Author
S. Prabu Seenivasan
Bio: S. Prabu Seenivasan is an academic researcher from Indian Council of Medical Research. The author has contributed to research in topics: Antimycobacterial & Quantitative structure–activity relationship. The author has an hindex of 4, co-authored 5 publications receiving 206 citations.
Papers
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TL;DR: In order to develop relatively small molecules as antimycobacterial agents, twenty-five chalcones were synthesized, their activity was evaluated, and quantitative structure-activity relationship (QSAR) was developed.
113 citations
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TL;DR: The efficiency and fidelity of the Cu(I)-catalyzed azide-alkyne reaction are substantiated by good yields and exclusive formation of the expected 1,4-disubstituted triazole product.
80 citations
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TL;DR: Based on bioisosteric similarities with isoniazid, a series of 1,2,3,4-tetrahydropyrimidine-5-carbonitrile derivatives has been designed and some compounds displayed promising antimycobacterial activity comparable or less than the standard drugs isoniaZid and rifampicin.
24 citations
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TL;DR: It is suggested that, these Piper betel derived compounds may be further tested for developing a novel class of broad-spectrum drugs against various common and MDR pathogens.
Abstract: Background Mycobacterium tuberculosis, Vibrio cholerae, and pathogenic Escherichia coli are global concerns for public health. The emergence of multi-drug resistant (MDR) strains of these pathogens is creating additional challenges in controlling infections caused by these deadly bacteria. Recently, we reported that Acetate kinase (AcK) could be a broad-spectrum novel target in several bacteria including these pathogens. Methods Here, using in silico and in vitro approaches we show that (i) AcK is an essential protein in pathogenic bacteria; (ii) natural compounds Chlorogenic acid and Pinoresinol from Piper betel and Piperidine derivative compound 6-oxopiperidine-3-carboxylic acid inhibit the growth of pathogenic E. coli and M. tuberculosis by targeting AcK with equal or higher efficacy than the currently used antibiotics; (iii) molecular modeling and docking studies show interactions between inhibitors and AcK that correlate with the experimental results; (iv) these compounds are highly effective even on MDR strains of these pathogens; (v) further, the compounds may also target bacterial two-component system proteins that help bacteria in expressing the genes related to drug resistance and virulence; and (vi) finally, all the tested compounds are predicted to have drug-like properties. Results and conclusion Suggesting that, these Piper betel derived compounds may be further tested for developing a novel class of broad-spectrum drugs against various common and MDR pathogens.
7 citations
Cited by
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TL;DR: The present work aims to summarize the current approaches adopted for the synthesis of the 1,2,3-triazole and medicinal significance of these architectures as a lead structure for the discovery of drug molecules such as COX-1/COX-2 inhibitors, HIV protease inhibitors, CB1 cannabinoid receptor antagonist and much more which are in the pipeline of clinical trials.
563 citations
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TL;DR: Molecules containing triazole moiety may show promising in vitro and in vivo anti-TB activities and might be able to prevent the drug resistant to certain extent.
327 citations
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TL;DR: A comparison of the drug potency of the hybrid molecules with their individual counterparts is discussed for quantifying the significance of the concept of molecular hybridisation.
313 citations
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TL;DR: The present review has collated published reports on this versatile core of quinoline to provide an insight so that its full therapeutic potential can be utilized for the treatment of tuberculosis.
187 citations
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TL;DR: Triazole core is considered as a privileged structure in medicinal chemistry and is widely used as ‘parental’ compounds to synthesize molecules with medical benefits, especially with infection‐related activities and triazole as a potential targeted core moiety against tuberculosis is explored.
Abstract: Tuberculosis is a contagious disease with comparatively high mortality worldwide. The statistics shows that around three million people throughout the world die annually from tuberculosis and there are around eight million new cases each year, of which developing countries showed major share. Therefore, the discovery and development of effective antituberculosis drugs with novel mechanism of action have become an insistent task for infectious diseases research programs. The literature reveals that, heterocyclic moieties have drawn attention of the chemists, pharmacologists, microbiologists, and other researchers owing to its indomitable biological potential as anti-infective agents. Among heterocyclic compounds, triazole (1,2,3-triazole/1,2,4-triazole) nucleus is one of the most important and well-known heterocycles, which is a common and integral feature of a variety of natural products and medicinal agents. Triazole core is considered as a privileged structure in medicinal chemistry and is widely used as ‘parental’ compounds to synthesize molecules with medical benefits, especially with infection-related activities. In the present review, we have collated published reports on this versatile core to provide an insight so that its complete therapeutic potential can be utilized for the treatment of tuberculosis. This review also explores triazole as a potential targeted core moiety against tuberculosis and various research ongoing worldwide. It is hoped that this review will be helpful for new thoughts in the quest for rational designs of more active and less toxic triazole-based antituberculosis drugs.
132 citations