Fluorinated 1,2,4-Triazolo[1,5-a]pyrimidine-6-carboxylic Acid Derivatives as Antimycobacterial Agents
Тип публикации: Journal Article
Дата публикации: 2009-02-01
SCImago Q2
WOS Q2
БС2
SJR: 0.527
CiteScore: 6.5
Impact factor: 3.5
ISSN: 03656233, 15214184
PubMed ID:
19173243
Drug Discovery
Pharmaceutical Science
Краткое описание
A series of fluorinated 1,2,4-triazolo[1,5-a]pyrimidine-6-carboxylic acid derivatives was designed and synthesized as fluoroquinolone analogues. The synthesized compounds were screened against Mycobacterium tuberculosis H37Rv strain at 6.25 μg/mL concentration. Compound 4, the 7-oxo-2-(trifluoromethyl)-4,7-dihydro-1,2,4-triazolo[5,1-a]pyrimidine-6-carboxylic acid was found to be a very potent inhibitor, being able to inhibit 92% growth of M. tuberculosis H37Rv at 6.25 μg/mL concentration. At the same time, it proofed to be nontoxic to mammalian cells (IC50 > 62.5 μg/mL in VERO cells).
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Abdel‐Rahman H. et al. Fluorinated 1,2,4-Triazolo[1,5-a]pyrimidine-6-carboxylic Acid Derivatives as Antimycobacterial Agents // Archiv der Pharmazie. 2009. Vol. 342. No. 2. pp. 94-99.
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Abdel‐Rahman H., El-KOUSSI N. A., HASSAN H. Y. Fluorinated 1,2,4-Triazolo[1,5-a]pyrimidine-6-carboxylic Acid Derivatives as Antimycobacterial Agents // Archiv der Pharmazie. 2009. Vol. 342. No. 2. pp. 94-99.
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TY - JOUR
DO - 10.1002/ardp.200800113
UR - https://doi.org/10.1002/ardp.200800113
TI - Fluorinated 1,2,4-Triazolo[1,5-a]pyrimidine-6-carboxylic Acid Derivatives as Antimycobacterial Agents
T2 - Archiv der Pharmazie
AU - Abdel‐Rahman, H.H.
AU - El-KOUSSI, Nawal A.
AU - HASSAN, Hoda Y.
PY - 2009
DA - 2009/02/01
PB - Wiley
SP - 94-99
IS - 2
VL - 342
PMID - 19173243
SN - 0365-6233
SN - 1521-4184
ER -
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@article{2009_Abdel‐Rahman,
author = {H.H. Abdel‐Rahman and Nawal A. El-KOUSSI and Hoda Y. HASSAN},
title = {Fluorinated 1,2,4-Triazolo[1,5-a]pyrimidine-6-carboxylic Acid Derivatives as Antimycobacterial Agents},
journal = {Archiv der Pharmazie},
year = {2009},
volume = {342},
publisher = {Wiley},
month = {feb},
url = {https://doi.org/10.1002/ardp.200800113},
number = {2},
pages = {94--99},
doi = {10.1002/ardp.200800113}
}
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MLA
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Abdel‐Rahman, H.H., et al. “Fluorinated 1,2,4-Triazolo[1,5-a]pyrimidine-6-carboxylic Acid Derivatives as Antimycobacterial Agents.” Archiv der Pharmazie, vol. 342, no. 2, Feb. 2009, pp. 94-99. https://doi.org/10.1002/ardp.200800113.
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