Recent developments of quinoline derivatives and their potential biological activities

2020 ◽  
Vol 17 ◽  
Author(s):  
Mustapha Dib ◽  
Hajiba Ouchetto ◽  
Khadija Ouchetto ◽  
Abderrafia Hafid ◽  
Mostafa Khouili
Keyword(s):  
Drug Discovery ◽  
Organic Synthesis ◽  
Heterocyclic Compounds ◽  
Recent Progress ◽  
Biological Activities ◽  
Quinoline Derivatives ◽  
Quinoline Ring ◽  
Research Groups ◽  
Drug Discovery And Development ◽  
Recent Developments

: Heterocyclic compounds containing the quinoline ring play a significant role in organic synthesis and therapeutic chemistry. Polyfunctionalized quinolines have attracted the attention of many research groups, especially those who work on the drug discovery and development. These derivatives have been widely explored by the research biochemists and are reported to possess wide biological activities. This review focuses on the recent progress in the synthesis of heterocyclic compounds based-quinoline and their potential biological activities.

Recent Advances in Transition Metal Mediated Synthetic Approaches to Quinoline Derivatives

2020 ◽  
Vol 17 ◽  
Author(s):  
Rukhsana Tabassum ◽  
Muhammad Ashfaq ◽  
Hiroyuki Oku
Keyword(s):  
Transition Metal ◽  
Heterocyclic Compounds ◽  
Therapeutic Agent ◽  
Biological Activities ◽  
Quinoline Derivatives ◽  
Quinoline Ring ◽  
Pharmacological Activities ◽  
Synthetic Routes ◽  
Synthetic Approaches ◽  
Significant Attention

Abstract:: Synthesis of heterocyclic compounds containing quinoline scaffold attracted a significant attention of organic chemists due to their importance as therapeutic agent in pharmaceutical industry. Quinolone molecule exhibit extensive biological activities a few of which are antiviral, anti-inflammatory antibacterial, antifungal, antiproliferative, anthelmintic and anticonvulsant. A variety of synthetic routes has been developed for construction compounds bearing quinoline nucleus due to its broad spectrum of pharmacological activities. This review describes recent development in transition metal mediated synthetic protocols of these important heterocycles by formation of quinoline ring or by substitution of quinoline rings including both modified conventional name reactions and novel routes with highly functionalized quinoline products.

scholarly journals Recent Developments and Biological Activities of 5-Oxo-Imidazolones Derivatives: A Review

2021 ◽  
pp. 287-305
Author(s):  
N. Yellasubbaiah ◽  
V. Velmurugan ◽  
B. Nagasudha
Keyword(s):  
Drug Discovery ◽  
Biological Property ◽  
Heterocyclic Compounds ◽  
Biological Activities ◽  
Ring System ◽  
Present Review ◽  
Modern Drug ◽  
Recent Developments ◽  
Biological Potency

Heterocyclic compounds are essential primary units for both the synthetic and natural starting points. 5-oxo-imidazolone is a 5-member ring system that contains 3 carbons and 2 nitrogens that are arranged at 3 and 1 positions, and ─C═O at the 5th position of the ring. 5-oxo-imidazolone is known as a privileged molecule because of its all biological potency. This biological property increased the attention of many investigators to analyze this ring system and expose several activities. The present review aims to outline the various activities reported on the synthesis and the biological potencies of 5-oxo-imidazolone derivatives. 5-oxo-imidazolone is an important pharmacophore in modern drug discovery.

Recent Synthetic Strategies for Monocyclic Azole Nucleus and Its Role in Drug Discovery and Development

2018 ◽  
Vol 15 (3) ◽  
pp. 321-340 ◽  
Author(s):  
Neha ◽  
Ashish Ranjan Dwivedi ◽  
Rakesh Kumar ◽  
Vinod Kumar
Keyword(s):  
Heterocyclic Compounds ◽  
Biological Activities ◽  
Review Article ◽  
Drug Discovery And Development ◽  
Drug Candidates ◽  
Drug Molecules ◽  
Current Review ◽  
Biological Potential ◽  
Recent Developments ◽  
Potent Drug

Background: In recent years, the development and diversification of heterocyclic compounds has become central to the discovery of bioactive compounds with novel or improved pharmacological properties. In particular, N-containing heterocycles are proved to be promising leads and drug candidates, and received huge attention of the medicinal chemists. Objective: Many drugs especially antibiotics are becoming obsolete due to the development of multidrug resistance. Moreover, toxicity and other side effects of some drugs necessitated the quest for safer and more potent drug candidates. The current review article described biological potential of various monocyclic azoles. Recent developments in the synthesis of azole derivatives have been also reviewed. Conclusion: The presence of N-heterocyclic rings can influence the pharmacokinetics, pharmacodynamics, pKa and bioavailability profile of the drug molecules. Compounds containing monocyclic azole rings showed various biological activities and number of molecules are in clinical practice. A number of important leads and potential drug candidates containing azole nucleus are in advance stages of drug developments. Thus, simple, atom economic and more efficient synthetic strategies are desired for the synthesis of new libraries of the compounds.

