Department of Pharmacy
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Item Plants from Annonaceae family as antimalarials: An ethnopharmacology and phytochemistry review to identify potential lead molecules(Elsevier, 2023-04) Sundriyal, SandeepMalaria is a life-threatening infectious disease, which affected more than 247 million people worldwide in 2021, causing close to 619,000 deaths. WHO recommends region-specific combination therapies based on the susceptibility of the parasite as the standard treatment for P. falciparum malaria. In recent years, the primary cause of concern is the upsurge of resistance against almost all clinically used antimalarial drugs. Herbal medicines have been reported to be therapeutically effective and have played an important role in the treatment of malaria since time immemorial. The discovery of quinine from the cinchona tree's bark and artemisinin from Artemisia annua L. are the leading examples of bioactive compounds used in modern medicine identified from plant-based traditional medicines. Several plants from the Annonaceae family are used traditionally as antimalarials in different parts of the world endemic to malaria.Item Recent trends in the design of antimicrobial agents using Ugi-multicomponent reaction(Elsevier, 2021-08) Sundriyal, SandeepMulti-drug resistant (MDR) forms of several bacteria, fungi, viruses, and parasites pose a serious challenge to human health and economy. Hence, the rise of antimicrobial resistance (AMR) requires the expedient discovery of novel antimicrobial agents with a unique mode of action. Ugi multicomponent reaction (Ugi-MCR) and its variants have proved to be an important tool in the hand of a medicinal chemist. Traditional Ugi reaction provides one-step access to peptide-like molecules. However, several modifications of Ugi products are now available, enabling the design of diverse molecular scaffolds. This has tremendously expanded the scope of Ugi-MCR in drug discovery. This review focuses on the recently reported application of Ugi reaction in the design of molecules against important pathogenic microbes and parasites. The design, synthesis, and bioactivities of important lead molecules from the literature is discussed. Towards the end, we also provide our perspective highlighting the overall trends in Ugi-MCR enabled antimicrobial drug design and future prospects.Item Non-hydroxamate inhibitors of 1-deoxy-d-xylulose 5-phosphate reductoisomerase (DXR): A critical review and future perspective(Elsevier, 2021-03) Sundriyal, Sandeep1-deoxy-d-xylulose 5-phosphate reductoisomerase (DXR) catalyzes the second step of the non-mevalonate (or MEP) pathway that functions in several organisms and plants for the synthesis of isoprenoids. DXR is essential for the survival of multiple pathogenic bacteria/parasites, including those that cause tuberculosis and malaria in humans. DXR function is inhibited by fosmidomycin (1), a natural product, which forms a chelate with the active site divalent metal (Mg2+/Mn2+) through its hydroxamate metal-binding group (MBG). Most of the potent DXR inhibitors are structurally similar to 1 and retain hydroxamate despite the unfavourable pharmacokinetic and toxicity profile of the latter. We provide our perspective on the lack of non-hydroxamate DXR inhibitors. We also highlight the fundamental flaws in the design of MBG in these molecules, primarily responsible for their failure to inhibit DXR. We also suggest that for designing next-generation non-hydroxamate DXR inhibitors, approaches followed for other metalloenzymes targets may be exploited.