Literature DB >> 24835630

Conventional and microwave assisted synthesis of pyrazolone Mannich bases possessing anti-inflammatory, analgesic, ulcerogenic effect and antimicrobial properties.

Kullampalayam Krishnasamy Sivakumar1, Aiyalu Rajasekaran2, Palaniappan Senthilkumar2, Prasad P Wattamwar2.   

Abstract

In the present study, an efficient synthesis of some Mannich base of 5-methyl-2-[(2-oxo-2H-chromen-3-yl)carbonyl]-2,4-dihydro-3H-pyrazol-3-one (4a-j) have been described by using conventional and non-conventional (microwave) techniques. Microwave assisted reactions showed that require shorter reaction time and good yield. The newly synthesized compounds were screened for their anti-inflammatory, analgesic activity, antioxidant, and antibacterial effects were compared with standard drug. Among the compounds studied, compound (4f) showing nearly equipotent anti-inflammatory and analgesic activity than the standard drug (indomethacin), along with minimum ulcerogenic index. Compounds (4b and 4i) showing 1.06 times more active than ciprofloxacin against tested Gram-negative bacteria.
Copyright © 2014 Elsevier Ltd. All rights reserved.

Entities:  

Keywords:  Analgesic; Anti-inflammatory; Antibacterial; Antioxidant; Coumarins; Pyrazolone

Mesh:

Substances:

Year:  2014        PMID: 24835630     DOI: 10.1016/j.bmcl.2014.04.067

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


  4 in total

1.  Synthesis and Hypoglycemic and Anti-inflammatory Activity Screening of Novel Substituted 5-[Morpholino(Phenyl)Methyl]-Thiazolidine-2,4-Diones and Their Molecular Docking Studies.

Authors:  Srikanth Kumar Karumanchi; Lakshmana Rao Atmakuri; V Basaveswara Rao Mandava; Srikala Rajala
Journal:  Turk J Pharm Sci       Date:  2019-11-11

Review 2.  Mannich bases: an important pharmacophore in present scenario.

Authors:  Suman Bala; Neha Sharma; Anu Kajal; Sunil Kamboj; Vipin Saini
Journal:  Int J Med Chem       Date:  2014-11-12

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.  Tyrosinase-mediated synthesis of larvicidal active 1,5-diphenyl pent-4-en-1-one derivatives against Culex quinquefasciatus and investigation of their ichthyotoxicity.

Authors:  SathishKumar Chidambaram; Daoud Ali; Saud Alarifi; Raman Gurusamy; SurendraKumar Radhakrishnan; Idhayadhulla Akbar
Journal:  Sci Rep       Date:  2021-10-20       Impact factor: 4.379

  4 in total

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