Potential anti-amoebic effects of synthetic 1,4-benzothiazine derivatives against Acanthamoeba castellanii

• Published in: Heliyon 2024-01, Vol.10 (1), p.e23258-e23258, Article e23258
• Main Authors: Alishba, Ahmed, Usman, Taha, Muhammad, Khan, Naveed Ahmed, Salar, Uzma, Khan, Khalid Mohammed, Anwar, Ayaz, Siddiqui, Ruqaiyyah
• Format: Article
• Language: English
• Subjects: Acanthamoeba; Amoebicidal; Benzothiazine; One-pot synthesis
• ISSN: 2405-8440; 2405-8440
• DOI: 10.1016/j.heliyon.2023.e23258

A rare but lethal central nervous system disease known as granulomatous amoebic encephalitis (GAE) and potentially blinding Acanthamoeba keratitis are diseases caused by free-living Acanthamoeba. Currently, no therapeutic agent can completely eradicate or prevent GAE. Synthetic compounds are a likely source of bioactive compounds for developing new drugs. This study synthesized seventeen 1,4-benzothiazine derivatives (I –XVII) by a base-catalyzed one-pot reaction of 2-amino thiophenol with substituted bromo acetophenones. Different spectroscopic techniques, such as EI-MS, 1H-, and 13C NMR (only for the new compounds), were used for the structural characterization and conformation of compounds. These compounds were assessed for the first time against Acanthamoeba castellanii. All compounds showed anti-amoebic potential in vitro against A. castellanii, reducing its ability to encyst and excyst at 100 μM. Compounds IX, X, and XVI showed the most potent activities among all derivatives and significantly reduced the viability to 5.3 × 104 (p