Literature DB >> 23960764

Microwave assisted synthesis of novel pyrazolone derivatives attached to a pyrimidine moiety and evaluation of their anti-inflammatory, analgesic and antipyretic activities.

Rishikesh V Antre1, A Cendilkumar, Divakar Goli, Ganesh S Andhale, Rajesh J Oswal.   

Abstract

In the present research work, the motto was to develop new chemical entities as potential anti-inflammatory, analgesic and antipyretic agents. Various 4-(2-amino-6-(substituted)pyrimidin-4-yl)-3-methyl-1-(substituted)-1H-pyrazol-5(4H)-one derivatives (5a-5j) and their Schiff bases (6a-6j) were synthesized. The newly synthesized compounds were characterized by TLC and spectral data. The compounds containing pyrazolone and amino pyrimidine as basic moieties (5a-5j), were screened for their anti-inflammatory, analgesic and antipyretic activities, compounds 5a, 5c-5f, 5h exhibited activities nearly similar to the standard. The pharmacological studies reveal that the presence of 4-hydroxy, 4-methoxy, 4-(N,N-dimethylamino) or 2-hydroxy groups on phenyl ring at C6 of amino pyrimidine exhibits anti-inflammatory, analgesic and antipyretic activities nearly similar to the standard and substitutions like 4-chloro, 2-nitro, 3-nitro or 4-nitro on same phenyl ring lead to a decrease in activities.

Entities:  

Keywords:  Amino pyrimidine; Analgesic; Anti-inflammatory; Antipyretic; Pyrazolone; Schiff bases

Year:  2011        PMID: 23960764      PMCID: PMC3745198          DOI: 10.1016/j.jsps.2011.05.006

Source DB:  PubMed          Journal:  Saudi Pharm J        ISSN: 1319-0164            Impact factor:   4.330


  27 in total

Review 1.  Targeting signal transduction as a strategy to treat inflammatory diseases.

Authors:  Luke A J O'Neill
Journal:  Nat Rev Drug Discov       Date:  2006-06-09       Impact factor: 84.694

2.  Nonsteroidal antiinflammatory agents-part 2 antiinflammatory, analgesic and antipyretic activity of some substituted 3-pyrazolin-5-ones and 1,2,4,5,6,7-3H-hexahydroindazol-3-ones.

Authors:  Soad A M El-Hawash; El-Sayed A M Badawey; Ibrahim M El-Ashmawey
Journal:  Eur J Med Chem       Date:  2005-12-20       Impact factor: 6.514

3.  Further studies on analgesic activity of cyclic imides.

Authors:  V Cechinel Filho; R Corrêa; Z Vaz; J B Calixto; R J Nunes; T R Pinheiro; A D Andricopulo; R A Yunes
Journal:  Farmaco       Date:  1998-01

Review 4.  Discovery and design of selective cyclooxygenase-2 inhibitors as non-ulcerogenic, anti-inflammatory drugs with potential utility as anti-cancer agents.

Authors:  A S Kalgutkar; Z Zhao
Journal:  Curr Drug Targets       Date:  2001-03       Impact factor: 3.465

5.  Hypothermic and antipyretic effects of 3-methyl- and 3-phenyl-5-hydroxy-5-trichloromethyl-4,5-dihydro-1H-pyrazole-1-carboxyamides in mice.

Authors:  Fabiane R Souza; Vanessa T Souza; Viviane Ratzlaff; Lysandro P Borges; Marlí R Oliveira; Helio G Bonacorso; Nilo Zanatta; Marcos A P Martins; Carlos F Mello
Journal:  Eur J Pharmacol       Date:  2002-09-13       Impact factor: 4.432

6.  Design, synthesis, and biological evaluation of novel Tri- and tetrasubstituted imidazoles as highly potent and specific ATP-mimetic inhibitors of p38 MAP kinase: focus on optimized interactions with the enzyme's surface-exposed front region.

