A new modification of anti-tubercular active molecules

Imramovský, Aleš; Polanc, Slovenko; Vinšová, Jarmila; Kočevar, Marijan; Jampílek, Josef; Rečková, Zuzana; Kaustová, Jarmila

doi:10.1016/j.bmc.2007.01.051

Cited by 105 publications

(63 citation statements)

References 19 publications

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“…These could be considered prodrugs because they contain two conventional drugs that are bound by a CH fragment. Although the results of activity are very similar to those presented by INH and PZA, the hydrolysis of new compounds ensures prolonged release of the active drugs (Imramovsky et al, 2007).…”

Section: Isoniazid Derivativessupporting

confidence: 61%

Antitubercular Drugs Development: Recent Advances in Selected Therapeutic Targets and Rational Drug Design

Bocanegra-García¹,

García²,

Palma-Nicolás³

et al. 2011

Drug Development - A Case Study Based Insight Into Modern Strategies

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Section: Isoniazid Derivativessupporting

confidence: 61%

Antitubercular Drugs Development: Recent Advances in Selected Therapeutic Targets and Rational Drug Design

Bocanegra-García¹,

García²,

Palma-Nicolás³

et al. 2011

Drug Development - A Case Study Based Insight Into Modern Strategies

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“…The synthesis is based on derivatives that originate from ciprofloxacin (k). The lipophilicity, hydrolysis (stability of the compound), and antitubercular activity as well as the structure lipophilicity and structure-activity relationship were studied 49 ( Figure 10). …”

Section: Current Synthetic Developmentsmentioning

confidence: 99%

Ciprofloxacin: review on developments in synthetic, analytical, and medicinal aspects

Sharma

Jain

et al. 2010

Journal of Enzyme Inhibition and Medicinal Chemistry

224

130

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“…Several derivatives were synthesized by linking INH with another conventional drug (morpholine, 2-amino methyl pyridine, benzylamine, PAS, ciprofloxacin) by the CH fragment and evaluated for the activities. The compounds 2-Hydroxy-4-{[(isonicotinoyl hydra zono) methyl] amino}benzoic acid (19) and 1-Cyclopropyl-6-fluoro-7-{4-[(isonicotinoyl hydra zono) methyl] piperazin-1-yl}-4-oxo-1,4-dihydro quinoline-3-carboxylic acid (20) were found to possess higher activity against non-tuberculous strains than INH 62 . …”

Section: Isoniazid As Targetmentioning

confidence: 99%

“…The synthesis is based on derivatives of activated pyrazine derivative with ciprofloxacin (52), p-aminosalicylic acid (PAS) (53) and isonicotinic acid (54) The compounds exhibited significant activity 62 . …”

Section: Isoniazid As Targetmentioning

confidence: 99%

“…The series consisted of 3-(benzylamino)-5-cyanopyrazine -2 -carboxamides and 3-(benzylamino) pyrazine-2, 5-dicarbonitriles with various substituents on the phenyl ring. Compound 3-(4-methylbenzylamino) pyrazine-2, 5-dicarbonitrile (61) possessed the best antimycobacterial activity against Mtb; 3-(benzylamino)pyrazine -2, 5 -dicarbonitrile (62) inhibited all of the tested strains and had the broadest activity spectrum; 3-(4-amino benzyl amino)-5-cyanopyrazine -2 -carboxamide (63) combined good antimycobacterial activity against Mtb with relatively low cytotoxicity (hepato toxicity) 96 . …”

Section: Isoniazid As Targetmentioning

confidence: 99%

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2017

IJPSR

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Tuberculosis (TB) remains one of the main causes of death from an infectious disease till date. Recent data shows that currently 9.6 million people are infected with TB. Over 95% of TB deaths occur in low-and middle-income countries and it is among the top 5 causes of death for women aged 15 to 44. TB is a leading killer of HIV-positive people and around 1 in 3HIV deaths was due to TB. Furthermore, multidrug-resistant (MDR)-TB and extensively drug-resistant (XDR)-TB is spreading and poses a major threat to progress in global TB control program. The emergence of drug resistant TB strains makes the invention of new molecular scaffold a priority. One of the possible strategies to overcome drug resistance in an economic and simple manner would involve re-engineering and repositioning of some old drugs to obtain derivatives that can work on resistant TB bacilli. These may have enhanced bioavailability, be more effective, and serve as cost-effective substitutes, as compared to new drugs identified through conventional methods of drug discovery and development. In view of this, the present review aims to provide a summarizing report on the derivatives of firstline drugs (isoniazid and pyrazinamide) that have the potential to conquer the resistance to the parental drug and could thus serve as effective alternatives.

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A new modification of anti-tubercular active molecules

Cited by 105 publications

References 19 publications

Antitubercular Drugs Development: Recent Advances in Selected Therapeutic Targets and Rational Drug Design

Antitubercular Drugs Development: Recent Advances in Selected Therapeutic Targets and Rational Drug Design

Ciprofloxacin: review on developments in synthetic, analytical, and medicinal aspects

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