A Novel Method for the Syntheses of Imidazo-Thiadiazoles as Potential Antioxidants and Anti-Inflammatory Agents

Abstract

Background: Nowadays, the researchers have focused their interest on the developmentof the novelanti-inflammatory and antioxidant agents. Literature survey reveals that many imidazo-thiadiazole molecules were used as key intermediates for development of novel drugs. The synthesized imidazo-thiadiazole derivatives were tested for in vitro antioxidant and anti-inflammatory study. The present research paper will give an idea to readers about diseases caused due to free radicals. Objective: To develop novel antioxidant and anti-inflammatory drugs Methods:: Imidazo-thiadiazole derivatives 5a-fweresynthesized by cyclo-condensation reactions in two steps. First, the synthesis of 2-amino-thiadiazole derivatives from substituted aromatic carboxylic acids and thiosemicarbazide by usingPOCl3as a solvent as well as catalyst. In next step, imidazo-thiadiazoles were prepared from 2-amino-thiadiazole derivatives with appropriate α-haloketones in presence of Polyethylene glycol-300 (PEG-300) as a green solvent. These imidazo-thiadiazole derivatives were prepared by using novel method. The synthesized compounds were in vitro tested for their antioxidant and anti-inflammatoryactivity. Results: In vitro evaluation reportshowed that nearly all molecules possess potential antioxidant activity against 2,2-Diphenyl-1-picrylhydrazyl (DPPH), Nitric oxide (NO), Superoxide radical (SOR) and Hydrogen Peroxide (H2O2)radical scavenging activity. Most of imidazo-thiadiazole derivatives have shown significant anti-inflammatory activity as compared withdiclofenac sodium asa reference standard. Conclusion: Our efforts to develop potent anti-inflammatory and antioxidant agents having a preeminent activity in the search to find novel therapies for treating inflammation and oxidation. Imidazo-thiadiazoles 5a, 5e as well as 5f showed potential anti-inflammatory activity. All tested imidazo-thiadiazole derivatives (5a-f) were showed potential antioxidant activity against one more radical scavenging species as compared to ascorbic acid as reference standard. Thus, imidazo-thiadiazole derivatives constitute an interesting template for design and development new antioxidant as well as anti-inflammatory agents.

One-Pot N-α-C(sp3)–H Bond Functionalisation Cascade for the Synthesis of Polysubstituted Imidazoles

“…[1][2][3][4][5] Especially, five-membered nitrogen-containing imidazoles have a broad range of pharmaceutical significance and different applications. [5][6][7][8][9][10][11][12][13][14] Bioactive molecules like histidine, biotin and histamine possess a nitrogen-containing imidazole nucleus. 15,16 In addition, imidazoles have revealed different biological activities such as antibacterial, 17 antifungal, 12 antituberculosis, 18 analgesic, 19 anthelmintic, 20 anti-inflammatory 21 and antitumor activities.…”

“…The most privileged nitrogen-containing azole motif has attracted increased attention of medicinal chemists due to its diverse relevance. [1][2][3][4][5] Especially, five-membered nitrogen-containing imidazoles have a broad range of pharmaceutical significance and different applications. [5][6][7][8][9][10][11][12][13][14] Bioactive molecules like histidine, biotin and histamine possess a nitrogen-containing imidazole nucleus.…”