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Can I read Design, synthesis and biological evaluation of (Quinazoline 4-yloxy)acetamide and (4-oxoquinazoline-3(4H)-yl)acetamide derivatives as inhibitors of Mycobacterium tuberculosis bd oxidase on EtoBox?

Design, synthesis and biological evaluation of (Quinazoline 4-yloxy)acetamide and (4-oxoquinazoline-3(4H)-yl)acetamide derivatives as inhibitors of Mycobacterium tuberculosis bd oxidase by Amit Kumar; Neetu Kumari; Sandeep Bhattacherjee; Umamageswaran Venugopal; Shahid Parwez; Mohammad Imran Siddiqi; Manju Y. Krishnan; Gautam Panda is a Chemistry article available to read on EtoBox.

What is Design, synthesis and biological evaluation of (Quinazoline 4-yloxy)acetamide and (4-oxoquinazoline-3(4H)-yl)acetamide derivatives as inhibitors of Mycobacterium tuberculosis bd oxidase about?

New chemical scaffolds with novel mechanism of action are urgently needed for the treatment of drug resistant tuberculosis. The oxidative phosphorylation pathway of Mycobacterium tuberculosis consists of multiple clinically validated drug targets. This pathway can function through any one of the two terminal oxidases-the proton pumping cytochrome bc 1 -aa 3 supercomplex, or the less energy efficient but high affinity cytochrome bd oxidase. Inhibiting the bc 1 complex alone has been found bacteriostatic and not bactericidal. On the other hand, inhibition of both these oxidases turns lethal to the pathogen. In the present study, we used a bc 1 complex mutant of M. tuberculosis to screen (Quinazoline 4-yloxy)acetamide and (4-oxoquinazoline-3(4H)-yl)acetamide derivatives against the alternate oxidase, i.e., cytochrome bd oxidase. Two molecules, S-021-0601 and S-021-0607 were found to inhibit the mutant with MICs 8 and 16 μM respectively, compared to MICs of 128 and 256 μM against the wild type M. tuberculosis. In the wild type, one of the compounds showed synergism with Q203, an inhibitor of bc 1 complex, in inhibiting growth under aerobic conditions. Both compounds showed synergism wi

Who reads Design, synthesis and biological evaluation of (Quinazoline 4-yloxy)acetamide and (4-oxoquinazoline-3(4H)-yl)acetamide derivatives as inhibitors of Mycobacterium tuberculosis bd oxidase?

It is typically read by researchers, students, and practitioners in Chemistry.

Author
Amit Kumar; Neetu Kumari; Sandeep Bhattacherjee; Umamageswaran Venugopal; Shahid Parwez; Mohammad Imran Siddiqi; Manju Y. Krishnan; Gautam Panda
Publisher
Elsevier BV
Published
2022
Language
EN
Field
Chemistry (Physical Sciences)

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