Synthesis and Biological Evaluation of New Diarylpyrazole and Triarylimidazoline Derivatives as Selective COX-2 Inhibitors

被引：19

作者：

Abdellatif, Khaled R. A. ^{[1
,2
]}

Abdelgawad, Mohamed A. ^{[1
,3
]}

Labib, Madlen B. ^{[1
]}

Zidan, Taha H.

机构：

[1] Beni Suef Univ, Fac Pharm, Dept Organ Pharmaceut Chem, Bani Suwayf 62514, Egypt

[2] Ibn Sina Natl Coll Med Studies, Dept Pharmaceut Sci, Jeddah, Saudi Arabia

[3] Aljouf Univ, Coll Pharm, Dept Pharmaceut Chem, Sakaka, Aljouf, Saudi Arabia

来源：

ARCHIV DER PHARMAZIE | 2017年 / 350卷 / 08期

关键词：

Anti-inflammatory; Imidazoline; Pyrazole; Selective COX-2 inhibitor; DONOR ESTER PRODRUGS; ANTIINFLAMMATORY EVALUATION; CYCLOOXYGENASE INHIBITION; DESIGN;

D O I：

10.1002/ardp.201600386

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

New series of diarylpyrazoles 8a-f and triarylimidazoline-5-ones 11a-g were synthesized and evaluated for their in vitro cyclooxygenase-1 (COX-1) and COX-2 inhibitory activity and in vivo anti-inflammatory activity. The synthesized compounds showed good selectivity for COX-2; compounds 8a, 8d, 8f, 11a, and 11c exhibited the highest COX-2 selectivity indexes (SI=4.77-5.43) compared to the reference drug celecoxib (SI=7.8). All compounds showed good in vivo anti-inflammatory activity, especially compounds 8a, 8f, 11c, and 11d, which also showed some similarities to the time interval pattern of celecoxib at all different time intervals (1, 3, and 6h).

引用

下载

页数：10

共 50 条

[1] Synthesis and biological evaluation of ester derivatives of indomethacin as selective COX-2 inhibitors
M. Arockia Babu
Rakesh Shukla
Chandishwar Nath
S. G. Kaskhedikar
Medicinal Chemistry Research, 2012, 21 : 2223 - 2228
[2] Synthesis and biological evaluation of resveratrol amide derivatives as selective COX-2 inhibitors
Xin, Min
Wu, Haoyu
Du, Yuan
Liu, Sheng
Zhao, Feng
Mou, Xiaofeng
CHEMICO-BIOLOGICAL INTERACTIONS, 2023, 380
[3] Synthesis and biological evaluation of ester derivatives of indomethacin as selective COX-2 inhibitors
Babu, M. Arockia
Shukla, Rakesh
Nath, Chandishwar
Kaskhedikar, S. G.
MEDICINAL CHEMISTRY RESEARCH, 2012, 21 (09) : 2223 - 2228
[4] Synthesis and Evaluation of Benzimidazole Derivatives as Selective COX-2 Inhibitors
Rathore, Ankita
Mujeeb-Ur-Rahman
Siddiqui, Anees A.
Ali, Abuzer
Yar, Mohammad Shahar
MEDICINAL CHEMISTRY, 2015, 11 (02) : 188 - 199
[5] Synthesis and Biological Evaluation of New imidazo[1,2-a]pyridine Derivatives as Selective COX-2 Inhibitors
Movahed, Mahsa Azami
Daraei, Bahram
Zarghi, Afshin
LETTERS IN DRUG DESIGN & DISCOVERY, 2016, 13 (08) : 793 - 799
[6] Sulfonilamidothiopyrimidone and thiopyrimidone derivatives as selective COX-2 inhibitors: Synthesis, biological evaluation, and docking studies
Basile, Livia
Alvarez, Susana
Blanco, Almudena
Santagati, Andrea
Granata, Giuseppe
Di Pietro, Patrizia
Guccione, Salvatore
Angeles Munoz-Fernandez, Ma
EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY, 2012, 57 : 149 - 161
[7] Design, Synthesis, and Biological Evaluation of New Peptide Analogues as Selective COX-2 Inhibitors
Ahmaditaba, Mohammad A.
Shahosseini, Soraya
Daraei, Bahram
Zarghi, Afshin
Tehrani, Mohammad H. Houshdar
ARCHIV DER PHARMAZIE, 2017, 350 (10)
[8] Synthesis of new imidazolones and their biological evaluation as COX-2 inhibitors
Mohamed, Lamia W.
El-Badry, Osama
El-Ansary, Afaf K.
Ismael, Ahmed
RESEARCH JOURNAL OF PHARMACEUTICAL BIOLOGICAL AND CHEMICAL SCIENCES, 2018, 9 (04): : 1029 - 1040
[9] Design, synthesis and biological evaluation of new imidazo[1,2-a]pyridine derivatives as selective COX-2 inhibitors
Ismael, Ahmed S.
Amin, Noha H.
Elsaadi, Mohammed T.
Ali, Mohammed R. A.
Abdel-Rahman, Hamdy M.
JOURNAL OF MOLECULAR STRUCTURE, 2022, 1250
[10] Design, synthesis and biological evaluation of new tricyclic spiroisoxazoline derivatives as selective COX-2 inhibitors and study of their COX-2 binding modes via docking studies
Abolhasani, Hoda
Dastmalchi, Siavoush
Hamzeh-Mivehroud, Maryam
Daraei, Bahram
Zarghi, Afshin
MEDICINAL CHEMISTRY RESEARCH, 2016, 25 (05) : 858 - 869

← 1 2 3 4 5 →