Rifamycin derivatives active against pathogenic rapidly-growing mycobacteria
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Rifamycin derivatives active against pathogenic rapidly-growing mycobacteria. / Combrink, Keith D; Ramos, Andrea Ramirez; Spring, Stephanie; Schmidl, Sebastian; Elizondo, Kira; Morin, Petronilo; De Jesus, Bryant; Maurer, Florian P.
In: BIOORG MED CHEM LETT, Vol. 29, No. 16, 15.08.2019, p. 2112-2115.Research output: SCORING: Contribution to journal › SCORING: Journal article › Research › peer-review
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TY - JOUR
T1 - Rifamycin derivatives active against pathogenic rapidly-growing mycobacteria
AU - Combrink, Keith D
AU - Ramos, Andrea Ramirez
AU - Spring, Stephanie
AU - Schmidl, Sebastian
AU - Elizondo, Kira
AU - Morin, Petronilo
AU - De Jesus, Bryant
AU - Maurer, Florian P
N1 - Copyright © 2019 Elsevier Ltd. All rights reserved.
PY - 2019/8/15
Y1 - 2019/8/15
N2 - Infections due to rapidly growing mycobacteria (RGM), and in particular the RGM species Mycobacterium abscessus (Mab), are very difficult to treat and reports on novel therapeutic options are scarce. A hallmark of all pathogenic RGM species is their resistance to the four first-line drugs used to treat infections with Mycobacterium tuberculosis including rifampicin. This study demonstrates that modification of the rifampicin scaffold can restore rifampicin activity against the three most commonly isolated pathogenic RGM species including Mab. We also note that the structure-activity relationship for Mab is different as compared to the non-pathogenic RGM species Mycobacterium smegmatis.
AB - Infections due to rapidly growing mycobacteria (RGM), and in particular the RGM species Mycobacterium abscessus (Mab), are very difficult to treat and reports on novel therapeutic options are scarce. A hallmark of all pathogenic RGM species is their resistance to the four first-line drugs used to treat infections with Mycobacterium tuberculosis including rifampicin. This study demonstrates that modification of the rifampicin scaffold can restore rifampicin activity against the three most commonly isolated pathogenic RGM species including Mab. We also note that the structure-activity relationship for Mab is different as compared to the non-pathogenic RGM species Mycobacterium smegmatis.
U2 - 10.1016/j.bmcl.2019.07.001
DO - 10.1016/j.bmcl.2019.07.001
M3 - SCORING: Journal article
C2 - 31281018
VL - 29
SP - 2112
EP - 2115
IS - 16
ER -