Secondary Metabolites of Plant Origin containing Carbazole as Lead Molecule: A Review

2019 ◽  
Vol 05 ◽  
Author(s):  
Atul Sharma ◽  
Devender Pathak
Keyword(s):  
Drug Discovery ◽  
Heterocyclic Compounds ◽  
Biological Activities ◽  
Chemical Compounds ◽  
Lethal Effect ◽  
Chemical Diversity ◽  
Chemical Transformations ◽  
Pharmacological Effects ◽  
Structural Class ◽  
Biological Targets

Keeping this fact that study of a body is biology but life is all about chemicals and chemical transformations, many medicinal chemist start research in finding new and novel chemical compounds which having pharmacological activities. Most of those chemical compounds which are having active pharmacological effects are heterocyclic compounds. Heterocyclic compounds clutch a particular place among pharmaceutically active natural and synthetic compounds. The ability to serve both as biomimetics and reactive pharmacophores of heterocyclic nuclei is incredible and it has principally contributed to their unique value as traditional key elements of numerous drugs. These heterocyclic nuclei offer a huge area for new lead molecules for drug discovery and for generation of activity relationships with biological targets to enhance pharmacological effects. For these reasons, it is not surprising that this structural class has received special attention in drug discovery. The hydrogen bond acceptors and donors arranged in a manner of a semi-rigid skeleton in heterocyclic rings and therefore they can present a varied display of significant pharmacophores. Lead identification and optimization of drug target probable can be achieved by generation of chemical diversity produced by derivatization of heterocyclic pharmacophores with different groups or substituents. A tricyclic carbazole nucleus is an integral part of naturally occurring alkaloids and synthetic derivatives, possessing various potential biological activities such as anticancer, antimicrobial and antiviral. Binding mechanism of carbazole with target receptor as a molecule or fused molecule exhibits the potential lethal effect.

scholarly journals Direct access to spirocycles by Pd/WingPhos-catalyzed enantioselective cycloaddition of 1,3-enynes

2021 ◽  
Vol 12 (1) ◽  
Author(s):  
Long Li ◽  
Shan Wang ◽  
Pengfei Luo ◽  
Ran Wang ◽  
Zheng Wang ◽  
...  
Keyword(s):  
Drug Discovery ◽  
Functional Groups ◽  
Organic Synthesis ◽  
Enantioselective Synthesis ◽  
Direct Access ◽  
Cycloaddition Reactions ◽  
Drug Discovery And Development ◽  
Spirocyclic Compounds ◽  
And Control ◽  
By Products

AbstractSpirocycles play an important role in drug discovery and development. The direct, catalytic, and enantioselective synthesis of spirocycles from readily available starting materials and in an atom economic manner remains a highly sought-after task in organic synthesis. Herein, an enantioselective Pd-hydride-catalyzed cycloaddition method for the synthesis of spirocyclic compounds directly from two classes of commonly available starting materials, 1,3-enynes and cyclic carbon−hydrogen (C−H) bonds, is reported. The reactions employ a chiral Pd/WingPhos catalyst to both suppress the formation of bis-allenyl by-products and control the stereoselectivity. 1,3-Enynes are used as dielectrophilic four-carbon units in the cycloaddition reactions, which also enables an enyne substrate-directed enantioselectivity switch with good levels of stereocontrol. The present spirocycle synthesis tolerates a broad range of functional groups of 1,3-enyne substrates, including alcohols, esters, nitriles, halides, and olefins. A variety of diverse cyclic nucleophiles, including pharmaceutically important heterocycles and carbocycles, can be flexibly incorporated with spiro scaffolds.

scholarly journals Synthesis of Imidazole-Based Medicinal Molecules Utilizing the van Leusen Imidazole Synthesis

2020 ◽  
Vol 13 (3) ◽  
pp. 37 ◽  
Author(s):  
Xunan Zheng ◽  
Zhengning Ma ◽  
Dawei Zhang
Keyword(s):  
Drug Discovery ◽  
Chemical Synthesis ◽  
Small Molecules ◽  
Medicinal Chemistry ◽  
Biological Activities ◽  
Structural Features ◽  
Pharmaceutical Companies ◽  
Recent Developments ◽  
Van Leusen Reaction

Imidazole and its derivatives are one of the most vital and universal heterocycles in medicinal chemistry. Owing to their special structural features, these compounds exhibit a widespread spectrum of significant pharmacological or biological activities, and are widely researched and applied by pharmaceutical companies for drug discovery. The van Leusen reaction based on tosylmethylisocyanides (TosMICs) is one of the most appropriate strategies to synthetize imidazole-based medicinal molecules, which has been increasingly developed on account of its advantages. In this review, we summarize the recent developments of the chemical synthesis and bioactivity of imidazole-containing medicinal small molecules, utilizing the van Leusen imidazole synthesis from 1977.

