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
收藏
页码：86 / 91
页数：6
相关论文
共 50 条
  • [1] In silico molecular mechanism of cannabigerol as a cyclooxygenase-2 inhibitor
    Shah, Muhammad Abdullah
    Abdullah, Syed Muhammad
    Khan, Muhammad Azim
    Amin, Hazrat
    Roohullah
    BANGLADESH JOURNAL OF PHARMACOLOGY, 2013, 8 (04) : 410 - 413
  • [2] Computational bioprospecting of andrographolide derivatives as potent cyclooxygenase-2 inhibitors
    Mujwar, Somdutt
    BIOMEDICAL AND BIOTECHNOLOGY RESEARCH JOURNAL, 2021, 5 (04): : 446 - 450
  • [3] The cyclooxygenase-2 inhibitor celecoxib is a potent inhibitor of human carbonic anhydrase II
    Knudsen, JF
    Carlsson, U
    Hammarström, P
    Sokol, GH
    Cantilena, LR
    INFLAMMATION, 2004, 28 (05) : 285 - 290
  • [4] The Cyclooxygenase-2 Inhibitor Celecoxib Is a Potent Inhibitor of Human Carbonic Anhydrase II
    James F. Knudsen
    Uno Carlsson
    Per Hammarström
    Gerald H. Sokol
    Louis R. Cantilena
    Inflammation, 2004, 28 : 285 - 290
  • [5] The Cyclooxygenase-2 Inhibitor Etoricoxib Is a Potent Chemopreventive Agent of Colon Carcinogenesis in the Rat Model
    Saini, Manpreet Kaur
    Sharma, Pinky
    Kaur, Jasmeet
    Sanyal, S. N.
    JOURNAL OF ENVIRONMENTAL PATHOLOGY TOXICOLOGY AND ONCOLOGY, 2009, 28 (01) : 39 - 46
  • [6] Natural products and their derivatives as cyclooxygenase-2 inhibitors
    Chandel, Priyanka
    Rawal, Ravindra K.
    Kaur, Rupinder
    FUTURE MEDICINAL CHEMISTRY, 2018, 10 (20) : 2471 - 2492
  • [7] Synthesis of new ibuprofen derivatives with their in silico and in vitro cyclooxygenase-2 inhibitions
    Gundogdu-Hizliates, Cevher
    Alyuruk, Hakan
    Gocmenturk, Mustafa
    Ergun, Yavuz
    Cavas, Levent
    BIOORGANIC CHEMISTRY, 2014, 52 : 8 - 15
  • [8] Development of a predictive pharmacokinetic model for a novel cyclooxygenase-2 inhibitor
    Kastrissios, H
    Rohatagi, S
    Moberly, J
    Truitt, K
    Gao, Y
    Wada, R
    Takahashi, M
    Kawabata, K
    Salazar, D
    JOURNAL OF CLINICAL PHARMACOLOGY, 2006, 46 (05) : 537 - 548
  • [9] Thiazolopyrimidine derivatives as novel class of small molecule tyrosinase inhibitor
    Ghasemi, Nastaran
    Moradi, Shahram
    Iraji, Aida
    Mahdavi, Mohammad
    BMC CHEMISTRY, 2023, 17 (01)
  • [10] An Improved and Scalable Process for Celecoxib: A Selective Cyclooxygenase-2 Inhibitor
    Reddy, Anumula Raghupathi
    Sampath, Alla
    Goverdhan, Gilla
    Yakambaram, Boja
    Mukkanti, Kagga
    Reddy, Padi Pratap
    ORGANIC PROCESS RESEARCH & DEVELOPMENT, 2009, 13 (01) : 98 - 101
12345