The underlying cause of many metabolic diseases is abnormal changes in enzyme activity in metabolism. Inhibition of metabolic enzymes such as cholinesterases (ChEs; acetylcholinesterase, AChE and b...

Novel inhibitors with sulfamethazine backbone: synthesis and biological study of multi-target cholinesterases and α-glucosidase inhibitors.

Design and synthesis of new flavonols as dual ɑ-amylase and ɑ-glucosidase inhibitors: Structure-activity relationship, drug-likeness, in vitro and in silico studies

Background Flavonoids, a group of natural dietary polyphenols, are known for their beneficial effects on human health. By virtue of their various pharmacological effects, like anti-oxidative, antiinflammatory, anti-carcinogenic and neuroprotective effects, flavonoids have now become an important component of herbal supplements, pharmaceuticals, medicinals and cosmetics. There has been enormous literature supporting neuroprotective effect of flavonoids. Recently their efficacy in various neurodegenerative diseases, like Alzheimer's disease and Parkinson diseases, has received particular attention. Objective The mechanism of flavanoids neuroprotection might include antioxidant, antiapoptotic, antineuroinflammatory and modulation of various cellular and intracellular targets. In in-vivo systems, before reaching to brain, they have to cross barriers like extensive first pass metabolism, intestinal barrier and ultimately blood brain barrier. Different flavonoids have varied pharmacokinetic characteristics, which affect their pharmacodynamic profile. Therefore, brain accessibility of flavonoids is still debatable. Methods This review emphasized on current trends of research and development on flavonoids, especially in neurodegenerative diseases, possible challenges and strategies to encounter using novel drug delivery system. Results Various flavonoids have elicited their therapeutic potential against neurodegenerative diseases, however by using nanotechnology and novel drug delivery systems, the bioavailability of favonoids could be enhanced. Conclusion This study bridges a significant opinion on medicinal chemistry, ethanopharmacology and new drug delivery research regarding use of flavonoids in management of neurodegeneration.

Role of Flavonoids in Neurodegenerative Diseases: Limitations and Future Perspectives

To explore new scaffolds as tyrosinase enzyme inhibitors remain an interesting goal in the drug discovery and development. In due course and our approach to synthesize bioactive compounds, a series...

/pdf/exploring-3-hydroxyflavone-scaffolds-as-mushroom-tyrosinase-4m2spmmicd.pdf

Exploring 3-Hydroxyflavone Scaffolds as Mushroom Tyrosinase Inhibitors: Synthesis, X-Ray Crystallography, Antimicrobial, Fluorescence Behaviour, Structure-Activity Relationship and Molecular Modelling Studies

The COVID-19 pandemic has claimed more than a million lives worldwide within a short time span. Due to the unavailability of specific antiviral drugs or vaccine, the infections are causing panic bo...

Synthetic flavonoids as potential antiviral agents against SARS-CoV-2 main protease.

Flavonols and 4-thioflavonols as potential acetylcholinesterase and butyrylcholinesterase inhibitors: Synthesis, structure-activity relationship and molecular docking studies.

\n\nHeterocyclic compounds are vital to life, since they constitute the most\ninteresting part of the pharmacologically active drugs. Dihydropyrimidine-2-one/thione (DHPM) as\nthe heterocyclic nucleus is the basic part of the most natural as well as synthetic drugs. Synthesis of\nnew derivatives of DHPM and screening their pharmacological potential appear to be an important\ngoal.\n\n\n\n In this study, we have synthesized 15 derivatives of 3,4-dihydropyrimidin-2(1H)-\nones/thiones through simple one-step synthetic method comprising one-pot condensation of variously\nsubstituted benzaldehydes, urea/thiourea and ethyl acetoacetate using ammonium chloride in\nmethanol as well as under solvent-free conditions. In comparison, the former methodology was\nproved more efficient, convenient and gave higher yields. Moreover, those compounds were screened\nfor their potential against bacterial strains (S. aureus and E. coli) and fungal strains (C. albicans and\nC. parapsilosis).\n\n\n\nThe experimental results revealed that the synthesized compounds are more\nactive against C. albicans fungus as compared to other tested microbes. Amongst all the synthesized\nderivatives, compound 3 showed significant non-competitive potential antifungal activity in vitro\nantimicrobial assay. Theoretically, molecular docking studies showed that these compounds can bind\neffectively to oxidoreductase enzyme of E. coli and CYP-51 oxidoreductase of C. albicans.\n\n\n\nHerein, we report improved and high yield reaction conditions for the synthesis of\nbiologically active dihydropyrimidine-2-one, and-thione derivatives. Remarkably, most of the\nsynthesized compounds demonstrated moderate to very good antifungal activity in comparison to the\nantibacterial activity.\n

Chaudhary Omer Javed

Papers

Flavonols and 4-thioflavonols as potential acetylcholinesterase and butyrylcholinesterase inhibitors: Synthesis, structure-activity relationship and molecular docking studies.

An Efficient Protocol for the Synthesis, Biological Screening and Molecular Docking Studies of 3,4-Dihydropyrimidine-2-one/thione Derivatives