A Recent Review on Drug Modification Using 1,2,3-triazole (original) (raw)

2,3-Triazoles: A Review on Current Trends in Synthetic and Biological Applications

The chemistry of 1,2,3-triazoles gained much attention since the discovery by Pechmann, since then several protocols have been developed for the synthesis of 1,2,3-triazoles, but after the copper catalyzed alkyne-azide cycloaddition (CuAAC) reaction, the mainly because of Huisgen's 1,3-dipolar cycloaddition reactions, it has evolved to become one of the most successful connective linkers and functional heterocyclic cores in modern organic chemistry. This review summarizes the up-to date developments in the synthetic methodologies and their biological applications, in particular of antimicrobial, anticancer, anti-inflammatory, anti-proliferative, antidiabetic properties of 1,2,3-triazoles. Also, the progress in the molecular hybridization; and physic-chemical properties have been highlighted.

1,2,3-Triazole Containing Hybrids as Potential Pharmacological Agents: A Review

Asian Journal of Chemistry/Asian journal of chemistry, 2024

; AJC-21601 1,2,3-Triazoles constitute a versatile class of nitrogen containing five-membered heterocycles, exhibiting wide range of pharmacological properties which include antibacterial, antifungal, anticancer, antimalarial, antidiabetic, anti-inflammatory, antihypertensive and antioxidant, among various others. Medicinal chemists have been interested in this aromatic ring as a framework since the inception of click chemistry as considered as the building block of contemporary organic chemistry. Extensive research into this framework's linker characteristic has led to the synthesis and evaluation of numerous 1,2,3-triazole hybrids bearing a wide range of heterocyclic moieties as potential leads for various biological targets. This molecular hybridization has also added advantage of the improved pharmacological activity overcoming the problem of multiple drug resistance and reduced toxicity. This review summarizes the pharmacological activities of various 1,2,3-triazole containing hybrids and conjugates, covering articles published in past decade (2013 till date) and will be of great assistance to medicinal chemistry researchers in providing a useful direction for the future drug discovery.

2, 3-Triazoles: scaffold with medicinal significance

Despite a significant work on 1, 2, 3-triazoles, continuous efforts are still being made to identify novel heterocyclic compounds with potent bioactivities. This review may help the medicinal chemists to develop new leads possessing 1, 2, 3-triazoles nucleus with higher efficacy. This review throws light on the detailed synthetic approaches which have been used for the synthesis of triazoles since the early development in the area of triazole chemistry. This has been followed by the in depth analysis of the triazoles with respect to their medicinal significance.

Advance Synthetic Approaches to 1,2,3-triazole Derived Compounds: State of the Art 2004-2020

Current Organocatalysis, 2021

Background: 1,2,3-triazole is considered a widely explored scaffold by medicinal chemists because of its therapeutic importance. The structural characteristics of 1,2,3-triazoles allow it to mimic certain functional groups demonstrating its utility to prepare new medicinal compounds using the concept of bioisosterism and molecular hybridization. Centered on Huisgens cycloaddition reaction, over the past decade and a half, developed click chemistry approaches to furnish triazole derivatives with various applications ranging from drugs to bioconjugation linkers. Objective: In the present review, we aim to highlight the different approaches developed for the synthesis of 1,2,3-triazole derivatives and in particular, advances in synthetic methods for the last 16 years. This review is also intended to help researchers for finding potential future directions and scope in the development of synthetic strategies. Conclucion: As summarized through the compilation of recent advances for 1,2,3...

Synthesis and Biological Applications of Triazole Derivatives – A Review

Mini-Reviews in Organic Chemistry, 2013

There has been considerable interest in the development of novel heterocyclic compounds with varied biological activities. Triazoles are a special class of heterocyclic compounds with a broad spectrum of biological activities such as antimicrobial, cytotoxic, antihistaminic, anticonvulsant, analgesic, anti-inflammatory, insecticidal, antimycotic, antimycobacterial, anticancer, antiprotozoal, antimalarial and anti-ulcer activity. Therefore, many researchers have synthesized these compounds as target structures and evaluated their biological activities. These observations help the researchers for the development of new triazole compounds with enhanced biological activities. This review focuses on the various synthetic strategies followed for the synthesis of triazoles, and their biological activities.

