A Potent Cyclooxygenase-2 Inhibitor for Synthesized Pyrimidine and Thiazolopyrimidine Derivatives

被引：5

作者：

Amr, Abd El-Galil E. ^{[1
,2
]}

Al-Omar, Mohamed A. ^{[1
]}

Abdalla, Mohamed M. ^{[3
]}

机构：

[1] King Saud Univ, Coll Pharm, DEDC, Dept Pharmaceut Chem, Riyadh 11451, Saudi Arabia

[2] Natl Res Ctr, Dept Appl Chem, Cairo, Egypt

[3] Saco Pharm Co, Res Unit, 6th October City 11632, Egypt

来源：

INTERNATIONAL JOURNAL OF PHARMACOLOGY | 2016年 / 12卷 / 02期

关键词：

Pyridine derivatives; thiazolopyrimidine; anti-inflammatory activities; COX-2; inhibitors; ANALGESIC ACTIVITY EVALUATION; ANTIINFLAMMATORY ACTIVITY; BIOLOGICAL EVALUATION; ANTICANCER; DESIGN;

D O I：

10.3923/ijp.2016.86.91

中图分类号：

R9 [药学];

学科分类号：

1007 ;

摘要：

Ten pyridine and pyrimidine and thiazolopyrimidine derivatives (1-10) were synthesized and screened as analgesic, anticonvulsant and antiparkinsonian agent before. Herein, all the target compounds showed anti-inflammatory activity. The active compounds showed selective inhibitory activity towards COX-2 enzyme as revealed by the in vitro enzymatic assay. All the tested compounds proved to have superior gastrointestinal (GI) safety profiles as compared to indomethacin, when tested for their ulcerogenic effects.

引用

页码：86 / 91

页数：6

共 50 条

[21] Novel Benzo[4,5]imidazo[1,2-a]pyrimidine derivatives as selective Cyclooxygenase-2 Inhibitors: Design, synthesis, docking studies, and biological evaluation
Bayanati, Maryam
Khoramjouy, Mona
Faizi, Mehrdad
Movahed, Mahsa Azami
Mahboubi-Rabbani, Mohammad
Zarghi, Afshin
MEDICINAL CHEMISTRY RESEARCH, 2023, 32 (03) : 495 - 505
[22] Acetaminophen (paracetamol) is a selective cyclooxygenase-2 inhibitor in man
Hinz, Burkhard
Cheremina, Olga
Brune, Kay
FASEB JOURNAL, 2008, 22 (02) : 383 - 390
[23] Structure-based design of phthalimide derivatives as potential cyclooxygenase-2 (COX-2) inhibitors: Anti-inflammatory and analgesic activities
Alanazi, Amer M.
El-Azab, Adel S.
Al-Suwaidan, Ibrahim A.
ElTahir, Kamal Eldin H.
Asiri, Yousif A.
Abdel-Aziz, Naglaa I.
Abdel-Aziz, Alaa A. -M.
EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY, 2015, 92 : 115 - 123
[24] Chalcones as Potential Cyclooxygenase-2 Inhibitors: A Review
Mahboubi-Rabbani, Mohammad
Zarei, Rosa
Baradaran, Mehdi
Bayanati, Maryam
Zarghi, Afshin
ANTI-CANCER AGENTS IN MEDICINAL CHEMISTRY, 2024, 24 (02) : 77 - 95
[25] Discovery of a potent cyclooxygenase-2 inhibitor, S4, through docking-based pharmacophore screening, in vivo and in vitro estimations
Tseng, Tien-Sheng
Chuang, Show-Mei
Hsiao, Nai-Wan
Chen, Yi-Wen
Lee, Yu-Ching
Lin, Chi-Chen
Huang, Cheng
Tsai, Keng-Chang
MOLECULAR BIOSYSTEMS, 2016, 12 (08) : 2541 - 2551
[26] Regression of Experimentally Induced Endometriosis with a New Selective Cyclooxygenase-2 Enzyme Inhibitor
Kilico, Ismail
Kokcu, Arif
Kefeli, Mehmet
Kandemir, Bedri
GYNECOLOGIC AND OBSTETRIC INVESTIGATION, 2014, 77 (01) : 35 - 39
[27] Cyclooxygenase-2 inhibitor: a potential therapeutic strategy for ultrafiltration failure in peritoneal dialysis
Kim, Yong-Lim
Park, Sun-Hee
Choi, Ji-Young
Kim, Chan-Duck
NEPHROLOGY DIALYSIS TRANSPLANTATION, 2009, 24 (12) : 3585 - 3588
[28] Discovery of Bis-sydnone styryl ketone as a selective cyclooxygenase-2 inhibitor
Abdualkader, Abdualrahman Mohammed
Taher, Muhammad
Nik Yusoff, Nik Idris
Alaama, Mohamed
FUTURE JOURNAL OF PHARMACEUTICAL SCIENCES, 2021, 7 (01)
[29] Triazole tethered organosilane based fluorescent sensor as a logic gate operation for selective detection of Sn2+ions: A potent Cyclooxygenase-2 inhibitor
Singh, Gurjaspreet
Mohit
Satija, Pinky
Malik, Pooja
Khurana, Sumesh
Sharma, Samiksha
Sharma, Devina
Kaur, Harshbir
Singh, K. N.
JOURNAL OF PHOTOCHEMISTRY AND PHOTOBIOLOGY A-CHEMISTRY, 2024, 446
[30] nido-Dicarbaborate Induces Potent and Selective Inhibition of Cyclooxygenase-2
Neumann, Wilma
Xu, Shu
Sarosi, Menyhart B.
Scholz, Matthias S.
Crews, Brenda C.
Ghebreselasie, Kebreab
Banerjee, Surajit
Marnett, Lawrence J.
Hey-Hawkins, Evamarie
CHEMMEDCHEM, 2016, 11 (02) : 175 - 178

← 1 2 3 4 5 →