1243683-03-5Relevant academic research and scientific papers
Design, synthesis and biological evaluation of nitrofuran-1,3,4-oxadiazole hybrids as new antitubercular agents
Wang, Apeng,Xu, Shijie,Chai, Yun,Xia, Guimin,Wang, Bin,Lv, Kai,Wang, Dan,Qin, Xiaoyu,Jiang, Bin,Wu, Wenhao,Liu, Mingliang,Lu, Yu
, (2021/12/02)
Three series of novel nitrofuran-1,3,4-oxadiazole hybrids were designed and synthesized as new anti-TB agents. The structure activity relationship study indicated that the linkers and the substituents on the oxadiazole moiety greatly influence the activity, and the substituted benzenes are more favoured than the cycloalkyl or heterocyclic groups. Besides, the optimal compound in series 2 was active against both MTB H37Rv strain and MDR-MTB 16883 clinical isolate and also displayed low cytotoxicity, low inhibition of hERG and good oral PK, indicating its promising potential to be a lead for further structural modifications.
5-Nitro-2-furoic acid hydrazones: Design, synthesis and in vitro antimycobacterial evaluation against log and starved phase cultures
Sriram, Dharmarajan,Yogeeswari, Perumal,Vyas, Devambatla Ravi Kumar,Senthilkumar, Palaniappan,Bhat, Pritesh,Srividya, Madala
scheme or table, p. 4313 - 4316 (2010/09/18)
Various 5-nitro-2-furoic acid hydrazones were synthesized and evaluated for in vitro activities against log and starved phase culture of two mycobacterial species and Mycobacterium tuberculosis (MTB) isocitrate lyase (ICL) enzyme inhibition studies. Among twenty one compounds, 5-nitro-N′-[(5-nitro-2- furyl)methylidene]-2-furohydrazide (4o) was found to be the most active compound in vitro with MICs of 2.65 and 10.64 μM against log- and starved-phase culture of MTB. Compound 4o also showed good enzyme inhibition of MTB ICL at 10 μM. The docking studies also confirmed the binding potential of the compounds at the ICL active site.
