Methods of Alkaloids Synthesis

The investigation of plants used in traditional medicine in the early nineteenth century found alkaloids have developed into a group of natural products with exceptional structural and taxonomic diversity, as well as important chemical, biological, and medicinal importance. Since the early twentieth century, only a few routes have been thoroughly explored, and researchers have struggled to grasp their biogenesis and biosynthesis. Even for many pharmaceutically important alkaloids, there is still much to learn about how alkaloids are generated in nature, despite recent enzymatic efforts that have significantly advanced our understanding of this process. Certain aspects of empirically determined or speculated mechanistic routes of alkaloids creation are explored, with an emphasis on clinically relevant alkaloids

Molecular Docking: Metamorphosis in Drug Discovery

Molecular docking is recognized a part of computer-aided drug design that is mostly used in medicinal chemistry. It has proven to be an effective, quick, and low-cost technique in both scientific and corporate contexts. It helps in rationalizing the ligands activity towards a target to perform structure-based drug design (SBDD). Docking assists the revealing of novel compound of therapeutic interest, forecasting ligand-protein interaction at a molecular basis and delineating structure activity relationships (SARs). Molecular docking acts as a boon to identify promising agents in emergence of diseases which endangering the human health. In this chapter, we engrossed on the techniques, types, opportunities, challenges and success stories of molecular docking in drug development

Pyrazole Scaffold: Strategies toward the Synthesis and Their Applications

Pyrazoles have a wide range of applications in medicinal chemistry, drug discovery, agrochemistry, coordination chemistry, and organometallic chemistry. Their popularity has skyrocketed since the early 1990s. Basically, Pyrazole (C3H3N2H) is a simple doubly unsaturated five membered heterocyclic aromatic ring molecule comprising two nitrogen (N) atoms at positions 1- and 2- and three carbon (C) atoms. Pyrazole nucleus is synthesized with various strategies such as multicomponent approach, dipolar cycloadditions, cyclocondensation of hydrazine with carbonyl system, using heterocyclic system and multicomponent approach. A special emphasis is placed on a thorough examination of response processes. Furthermore, the reasons for the increasing popularity of pyrazoles in several fields of science are examined. Pyrazoles have recently been the focus of many techniques, mostly because of how frequently they are used as scaffolds in the synthesis of bioactive chemicals and reactions in various media. The goal of this chapter is to discuss the current developments in synthetic techniques and biological activity related to pyrazole derivatives. The many pharmacological functions of the pyrazole moiety and different synthesis techniques were discussed. This chapter has summarized novel strategies and wide applications of pyrazole scaffold

Schiff Base as Multifaceted Bioactive Core

Schiff bases are the condensation products of primary amines and carbonyl compounds, which are becoming more and more significant. Schiff bases are imine or azomethine (–C=N–) functional group containing compounds that are produced through a nucleophile addition process. Excellent chelators called Schiff bases have a place in both qualitative and quantitative analysis of metals in aqueous media. Schiff bases were discovered to be auxiliary scaffolds and adaptable pharmacophore for the creation and production of numerous bioactive leads compounds, and this special quality made them accessible for a wide range of biological applications. Schiff bases exhibit significant biological properties including analgesic, anti-inflammatory, antibacterial, anticonvulsant, anti-tubercular, anticancer, antioxidant, anthelmintic antiglycation, and antidepressant activities. In situ cross-linked hydrogel systems are created using the Schiff bases, which are frequently utilized in coordination, organometallic chemistry, and tissue engineering applications. The role of Schiff bases to the design and creation of new lead with potential biological functions is highlighted in this chapter. Researchers’ interest in obtaining the most conclusive and suggestive information on the numerous Schiff bases that have been important for therapeutic purposes over the last few decades and their use in coordination complexes has been maintained by this bioactive core

Effect of quercetinon drug induced hepatotoxicity

Objectives-The present study was designed 1. To achieved maximum yield of bioactive extract from the plant through extraction process. 2. To investigated phytochemicals constituents. 3. To determined pharmacological screening of quercetin against hepatotoxicity. Methods- Crude extracts of Moringa oleifera leaves were prepared using various solvents using petroleum ether, chloroform, ethanol, methanol in succession using soxhlet apparatus. The plant extracts were subjected for photochemical analysis, total phenolic content and total flavonoid content. The extracts were then subjected to column chromatography followed by TLC. The isolated compound was subjected to experimental animals and hepatoprotective activity was studied. Results-The ethanol extract showed the presence of higher flavonoid content when compared with other solvent extracts. The ethanol extract was subjected to fractionalization by column chromatography. The eluted fractions were run in TLC mobile phase with the different solvent ratio. Chromatographic fingerprinting showed the presence of flavonoids. It was found that there was significant decrease in the SGOT, SGPT, ALP and Total Bilirubin level in animal by giving quercetin of ethanolic extract of Moringa oleifera plant. Conclusion - The present investigation revealed that the extract containing quercetin of Moringa oleifera showed excellent hepatoprotective activity against Paracetamol induced hepatotoxicity