1331969-80-2Relevant academic research and scientific papers
Synthesis and binary QSAR study of antitubercular quinolylhydrazides
Manvar, Atul,Khedkar, Vijay,Patel, Jignesh,Vora, Vipul,Dodia, Narsinh,Patel, Gautam,Coutinho, Evans,Shah, Anamik
supporting information, p. 4896 - 4902 (2013/09/02)
In continuation with our previous work in anti-TB research area, in the present study we have demonstrated the structural diversity of quinolylhydrazides as potent anti-tuberculars. The compound library was synthesized by molecular hybridization approach and tested in vitro against Mycobacterium tuberculosis H37Rv strains. Among the designed conjugates, the most promising molecules were found to exhibit 100% Growth Inhibition (GI) at MIC 6.25 μg/mL. Moreover, several analogs in the designed series were also turned out as excellent anti-tuberculars. To probe the structural characteristics influencing on the SAR, the classification model was generated using a binary QSAR approach termed recursive partitioning (RP) analysis. The significant features outlined by the RP model act as a guide in order to design the 'lead' compound.
Diversity oriented design of various hydrazides and their in vitro evaluation against Mycobacterium tuberculosis H37Rv strains
Manvar, Atul,Bavishi, Abhay,Radadiya, Ashish,Patel, Jignesh,Vora, Vipul,Dodia, Narshih,Rawal, Kena,Shah, Anamik
supporting information; experimental part, p. 4728 - 4731 (2011/09/16)
Control and prevention of tuberculosis is a major challenge, as one-third of the world's population is infected with Mycobacterium tuberculosis. The resurgence of tuberculosis and the emergence of multidrug-resistance strains of mycobacteria, necessitate the search for new class of antimycobacterial agents. As a part of investigation of new antitubercular agents in this laboratory, we describe the syntheses of various hydrazides of comarins, quinolones and pyrroles and screening against M. tuberculosis (Mtb) H37Rv by using rifampin as a standard drug. Among the designed molecules, the most prominent compounds 2a-g, 4a and 9a showed >90% GI at MIC 6.25 μg/mL. Finally, these studies suggests that compounds 2a-g, 4a and 9a may serve as promising lead scaffolds for further generation of new anti-TB agents.
