2, 3-Triazoles: scaffold with medicinal significance (original) (raw)

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

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.

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: Synthetic Strategies and Pharmacological Profiles

International Journal of Pharmacy and Pharmaceutical Sciences

Multicomponent, solid-phase, microwave and grinding methods are the constructive modes in the sustainable synthesis of 1, 2, 4-triazoles and such reactions have attracted enormous interest in recent years. The alternative reaction conditions getting popularity in the recent ecofriendly-economical time have been thoroughly investigated. Literature studies on 1, 2, 4-triazoles have shown that these derivatives possess broad spectrum of biological activities. This review focuses on synthetic strategies and pharmacological properties of 1, 2, 4-triazoles.

2,4-TRIAZOLES: SYNTHETIC STRATEGIES AND PHARMACOLOGICAL PROFILES Review Article

International journal of Pharmacy and Pharmaceutical Sciences, 2014

Multicomponent, solid-phase, microwave and grinding methods are the constructive modes in the sustainable synthesis of 1, 2, 4-triazoles and such reactions have attracted enormous interest in recent years. The alternative reaction conditions getting popularity in the recent ecofriendlyeconomical time have been thoroughly investigated. Literature studies on 1, 2, 4-triazoles have shown that these derivatives possess broad spectrum of biological activities. This review focuses on synthetic strategies and pharmacological properties of 1, 2, 4-triazoles.

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.

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...

Recent advances in the chemistry of 1,2,4-triazoles: Synthesis, reactivity and biological activities

Tetrahedron Letters, 2021

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Recent advances in the synthesis of triazole derivatives

Afinidad, 2015

Triazole ring system has attracted a continuously growing interest of synthetic organic chemists and those dealing with the medicinal compounds due to its versatile potential to interact with biological systems. The triazole compounds possess a wide range of biological activities and are especially focused for antifungal behavior. In this review article, we have summarized the recent developments in the synthetic methodologies of this ring system. The main focus was on the methodologies which deal with the facile and convenient synthesis.