1447710-60-2Relevant academic research and scientific papers
Design, synthesis and evaluation of arylidene pyrrolo and pyrido fused quinazolones as antimicrobial agents
Nepali, Kunal,Ojha, Ritu,Singh, Aninder,Budhiraja, Abhishek,Bedi, Preet Mohinder Singh,Dhar, Kanaya Lal
, p. 522 - 528 (2013/07/26)
Keeping in view the potential of heterocyclic fused quinazolones and arylidene linked heterocycles , hybrid molecules of these functionalities were designed and synthesised. All the synthesised molecules were characterized by spectroscopic techniques and evaluated for antimicrobial activity against 2 Gram positive bacterial strains; Staphylococcus aureus (MTCC 96) and Bacillus subtilis (MTCC 2451), 3 Gram negative bacterial strains; Escherichia coli (MTCC 82), Pseudomonas aeruginosa (MTCC 2642) and Salmonella typhimurium (MTCC 1251) and 2 fungal strains; Saccharomyces cerevisiae (MTCC 2799) and Candida albicans (MTCC 3018). Among the synthesised molecules, arylidene pyrrolo fused quinazolones displayed significant antimicrobial activity in comparison to arylidene pyrido fused quinazolones. The influence of the electronic factors linked with the arylidene ring was also observed on the antimicrobial potential. Thus the present study highlights the potential of such hybrid molecules as a new class of antimicrobials.
Structure activity relationship of arylidene pyrrolo and pyrido [2,1-b] quinazolones as cytotoxic agents: Synthesis, SAR studies, biological evaluation and docking studies
Mangla, Veenu,Nepali, Kunal,Singh, Gagandip,Singh, Jagjeet,Guru, Santosh,Gupta, Manish Kumar,Mahajan, Priya,Saxena, Ajit Kumar,Dhar, Kanaya Lal
, p. 642 - 650 (2013/09/23)
Tubulin is the one of the most useful and strategic molecular targets for anticancer drugs. Agents that bind in Colchicine-binding site of tubulin include Phenstatin, Combretastatin A-4, Colchicine, Steganacin, Podophyllotoxin and certain other synthetic analogues of these compounds. Arylidene pyrollo and pyrido [2,1-b] quinazolones (isoindigatone and its synthetic analogues) have been earlier reported to be tubulin inhibitors evidenced by tubulin polymerization assay. The present study is an extension of the library of the isoindigatone and its synthetic analogues to generate the structure activity relationship. The study explores the role of the arylidene ring and also provides some intresting observations such as the placement of bicyclic ring such as naphylidene for potential activity. Some of the important interactions of KNH-3 and KNH-11 with the amino acid residues of active site of Tubulin have also been observed by molecular modeling.