scholarly journals 1,2,3-Triazoles: Synthesis and Biological Application

2020 ◽  
Author(s):  
Abdul Aziz Ali
Keyword(s):  
Drug Discovery ◽  
Supramolecular Chemistry ◽  
Organic Synthesis ◽  
Chemical Biology ◽  
Materials Science ◽  
Biological Activities ◽  
Fluorescent Imaging ◽  
Polymer Chemistry ◽  
Privileged Structure ◽  
Synthetic Approaches

Among nitrogen-containing heterocyclic compounds, 1,2,3-triazoles are privileged structure motif and received a great deal of attention in academics and industry. Even though absent in nature, 1,2,3-triazoles have found broad applications in drug discovery, organic synthesis, polymer chemistry, supramolecular chemistry, bioconjugation, chemical biology, fluorescent imaging, and materials science. Therefore, the development of facile and straightforward methodology for the synthesis of 1,2,3-triazoles is of noteworthy interest. In this study, emphasis will be given to numerous synthetic approaches for the synthesis of 1,2,3-triazoles, especially the popular click chemistry approach. Furthermore, several biological activities of this promising heterocycle will also be discussed.

scholarly journals Strategies To Access γ-Hydroxy-γ-butyrolactams

Synthesis ◽  
2018 ◽  
Vol 50 (06) ◽  
pp. 1175-1198 ◽  
Author(s):  
Laurent Commeiras ◽  
Muhammad Idham Darussalam Mardjan ◽  
Jean-Luc Parrain
Keyword(s):  
Natural Products ◽  
Organic Synthesis ◽  
Broad Spectrum ◽  
Heterocyclic Compounds ◽  
Biological Activities ◽  
Building Blocks ◽  
Pharmaceutical Molecules

α,β-Unsaturated γ-hydroxy-γ-butyrolactams are of a great interest due to their presence in designed pharmaceutical molecules and numerous natural products displaying a broad spectrum of biological activities. In addition, these five-membered heterocyclic compounds are also relevant and versatile building blocks in organic synthesis. In this context, strategies for the construction of these scaffolds has triggered considerable attention and this review highlights the progress in the formation of α,β-unsaturated γ-hydroxy-γ-butyrolactams (5-hydroxy-1,5-dihydro-2H-pyrrol-2-ones).1 Introduction2 Intramolecular Routes3 Intermolecular Routes4 Oxidation of Heterocyclic Compounds5 Miscellaneous6 Conclusion

scholarly journals The Chemistry, Biochemistry and Pharmacology of Marine Natural Products from Leptolyngbya, a Chemically Endowed Genus of Cyanobacteria

Marine Drugs ◽  
2020 ◽  
Vol 18 (10) ◽  
pp. 508
Author(s):  
Yueying Li ◽  
C. Benjamin Naman ◽  
Kelsey L. Alexander ◽  
Huashi Guan ◽  
William H. Gerwick
Keyword(s):  
Nitrogen Fixation ◽  
Drug Discovery ◽  
Secondary Metabolites ◽  
Primary Productivity ◽  
Algal Blooms ◽  
Biological Activities ◽  
Biosynthetic Pathways ◽  
Drug Discovery And Development ◽  
Ecological Habitats ◽  
Product Chemistry

Leptolyngbya, a well-known genus of cyanobacteria, is found in various ecological habitats including marine, fresh water, swamps, and rice fields. Species of this genus are associated with many ecological phenomena such as nitrogen fixation, primary productivity through photosynthesis and algal blooms. As a result, there have been a number of investigations of the ecology, natural product chemistry, and biological characteristics of members of this genus. In general, the secondary metabolites of cyanobacteria are considered to be rich sources for drug discovery and development. In this review, the secondary metabolites reported in marine Leptolyngbya with their associated biological activities or interesting biosynthetic pathways are reviewed, and new insights and perspectives on their metabolic capacities are gained.

Tetralone scaffolds and their potential therapeutic applications

2020 ◽  
Vol 17 ◽  
Author(s):  
Bhagwati Gauni ◽  
Krunal Mehariya ◽  
Anamik Shah ◽  
Srinivas Murty Duggirala
Keyword(s):  
Antitumor Activity ◽  
Organic Synthesis ◽  
Small Molecule ◽  
Heterocyclic Compounds ◽  
Biological Activities ◽  
Acetylcholinesterase Inhibitors ◽  
Building Blocks ◽  
Structural Features ◽  
Therapeutic Applications ◽  
Small Molecule Library

: Substituted tetralones have played a substantial role in organic synthesis due to their strong reactivity and suitability as a starting material for a range of synthetic heterocyclic compounds, pharmaceuticals along with biological activities as well as precursors of many natural products and their derivatives. Many α-tetralone derivatives are building blocks, that have been used in the synthesis of therapeutically functional compounds like some antibiotics, antidepressants, acetylcholinesterase inhibitors effective for treating Alzheimer’s disease and alkaloids possessing antitumor activity. In this review, there has been an attempt to explore the small molecule library having α-tetralone scaffold along with their diverse biological activities. Structural features of α-tetralone derivatives responsible for potential therapeutic applications are also described.

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