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.

SOMOphilic Alkynylation Using Acetylenic Sulfones as Functional Reagents

2021 ◽  
Author(s):  
Danhua Ge ◽  
Xin Wang ◽  
Xue-Qiang Chu
Keyword(s):  
Drug Discovery ◽  
Organic Synthesis ◽  
Materials Science ◽  
Polymer Chemistry ◽  
The Past ◽  
Acetylenic Sulfones

The past decades have witnessed a boom in alkynylation mainly owing to the importance of alkynyl-containing molecules in organic synthesis, drug discovery, polymer chemistry, and materials science. Besides conventional strategies,...

scholarly journals Steroid diversification by multicomponent reactions

2019 ◽  
Vol 15 ◽  
pp. 1236-1256 ◽  
Author(s):  
Leslie Reguera ◽  
Cecilia I Attorresi ◽  
Javier A Ramírez ◽  
Daniel G Rivera
Keyword(s):  
Amino Acids ◽  
Drug Discovery ◽  
Carboxylic Acid ◽  
Supramolecular Chemistry ◽  
Boronic Acid ◽  
Chemical Biology ◽  
Multicomponent Reactions ◽  
Naturally Occurring ◽  
Almost All ◽  
Structural Diversification

Reports on structural diversification of steroids by means of multicomponent reactions (MCRs) have significantly increased over the last decade. This review covers the most relevant strategies dealing with the use of steroidal substrates in MCRs, including the synthesis of steroidal heterocycles and macrocycles as well as the conjugation of steroids to amino acids, peptides and carbohydrates. We demonstrate that steroids are available with almost all types of MCR reactive functionalities, e.g., carbonyl, carboxylic acid, alkyne, amine, isocyanide, boronic acid, etc., and that steroids are suitable starting materials for relevant MCRs such as those based on imine and isocyanide. The focus is mainly posed on proving the amenability of MCRs for the diversity-oriented derivatization of naturally occurring steroids and the construction of complex steroid-based platforms for drug discovery, chemical biology and supramolecular chemistry applications.

Pyrrolo[2,1-a]isoquinoline scaffold in drug discovery: advances in synthesis and medicinal chemistry

2019 ◽  
Vol 11 (20) ◽  
pp. 2735-2755 ◽  
Author(s):  
Maria D Matveeva ◽  
Rosa Purgatorio ◽  
Leonid G Voskressensky ◽  
Cosimo D Altomare
Keyword(s):  
Multidrug Resistance ◽  
Drug Discovery ◽  
Tumor Cells ◽  
Mechanism Of Action ◽  
Biological Activities ◽  
Antitumor Drugs ◽  
Antitumor Activities ◽  
Structure Activity ◽  
Synthetic Approaches ◽  
Potential Exploitation

Pyrrolo[2,1- a]isoquinoline (PIq) is a nitrogen heterocyclic scaffold of diverse alkaloids endowed with several biological activities, including antiretroviral and antitumor activities. Several 5,6-dihydro-PIq (DHPIq) alkaloids, belonging to the lamellarins’ family, have proved to be cytotoxic to tumor cells, as well as reversers of multidrug resistance. In this review, we provide an overview of the main achievements over the last decade in the synthetic approaches to access libraries of PIq compounds along with a survey, as comprehensive as possible, of bioactivity, mechanism of action, pharmacophore and structure–activity relationships of synthetic analogs of DHPIq-based alkaloids. The focus is mainly on the potential exploitation of the (DH)PIq scaffold in design and development of novel antitumor drugs.

scholarly journals Aqueous olefin metathesis: recent developments and applications

2019 ◽  
Vol 15 ◽  
pp. 445-468 ◽  
Author(s):  
Valerio Sabatino ◽  
Thomas R Ward
Keyword(s):  
Double Bond ◽  
Organic Synthesis ◽  
Olefin Metathesis ◽  
Chemical Biology ◽  
Polymer Chemistry ◽  
Attractive Alternative ◽  
Bond Forming ◽  
Recent Developments ◽  
Tremendous Impact ◽  
Made In

Olefin metathesis is one of the most powerful C–C double-bond-forming reactions. Metathesis reactions have had a tremendous impact in organic synthesis, enabling a variety of applications in polymer chemistry, drug discovery and chemical biology. Although challenging, the possibility to perform aqueous metatheses has become an attractive alternative, not only because water is a more sustainable medium, but also to exploit biocompatible conditions. This review focuses on the progress made in aqueous olefin metatheses and their applications in chemical biology.

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.

scholarly journals SnCl2 Catalyzed Direct Synthesis of Pyrroles under Aqueous Conditions

2020 ◽  
Vol 32 (4) ◽  
pp. 795-802
Author(s):  
D. Tejeswararao ◽  
B. Srikanth
Keyword(s):  
Drug Discovery ◽  
Biological Activities ◽  
Direct Synthesis ◽  
Pyrrole Derivatives ◽  
Chloride Dihydrate ◽  
Substituted Pyrroles ◽  
High Yields ◽  
Aqueous Conditions ◽  
Synthetic Approaches

Synthetic substituted pyrroles are related with interesting biological activities, yet they remain inadequately explored within drug discovery. Late years have seen a growing interest in synthetic approaches that can provide access to structurally novel pyrroles so that the biological usefulness of this compound class can be more fully investigated. Herein, an efficient and versatile practical protocol for the pyrroles using stannous(II) chloride dihydrate as catalyst is described under aqueous conditions at 55 ºC in high yields. Also, this method is applicable for the preparation of diversity and oriented pyrrole derivatives.

