Synthesis, Pharmacological Evaluation and Docking Study of Novel 3-Phenyl-5-Aryl-4, 5-Dihydro-1h-Pyrazole-1-Carbaldehyde as Anti-Inflammatory Agents

被引:0
作者
Nikalje, Anna Pratima G. [1 ]
Gaikwad, Gaurav [1 ]
Nawale, Rajesh [2 ]
Sangshetti, Jaiprakash [1 ]
Khan, Firoz A. [1 ]
机构
[1] YB Chavan Coll Pharm, Dept Pharmaceut Chem, Dr Rafiq Zakaria Campus,Rauza Bagh,PB 33, Aurangabad 431001, Maharashtra, India
[2] Govt Coll Pharm, Dept Pharmacol, Aurangabad 431001, Maharashtra, India
来源
RESEARCH JOURNAL OF PHARMACEUTICAL BIOLOGICAL AND CHEMICAL SCIENCES | 2015年 / 6卷 / 02期
关键词
Pyrazloe; carbaldehyde; Anti-inflammatory; NSAIDs; Rat paw edema; Molecular docking;
D O I
暂无
中图分类号
O [数理科学和化学]; P [天文学、地球科学]; Q [生物科学]; N [自然科学总论];
学科分类号
07 ; 0710 ; 09 ;
摘要
A series of novel 3-phenyl-5-aryl-4, 5-dihydro-1H-pyrazole-1-carbaldehyde derivatives 4(a-j) were obtained by refluxing chalcones 3(a-j) and hydrazine hydrate in presence of formic acid in milder reaction conditions. The synthesized compounds 4(a-j) were investigated for in-vivo anti-inflammatory activity in Carrageenan induced rat paw edema model. Some of the synthesized derivatives exhibited good anti-inflammatory activity compaired with diclofenac, while some derivatives have shown comparable anti-inflammatory activity to that of diclofenac. All the synthesized derivatives were found to be potent anti-inflammatory agents. Some of the derivatives were evaluated for ulcerogenic potential and their ulcer index was found to be less than the standard drug diclofenac. The molecular docking analysis was performed to understand the binding interactions of these compounds to COX-2 enzyme. The results from the present investigation suggests that 3-phenyl-5-aryl-4, 5-dihydro-1H-pyrazole-1-carbaldehyde as a promising template for the design of new anti-inflammatory agents.
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收藏
页码:423 / 431
页数:9
相关论文
共 17 条
  • [1] Design, synthesis and pharmacological screening of novel nitric oxide donors containing 1,5-diarylpyrazolin-3-one as nontoxic NSAIDs
    Bhandari, Shashikant V.
    Dangre, Sudarshan C.
    Bothara, Kailash G.
    Patil, Ajit A.
    Sarkate, Aniket P.
    Lokwani, Deepak K.
    Gore, Suraj T.
    Deshmane, Bhavana J.
    Raparti, Vyankatesh T.
    Khachane, Chetan V.
    [J]. EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY, 2009, 44 (11) : 4622 - 4636
  • [2] BRZOZOWSKI Z, 1979, ACTA POL PHARM, V36, P645
  • [3] Delay F, 1992, PATENTSCHRIFF, V117, P90276
  • [4] Hiroyuti O, 1988, J P APPL, Patent No. 295695
  • [5] Synthesis and pharmacological evaluation of a novel series of 5-(substituted) aryl-3-(3-coumarinyl)-1-phenyl-2-pyrazolines as novel anti-inflammatory and analgesic agents
    Khode, Suresh
    Maddi, Veeresh
    Aragade, Prashant
    Palkar, Mahesh
    Ronad, Pradeep Kumar
    Mamledesai, Shivalingarao
    Thippeswamy, A. H. M.
    Satyanarayana, D.
    [J]. EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY, 2009, 44 (04) : 1682 - 1688
  • [6] Korgaokar S. S., 1996, Indian Journal of Pharmaceutical Sciences, V58, P222
  • [7] Synthesis of 1-substituted 5-aryl-3-(3-coumarinyl)-2-pyrazolines by the reaction of 3-aryl-1-(3-coumarinyl)propen-1-ones with hydrazines
    Lévai, A
    Jekö, J
    Brahmbhatt, DI
    [J]. JOURNAL OF HETEROCYCLIC CHEMISTRY, 2005, 42 (06) : 1231 - 1235
  • [8] Malhora P, 2010, INT J PHARM PHARM SC, V2, P21
  • [9] Menozzi Giulia, 2003, Farmaco (Lausanne), V58, P795, DOI 10.1016/S0014-827X(03)00136-8
  • [10] Nauduri D, 1998, CHEM PHARM BULL, V46, P1254, DOI 10.1248/cpb.46.1254