Literature DB >> 18395299

1,3,4-Oxadiazole/thiadiazole and 1,2,4-triazole derivatives of biphenyl-4-yloxy acetic acid: synthesis and preliminary evaluation of biological properties.

Harish Kumar1, Sadique A Javed, Suroor A Khan, Mohammad Amir.   

Abstract

A series of 1,3,4-oxadiazole/thiadiazole and 1,2,4-triazole derivatives of biphenyl-4-yloxy acetic acid were synthesized in order to obtain new compounds with potential anti-inflammatory activity, analgesic activity and lower ulcerogenic potential. All compounds were evaluated for their anti-inflammatory activity by the carrageenan induced rat paw edema test method. The compounds possessing potent anti-inflammatory activity were further tested for their analgesic, ulcerogenic and antioxidant activities. Out of all tested compounds, the compounds 3, 7, 17 and 20, showed significant reduction in rat paw edema induced by carrageenan treatment. These compounds showed significant analgesic effect and at an equimolar oral doses relative to flurbiprofen were also found to be non-gastrotoxic in rats. Compound 17 was evaluated as the lead compound having more anti-inflammatory activity (81.81%) than the reference drug (79.54%), low ulcerogenic potential and protective effect on lipid peroxidation.

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Year:  2008        PMID: 18395299     DOI: 10.1016/j.ejmech.2008.01.039

Source DB:  PubMed          Journal:  Eur J Med Chem        ISSN: 0223-5234            Impact factor:   6.514


  15 in total

1.  Severe acute respiratory syndrome coronavirus replication inhibitor that interferes with the nucleic acid unwinding of the viral helicase.

Authors:  Adeyemi O Adedeji; Kamalendra Singh; Nicholas E Calcaterra; Marta L DeDiego; Luis Enjuanes; Susan Weiss; Stefan G Sarafianos
Journal:  Antimicrob Agents Chemother       Date:  2012-06-25       Impact factor: 5.191

2.  A convenient four-component one-pot synthesis of 2-amino-1,3,4-thiadiazoles in water.

Authors:  Peng Liu; Ao-Ze Su; Yuan-Qiang Wang; Ze-Mei Ge; Tie-Ming Cheng; Run-Tao Li
Journal:  Mol Divers       Date:  2014-06-29       Impact factor: 2.943

3.  2-(Biphenyl-4-yl-oxy)acetic acid.

Authors:  En-Ju Wang; Guang-Ying Chen
Journal:  Acta Crystallogr Sect E Struct Rep Online       Date:  2011-01-29

4.  Selective Cytotoxicity of 1,3,4-Thiadiazolium Mesoionic Derivatives on Hepatocarcinoma Cells (HepG2).

Authors:  Gustavo Jabor Gozzi; Amanda do Rocio Andrade Pires; Glaucio Valdameri; Maria Eliane Merlin Rocha; Glaucia Regina Martinez; Guilhermina Rodrigues Noleto; Alexandra Acco; Carlos Eduardo Alves de Souza; Aurea Echevarria; Camilla Moretto Dos Reis; Attilio Di Pietro; Sílvia Maria Suter Correia Cadena
Journal:  PLoS One       Date:  2015-06-17       Impact factor: 3.240

5.  Novel 2,5-disubstituted-1,3,4-oxadiazoles as anti-inflammatory drugs.

Authors:  Ega Durgashivaprasad; Geetha Mathew; Sarine Sebastian; S A Manohar Reddy; Jayesh Mudgal; Gopalan Kutty Nampurath
Journal:  Indian J Pharmacol       Date:  2014 Sep-Oct       Impact factor: 1.200

Review 6.  Synthetic methods, chemistry, and the anticonvulsant activity of thiadiazoles.

Authors:  Bhawna Sharma; Amita Verma; Sunil Prajapati; Upendra Kumar Sharma
Journal:  Int J Med Chem       Date:  2013-04-30

7.  Synthesis and Anticancer Evaluation of New 1,3,4-Oxadiazole Derivatives.

Authors:  Camelia Elena Stecoza; George Mihai Nitulescu; Constantin Draghici; Miron Teodor Caproiu; Octavian Tudorel Olaru; Marinela Bostan; Mirela Mihaila
Journal:  Pharmaceuticals (Basel)       Date:  2021-05-06

8.  Synthesis and antimicrobial evaluation of some novel 1,2,4-triazole and 1,3,4-thiadiazole derivatives.

Authors:  Lukasz Popiołek; Urszula Kosikowska; Liliana Mazur; Maria Dobosz; Anna Malm
Journal:  Med Chem Res       Date:  2012-11-11       Impact factor: 1.965

9.  Synthesis and antioxidant activity evaluation of new compounds from hydrazinecarbothioamide and 1,2,4-triazole class containing diarylsulfone and 2,4-difluorophenyl moieties.

Authors:  Stefania-Felicia Barbuceanu; Diana Carolina Ilies; Gabriel Saramet; Valentina Uivarosi; Constantin Draghici; Valeria Radulescu
Journal:  Int J Mol Sci       Date:  2014-06-17       Impact factor: 5.923

10.  4-[(5-Bromo-2-hy-droxy-benzyl-idene)amino]-3-ethyl-1H-1,2,4-triazole-5(4H)-thione.

Authors:  Cai-Xia Yuan; Shu-Fen Lan; Xin-Yu Liu; Miao-Li Zhu
Journal:  Acta Crystallogr Sect E Struct Rep Online       Date:  2014-07-26
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