School Of Basic And Applied Sciences

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    Tetrazoles as anticancer agents: A review on synthetic strategies, mechanism of action and SAR studies
    (Elsevier, 2020) Dhiman, N; Kaur, K; Jaitak, Vikas
    Cancer is a leading cause of death worldwide. Even after the availability of numerous drugs and treatments in the market, scientists and researchers are focusing on new therapies because of their resistance and toxicity issues. The newly synthesized drug candidates are able to demonstrate in vitro activity but are unable to reach clinical trials due to their rapid metabolism and low bioavailability. Therefore there is an imperative requisite to expand novel anticancer negotiators with tremendous activity as well as in vivo efficacy. Tetrazole is a promising pharmacophore which is metabolically more stable and acts as a bioisosteric analogue for many functional groups. Tetrazole fragment is often castoff with other pharmacophores in the expansion of novel anticancer drugs. This is the first systematic review that emphasizes on contemporary strategies used for the inclusion of tetrazole moiety, mechanistic targets along with comprehensive structural activity relationship studies to provide perspective into the rational design of high-efficiency tetrazole-based anticancer drug candidates. - 2020 Elsevier Ltd
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    Essential Oils: An Impending Substitute of Synthetic Antimicrobial Agents to Overcome Antimicrobial Resistance
    (Bentham Science, 2019) Pal, Rajinder; Rana, Abhilash; Jaitak, Vikas
    ntimicrobial resistance (AMR) is an emerging problem in the world that has a significant impact on our society. AMR made conventional drugs futile against microorganisms and diseases untreatable. Plant-derived medicines are considered safe alternatives to synthetic drugs. The active ingredients and the mixtures of these natural medicines have been used for centuries, due to their easy availability, low cost, and negligible side effects. Essential oils (EOs) are the secondary metabolites that are produced by aromatic plants to protect them from microorganisms. However, these EOs and their constituents have shown good fighting potential against drug-resistant pathogens. These oils have been proved extremely effective antimicrobial agents in comparison to antibiotics. Also, the combination of synthetic drugs with EOs or their components improves their efficacy. So, EOs can be established as an alternative to synthetic antimicrobial agents to eradicate tough form of infectious microorganisms. Due to a number of constituents, it can interact with multiple target sites, like the destruction of cytoplasm membrane or inhibition of protein synthesis and efflux pump. The purpose of this review is to provide information about the antimicrobial activity of EOs attained from different plants, their combination with synthetic antimicrobials. In addition, mechanism of antimicrobial activity of several EOs and their constituents was reported.