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形式
powder
质量水平
mp
189-191 °C (lit.)
抗生素抗菌谱
mycobacteria
作用机制
cell membrane | interferes
SMILES字符串
NC(=O)c1cnccn1
InChI
1S/C5H5N3O/c6-5(9)4-3-7-1-2-8-4/h1-3H,(H2,6,9)
InChI key
IPEHBUMCGVEMRF-UHFFFAOYSA-N
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应用
吡嗪酰胺在治疗上用作抗结核药。吡嗪酰胺用于形成聚合铜络合物，生成吡嗪甲酰胺支架，用作 FXs 抑制剂，以及作为分枝杆菌鉴定试剂盒的组分。用于研究肝脏毒性预防 和抗性机制 。
生化/生理作用
吡嗪酰胺的活性部分是吡嗪酸（POA）。在 结核分枝杆菌 中，POA 视为在酸性 pH 下破坏膜能量并抑制膜输送功能。铁可增强吡嗪酰胺的抗结核活性 。经验证，吡嗪酰胺及其类似物可抑制纯化 FAS I 的活性。
其他说明
保存于密闭容器内，置于干燥通风处。
WGK
WGK 3
闪点(°F)
Not applicable
闪点(°C)
Not applicable
个人防护装备
Eyeshields, Gloves, type N95 (US)
C Raynaud et al.
Microbiology (Reading, England), 145 ( Pt 6), 1359-1367 (1999-07-20)
Mycobacteria are known to acquire resistance to the antituberculous drug pyrazinamide (PZA) through mutations in the gene encoding pyrazinamidase (PZase), an enzyme that converts PZA into pyrazinoic acid, the presumed active form of PZA against bacteria. Additional mechanisms of resistance
Akos Somoskovi et al.
The Journal of antimicrobial chemotherapy, 53(2), 192-196 (2004-01-20)
Pyrazinamide is a paradoxical frontline tuberculosis drug characterized by high in vivo sterilizing activity but poor in vitro activity. This separation in pyrazinamide activity reflects differences between the in vivo tissue environment and in vitro culture conditions. The well-known acid
S A Tasduq et al.
Human & experimental toxicology, 25(3), 111-118 (2006-04-26)
Terminalia chebula Gertn. (Combetraceae) is an important herbal drug in Ayurvedic pharmacopea. In the present study, a 95% ethanolic extract of T. chebula (fruit) (TC extract), which was chemically characterized on the basis of chebuloside II as a marker, was
Pontus Juréen et al.
Antimicrobial agents and chemotherapy, 52(5), 1852-1854 (2008-03-05)
Thirty-four pyrazinamide-resistant and 37 pyrazinamide-susceptible Mycobacterium tuberculosis complex strains were analyzed for pncA gene mutations. None of the sensitive strains had any mutations, apart from silent mutations, whereas all but one resistant strain showed pncA mutations. By using sequencing as
Emmanuel Chigutsa et al.
Antimicrobial agents and chemotherapy, 57(2), 789-795 (2012-11-28)
Days to positivity in automated liquid mycobacterial culture have been shown to correlate with mycobacterial load and have been proposed as a useful biomarker for treatment responses in tuberculosis. However, there is currently no quantitative method or model to analyze
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