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

页码：645 / 654

页数：10

共 50 条

[1] 1,3,4-Trisubstituted pyrazole analogues as promising anti-inflammatory agents
Alegaon, S. G.
Alagawadi, K. R.
Garg, M. K.
Dushyant, K.
Vinod, D.
BIOORGANIC CHEMISTRY, 2014, 54 : 51 - 59
[2] Synthesis of novel pyrazole and dihydropyrazoles derivatives as potential anti-inflammatory and analgesic agents
Abd-El Gawad, Nagwa M.
Georgey, Hanan H.
Ibrahim, Nashwa A.
Amin, Noha H.
Abdelsalam, Rania M.
ARCHIVES OF PHARMACAL RESEARCH, 2012, 35 (05) : 807 - 821
[3] Synthesis and biological evaluation of 1,3,4-trisubstituted pyrazole analogues as anti-mycobacterial agents
Alegaon, Shankar G.
Hirpara, Mita B.
Alagawadi, K. R.
Jalalpure, S. S.
Rasal, V. P.
Salve, Preeti S.
Kumbar, V. M.
MEDICINAL CHEMISTRY RESEARCH, 2017, 26 (06) : 1127 - 1138
[4] Novel anti-inflammatory and analgesic agents: synthesis, molecular docking and in vivo studies
Ugwu, David Izuchukwu
Okoro, Uchechukwu Christopher
Ukoha, Pius Onyeoziri
Gupta, Astha
Okafor, Sunday N.
JOURNAL OF ENZYME INHIBITION AND MEDICINAL CHEMISTRY, 2018, 33 (01) : 405 - 415
[5] Synthesis of New Nicotinic Acid Derivatives and Their Evaluation as Analgesic and Anti-inflammatory Agents
Khalil, Nadia Abdalla
Ahmed, Eman Mohamed
Mohamed, Khaled Omar
Zaitone, Sawsan Abo-Bakr
CHEMICAL & PHARMACEUTICAL BULLETIN, 2013, 61 (09) : 933 - 940
[6] Investigations of new N1-substituted pyrazoles as anti-inflammatory and analgesic agents having COX inhibitory activity
Said, Mona F.
George, Riham F.
Fayed, Walid
Soliman, Ahmed A. F.
Refaey, Rana H.
FUTURE MEDICINAL CHEMISTRY, 2024, 16 (04) : 349 - 368
[7] Synthesis and pharmacological evaluation of new pyrazolyl benzenesulfonamides linked to polysubstituted pyrazoles and thiazolidinones as anti-inflammatory and analgesic agents
Ashour, Hayam M. A.
El-Ashmawy, Ibrahim M.
Bayad, Aida E.
MONATSHEFTE FUR CHEMIE, 2016, 147 (03): : 605 - 618
[8] Novel 1,3,4-oxadiazole/oxime hybrids: Synthesis, docking studies and investigation of anti-inflammatory, ulcerogenic liability and analgesic activities
Abd-Ellah, Heba S.
Abdel-Aziz, Mohamed
Shoman, Mai E.
Beshr, Eman A. M.
Kaoud, Tamer S.
Ahmed, Al-Shaimaa F. F.
BIOORGANIC CHEMISTRY, 2016, 69 : 48 - 63
[9] Synthesis, characterization, and cytotoxic activity of some new 1,3,4-trisubstituted pyrazoles against diverse tumor cell lines
Srour, Aladdin M.
Fahmy, Hoda H.
Khater, Mai A.
El-Manawaty, May A.
Shalaby, ElSayed M.
MONATSHEFTE FUR CHEMIE, 2018, 149 (06): : 1137 - 1147
[10] 1,3,4-Trisubstituted Pyrazoles: Synthesis, Antimicrobial Evaluation, and Time Resolved Studies
Kumar, Parmod
Sood, Sumit
Kumar, Anil
Verma, Anurakshee
Kumar, Lalit
Kumar, Sunil
Kumar, Vijay
Kumar, Anil
Singh, Karan
POLYCYCLIC AROMATIC COMPOUNDS, 2023, 43 (04) : 2960 - 2972

← 1 2 3 4 5 →