Design, synthesis, antinociceptive, and anti-inflammatory properties of thiazolopyrimidine derivatives

被引:9
|
作者
Selvam, T. Panneer [2 ]
Karthik, V. [1 ]
Kumar, P. Vijayaraj [3 ]
Ali, M. Ashraf [4 ]
机构
[1] Acharya Nagarjuna Univ, Dept Biotechnol, Guntur 522510, Andhra Pradesh, India
[2] Ponda Educ Soc, Rajaram & Tarabai Bandekar Coll Pharm, Dept Pharmaceut Chem, Ponda 403401, Goa, India
[3] Sadaya Int Univ, Univ Coll, Sch Pharm, Kuala Lumpur 56000, Malaysia
[4] Univ Sains Malaysia, Inst Res Mol Med INFORM, Pennag 11800, Malaysia
来源
TOXICOLOGICAL AND ENVIRONMENTAL CHEMISTRY | 2012年 / 94卷 / 07期
关键词
thiazolopyrimidine; antinociceptive activity; anti-inflammatory activity; PYRIMIDINE;
D O I
10.1080/02772248.2012.703204
中图分类号
X [环境科学、安全科学];
学科分类号
08 ; 0830 ;
摘要
Ten 2-(substituted benzylidene)-7-(4-chlorophenyl)-5-(furan-2-yl)-2H-thiazolo[ 3,2-a]pyrimidin-3(7H)-one derivatives were synthesized and evaluated. A series of heterocyclic, 2-(substituted benzylidene)-7-(4-chlorophenyl)-5-(furan-2-yl)-2H-thiazolo[3,2-a] pyrimidin-3(7H)-one were synthesized by reaction of 7-(4-chloro phenyl)-5-(furan-2-yl)-2H-thiazolo[3,2-a] pyrimidin-3(7H)-one with appropriately substituted aldehydes in the presence of anhydrous sodium acetate and glacial acetic acid. The antinociceptive activity was evaluated by tail-flick technique, anti-inflammatory activity was evaluated by carrageenan-induced paw edema test and their ulcerogenicity index was determined. The para-substituted methyl, hydroxy, fluoro, chloro, bromo, and nitro derivatives showed significant antinociceptive and anti-inflammatory activities. The detailed synthesis, spectroscopic data, and pharmacological screening of the synthesized compounds were reported.
引用
收藏
页码:1247 / 1258
页数:12
相关论文
共 50 条
  • [21] Antipyretic, antinociceptive and anti-inflammatory activities of certain γ-oxobutanoic acid derivatives
    Abouzid, KAM
    Youssef, KM
    Ahmed, AAE
    Al-Zuhair, HH
    MEDICINAL CHEMISTRY RESEARCH, 2005, 14 (01) : 26 - 39
  • [22] INVESTIGATION OF THE ANTINOCICEPTIVE AND ANTI-INFLAMMATORY PROPERTIES OF HETEROMORPHA ARBORESCENS (APIACEAE)
    Nkomo, Mpumelelo
    Nkeh-Chungag, Benedicta N.
    Kambizi, Learnmore
    Ndebia, Eugene Jamot
    Sewani-Rusike, Constance
    Iputo, Jehu E.
    AFRICAN JOURNAL OF TRADITIONAL COMPLEMENTARY AND ALTERNATIVE MEDICINES, 2011, 8 (04) : 412 - 419
  • [23] Antinociceptive and anti-inflammatory properties of Daucus carota seeds extract
    Vasudevan, Mani
    Gunnam, Kumar Kishore
    Parle, Milind
    JOURNAL OF HEALTH SCIENCE, 2006, 52 (05) : 598 - 606
  • [24] Anti-inflammatory and antinociceptive properties of blueberry extract (Vaccinium corymbosum)
    Torri, Eliane
    Lemos, Marivane
    Caliari, Vinicius
    Kassuya, Candida A. L.
    Bastos, Jairo K.
    Andrade, Sergio F.
    JOURNAL OF PHARMACY AND PHARMACOLOGY, 2007, 59 (04) : 591 - 596
  • [25] Anti-inflammatory and antinociceptive properties of dantrolene sodium in rats and mice
    Büyükokuroglu, ME
    PHARMACOLOGICAL RESEARCH, 2002, 45 (06) : 455 - 460
  • [26] Anti-inflammatory, antinociceptive and antioxidant properties of Schinopsis brasiliensis bark
    de Souza Santos, Clisiane Carla
    Guilhon, Carolina Carvalho
    Alviano Moreno, Daniela Sales
    Alviano, Celuta Sales
    Estevam, Charles dos Santos
    Blank, Arie Fitzgerald
    Fernandes, Patricia Dias
    JOURNAL OF ETHNOPHARMACOLOGY, 2018, 213 : 176 - 182
  • [27] Antinociceptive, anti-inflammatory, and antioxidant properties of Phoradendron piperoides leaves
    Vasconcellos, Cleonice L. C.
    Vitorio, Kelly C. D.
    Andrade, Priscilla A.
    Cambui, Erica V. F.
    Lira, Amintas F.
    Cavalcante, Socrates C. H.
    Estevam, Charles S.
    Antoniolli, Angelo R.
    Thomazzi, Sara M.
    PHARMACEUTICAL BIOLOGY, 2009, 47 (07) : 645 - 652
  • [28] gem-Difluorobisarylic derivatives: design, synthesis and anti-inflammatory effect
    Abeer J. Ayoub
    Layal Hariss
    Nehme El-Hachem
    Ghewa A. El-Achkar
    Sandra E. Ghayad
    Oula K. Dagher
    Nada Borghol
    René Grée
    Bassam Badran
    Ali Hachem
    Eva Hamade
    Aida Habib
    BMC Chemistry, 13
  • [29] Design and synthesis of anti-inflammatory drug derivatives for potential CNS delivery
    Rice, Andrew
    Eden, Brandon
    Bowman, William
    Lovett, Troy
    Geissler, Evan
    Young, Sherri
    ABSTRACTS OF PAPERS OF THE AMERICAN CHEMICAL SOCIETY, 2018, 256
  • [30] Analgesic and anti-inflammatory activity of quinoxaline derivatives: Design synthesis and characterization
    Meka, Geethavani
    Chintakunta, Ramakrishna
    RESULTS IN CHEMISTRY, 2023, 5