Synthesis and Antitubercular Activity of Novel 1,3,4-Oxadiazole and 1,3,4-Thiadiazole Derivatives

被引:0
|
作者
Joshi, Shrinivas D. [1 ]
Tiwari, Sahilkumar [1 ]
Kulkarni, Venkatarao H. [1 ]
机构
[1] Soniya Educ Trusts, Coll Pharm, Dept Pharmaceut Chem, Novel Drug Design & Discovery Lab, Dharwad, Karnataka, India
关键词
Oxadiazoles; Thiadiazoles; 2-(1H-Benzotriazol-1-yl)-1,1,3,3-tetramethyluronium hexafluorophosphate; N'; N'-Diisopropylethylamine; N'-Dimethyl formamide; Mycobacterium tuberculosis H(37)Rv; Antitubercular activity; ACID HYDRAZIDE ANALOGS; PYRROLE RING-SYSTEMS; ANTIMYCOBACTERIAL AGENTS; POTENTIAL ANTIBACTERIAL; INHIBITORS; OXADIAZOLE; TRIAZOLE;
D O I
暂无
中图分类号
O62 [有机化学];
学科分类号
070303 ; 081704 ;
摘要
Oxadiazole pyrrolyl benzamide derivatives (4a-e) and thiadiazole pyrrolyl benzamide derivatives (5a-e) were synthesized by the reaction of 4-(1H-pyrrol-1-yl) benzoic acid with N-(5-(4substituted phenyl)-1,3,4-oxadiazole-2-amines and N-(5-(4-substituted phenyl)-1,3,4-thiadiazole-2-amines, respectively, in N', N'-dimethyl formamide using 2-(1H-benzotriazol-1-yl)-1,1,3,3-tetramethyluronium hexafluorophosphate as amide coupling agent and N', N'-Diisopropylethylamine as a catalyst. All the newly synthesized compounds (4a-e/5a-e) were screened for in vitro antitubercular activity against Mycobacterium tuberculosis H(37)Rv, and compounds 4c, 4d, 5c, and 5d have exhibited significant minimum inhibitory concentration values.
引用
收藏
页码:417 / 421
页数:5
相关论文
共 50 条
  • [41] Synthesis, Nematicidal Activity, and 3D-QSAR of Novel 1,3,4-Oxadiazole/ Thiadiazole Thioether Derivatives
    Chen, Jixiang
    Gan, Xiuhai
    Yi, Chongfen
    Wang, Shaobo
    Yang, Yuyuan
    He, Fangcheng
    Hu, Deyu
    Song, Baoan
    CHINESE JOURNAL OF CHEMISTRY, 2018, 36 (10) : 939 - 944
  • [42] A novel isomers of 1,3,4-thiadiazole derivatives
    Kunafiev, Rishad
    Babaev, Bakhrom
    Ziyaev, Abdukhakim
    Khayitbaev, Khamid
    Talipov, Samat
    Ibragimov, Bakhtiyar
    ACTA CRYSTALLOGRAPHICA A-FOUNDATION AND ADVANCES, 2017, 73 : C433 - C433
  • [43] Novel 1,3,4-Oxadiazole Fused Thiadiazole Derivatives: Synthesis and Study of Anticancer Activities
    Spandana, Zanjam
    Sreenivasulu, Reddymasu
    MalathiRekha, Tadigiri
    Rao, Mandava Venkata Basaveswara
    LETTERS IN DRUG DESIGN & DISCOVERY, 2019, 16 (06) : 656 - 662
  • [44] Synthesis and antitumor activities of novel hybrid molecules containing 1,3,4-oxadiazole and 1,3,4-thiadiazole bearing Schiff base moiety
    Zhang, Kai
    Wang, Peng
    Xuan, Li-Na
    Fu, Xiao-Yun
    Jing, Fen
    Li, Sha
    Liu, Yu-Ming
    Chen, Bao-Quan
    BIOORGANIC & MEDICINAL CHEMISTRY LETTERS, 2014, 24 (22) : 5154 - 5156
  • [45] Synthesis and Nematicidal Activity of Novel 1,3,4-Oxadiazole (Thiadiazole) Thioether Derivatives Containing Trifluorobuten Moiety
    Chen, Xuewen
    Gan, Xiuhai
    Chen, Jixiang
    Chen, Yongzhong
    Wang, Yanjiao
    Hu, Deyu
    Song, Baoan
    CHINESE JOURNAL OF ORGANIC CHEMISTRY, 2017, 37 (09) : 2343 - 2351
  • [46] HERBICIDAL ACTIVITY OF 1,3,4-THIADIAZOLE DERIVATIVES
    KUBO, H
    SATO, R
    HAMURA, I
    OHI, T
    JOURNAL OF AGRICULTURAL AND FOOD CHEMISTRY, 1970, 18 (01) : 60 - &
  • [47] Synthesis of bipyrazole and 1,3,4-thiadiazole derivatives
    Dawood, Kamal M.
    Ragab, Eman A.
    Farag, Ahmad M.
    JOURNAL OF CHEMICAL RESEARCH, 2009, (10) : 630 - 634
  • [48] SYNTHESIS OF ORGANOSILICON DERIVATIVES OF 1,3,4-OXADIAZOLES AND 1,3,4-THIADIAZOLE
    GOLDIN, GS
    MAKSAKOVA, MV
    PODDUBNYI, VG
    KOLTSOVA, AN
    ZHURNAL OBSHCHEI KHIMII, 1975, 45 (12): : 2661 - 2665
  • [49] Synthesis and antiviral activity of novel thioether derivatives containing 1,3,4-oxadiazole/thiadiazole and emodin moieties
    Dong, Liangrun
    Song, Baojing
    Wu, Jian
    Wu, Zengxue
    Zhu, Yunying
    Chen, Xuewen
    Hu, Deyu
    PHOSPHORUS SULFUR AND SILICON AND THE RELATED ELEMENTS, 2016, 191 (06) : 904 - 907
  • [50] Syntheses, crystal structure and photophysical property of iridium complexes with 1,3,4-oxadiazole and 1,3,4-thiadiazole derivatives as ancillary ligands
    Liu, Xuan
    Zhang, Song
    Jin, Yi-Ming
    Lu, Guang-Zhao
    Jiang, Liang
    Liang, Xiao
    Xu, Qiu-Lei
    Zheng, You-Xuan
    JOURNAL OF ORGANOMETALLIC CHEMISTRY, 2015, 785 : 11 - 18