Synthesis and evaluation of small libraries of triazolylmethoxy chalcones, flavanones and 2-aminopyrimidines as inhibitors of mycobacterial FAS-II and PknG

Anand, Namrata; Singh, Priyanka; Sharma, Anindra; Tiwari, Sameer K.; Singh, V. K.; Singh, Diwakar; Srivastava, Kirti; Singh, B. N.; Tripathi, Rama Pati

doi:10.1016/j.bmc.2012.07.009

Cited by 50 publications

(38 citation statements)

References 33 publications

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“…The adaptation of the double recombinant strains for ex vivo studies and in vivo imaging requires a detailed analysis of the activities of pathway-specific promoters upon infection in macrophages and under in vivo conditions. Earlier, we had used this M. tuberculosis kas operon promoter to generate a recombinant M. aurum strain (11) which was subsequently utilized for screening antimycobacterial compounds against the FAS-II pathway (29,30). In a separate study (31), the primary recombinant strain M. bovis BCG hsp60p-Fluc was used to test the efficacy of a beta-casein fragment peptide on the clearance of M. bovis BCG from THP-1 cells.…”

Section: Figmentioning

confidence: 99%

Double Recombinant Mycobacterium bovis BCG Strain for Screening of Primary and Rationale-Based Antimycobacterial Compounds

Singh

Biswas

Singh

2014

Antimicrob Agents Chemother

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Conventional antimycobacterial screening involves CFU analysis, which poses a great challenge due to slow growth of mycobacteria. Recombinant strains carrying reporter genes under the influence of constitutive promoters allow rapid and wide screening of compounds but without revealing their modes of action. Reporter strains using pathway-specific promoters provide a better alternative but allow a limited screening of compounds interfering with only a particular metabolic pathway. This reduces these strains to merely a second-line screening system, as they fail to identify even the more potent compounds if they are not inhibiting the pathway of interest. In this study, we have generated a double recombinant Mycobacterium bovis BCG strain carrying firefly and Renilla luciferase genes as two reporters under the control of a constitutive and an inducible mycobacterial promoter. The presence of dual reporters allows simultaneous expression and analysis of two reporter enzymes within a single system. The expression profile of the firefly luciferase gene, rendered by a constitutive mycobacterial promoter, coincides with the decline in bacterial growth in response to a wide range of antimycobacterial drugs, while the enhanced expression of Renilla luciferase mirrors the selective induction of the reporter gene expression as a result of pathway-specific inhibition. Thus, the double recombinant strain allows the screening of both primary and rationally synthesized antimycobacterial compounds in a single assay. The inhibiting response of drugs was monitored with a dual-luciferase reporter assay which can be easily adapted in high-throughput mode.

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Section: Figmentioning

confidence: 99%

Double Recombinant Mycobacterium bovis BCG Strain for Screening of Primary and Rationale-Based Antimycobacterial Compounds

Singh

Biswas

Singh

2014

Antimicrob Agents Chemother

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“…Molecular hybridization involves the combination of two distinct pharmacophores or chemical entities by either linking or fusing each other to form new hybrid moieties [4,5]. The selection of the pharmacophores or chemical moieties is based upon their known bio profiles and it is expected that the hybrid molecules might exhibit synergistic or additive pharmacological activities [6,7].…”

Section: Introductionmentioning

confidence: 99%

Design, synthesis and biological evaluation of some isatin-linked chalcones as novel anti-breast cancer agents: A molecular hybridization approach

Karthikeyan

Solomon

Lee

et al. 2013

Biomedicine & Preventive Nutrition

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“…The formed precipitate was filtered, washed with ethanol, dried and recrystallized from acetic acid to give the title compound 18. (1,2,3,4-Tetrahydronaphthalen-6-yl)-2-substituted-4-(1,3-diphenyl-1H-pyrazol-4yl)pyridine-3-carbonitrile (19)(20)(21) A mixture of compound 18 (1.88 g, 0.004 mol), different alkyl halide namely; methyl iodide, chloroacetone and/or ethyl bromoacetate (0.004 mol) and potassium carbonate (0.56 g, 0.004 mol) in DMF (10 ml) was refluxed for 8-10hr. Then, the reaction mixture was cooled and poured onto ice/cold water.…”

Section: 2-dihydro-6-(1234-tetrahydronaphthalen-6-yl)-2-oxo-4-(1mentioning

confidence: 99%

“…Molecular hybridization involves the combination of two or more chemical entities by either linking or fusing each other to form new hybrid moieties (19) . The selection of the chemical moieties is based upon their known bio-profiles and it is expected that the hybrid molecules might exhibit additive pharmacological activities (20,21) .…”

mentioning

confidence: 99%

Synthesis and Cytotoxicity Evaluation of Some Novel Tetrahydronaphthalene-Pyrazole Derivatives

2014

Egypt. J. Chem.

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Synthesis and evaluation of small libraries of triazolylmethoxy chalcones, flavanones and 2-aminopyrimidines as inhibitors of mycobacterial FAS-II and PknG

Cited by 50 publications

References 33 publications

Double Recombinant Mycobacterium bovis BCG Strain for Screening of Primary and Rationale-Based Antimycobacterial Compounds

Double Recombinant Mycobacterium bovis BCG Strain for Screening of Primary and Rationale-Based Antimycobacterial Compounds

Design, synthesis and biological evaluation of some isatin-linked chalcones as novel anti-breast cancer agents: A molecular hybridization approach

Synthesis and Cytotoxicity Evaluation of Some Novel Tetrahydronaphthalene-Pyrazole Derivatives

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