Research output: Contribution to journal › Article › peer-review
The synthesis of 1-oxa-9-azaspiro[5.5]undecane derivatives and optimization of antituberculosis activity thereof. / Komarova, Kristina Yu.; Lukin, Alexey Yu.; Vinogradova, Lyubov V.; Zhuravlev, Maxim E.; Dogonadze, Marine Z.; Vinogradova, Tatiana I.; Gureev, Maxim A.; Chudinov, Mikhail V.; Dar’in, Dmitry V.
In: Chemistry of Heterocyclic Compounds, Vol. 60, No. 5-6, 21.08.2024, p. 245-250.Research output: Contribution to journal › Article › peer-review
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TY - JOUR
T1 - The synthesis of 1-oxa-9-azaspiro[5.5]undecane derivatives and optimization of antituberculosis activity thereof
AU - Komarova, Kristina Yu.
AU - Lukin, Alexey Yu.
AU - Vinogradova, Lyubov V.
AU - Zhuravlev, Maxim E.
AU - Dogonadze, Marine Z.
AU - Vinogradova, Tatiana I.
AU - Gureev, Maxim A.
AU - Chudinov, Mikhail V.
AU - Dar’in, Dmitry V.
PY - 2024/8/21
Y1 - 2024/8/21
N2 - (Figure presented.) The aim of this work was to synthesize and study the antituberculosis activity of spirocyclic inhibitors of the MmpL3 protein of M. tu- berculosis containing the 1-oxa-9-azaspiro[5.5]undecane scaffold. Optimization of the initial structure was performed with consideration of the results of molecular docking. The resulting compounds, characterized by the chemical diversity of the peripheral fragment, showed high activity against the antibiotic-sensitive strain H37Rv and some multiresistant strains of M. tuberculosis, exceeding the activity of the comparator drug.
AB - (Figure presented.) The aim of this work was to synthesize and study the antituberculosis activity of spirocyclic inhibitors of the MmpL3 protein of M. tu- berculosis containing the 1-oxa-9-azaspiro[5.5]undecane scaffold. Optimization of the initial structure was performed with consideration of the results of molecular docking. The resulting compounds, characterized by the chemical diversity of the peripheral fragment, showed high activity against the antibiotic-sensitive strain H37Rv and some multiresistant strains of M. tuberculosis, exceeding the activity of the comparator drug.
KW - 1-oxa-9-azaspiro[5.5]undecane
KW - MmpL3 protein
KW - Prins cyclization
KW - antituberculosis activity
KW - spirocyclic compounds
UR - https://www.mendeley.com/catalogue/bee764e3-be52-3560-b25b-5b8f7b832679/
U2 - 10.1007/s10593-024-03328-w
DO - 10.1007/s10593-024-03328-w
M3 - Article
VL - 60
SP - 245
EP - 250
JO - Chemistry of Heterocyclic Compounds
JF - Chemistry of Heterocyclic Compounds
SN - 0009-3122
IS - 5-6
ER -
ID: 124082336