TiO2 nanoparticle as catalyst for an efficient green one-pot synthesis of 1H-3-Indolyl Derivatives as significant antiviral activity

• Published in: Bioorganic chemistry 2022-07, Vol.124, p.105805-105805, Article 105805
• Main Authors: Elsayed, Doaa A., Assy, Mohamed G., Mousa, Sahar M., El-Bassyouni, Gehan T., Mouneir, Samar M., Shehab, Wesam S.
• Format: Article
• Language: English
• Subjects: Antiviral; HAV; Nanoparticles; Vero cell
• ISSN: 0045-2068; 1090-2120
• DOI: 10.1016/j.bioorg.2022.105805

[Display omitted] •Novel the existence of TiO2 nanoparticle yields 2-amino-6-(1H-indol-3-yl)-4-(thiophen-2-yl)-4H-pyran-3-carbonitrile derivatives.•A cost-effective, and eco-friendly protocol has been developed for creating the 1H-3-Indolyl Derivatives by a one-pot three-component condensation.•The newly synthesized chemicals were tested on Vero cell which was extracted from kidney tissues.•Compound 5 was the best one which had antiviral activity against HAV. Titanium dioxide nanoparticles (TiO2- NPs) are produced in large quantities for an extensive range of applications. They retain variable physicochemical properties, which influence their bioactivity. The condensation synthesis of 3-acetylindol, thiophene-2-carbaldehyde and malononitrile in the existence of TiO2 nanoparticle yields 2-amino-6-(1H-indol-3-yl)-4-(thiophen-2-yl)-4H-pyran-3-carbonitrile derivatives. The yielded compound 2 reacted with (formic acid, formamide, ethyl chloroacetate, chloroacetyl chloride, thiourea and sodium nitrite). This three-combination system is safe, ecologically friendly, and non-toxic. The proposed system helped in time preservation and reduction in chemical consumption. The synthesized compounds were screened for antiviral activity against Vero cells (HAV). Antiviral impact percent for samples 2, 5, 6 and 7 versus HAV were 81.98, 91.05, 9.21, and 21.95%, respectively. The viral efficacy of Sample 5 was the strongest against HAV.