Synthesis and Anti-Inflammatory Activity of New Alkyl-Substituted Phthalimide 1H-1,2,3-Triazole Derivatives

Abstract

Four new 1,2,3-triazole phthalimide derivatives with a potent anti-inflammatory activity have been synthesized in the good yields by the 1,3-dipolar cycloaddition reaction from N-(azido-alkyl)phthalimides and terminal alkynes. The anti-inflammatory activity was determined by injecting carrageenan through the plantar tissue of the right hind paw of Swiss white mice to produce inflammation. All the compounds 3a–c and 5a–c exhibited an important anti-inflammatory activity; the best activity was found for the compounds 3b and 5c, which showed to be able to decrease by 69% and 56.2% carrageenan-induced edema in mice. These compounds may also offer a future promise as a new anti-inflammatory agent.

Regioselective Synthesis, Antibacterial, Molecular Docking and Fingerprint Applications of 1‐Benzhydrylpiperazine Derivatized 1,4‐Disubstituted 1,2,3‐Triazoles

“…In search of new potent drug molecules, among the most biologically active five membered heterocycles, 1,2,3‐triazoles have attracted the interest of many medicinal chemists due to their vast biological importance in medicine and drug discovery. Many scientific reports reveals that 1,2,3‐triazole derivatives showed many biological activities including antimicrobial,, anticancer, anticonvulsant, anti‐inflammatory, analgesic and antiviral . Some of the triazoles have been used as cytotoxic and anti‐tubular agents .…”

Click chemistry inspired synthesis of piperazine-triazole derivatives and evaluation of their antimicrobial activities

“…Piperazine is also found along with azoles moieties in several antifungal drugs such as itraconazole and ketoconazole. In recent years, 1,2,3-triazoles gained the interest owing to their broad range of biological activities such as anti-HIV (Alvarez et al, 1994), anti-inflammatory (de Oliveira Assis et al, 2012), anti-malarial (Manohar et al, 2011), anti-viral (Ferreira et al, 2014), and anticancer activities (Kamal et al, 2008;Yan et al, 2010). Particularly, these aza-heterocyclic motifs were widely studied as antifungal agents due to their low toxicity and broad antifungal spectrum (Agalave et al, 2011;Jiang et al, 2011;Pore et al, 2012).…”

Synthesis and antioxidant activity of nitroaryl-1,2,3-triazoles

“…[1][2][3] The nitroaryls and nitroheterocycles are considered to be medicinally a valuable group of compounds, broadly redox properties of nitroaromatic compounds are associated to biological activities. 4 In our antioxidative screening study of nitroaryl-1,2,3-triazoles using free radical scavenging activity of DPPH and ABTS, we report here some active compounds.…”