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
  • [31] Synthesis of some new amide-linked bipyrazoles and their evaluation as anti-inflammatory and analgesic agents
    Faour, Wissam H.
    Mroueh, Mohamed
    Daher, Costatantine F.
    Elbayaa, Rasha Y.
    Ragab, Hanan M.
    Ghoneim, Asser I.
    El-mallah, Ahmed I.
    Ashour, Hayam M. A.
    JOURNAL OF ENZYME INHIBITION AND MEDICINAL CHEMISTRY, 2016, 31 (06) : 1079 - 1094
  • [32] Synthesis and biological evaluation of new pyrazolone-pyridazine conjugates as anti-inflammatory and analgesic agents
    Khalil, Nadia Abdalla
    Ahmed, Eman Mohamed
    Mohamed, Khaled Omar
    Nissan, Yassin Mohammed
    Zaitone, Sawsan Abo-Bakr
    BIOORGANIC & MEDICINAL CHEMISTRY, 2014, 22 (07) : 2080 - 2089
  • [33] Design and synthesis of tryptophan containing peptides as potential analgesic and anti-inflammatory agents
    Suhas, R.
    Gowda, D. Channe
    JOURNAL OF PEPTIDE SCIENCE, 2012, 18 (08) : 535 - 540
  • [34] Anti-inflammatory, analgesic and COX-2 inhibitory activity of novel thiadiazoles in irradiated rats
    Ragab, Fatma A.
    Heiba, Helmi I.
    El-Gazzar, Marwa G.
    Abou-Seri, Sahar M.
    El-Sabbagh, Walaa A.
    El-Hazek, Reham M.
    JOURNAL OF PHOTOCHEMISTRY AND PHOTOBIOLOGY B-BIOLOGY, 2017, 166 : 285 - 300
  • [35] Synthesis and Molecular Docking Study of Novel Hybrids of 1,3,4-Oxadiazoles and Quinoxaline as a Potential Analgesic and Anti-Inflammatory Agents
    Dewangan, Dhansay
    Nakhate, Kartik T.
    Verma, Vinay Sagar
    Nagori, Kushagra
    Badwaik, Hemant
    Nair, Nisha
    Tripathi, Dulal Krishna
    Mishra, Achal
    JOURNAL OF HETEROCYCLIC CHEMISTRY, 2018, 55 (12) : 2901 - 2910
  • [36] N-arylmethylideneaminophthalimide: Design, Synthesis and Evaluation as Analgesic and Anti-inflammatory Agents
    Banarouet, Nasimossadat
    Davood, Asghar
    Shafaroodi, Hamed
    Saeedi, Ghazaleh
    Shafiee, Abbas
    MINI-REVIEWS IN MEDICINAL CHEMISTRY, 2019, 19 (08) : 679 - 687
  • [37] Design, synthesis and biological evaluation of 1,3,4-oxadiazoles as promising anti-inflammatory agents
    Iyer, Vishwanathan Balasubramanya
    Gurupadayya, Bannimath
    Koganti, Venkata Sairam
    Inturi, Bharthkumar
    Chandan, Ravandur Shivanna
    MEDICINAL CHEMISTRY RESEARCH, 2017, 26 (01) : 190 - 204
  • [38] Synthesis and Evaluation of Analgesic and Anti-Inflammatory Properties of Novel Ibuprofen Analogs
    Ahmadi, Abbas
    Khalili, Mohsen
    Zandieh, Haniyeh
    Nahri-Niknafs, Babak
    PHARMACEUTICAL CHEMISTRY JOURNAL, 2015, 49 (08) : 530 - 536
  • [39] New 1,3,4-thiadiazole Derivatives Endowed with Analgesic and Anti-inflammatory Activities
    Pandey, Ajit Kumar
    Kashyap, Pranita P.
    Kaur, Chanchal Deep
    Sawarkar, Hemant A.
    Dhongade, Hemant J.
    Singh, Mukesh Kumar
    CHIANG MAI JOURNAL OF SCIENCE, 2018, 45 (02): : 917 - 926
  • [40] Pyrazoles as Promising Scaffold for the Synthesis of Anti-Inflammatory and/or Antimicrobial Agent: A Review
    Bekhit, Adnan A.
    Hymete, Ariaya
    Bekhit, Alaa El-Din A.
    Damtew, Ashenafi
    Aboul-Enein, Hassan Y.
    MINI-REVIEWS IN MEDICINAL CHEMISTRY, 2010, 10 (11) : 1014 - 1033
12345