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Development of Delpazolid for the Treatment of Tuberculosis
Open AccessFeature PaperReview

Development of Macozinone for TB treatment: An Update

Federal Research Center “Fundamentals of Biotechnology RAS”, Leninsky prospect 33, bld. 2, 119071 Moscow, Russia
Department of Biochemistry, Faculty of Natural Sciences, Comenius University in Bratislava, Mlynská dolina, Ilkovičova 6, 84215 Bratislava, Slovakia
Author to whom correspondence should be addressed.
Appl. Sci. 2020, 10(7), 2269;
Received: 5 March 2020 / Revised: 25 March 2020 / Accepted: 25 March 2020 / Published: 26 March 2020
(This article belongs to the Special Issue Tuberculosis Drug Discovery and Development 2019)
Macozinone, a piperazine-benzothiazinone PBTZ169, is currently undergoing Phase 1/2 clinical studies for the treatment of tuberculosis (TB). In this review we summarize the key findings that led to the development of this compound and to identification of its target, decaprenylphospohoryl ribose oxidase DprE1, which is involved in the synthesis of the essential arabinan polymers of the cell wall in a TB pathogen, Mycobacterium tuberculosis. We present the results of the pilot clinical studies, which raise optimism regarding its further development towards more efficient TB drug regimens. View Full-Text
Keywords: macozinone; DprE1 inhibitor; clinical studies macozinone; DprE1 inhibitor; clinical studies
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Makarov, V.; Mikušová, K. Development of Macozinone for TB treatment: An Update. Appl. Sci. 2020, 10, 2269.

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