Authors:  Stefan A Laufer; Dominik R J Hauser; David M Domeyer; Katrin Kinkel; Andy J Liedtke
Journal:  J Med Chem       Date:  2008-06-26       Impact factor: 7.446

7.  Design, synthesis and pharmacological screening of novel nitric oxide donors containing 1,5-diarylpyrazolin-3-one as nontoxic NSAIDs.

Authors:  Shashikant V Bhandari; Sudarshan C Dangre; Kailash G Bothara; Ajit A Patil; Aniket P Sarkate; Deepak K Lokwani; Suraj T Gore; Bhavana J Deshmane; Vyankatesh T Raparti; Chetan V Khachane
Journal:  Eur J Med Chem       Date:  2009-07-04       Impact factor: 6.514

8.  Antioxidant and antibacterial studies of arylazopyrazoles and arylhydrazonopyrazolones containing coumarin moiety.

Authors:  P Manojkumar; T K Ravi; S Gopalakrishnan
Journal:  Eur J Med Chem       Date:  2009-07-16       Impact factor: 6.514

9.  Synthesis of novel 1-pyrazolylpyridin-2-ones as potential anti-inflammatory and analgesic agents.

Authors:  Magda M F Ismail; Yousry A Ammar; Heba S A El-Zahaby; Sally I Eisa; Saber El-Sayed Barakat
Journal:  Arch Pharm (Weinheim)       Date:  2007-09       Impact factor: 3.751

10.  Edaravone derivatives containing NO-donor functions.

Authors:  Konstantin Chegaev; Clara Cena; Marta Giorgis; Barbara Rolando; Paolo Tosco; Massimo Bertinaria; Roberta Fruttero; Pierre-Alain Carrupt; Alberto Gasco
Journal:  J Med Chem       Date:  2009-01-22       Impact factor: 7.446

View more
  4 in total

1.  In vitro antioxidant and in vivo antidepressant activity of green synthesized azomethine derivatives of cinnamaldehyde.

Authors:  Sridevi Chigurupati; Sohrab Akhtar Shaikh; Jahidul Islam Mohammad; Kesavanarayanan Krishnan Selvarajan; Appala Raju Nemala; Chu How Khaw; Chun Foo Teoh; Ting Hei Kee
Journal:  Indian J Pharmacol       Date:  2017 May-Jun       Impact factor: 1.200

2.  Design, synthesis and the biological evaluation of new 1,3-thiazolidine-4-ones based on the 4-amino-2,3-dimethyl-1-phenyl-3-pyrazolin-5-one scaffold.

Authors:  Maria Apotrosoaei; Ioana Mirela Vasincu; Maria Dragan; Frédéric Buron; Sylvain Routier; Lenuta Profire
Journal:  Molecules       Date:  2014-09-04       Impact factor: 4.411

Review 3.  Pyrazolone structural motif in medicinal chemistry: Retrospect and prospect.

Authors:  Zefeng Zhao; Xufen Dai; Chenyang Li; Xiao Wang; Jiale Tian; Ying Feng; Jing Xie; Cong Ma; Zhuang Nie; Peinan Fan; Mingcheng Qian; Xirui He; Shaoping Wu; Yongmin Zhang; Xiaohui Zheng
Journal:  Eur J Med Chem       Date:  2019-11-16       Impact factor: 6.514

4.  Rational Design and Synthesis of Diverse Pyrimidine Molecules Bearing Sulfonamide Moiety as Novel ERK Inhibitors.

Authors:  Ahmed H Halawa; Areej A Eskandrani; Walid E Elgammal; Saber M Hassan; Ahmed H Hassan; Hassan Y Ebrahim; Ahmed B M Mehany; Ahmed M El-Agrody; Rawda M Okasha
Journal:  Int J Mol Sci       Date:  2019-11-08       Impact factor: 5.923

  4 in total

北京卡尤迪生物科技股份有限公司 © 2022-2023.