Please use this identifier to cite or link to this item: https://hdl.handle.net/10356/153933
Title: Syntheses and structure–activity relationships of N-phenethyl-quinazolin-4-yl-amines as potent inhibitors of cytochrome bd oxidase in Mycobacterium tuberculosis
Authors: Hopfner, Sarah M.
Lee, Bei Shi
Kalia, Nitin P.
Miller Marvin J.
Pethe, Kevin
Moraski, Garrett C.
Keywords: Science::Biological sciences
Issue Date: 2021
Source: Hopfner, S. M., Lee, B. S., Kalia, N. P., Miller Marvin J., Pethe, K. & Moraski, G. C. (2021). Syntheses and structure–activity relationships of N-phenethyl-quinazolin-4-yl-amines as potent inhibitors of cytochrome bd oxidase in Mycobacterium tuberculosis. Applied Sciences, 11(19), 9092-. https://dx.doi.org/10.3390/app11199092
Project: NRF–CRP18–2017–01
NRF-I06-2020-0012
Journal: Applied Sciences
Abstract: The development of cytochrome bd oxidase (cyt‐bd) inhibitors are needed for comprehensive termination of energy production in Mycobacterium tuberculosis (Mtb) to treat tuberculosis infections. Herein, we report on the structure‐activity‐relationships (SAR) of 22 new N‐phenethyl‐quinazolin‐4‐ yl‐amines that target cyt‐bd. Our focused set of compounds was synthesized and screened against three mycobacterial strains: Mycobacterium bovis BCG, Mycobacterium tuberculosis H37Rv and the clinical isolate Mycobacterium tuberculosis N0145 with and without the cytochrome bcc:aa3 inhibitor Q203 in an ATP depletion assay. Two compounds, 12a and 19a, were more active against all three strains than the naturally derived cyt‐bd inhibitor aurachin D.
URI: https://hdl.handle.net/10356/153933
ISSN: 2076-3417
DOI: 10.3390/app11199092
Rights: © 2021 The Author(s). Licensee MDPI, Basel, Switzerland. This article is an open access article distributed under the terms and conditions of the Creative Commons Attribution (CC BY) license (https://creativecommons.org/licenses/by/4.0/).
Fulltext Permission: open
Fulltext Availability: With Fulltext
Appears in Collections:LKCMedicine Journal Articles
SBS Journal Articles

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