Potential inhibitors of human carbonic anhydrase isozymes I and II: Design, synthesis and docking studies of new 1,3,4-thiadiazole derivatives.

In the last years, inhibition of carbonic anhydrase (CA) has emerged as a promising approach for pharmacologic intervention in a variety of disorders such as glaucoma, epilepsy, obesity, and cancer. As a consequence, the design of CA inhibitors (CAIs) is a highly dynamic field of medicinal chemistry. Due to the therapeutic potential of thiadiazoles as CAIs, new 1,3,4-thiadiazole derivatives were synthesized and investigated for their inhibitory effects on hCA I and hCA II. Although the tested compounds did not carry a sulfonamide group, an important pharmacophore for CA inhibitory activity, it was a remarkable finding that most of them were more effective on hCAs than acetazolamide (AAZ), the reference agent. Among these compounds, N'-((5-(4-chlorophenyl)furan-2-yl)methylene)-2-((5-(phenylamino)-1,3,4-thiadiazol-2-yl)thio)acetohydrazide (3) was found to be the most effective compound on hCA I with an IC50 value of 0.14nM, whereas N'-((5-(2-chlorophenyl)furan-2-yl)methylene)-2-((5-(phenylamino)-1,3,4-thiadiazol-2-yl)thio)acetohydrazide (1) was found to be the most potent compound on hCA II with an IC50 value of 0.15nM. According to molecular docking studies, all compounds exhibited high affinity and good amino acid interactions similar to AAZ on the both active sites of hCA I and hCA II enzymes.

Green synthesis of Ce2O3 NPs and determination of its antioxidant activity.

In this study, the authors presented synthesis of ceria nanoparticles (NPs) by the bio-reduction method and their antioxidative activity. Aqueous extract of Euphorbia (Euphorbia amygdaloides) was used as reducing and stabilising agents. They used aqueous extract of Euphorbia (E. amygdaloides) as reducing and stabilising agent. Ultraviolet-visible (UV-vis) absorption spectroscopy was used to monitor the quantitative formation of ceria NPs. They also addressed the characteristics of the obtained ceria NPs using scanning electron microscopy (SEM), X-ray diffraction (XRD) and transmitting electron microscope (TEM). The synthesised cerium (III) oxide (Ce2O3) NPs were initially noted through visual colour change from colourless pale yellow cerium (III) to light yellow cerium (IV) and further confirmed the band at 345 nm employing UV-vis spectroscopy. The average diameter of the prepared NPs was about 8.6-10.5 nm. In addition, the synthesised Ce2O3 NPs were tested for antioxidant and anti-bacterial activities using ferric reducing antioxidant power, cupric reducing antioxidant capacity, ferrous ions chelating activity, superoxide the anion radical scavenging and 2, 2'-azinobis 3-ethylbenzothiazol to-6-sulphonic acid scavenging activity. It could be concluded that Euphorbia (E. amygdaloides) extract can be used efficiently in the production of potential antioxidant and anti-bacterial Ce2O3 NPs for commercial applications.