Fighting Tuberculosis: An Old Disease with New Challenges

Tripathi, Rama Pati; Tewari, Neetu; Dwivedi, Namrata; Tiwari, Vinod

doi:10.1002/chin.200511291

Cited by 19 publications

(22 citation statements)

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“…Owing to the rapid spread of tuberculosis strains resistant to all first-line anti-tubercular drugs such as isoniazid, rifamcin, and ethionamide, and due to the toxicity of second-line drugs, such as ethionamide, aminosalicylic acid, cycloserine, amikacin, kanamycin, and capreomycin, the discovery of new anti-tubercular agents with potential activity, less toxicity, broader spectrum, and safer therapeutic profiles, is an urgent need (Scior et al, 2002;Tripathi et al, 2005).…”

Section: Introductionmentioning

confidence: 99%

Synthesis and anti-tubercular evaluation of some novel pyrazolo[3,4-d]pyrimidine derivatives

et al. 2011

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A series of phenothiazine clubbed pyrazolo[3,4-d]pyrimidines have been synthesized by using the Biginelli multi-component cyclocondensation reaction and their ability to inhibit growth of Mycobacterium tuberculosis in vitro have been determined. The results show that compounds 4b, 4d, and 4f exhibited excellent anti-tubercular activity with percentage inhibition of 93, 91, and 96, respectively, at a minimum inhibitory concentration (MIC) of\6.25 lg/ml, whereas compounds 4a, 4c, 4e, 4g, and 4h exhibited moderate to good anti-tubercular activity with percentage inhibition of 75, 68, 74, 54, and 63, respectively at a MIC of [6.25 lg/ml.

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Section: Introductionmentioning

confidence: 99%

Synthesis and anti-tubercular evaluation of some novel pyrazolo[3,4-d]pyrimidine derivatives

et al. 2011

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“…capreomycin, cycloserine, kanamycin, ethionamide) have to be used which have significant side effects with approximately 50% cure rate. However, fluoroquinolones such as ofloxacin, norfloxacin can be used which are safer than above-mentioned second-line drugs but have the disadvantage of expense (Tripathi et al, 2005). There have been no anti-TB drugs introduced in past 30 years.…”

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Indian medicinal plants as a source of antimycobacterial agents

Gautam

Saklani

Jachak

2007

Journal of Ethnopharmacology

252

162

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“…Millions of people die every year from tuberculosis which meager the human immune system (Young, 1998;Tripathi et al, 2005). A detailed understanding of this slow-growing pathogen organism is essential in order to create more effective drugs.…”

Section: Introductionmentioning

confidence: 99%

Pyrazolo[3,4-d]pyrimidines as the inhibitors of mycobacterial β-oxidation trifunctional enzyme

2015

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Tuberculosis, one of the oldest known human diseases, is still one of the major causes of mortality. Mycobacterium, a genus of Actinobacteria, is responsible for tuberculosis (Mycobacterium tuberculosis) and leprosy (Mycobacterium leprae). Because of producing high toxicity and resistance of existing drugs, the antitubercular drugs with less toxicity, potential activity and safer therapeutic profiles is an urgent need. Pyrazolo[3,4-d]pyrimidine compounds show various pharmacological activities including antitubercular. Molecular docking studies of eight pyrazolo[3,4-d]pyrimidine derivatives have been carried out with the mycobacterial b-oxidation trifunctional enzyme (mtTFE) using Autodock and Glide docking protocols. The docking results demonstrate good binding capabilities of these molecules with mtTFE. Molecular dynamics simulations of the best docked complexes of the compounds demonstrating better binding affinities and satisfactory ADME properties have been carried out using DESMOND for 10.0 ns duration. The average RMSD variation and simulation interaction study indicate that the complexes remain stable during the course of dynamics. However, molecules 6 and 7 exhibit better stability than other molecules and are the suitable candidates to be carried forward as a potential lead in the discovery of drugs to contest tuberculosis.

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Fighting Tuberculosis: An Old Disease with New Challenges

Abstract: Biochemistry Z 0250 Fighting Tuberculosis: An Old Disease with New Challenges -[332 refs.]. -(TRIPATHI, R. P.; TEWARI, N.; DWIVEDI, N.; TIWARI, V. K.; Med. Res. Rev. 25 (2005) 1, 93-131; Process Dev. Div., Cent. Drug Res. Inst., Lucknow 226 001, India; Eng.) -Lindner 11-291

Cited by 19 publications

References 1 publication

Synthesis and anti-tubercular evaluation of some novel pyrazolo[3,4-d]pyrimidine derivatives

Synthesis and anti-tubercular evaluation of some novel pyrazolo[3,4-d]pyrimidine derivatives

Indian medicinal plants as a source of antimycobacterial agents

Pyrazolo[3,4-d]pyrimidines as the inhibitors of mycobacterial β-oxidation trifunctional enzyme

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