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α-pyrones and their hydroxylated analogs as promising scaffolds against Mycobacterium tuberculosis
被引:15
作者:
Bhat, Zubair Shanib
[1
,2
]
Rather, Muzafar Ahmad
[1
]
Syed, Khalid Yousuf
[2
,3
]
Ahmad, Zahoor
[1
,2
]
机构:
[1] IIIM, Clin Microbiol & PK PD Div, Campus Sanat Nagar, Srinagar 190005, J&K, India
[2] IIIM, CSIR, Acad Sci & Innovat Res AcSIR, Campus Sanat Nagar, Srinagar 190005, Jammu & Kashmir, India
[3] IIIM, Med Chem Div, Campus Sanat Nagar, Srinagar 190005, Jammu & Kashmir, India
关键词:
anti-TB agents;
clinical trials;
drug-drug interactions;
HIV;
MDR-TB;
Mycobacterium tuberculosis;
pyrone;
NONPEPTIDIC PROTEASE INHIBITOR;
TRIACETIC ACID LACTONE;
NATURAL-PRODUCTS;
HIV-PROTEASE;
ANTIMYCOBACTERIAL ACTIVITY;
RNA-POLYMERASE;
DNA GYRASE;
CELL-WALL;
ANTI-TB;
BACTERICIDAL ACTIVITY;
D O I:
10.4155/fmc-2017-0116
中图分类号:
R914 [药物化学];
学科分类号:
100701 ;
摘要:
Tuberculosis ranks as the leading cause of global human mortality from a single infectious agent. To address the uprising issues of drug resistance, intense research efforts have been directed towards drug discovery. However, it is a long and economically challenging process that is often associated with high failure rates. Therefore, it seems prudent to take forward the core scaffolds that have already acclaimed clinical relevance. In this direction, hydroxylated alpha-pyrone scaffold has received US FDA approval for human use against HIV. Interestingly, literature review reveals the potential applicability of alpha-pyrones in TB drug discovery. On one hand, alpha-pyrones play a vital role in the cell wall of Mycobacterium tuberculosis and on the other hand natural alpha-pyrones display appreciable anti-TB activity. This review aims to rekindle the interest of researchers toward alpha-pyrone as a new anti-TB drug thatmay possibly tackle drug resistance and open a dual frontier in TB and HIV drug discovery.
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页码:2053 / 2067
页数:15
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