Biological Evaluation of Novel Curcumin–Pyrazole–Mannich Derivative Active Against Drug-Resistant
            <i>Mycobacterium Tuberculosis</i>

Singh, Alok; Yadav, Pragya; Karaulia, Pratiksha; Singh, Vinay Kumar; Gupta, Pushpa; Puttrevu, Santosh Kumar; Chauhan, Sanjay; Bhatta, R. S.; Narender, Tadigoppula; Gupta, Umesh Datta; Chopra, Sidharth; Dasgupta, Arunava

doi:10.2217/fmb-2017-0054

Cited by 10 publications

(12 citation statements)

References 20 publications

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“…Moreover, curcumin and the isoxazole analogs, fashioned untimely reductions in the amounts of relevant gene transcripts which were diverse. [43] Among them, compounds 17 and 18 demonstrated potent cytotoxic activity against HNSCC cell lines. [59] Isoxazole and pyrazole derivatives were less prone to nucleophilic benzyl mercaptan addition than curcumin.…”

Section: Curcumin Pyrazole and Isoxazole Analogs As Anticancer Agentsmentioning

confidence: 99%

“…Molecular docking studies discovered the promising binding type of pyrazole compound 2 in the SH2 domain of STAT3 (curcumin pyrazole and curcumin click chemistry analogs 6 and 16-18). [43] Among them, compounds 17 and 18 demonstrated potent cytotoxic activity against HNSCC cell lines. Amusingly, derivatives 16 and 17 have important effect on pSTAT3 phosphorylation.…”

Section: Curcumin Pyrazole and Isoxazole Analogs As Anticancer Agentsmentioning

confidence: 99%

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Recent Updates in Curcumin Pyrazole and Isoxazole Derivatives: Synthesis and Biological Application

Patel

Halpani

2019

Chemistry & Biodiversity

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Curcumin is an admired, plant-derived compound that has been extensively investigated for diverse range of biological activities, but the use of this polyphenol is limited due to its instability. Chemical modifications in curcumin are reported to seize this limitation; such efforts are intensively performed to discover molecules with similar but improved stability and better properties. Focal points of these reviews are synthesis of stable pyrazole and isoxazole analogs of curcumin and application in various biological systems. This review aims to emphasize the latest evidence of curcumin pyrazole analogs as a privileged scaffold in medicinal chemistry. Manifold features of curcumin pyrazole analogs will be summarized herein, including the synthesis of novel curcumin pyrazole analogs and the evaluation of their biological properties. This review is expected to be a complete, trustworthy and critical review of the curcumin pyrazole analogs template to the medicinal chemistry community.

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Section: Curcumin Pyrazole and Isoxazole Analogs As Anticancer Agentsmentioning

confidence: 99%

Section: Curcumin Pyrazole and Isoxazole Analogs As Anticancer Agentsmentioning

confidence: 99%

Recent Updates in Curcumin Pyrazole and Isoxazole Derivatives: Synthesis and Biological Application

Patel

Halpani

2019

Chemistry & Biodiversity

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“…Three-week treatment with 25 mg/kg of CPMD-6-dihydrochloride showed a significant reduction in the bacterial load in the lung of infected six-week-old BALB/c mice by 1.06 log10 in comparison to 100 mg/kg of EMB treated group. CPMD-6-dihydrochloride also reduced bacterial counts by 0.63 log10 while EMB reduced by 0.51 log10 in the spleen, demonstrating that CPMD-6 dihydrochloride has superior efficacy with respect to a reduction in mycobacterial CFU at one-fourth of the dosage in comparison to EMB in the murine MTB infection model [ 45 ].…”

Section: Antimycobacterial Activity Of Curcumin Synthetic Derivativesmentioning

confidence: 99%

Therapeutic Potential of Curcumin as an Antimycobacterial Agent

Barua

Buragohain

2021

Biomolecules

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Curcumin is the principal curcuminoid obtained from the plant Curcuma longa and has been extensively studied for its biological and chemical properties. Curcumin displays a vast range of pharmacological properties, including antimicrobial, anti-inflammatory, antioxidant, and antitumor activity. Specifically, curcumin has been linked to the improvement of the outcome of tuberculosis. There are many reviews on the pharmacological effects of curcumin; however, reviews of the antitubercular activity are comparatively scarcer. In this review, we attempt to discuss the different aspects of the research on the antitubercular activity of curcumin. These include antimycobacterial activity, modulation of the host immune response, and enhancement of BCG vaccine efficacy. Recent advances in the antimycobacterial activity of curcumin synthetic derivatives, the role of computer aided drug design in identifying curcumin targets, the hepatoprotective role of curcumin, and the dosage and toxicology of curcumin will be discussed. While growing evidence supports the use of curcumin and its derivatives for tuberculosis therapy, further preclinical and clinical investigations are of pivotal importance before recommending the use of curcumin formulations in public health.

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“…Multiple studies made earlier reveal that the MTB growth inhibiting potential of curcumin is satisfactory but not that excellent. To overcome this disadvantage, Singh et al 116 synthesized 21 curcumin derivatives and evaluated them for their in vitro and in vivo antimycobacterial activity. They reported that a derivative named CPMD-6d dihydrochloride exhibited bactericidal activity against MTB in a concentrationdependent manner (MIC = 2 μg/ml), even against drugresistant strains.…”

Section: Curcumin and Its Important Nanoformulations Against Mtb Infe...mentioning

confidence: 99%

Antibacterial activity of curcumin and its essential nanoformulations against some clinically important bacterial pathogens: A comprehensive review

Shome

Talukdar

Upadhyaya

2021

Biotech and App Biochem

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Multidrug‐resistant bacterial infections can kill 700,000 individuals globally each year and is considered among the top 10 global health threats faced by humanity as the arsenal of antibiotics is becoming dry and alternate antibacterial molecule is in demand. Nanoparticles of curcumin exhibit appreciable broad‐spectrum antibacterial activity using unique and novel mechanisms and thus the process deserves to be reviewed and further researched to clearly understand the mechanisms. Based on the antibiotic resistance, infection, and virulence potential, a list of clinically important bacteria was prepared after extensive literature survey and all recent reports on the antibacterial activity of curcumin and its nanoformulations as well as their mechanism of antibacterial action have been reviewed. Curcumin, nanocurcumin, and its nanocomposites with improved aqueous solubility and bioavailability are very potential, reliable, safe, and sustainable antibacterial molecule against clinically important bacterial species that uses multitarget mechanism such as inactivation of antioxidant enzyme, reactive oxygen species‐mediated cellular damage, and inhibition of acyl‐homoserine‐lactone synthase necessary for quorum sensing and biofilm formation, thereby bypassing the mechanisms of bacterial antibiotic resistance. Nanoformulations of curcumin can thus be considered as a potential and sustainable antibacterial drug candidate to address the issue of antibiotic resistance.

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Biological Evaluation of Novel Curcumin–Pyrazole–Mannich Derivative Active Against Drug-Resistant Mycobacterium Tuberculosis

Abstract: Taken together, CPMD-6d dihydrochloride exhibits all properties to be positioned as a novel molecule of interest for treatment of tuberculosis. Graphical abstract: [Formula: see text].

Cited by 10 publications

References 20 publications

Recent Updates in Curcumin Pyrazole and Isoxazole Derivatives: Synthesis and Biological Application

Recent Updates in Curcumin Pyrazole and Isoxazole Derivatives: Synthesis and Biological Application

Therapeutic Potential of Curcumin as an Antimycobacterial Agent

Antibacterial activity of curcumin and its essential nanoformulations against some clinically important bacterial pathogens: A comprehensive review

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