1,2,4-Triazoles: A Review of Synthetic Approaches and the Biological Activity

Letters in Organic Chemistry, 2013

1,2,4-Triazoles and their derivatives have a distinct place in the field of medicinal and pharmaceutical chemistry. These are used as lead compounds for the synthesis of numerous heterocyclic compounds which possess diverse biological activities and play pivotal roles. This review covers the latest literature and knowledge on the synthetic procedures for various triazoles derivatives, their activities and pharmacological applications.

Medicinal attributes of 1,2,3-triazoles: Current developments

Bioorganic Chemistry, 2017

1,2,3-Triazoles are important five-membered heterocyclic scaffold due to their extensive biological activities. This framework can be readily obtained in good to excellent yields on the multigram scale through click chemistry via reaction of aryl/alkyl halides, alkynes and NaN 3 under ambient conditions. It has been an emerging area of interest for many researchers throughout the globe owing to its immense pharmacological scope. The present work aims to summarize the current approaches adopted for the synthesis of the 1,2,3-triazole and medicinal significance of these architectures as a lead structure for the discovery of drug molecules such as COX-1/COX-2 inhibitors (celecoxib, pyrazofurin), HIV protease inhibitors, CB1 cannabinoid receptor antagonist and much more which are in the pipeline of clinical trials. The emphasis has been given on the major advancements in the medicinal prospectus of this pharmacophore for the period during 2008-2016. 1. Introduction 2. Synthetic Strategies 2.1 Metal free synthesis of 1,2,3-Triazoles 2.2 Metal-catalyzed synthesis of 1,2,3-Triazoles 3. Biological Activity 3.1 Anti-cancer Activity 3.2 Anti-inflammatory activity 3.3 Antitubercular activity 3.4 Antileishmanial and antitrypanosomal activity 3.5 Antimicrobial activity 3.6 Antiviral activity 3.7 Antibacterial activity 3.8 Miscellaneous 4. Conclusion

Triazole analogues as potential pharmacological agents: a brief review

Future Journal of Pharmaceutical Sciences

Background A large number of studies have recently reported that, because of their significant biological and pharmacological properties, heterocyclic compounds and their derivatives have attracted a strong interest in medicinal chemistry. The triazole nucleus is one of the most important heterocycles which has a feature of natural products as well as medicinal agents. Heterocyclic nitrogen is abundantly present in most medicinal compounds. The derivatization of triazole ring is based on the phenomenon of bio-isosteres in which substituted the oxygen atom of oxadiazole nucleus with nitrogen triazole analogue. Main text This review focuses on recent synthetic procedure of triazole moiety, which comprises of various pharmacological activities such as antimicrobial, anticonvulsant, anti-inflammatory, analgesic, antitubercular, anthelmintic, antioxidant, antimalarial, antiviral, etc.. Conclusion This review highlights the current status of triazole compounds as different multi-target ph...

Triazoles: A valuable insight into recent developments and biological activities

Chinese Journal of Natural Medicines, 2013

In recent years, heterocyclic compounds, analogs, and derivatives have attracted strong interest due to their useful biological and pharmacological properties. The small and simple triazole nucleus is present in compounds aimed at evaluating new entities that possess anti-microbial, anti-tumor, antitubercular, anti-convulsant, anti-depressant, antimalarial, and anti-inflammatory activities. Triazoles display a broad range of biological activities and are found in many potent, biologically active compounds, such as trazodone (antidepressant drug), rizatriptan (antimigrane drug), hexaconazole (antifungal drug) and alprazolam (hyptonic, sedative and tranquilizer drug). So far, modifications of the triazole ring have proven highly effective with improved potency and lesser toxicity. The present review highlights the recently synthesized triazoles possessing important biological activities.

SYNTHESIS, REACTIVITY AND BIOLOGICAL EVALUATION OF TRIAZOLE: RECENT Review Article DEVELOPMENTS

International Journal of Pharmacy and Pharmaceutical Sciences, 2015

This review summarizes the synthetic methods, reactions and biological applications of pharmacological important 1, 2, 4-triazole isomer and recent developments in their derivatives such as Mannich base, Schiff's base, chalcone, mercapto/thione-substituted derivatives etc. over the last years. Most reactions type have been successfully applied and used in the production of biological active compounds.