This study reports the synthesis of new 2H-chromene or coumarin based acylhydrazones, which were evaluated for their in vitro antimycobacterial activity against reference strain Mycobacterium tuberculosis H37Rv and compared to the first-line antituberculosis drugs, isoniazid (INH) and ethambutol (EMB). The most active compounds 7m (MIC 0.13 mu M), 7o (MIC 0.15 mu M) and 7k (MIC 0.17 mu M) demonstrated antimycobacterial activity at submicromolar concentration level and remarkably minimal associated cytotoxicity in the human embryonic kidney cell line HEK-293T. Structure-activity relationship for this class of compounds has been established.
TY - JOUR
AU - Angelova, Violina T.
AU - Valcheva, Violeta
AU - Vassilev, Nikolay G.
AU - Buyukliev, Rosen
AU - Momekov, Georgi
AU - Dimitrov, Ivan
AU - Saso, Luciano
AU - Đukić, Mirjana
AU - Shivachev, Boris
PY - 2017
UR - https://farfar.pharmacy.bg.ac.rs/handle/123456789/2940
AB - This study reports the synthesis of new 2H-chromene or coumarin based acylhydrazones, which were evaluated for their in vitro antimycobacterial activity against reference strain Mycobacterium tuberculosis H37Rv and compared to the first-line antituberculosis drugs, isoniazid (INH) and ethambutol (EMB). The most active compounds 7m (MIC 0.13 mu M), 7o (MIC 0.15 mu M) and 7k (MIC 0.17 mu M) demonstrated antimycobacterial activity at submicromolar concentration level and remarkably minimal associated cytotoxicity in the human embryonic kidney cell line HEK-293T. Structure-activity relationship for this class of compounds has been established.
PB - Pergamon-Elsevier Science Ltd, Oxford
T2 - Bioorganic & Medicinal Chemistry Letters
T1 - Antimycobacterial activity of novel hydrazide-hydrazone derivatives with 2H-chromene and coumarin scaffold
VL - 27
IS - 2
SP - 223
EP - 227
DO - 10.1016/j.bmcl.2016.11.071
ER -
@article{
author = "Angelova, Violina T. and Valcheva, Violeta and Vassilev, Nikolay G. and Buyukliev, Rosen and Momekov, Georgi and Dimitrov, Ivan and Saso, Luciano and Đukić, Mirjana and Shivachev, Boris",
year = "2017",
abstract = "This study reports the synthesis of new 2H-chromene or coumarin based acylhydrazones, which were evaluated for their in vitro antimycobacterial activity against reference strain Mycobacterium tuberculosis H37Rv and compared to the first-line antituberculosis drugs, isoniazid (INH) and ethambutol (EMB). The most active compounds 7m (MIC 0.13 mu M), 7o (MIC 0.15 mu M) and 7k (MIC 0.17 mu M) demonstrated antimycobacterial activity at submicromolar concentration level and remarkably minimal associated cytotoxicity in the human embryonic kidney cell line HEK-293T. Structure-activity relationship for this class of compounds has been established.",
publisher = "Pergamon-Elsevier Science Ltd, Oxford",
journal = "Bioorganic & Medicinal Chemistry Letters",
title = "Antimycobacterial activity of novel hydrazide-hydrazone derivatives with 2H-chromene and coumarin scaffold",
volume = "27",
number = "2",
pages = "223-227",
doi = "10.1016/j.bmcl.2016.11.071"
}
Angelova, V. T., Valcheva, V., Vassilev, N. G., Buyukliev, R., Momekov, G., Dimitrov, I., Saso, L., Đukić, M.,& Shivachev, B.. (2017). Antimycobacterial activity of novel hydrazide-hydrazone derivatives with 2H-chromene and coumarin scaffold. in Bioorganic & Medicinal Chemistry Letters
Pergamon-Elsevier Science Ltd, Oxford., 27(2), 223-227.
https://doi.org/10.1016/j.bmcl.2016.11.071
Angelova VT, Valcheva V, Vassilev NG, Buyukliev R, Momekov G, Dimitrov I, Saso L, Đukić M, Shivachev B. Antimycobacterial activity of novel hydrazide-hydrazone derivatives with 2H-chromene and coumarin scaffold. in Bioorganic & Medicinal Chemistry Letters. 2017;27(2):223-227.
doi:10.1016/j.bmcl.2016.11.071 .
Angelova, Violina T., Valcheva, Violeta, Vassilev, Nikolay G., Buyukliev, Rosen, Momekov, Georgi, Dimitrov, Ivan, Saso, Luciano, Đukić, Mirjana, Shivachev, Boris, "Antimycobacterial activity of novel hydrazide-hydrazone derivatives with 2H-chromene and coumarin scaffold" in Bioorganic & Medicinal Chemistry Letters, 27, no. 2 (2017):223-227,
https://doi.org/10.1016/j.bmcl.2016.11.071 . .
