Synthesis and biological evaluation of some 1,3,4-oxadiazole derivatives

被引：137
作者：
Manjunatha, K. [1 ]
Poojary, Boja [1 ]
Lobo, Prajwal L. [1 ]
Fernandes, Jennifer [2 ]
Kumari, N. Suchetha [3 ]
机构：
[1] Mangalore Univ, Dept Chem, Mangalagangothri 574199, Karnataka, India
[2] NGSM Coll Pharm, Dept Pharmachem, Derlakatte 574160, Karnataka, India
[3] KS Hegde Med Acad, Dept Biochem, Derlakatte 574162, Karnataka, India
来源：
EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY | 2010年 / 45卷 / 11期
关键词：
1,3,4-Oxadiazol-2-thiones; Ibuprofen; 4-Methylthiophenyl; Antimicrobial activity; Anti-inflammatory activity; NONSTEROIDAL ANTIINFLAMMATORY DRUGS; ANTIMICROBIAL ACTIVITIES; CIPROFLOXACIN;
D O I：
10.1016/j.ejmech.2010.08.039
中图分类号：
R914 [药物化学];
学科分类号：
100701 ;
摘要：
The acid hydrazides (2) derived from ibuprofen and 4-methylthiophenyl acetic acids have been subjected to cyclization with carbon disulphide under basic conditions to yield 1,3,4-oxadiazol-2-thiones (3) which on aminomethylation with formaldehyde and secondary amines afforded a series of Mannich bases (4 and 5). Purity of the compounds has been confirmed by TLC. Structures of these compounds were established on the basis of elemental analyses and spectral studies. The newly synthesized compounds were evaluated for their anti-inflammatory, analgesic, ulcerogenic and antimicrobial activities. (C) 2010 Elsevier Masson SAS. All rights reserved.
引用
收藏
页码：5225 / 5233
页数：9
相关论文
共 50 条
  • [1] Design, synthesis and biological evaluation of 1,3,4-oxadiazole derivatives
    Jha, Keshari Kishore
    Samad, Abdul
    Kumar, Yatendra
    Shaharyar, Mohd.
    Khosa, Ratan Lal
    Jain, Jainendra
    Kumar, Vikash
    Singh, Priyanka
    EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY, 2010, 45 (11) : 4963 - 4967
  • [2] Design, Synthesis and Biological Evaluation of 1,3,4-Oxadiazole derivatives
    Jha, Keshari Kishore
    Kumar, Yatendra
    Shaharyar, Mohd.
    ASIAN JOURNAL OF CHEMISTRY, 2009, 21 (09) : 7403 - 7410
  • [3] Synthesis of novel 1,3,4-oxadiazole derivatives and their biological properties
    Husain, Asif
    Ajmal, Mohammed
    ACTA PHARMACEUTICA, 2009, 59 (02) : 223 - 233
  • [4] Synthesis and antimicrobial activity of some 1,3,4-oxadiazole derivatives
    Sahin, G
    Palaska, E
    Ekizoglu, M
    Özalp, M
    FARMACO, 2002, 57 (07): : 539 - 542
  • [5] REVIEW OF SYNTHESIS OF 1,3,4-OXADIAZOLE DERIVATIVES
    Patel, Kinjal D.
    Prajapati, Shraddha M.
    Panchal, Shyamali N.
    Patel, Hitesh D.
    SYNTHETIC COMMUNICATIONS, 2014, 44 (13) : 1859 - 1875
  • [6] 1,3,4-Oxadiazole Derivatives as Potential Biological Agents
    Sun, Juan
    Makawana, Jigar A.
    Zhu, Hai-Liang
    MINI-REVIEWS IN MEDICINAL CHEMISTRY, 2013, 13 (12) : 1725 - 1743
  • [7] SYNTHESIS AND ANTIINFLAMMATORY ACTIVITY OF SOME NOVEL 1,3,4-OXADIAZOLE DERIVATIVES
    ELSAMII, ZKA
    JOURNAL OF CHEMICAL TECHNOLOGY AND BIOTECHNOLOGY, 1992, 53 (02) : 143 - 146
  • [8] Design, synthesis and antiinflammatory activity of some 1,3,4-oxadiazole derivatives
    Omar, FA
    Mahfouz, NM
    Rahman, MA
    EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY, 1996, 31 (10) : 819 - 825
  • [9] Synthesis, molecular docking and biological evaluation of 1,3,4-oxadiazole derivatives as potential immunosuppressive agents
    Yan, Ru
    Zhang, Zhi-Ming
    Fang, Xian-Ying
    Hu, Yang
    Zhu, Hai-Liang
    BIOORGANIC & MEDICINAL CHEMISTRY, 2012, 20 (04) : 1373 - 1379
  • [10] Updates on synthesis and biological activities of 1,3,4-oxadiazole: A review
    Salahuddin
    Mazumder, A.
    Yar, M. Shahar
    Mazumder, R.
    Chakraborthy, G. S.
    Ahsan, Mohamed Jawed
    Rahman, Mujeeb Ur
    SYNTHETIC COMMUNICATIONS, 2017, 47 (20) : 1805 - 1847
12345