Synthesis of novel 1,3,4-trisubstituted pyrazoles as anti-inflammatory and analgesic agents

被引：87
|
作者：
Ragab, Fatma A. [1 ]
Gawad, Nagwa M. Abdel [1 ]
Georgey, Hanan H. [1 ]
Said, Mona F. [1 ]
机构：
[1] Cairo Univ, Fac Pharm, Dept Pharmaceut Chem, Cairo, Egypt
来源：
EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY | 2013年 / 63卷
关键词：
Pyrazole; Schiff's base; Pyrrole; Anti-inflammatory; Analgesic; COX inhibition; SELECTIVE COX-2 INHIBITORS; BIOLOGICAL EVALUATION; CYCLOOXYGENASE-2; INHIBITORS; DERIVATIVES; DESIGN; SYNTHASE; ASPIRIN; DRUGS; ACIDS; RAT;
D O I：
10.1016/j.ejmech.2013.03.005
中图分类号：
R914 [药物化学];
学科分类号：
100701 ;
摘要：
Some novel 1,3,4-trisubstituted pyrazoles were synthesized and screened for their anti-inflammatory and analgesic activities as well as their ulcerogenic liability. They showed anti-inflammatory and analgesic activities with better GIT tolerance than the standard drug phenylbutazone. In addition, IC50 values for 5e and 8e were recorded. Compound 5e was found to be the most active one as anti-inflammatory and analgesic agent. On the other hand, COX-1/COX-2 isozyme selectivity was also done which showed equal inhibition to both isoforms. (c) 2013 Elsevier Masson SAS. All rights reserved.
引用
收藏
页码：645 / 654
页数：10
相关论文
共 50 条
  • [21] Synthesis and pharmacological evaluation of 1,3,4-oxadiazole bearing bis(heterocycle) derivatives as anti-inflammatory and analgesic agents
    Jayashankar, B.
    Rai, K. M. Lokanath
    Baskaran, N.
    Sathish, H. S.
    EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY, 2009, 44 (10) : 3898 - 3902
  • [22] Chitosan/CuO nanocomposite films mediated regioselective synthesis of 1,3,4-trisubstituted pyrazoles under microwave irradiation
    Aljuhani, Ateyatallah
    Riyadh, Sayed M.
    Khalil, Khaled D.
    JOURNAL OF SAUDI CHEMICAL SOCIETY, 2021, 25 (08)
  • [23] The synthesis of cytotoxic 1,3,4-trisubstituted azetidinones-2
    Veiberg, G
    Bokaldere, R
    Vorona, M
    Kanepe, I
    Shestakova, I
    Lukevics, E
    KHIMIYA GETEROTSIKLICHESKIKH SOEDINENII, 2003, (05): : 680 - 687
  • [24] Synthesis, in silico experiments and biological evaluation of 1,3,4-trisubstituted pyrazole derivatives as antimalarial agents
    Bekhit, Adnan A.
    Saudi, Manal N.
    Hassan, Ahmed M. M.
    Fahmy, Salwa M.
    Ibrahim, Tamer M.
    Ghareeb, Doaa
    El-Seidy, Aya M.
    Nasralla, Sherry N.
    Bekhit, Alaa El-Din A.
    EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY, 2019, 163 : 353 - 366
  • [25] Design, synthesis and biological evaluation of novel 1,3,4-trisubstituted pyrazole derivatives as potential chemotherapeutic agents for hepatocellular carcinoma
    Harras, Marwa F.
    Sabour, Rehab
    BIOORGANIC CHEMISTRY, 2018, 78 : 149 - 157
  • [26] Pyrazoles and Pyrazolines as Anti-Inflammatory Agents
    Mantzanidou, Martha
    Pontiki, Eleni
    Hadjipavlou-Litina, Dimitra
    MOLECULES, 2021, 26 (11):
  • [27] NOVEL FORMAZANS AS POTENT ANTI-INFLAMMATORY AND ANALGESIC AGENTS
    KALSI, R
    PANDE, K
    BHALLA, TN
    PARMAR, SS
    BARTHWAL, JP
    PHARMACOLOGY, 1988, 37 (04) : 218 - 224
  • [28] NOVEL THIAZOLIDINONES AS POTENT ANTI-INFLAMMATORY AND ANALGESIC AGENTS
    TANDON, M
    KUMAR, P
    PANDE, K
    BHALLA, TN
    BARTHWAL, JP
    PHARMACOLOGY, 1985, 31 (05) : 260 - 267
  • [29] Synthesis of novel 1-pyrazolylpyridin-2-ones as potential anti-inflammatory and analgesic agents
    Ismail, Magda M. F.
    Ammar, Yousry A.
    El-Zahaby, Heba S. A.
    Eisa, Sally I.
    Barakat, Saber El-Sayed
    ARCHIV DER PHARMAZIE, 2007, 340 (09) : 476 - 482
  • [30] Synthesis, characterization, and cytotoxic activity of some new 1,3,4-trisubstituted pyrazoles against diverse tumor cell lines
    Aladdin M. Srour
    Hoda H. Fahmy
    Mai A. Khater
    May A. El-Manawaty
    ElSayed M. Shalaby
    Monatshefte für Chemie - Chemical Monthly, 2018, 149 : 1137 - 1147
12345