161226-49-9Relevant academic research and scientific papers
Novel isoniazid-spirooxindole derivatives: design, synthesis, biological evaluation, in silico ADMET prediction and computational studies
Bhoi, Manoj N.,Borad, Mayuri A.,Jethava, Divya J.,Pandya, Himanshu A.,Patel, Chirag N.,Patel, Hitesh D.
, (2020)
In the present scenario, the Synthesis of new and desired antimycobacterial agent has an eternal demand to resist Mycobacterium tuberculosis (MTB). The design and identification of new molecules for the treatment of tuberculosis is an important task in organic as well as medicinal chemistry research. In the present study, we have reported the combination of the desired compound using two versatile and significant moieties, isoniazid and spirooxindole derivatives. A series of novel isoniazid-spirooxindole hybrid molecules (6a-6ao) were designed, synthesized, and well-characterized by various spectroscopic methods. We have evaluated for their in vitro antimycobacterial activity against Mycobacterium tuberculosis H37Rv (MTB) strain and MDR-TB. Among them, Compound 6ab was found to be the most effective compare to other compounds. ADMET-related descriptors were to be calculated of all the compounds to predict the pharmacokinetic properties for the selection of the effective and bioavailable compounds. In addition, molecular docking and molecular dynamics studies reveal that the binding modes of all the compounds in the active site of isoniazid-resistant enoyl-ACP(COA) reductase, which helped to establish a structural basis of inhibition of Mycobacterium tuberculosis.
Asymmetric organocatalytic quadruple cascade reaction of 2-hydroxychalcone with cinnamaldehyde for the construction of tetrahydro-6H-benzo[c]chromene containing five stereocenters
Liu, Lingyan,Zhu, Yunna,Huang, Kaimeng,Wang, Bing,Chang, Weixing,Li, Jing
supporting information, p. 4342 - 4350 (2014/07/21)
An asymmetric organocatalytic quadruple cascade reaction was developed for the stable and sterically hindered 2-hydroxychalcones and substituted cinnamaldehydes. This process proceeded through an oxa-Michael-Michael-Michael- aldol condensation to afford h
Synthesis and antimicrobial activity of some pyrazoline derivatives
Ahirwar,Gautam,Shrivastava
experimental part, p. 5297 - 5302 (2012/07/28)
The objective of present study is to synthesize and screening of antimicrobial activity of some derivatives of pyrazoline. 1H-[4-nitro phenyl-5-(substituted phenyl)]pyrazoline has been used as a precursor to synthesize some biologically active heterocycles. Reaction of 1-(4-nitrophenyl)-3-(substituted phenyl) prop-2-en-1-one with hydrazine hydrate gave 1H-(3-nitrophenyl-5-(substituted phenyl) pyrazoline which on reaction with benzoyl chloride in pyridine gave 1-benzoyl-(4-nitrophenyl)-5-(substituted phenyl) prazoline and on reaction with acetic acid yields 1-acetyl-(4- nitrophenyl)-5-(substituted phenyl) pyrazoline derivatives. Several derivatives have been synthesized and screened for their antimicrobial efficacy against Bacillus subtilis, Escherichia coli, Staphylococcus aureus and Klebsiella pneumoniae. Antifungal activity against, Aspergillus flavus, Fusarium oxisporum, Aspergillus niger and Trichoderma viridae.