Antimicrobial Potential of Benzimidazole Derived Molecules

2019 ◽  
Vol 19 (8) ◽  
pp. 624-646 ◽  
Author(s):  
Yogita Bansal ◽  
Manjinder Kaur ◽  
Gulshan Bansal
Keyword(s):  
Biological Activities ◽  
Benzimidazole Derivative ◽  
Structural Similarity ◽  
Living System ◽  
Axial Ligand ◽  
Benzimidazole Derivatives ◽  
Research Groups ◽  
Structural Resemblance ◽  
Privileged Structure ◽  
Anti Hiv

Structural resemblance of benzimidazole nucleus with purine nucleus in nucleotides makes benzimidazole derivatives attractive ligands to interact with biopolymers of a living system. The most prominent benzimidazole compound in nature is N-ribosyldimethylbenzimidazole, which serves as an axial ligand for cobalt in vitamin B12. This structural similarity prompted medicinal chemists across the globe to synthesize a variety of benzimidazole derivatives and to screen those for various biological activities, such as anticancer, hormone antagonist, antiviral, anti-HIV, anthelmintic, antiprotozoal, antimicrobial, antihypertensive, anti-inflammatory, analgesic, anxiolytic, antiallergic, coagulant, anticoagulant, antioxidant and antidiabetic activities. Hence, benzimidazole nucleus is considered as a privileged structure in drug discovery, and it is exploited by many research groups to develop numerous compounds that are purported to be antimicrobial. Despite a large volume of research in this area, no novel benzimidazole derived compound has emerged as clinically effective antimicrobial drug. In the present review, we have compiled various reports on benzimidazole derived antimicrobials, classified as monosubstituted, disubstituted, trisubstituted and tetrasubstituted benzimidazoles, bisbenzimidazoles, fused-benzimidazoles, and benzimidazole derivative-metal complexes. The purpose is to collate these research reports, and to generate a generalised outlay of benzimidazole derived molecules that can assist the medicinal chemists in selecting appropriate combination of substituents around the nucleus for designing potent antimicrobials.

Experimental and Computational Approaches to Improve Binding Affinity in Chemical Biology and Drug Discovery

2020 ◽  
Vol 20 (19) ◽  
pp. 1651-1660
Author(s):  
Anuraj Nayarisseri
Keyword(s):  
Drug Discovery ◽  
Drug Design ◽  
Binding Affinity ◽  
Chemical Biology ◽  
De Novo ◽  
Structure Based Drug Design ◽  
Computational Approaches ◽  
Drug Designing ◽  
Traditional Drug ◽  
Computer Based

Drug discovery is one of the most complicated processes and establishment of a single drug may require multidisciplinary attempts to design efficient and commercially viable drugs. The main purpose of drug design is to identify a chemical compound or inhibitor that can bind to an active site of a specific cavity on a target protein. The traditional drug design methods involved various experimental based approaches including random screening of chemicals found in nature or can be synthesized directly in chemical laboratories. Except for the long cycle design and time, high cost is also the major issue of concern. Modernized computer-based algorithm including structure-based drug design has accelerated the drug design and discovery process adequately. Surprisingly from the past decade remarkable progress has been made concerned with all area of drug design and discovery. CADD (Computer Aided Drug Designing) based tools shorten the conventional cycle size and also generate chemically more stable and worthy compounds and hence reduce the drug discovery cost. This special edition of editorial comprises the combination of seven research and review articles set emphasis especially on the computational approaches along with the experimental approaches using a chemical synthesizing for the binding affinity in chemical biology and discovery as a salient used in de-novo drug designing. This set of articles exfoliates the role that systems biology and the evaluation of ligand affinity in drug design and discovery for the future.

Metal and Non-Metal Catalysts in the Synthesis of Five-Membered S-Heterocycles

2019 ◽  
Vol 16 (2) ◽  
pp. 258-275 ◽  
Author(s):  
Navjeet Kaur
Keyword(s):  
Organic Synthesis ◽  
Biological Activities ◽  
Reaction Times ◽  
Research Field ◽  
Environmentally Benign ◽  
Metal Catalyst ◽  
Efficient Synthesis ◽  
Heterocyclic Molecules ◽  
The Past ◽  
Harsh Conditions

Background:A wide variety of biological activities are exhibited by N, O and S containing heterocycles and recently, many reports appeared for the synthesis of these heterocycles. The synthesis of heterocycles with the help of metal and non-metal catalyst has become a highly rewarding and important method in organic synthesis. This review article concentrated on the synthesis of S-heterocylces in the presence of metal and non-metal catalyst. The synthesis of five-membered S-heterocycles is described here.Objective:There is a need for the development of rapid, efficient and versatile strategy for the synthesis of heterocyclic rings. Metal, non-metal and organocatalysis involving methods have gained prominence because traditional conditions have disadvantages such as long reaction times, harsh conditions and limited substrate scope.Conclusion:The metal-, non-metal-, and organocatalyst assisted organic synthesis is a highly dynamic research field. For ßthe chemoselective and efficient synthesis of heterocyclic molecules, this protocol has emerged as a powerful route. Various methodologies in the past few years have been pointed out to pursue more sustainable, efficient and environmentally benign procedures and products. Among these processes, the development of new protocols (catalysis), which avoided the use of toxic reagents, are the focus of intense research.

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