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Synthesis and Antimycobacterial Assays of Some New Ethambutol Analogs

Affiliation
Institut für Pharmazie, Martin-Luther-Universität Halle-Wittenberg, 06120 Halle (Saale), Germany;(R.A.);(M.D.);(L.M.);(A.R.);(D.R.)
Abdelaziz, Rana;
ORCID
0000-0002-1043-0480
Affiliation
Institut für Pharmazie, Martin-Luther-Universität Halle-Wittenberg, 06120 Halle (Saale), Germany;(R.A.);(M.D.);(L.M.);(A.R.);(D.R.)
Dube, Mthandazo;
Affiliation
Institut für Pharmazie, Martin-Luther-Universität Halle-Wittenberg, 06120 Halle (Saale), Germany;(R.A.);(M.D.);(L.M.);(A.R.);(D.R.)
Mann, Lea;
ORCID
0000-0002-0062-7896
Affiliation
Institut für Pharmazie, Martin-Luther-Universität Halle-Wittenberg, 06120 Halle (Saale), Germany;(R.A.);(M.D.);(L.M.);(A.R.);(D.R.)
Richter, Adrian;
Affiliation
Institut für Pharmazie, Martin-Luther-Universität Halle-Wittenberg, 06120 Halle (Saale), Germany;(R.A.);(M.D.);(L.M.);(A.R.);(D.R.)
Robaa, Dina;
ORCID
0000-0001-6673-4291
Affiliation
RG Microbial Interface Biology, Research Center Borstel, Leibniz Lung Center, Parkallee 1–40, 23845 Borstel, Germany;
Reiling, Norbert;
ORCID
0000-0003-1326-4219
Affiliation
Department of Pharmaceutical Chemistry, Faculty of Pharmacy, German University in Cairo, Cairo 11835, Egypt;
Abdel-Halim, Mohammad;
Affiliation
Institut für Pharmazie, Martin-Luther-Universität Halle-Wittenberg, 06120 Halle (Saale), Germany;(R.A.);(M.D.);(L.M.);(A.R.);(D.R.)
Imming, Peter

Ethambutol (EMB) is a first-line anti-tuberculosis drug that is also considered in treatment regimens for infections caused by non-tuberculous mycobacteria (NTM). EMB targets the arabinosyl transferases EmbCAB, which are important for the synthesis of cell wall constituents. To further explore and narrow down the structural variability of EMB, we synthesized three series of new EMB analogs. We tested their activity against Mycobacterium tuberculosis , Mycobacterium smegmatis , Mycobacterium abscessus and Mycobacterium intracellulare . Only analogs that very closely resembled EMB showed comparable antimycobacterial activity.

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Category

Editor:
Mangalagiu, Ionel
Published in:
Molecules  
Vol. 30, No. 3 (29.01.2025)
Volume:
30
No.:
3
Date Issued:
29.01.2025
DOI:
10.3390/molecules30030600
Language:
English
Type of Resource:
Text
Keywords:
mycobacteria; ethambutol (EMB); Mycobacterium tuberculosis; non-tuberculous mycobacteria (NTM)
DDC:
610 Medizin und Gesundheit

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