31 research outputs found

    Molecular insights into Coumarin analogues as antimicrobial agents: Recent developments in drug discovery

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    A major global health risk has been witnessed with the development of drug-resistant bacteria and multidrug-resistant pathogens linked to significant mortality. Coumarins are heterocyclic compounds belonging to the benzophenone class enriched in different plants. Coumarins and their derivatives have a wide range of biological activity, including antibacterial, anticoagulant, antioxidant, anti-inflammatory, antiviral, antitumour, and enzyme inhibitory effects. In the past few years, attempts have been reported towards the optimization, synthesis, and evaluation of novel coumarin analogues as antimicrobial agents. Several coumarin-based antibiotic hybrids have been developed, and the majority of them were reported to exhibit potential antibacterial effects. In the present work, studies reported from 2016 to 2020 about antimicrobial coumarin analogues are the focus. The diverse biological spectrum of coumarins can be attributed to their free radical scavenging abilities. In addition to various synthetic strategies developed, some of the structural features include a heterocyclic ring with electron-withdrawing/donating groups conjugated with the coumarin nucleus. The suggested structure−activity relationship (SAR) can provide insight into how coumarin hybrids can be rationally improved against multidrug-resistant bacteria. The present work demonstrates molecular insights for coumarin derivatives having antimicrobial properties from the recent past. The detailed SAR outcomes will benefit towards leading optimization during the discovery and development of novel antimicrobial therapeutics

    Therapeutic Outcomes of Isatin and Its Derivatives against Multiple Diseases: Recent Developments in Drug Discovery

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    Isatin (1H indole 2, 3-dione) is a heterocyclic, endogenous lead molecule recognized in humans and different plants. The isatin nucleus and its derivatives are owed the attention of researchers due to their diverse pharmacological activities such as anticancer, anti-TB, antifungal, antimicrobial, antioxidant, anti-inflammatory, anticonvulsant, anti-HIV, and so on. Many research chemists take advantage of the gentle structure of isatins, such as NH at position 1 and carbonyl functions at positions 2 and 3, for designing biologically active analogues via different approaches. Literature surveys based on reported preclinical, clinical, and patented details confirm the multitarget profile of isatin analogues and thus their importance in the field of medicinal chemistry as a potent chemotherapeutic agent. This review represents the recent development of isatin analogues possessing potential pharmacological action in the years 2016–2020. The structure–activity relationship is also discussed to provide a pharmacophoric pattern that may contribute in the future to the design and synthesis of potent and less toxic therapeutics

    Imaginaries of development of Polavaram dam project

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    In recent decades, there has been much discussion on the societal effects of large dams. The National River Linking Project (NRLP), the largest water project now under development in the world that would include the building of multiple dams, has been the subject of much discussion in India. The purpose of the $168 billion project is to link most Indian rivers to a massive water system. As highlighted by Nehru's famous remark that huge dams are "the temples of contemporary India," substantial water infrastructure has historically been discursively tied to imaginaries of development and national progress in the subcontinent. The experiences of people impacted by the construction of dams.  However, these visions clash with reality due to the fact that the displaced people are not only among the most disadvantaged in Indian society but also stand to benefit the least and lose the most from such programmes. Starting with a review of the media coverage given to the Polavaram Project, the first project to be undertaken under the NRLP programme, this paper examines the extent to which such imaginaries remain prevalent in modern political discourse.&nbsp

    Synthesis of some important partial methyl ethers of flavonols

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    Domino multicomponent intramolecular cyclization strategy for the multi functionalized Imidazo[1,2-a]pyrimidin-5(1h)-one derivatives

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    A microwave assisted novel domino synthetic approach to trifluoromethyl substituted imidazo[1,2-a]pyrimidin-5(1H)-one derivatives has been developed via a multi component cascade strategy in a single operation. The synthesized compounds can find application as structural components of biologically active compounds
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