam Ullah Khan; Shahzad Sharif
Journal:  Acta Crystallogr Sect E Struct Rep Online       Date:  2010-03-20

3.  A novel NSAID derivative, phospho-ibuprofen, prevents AOM-induced colon cancer in rats.

Authors:  Nengtai Ouyang; Ping Ji; Jennie L Williams
Journal:  Int J Oncol       Date:  2012-12-28       Impact factor: 5.650

4.  Synthesis and evaluation of antiinflammatory, analgesic and ulcerogenic potential of NSAIDs bearing 1,3,4-oxadiazole scaffold.

Authors:  R R Somani; U V Bhanushali
Journal:  Indian J Pharm Sci       Date:  2011-11       Impact factor: 0.975

5.  A tale of switched functions: from cyclooxygenase inhibition to M-channel modulation in new diphenylamine derivatives.

Authors:  Asher Peretz; Nurit Degani-Katzav; Maya Talmon; Eyal Danieli; Anna Gopin; Eti Malka; Rachel Nachman; Amiram Raz; Doron Shabat; Bernard Attali
Journal:  PLoS One       Date:  2007-12-26       Impact factor: 3.240

6.  Benzimidazole derivatives: search for GI-friendly anti-inflammatory analgesic agents.

Authors:  Monika Gaba; Punam Gaba; Deepika Uppal; Neelima Dhingra; Malkeet Singh Bahia; Om Silakari; Chander Mohan
Journal:  Acta Pharm Sin B       Date:  2015-06-25       Impact factor: 11.413

7.  4-[(4-Bromo-phenyl)amino]-2-methyl-idene-4-oxo-butanoic acid.

Authors:  B Narayana; Prakash S Nayak; Balladka K Sarojini; Jerry P Jasinski
Journal:  Acta Crystallogr Sect E Struct Rep Online       Date:  2014-06-14

8.  4-[(4-Acetyl-phen-yl)amino]-2-methyl-idene-4-oxo-butanoic acid.

Authors:  B Narayana; Prakash S Nayak; Balladka K Sarojini; Jerry P Jasinski
Journal:  Acta Crystallogr Sect E Struct Rep Online       Date:  2014-06-07

9.  Synthesis, In Vivo Anti-Inflammatory Activity, and Molecular Docking Studies of New Isatin Derivatives.

Authors:  Ravi Jarapula; Kiran Gangarapu; Sarangapani Manda; Sriram Rekulapally
Journal:  Int J Med Chem       Date:  2016-02-14

Review 10.  Prodrugs of NSAIDs: A Review.

Authors:  Kamal Shah; Jeetendra K Gupta; Nagendra S Chauhan; Neeraj Upmanyu; Sushant K Shrivastava; Pradeep Mishra
Journal:  Open Med Chem J       Date:  2017-11-30
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