Synthesis and anti-inflammatory evaluation of new pyrazoles bearing biodynamic thiazole and thiazolidinone scaffolds

被引:0
|
作者
Lalit D. Khillare
Manisha R. Bhosle
Amarsinh R. Deshmukh
Ramrao A. Mane
机构
[1] Dr. Babasaheb Ambedkar Marathwada University,Department of Chemistry
来源
关键词
Pyrazole; Thiazole; Thiazolidinone; Anti-inflammatory activity;
D O I
暂无
中图分类号
学科分类号
摘要
New trisubstituted pyrazoles bearing thiazolyl and thiazolidinonyl moieties have been successfully and conveniently synthesized in three steps using 5-acetyl thiazoles (1a–b) as starting materials. The route includes the synthesis of new intermediates, 4-formyl 5-thiazolyl pyrazoles (4a–b). The formyl pyrazoles on one pot cyclocondensation with anilines and thioglycolic acid have been found to yield the titled compounds (7a–j). The new pyrazoles have been screened to evaluate in vivo anti-inflammatory activity and compounds 7c, 7d, 7f, 7g, 7h, and 7i have better anti-inflammatory activity than reference drug Celecoxib. The synthetic details and results of anti-inflammatory activity are discussed.
引用
收藏
页码:1380 / 1386
页数:6
相关论文
共 50 条
  • [21] An overview on synthetic routes of anti-inflammatory active scaffolds including thiazole and thiazolidine cores
    Bhatnagar, Ayushi
    Pemawat, Gangotri
    PHOSPHORUS SULFUR AND SILICON AND THE RELATED ELEMENTS, 2023, 198 (07) : 554 - 565
  • [22] Synthesis, Antimicrobial, and Anti-inflammatory Activity of Some New Coumarin Incorporated 4-Thiazolidinone Derivatives
    Bhat, K. Ishwar
    Apoorva, A.
    Kumar, Abhishek
    Kumar, Pankaj
    INDIAN JOURNAL OF HETEROCYCLIC CHEMISTRY, 2019, 29 (02) : 139 - 144
  • [23] SYNTHESIS OF NOVEL THIAZOLES BEARING HYDRAZINE, THIOSEMICARBAZIDE, THIAZOLE, AND THIAZOLIDINONE MOIETIES
    MAMEDOV, VA
    NURETDINOV, IA
    SIBGATULLINA, FG
    BULLETIN OF THE ACADEMY OF SCIENCES OF THE USSR DIVISION OF CHEMICAL SCIENCE, 1991, 40 (12): : 2470 - 2474
  • [24] Synthesis, molecular docking and anti-inflammatory evaluation of new trisubstituted pyrazoline derivatives bearing benzenesulfonamide moiety
    Raauf, Ayad M. R.
    Omar, Tagreed N-A
    Mahdi, Monther F.
    Fadhil, Hayder R.
    NATURAL PRODUCT RESEARCH, 2024, 38 (02) : 253 - 260
  • [25] Pyrazoles as Promising Scaffold for the Synthesis of Anti-Inflammatory and/or Antimicrobial Agent: A Review
    Bekhit, Adnan A.
    Hymete, Ariaya
    Bekhit, Alaa El-Din A.
    Damtew, Ashenafi
    Aboul-Enein, Hassan Y.
    MINI-REVIEWS IN MEDICINAL CHEMISTRY, 2010, 10 (11) : 1014 - 1033
  • [26] New Naproxen Analogs: Synthesis, Docking and Anti-Inflammatory Evaluation
    Ammar, Yousry A.
    Khalifa, Maha M.
    Eisa, Sally I.
    Ismail, Magda M. F.
    POLYCYCLIC AROMATIC COMPOUNDS, 2022, 42 (06) : 3586 - 3605
  • [27] Synthesis of new analogs of AKBA and evaluation of their anti-inflammatory activities
    Meka, Bharani
    Ravada, Suryachandra Rao
    Muthyala, Murali Krishna Kumar
    Kurre, Puma Nagasree
    Golakoti, Trimurtulu
    BIOORGANIC & MEDICINAL CHEMISTRY, 2017, 25 (04) : 1374 - 1388
  • [28] Design, synthesis and pharmacological evaluation of new anti-inflammatory compounds
    Cidade, Amanda F.
    Vasconcelos, Patricia A.
    Silva, Daiany P. B.
    Florentino, Iziara E.
    Vasconcelos, Gessica A.
    Vaz, Boniek G.
    Costa, Elson A.
    Liao, Luciano M.
    Menegatti, Ricardo
    EUROPEAN JOURNAL OF PHARMACOLOGY, 2016, 791 : 195 - 204
  • [29] SYNTHESIS AND BIOLOGICAL EVALUATION OF SOME NEW HYDRAZONE DERIVATIVES BEARING PYRIMIDINE RING AS ANALGESIC AND ANTI-INFLAMMATORY AGENTS
    Akdag, Kadryiye
    Unal, Gokhan
    Tok, Fatih
    Aricioglu, Feyza
    Temel, Halide Edip
    Kocyigit-Kaymakcioglu, Bedia
    ACTA POLONIAE PHARMACEUTICA, 2018, 75 (05): : 1147 - 1159
  • [30] SYNTHESIS AND ANTI-INFLAMMATORY EVALUATION OF NOVEL BENZIMIDAZOLE ANALOGUES CONTAINING TRIAZOLE, THIAZOLE, ARYLAZETIDINONE AND ARYLTHIAZOLIDINONE MOIETIES
    Sharma, Suneel Kumar
    Sharma, Pooja Sapra
    HETEROCYCLIC LETTERS, 2014, 4 (04): : 571 - 585