On July 1, 2020, Amorim, Carina R.; Pavani, Thais F. A.; Lopes, Andrey F. S.; Duque, Marcelo D.; Mengarda, Ana C. A.; Silva, Marcos P.; de Moraes, Josue; Rando, Daniela G. G. published an article.Name: 4-Phenylthiazol-2-amine The title of the article was Schiff bases of 4-Phenyl-2-Aminothiazoles as hits to new antischistosomals: Synthesis, in-vitro, in-vivo and in-silico studies. And the article contained the following:
The synthesis of seventeen Schiff bases of 4-(4-Substituted phenyl)-N-(4-substituted benzylidene)thiazole-2-amines I [X = S, CH=CH; Z =H, O2N; R = H, 4-Me, 4-Et] which were tested in-vitro and in-vivo against Schistosoma mansoni adult worms. Moreover, in-silico studies to propose potential macromol. targets and to predict the oral bioavailability were also performed. The analog I [X = S; Z = O2N; R = H] exhibited the best in-vitro performance (IC50: 29.4μM, SI:6.1) associated with promising in-vivo activity, with a significant decrease in the adult life forms and oviposition. Oral bioavailability was impaired by the predicted low water solubility of I [X = S; Z = O2N; R = H] although it also exhibited good membrane permeability. The water solubility, however, was improved by decreasing the particles size. Serine/Threonine- and Tyrosine Kinases, Carbonic Anhydrase, Tyrosine Phosphatase and Arginase were predicted as potential macromol. targets through which the I [X = S; Z = O2N; R = H] was acting against the helminth. This class of compounds I exhibited an interesting initial therapeutic profile with the advantage of being chem. diverse from the PZQ and be easily synthesized from com. reagents which could lead to low-cost drugs. These aspects make this class of compounds I interesting hits to be explored against schistosomiasis. The experimental process involved the reaction of 4-Phenylthiazol-2-amine(cas: 2010-06-2).Name: 4-Phenylthiazol-2-amine
The Article related to phenyl aminothiazole diastereoselective preparation antischistosomal agent mol modeling, 4-phenyl-2-aminothiazoles, antischistosomal, schiff bases, schistosoma mansoni, target fishing and other aspects.Name: 4-Phenylthiazol-2-amine
Referemce:
Thiazole | C3H3NS – PubChem,
Thiazole | chemical compound | Britannica