Nanoformulation-Based 1,2,3-Triazole Sulfonamides for Anti-Toxoplasma In Vitro Study

Abstract

Toxoplasma gondii is deemed a successful parasite worldwide with a wide range of hosts. Currently, a combination of pyrimethamine and sulfadiazine serves as the first-line treatment; however, these drugs have serious adverse effects. Therefore, it is imperative to focus on new therapies that produce the desired effect with the lowest possible dose. The designation and synthesis of sulfonamide-1,2,3-triazole hybrids (3a–c) were performed to create hybrid frameworks. The newly synthesized compounds were loaded on chitosan nanoparticles (CNPs) to form nanoformulations (3a.CNP, 3b.CNP, 3c.CNP) for further in vitro investigation as an anti-Toxoplasma treatment. The current study demonstrated that all examined compounds were active against T. gondii in vitro relative to the control drug, sulfadiazine. 3c.CNP showed the best impact against T. gondii with the lowest IC50 value of 3.64 µg/mL. Using light microscopy, it was found that Vero cells treated with the three nanoformulae showed remarkable morphological improvement, and tachyzoites were rarely seen in the treated cells. Moreover, scanning and transmission electron microscopic studies confirmed the efficacy of the prepared nanoformulae on the parasites. All of them caused parasite ultrastructural damage and altered morphology, suggesting a cytopathic effect and hence confirming their promising anti-Toxoplasma activity.

Design and synthesis of chromene-1,2,3-triazole benzene sulfonamide hybrids as potent carbonic anhydrase-IX inhibitors against prostate cancer

“…[25][26][27] Our main efforts have been mainly devoted to the research and development of novel approaches for synthesizing new heterocyclic hybrid compounds, beginning with particular biologically functionalized constituents, [28][29][30][31][32][33][34][35] and exploring the biological significance of benzene sulfonamides, which constitute an important class of organic compounds with high potency and selectivity against parasitic, bacterial, fungal, and cancer cells, [36][37][38][39] along with the broad pharmacological spectrum of the 1,2,3-triazole nucleus, [40][41][42][43] resulting in their selection as preferred frameworks for library design and the generation of tailored therapeutic agents. [44][45][46][47] Furthermore, their possession of numerous functions in the structures has resulted in a resurgence of interest in improving their synergetic effects. 48 Human carbonic anhydrase IX (hCA-IX) is a transmembrane cell surface glycoprotein that is over-expressed in tumors under hypoxic conditions, which are key factors of the tumor microenvironment.…”