Politi, Flavio Augusto Sanches; Bueno, Renata Vieira; Zeoly, Lucas Andre; Fantatto, Rafaela Regina; Eloy, Josimar de Oliveira; Chorilli, Marlus; Coelho, Fernando; Guido, Rafael Victorio Carvalho; Chagas, Ana Carolina de Souza; Furlan, Maysa published the artcile< Anthelmintic activity of a nanoformulation based on thiophenes identified in Tagetes patula L. (Asteraceae) against the small ruminant nematode Haemonchus contortus>, Product Details of C8H5BrS2, the main research area is Tagetes patula Haemonchus contortus nematode anthelmintic activity nanoformulation thiophene; Docking; French marigold; Gastrointestinal nematode; UNC-49 receptor; in vitro; in vivo.
The synthesis of thiophenic compounds, previously identified in Tagetes patula, revealed that 4-(5′-(hydroxymethyl)-[2,2′-bithiophene]-5-yl)but-3-yn-1-ol, or simply Thio1, has a pronounced in vitro anthelmintic effect against Haemonchus contortus, showing 100% efficacy in the egg hatch and larval development tests presenting EC50 = 0.1731 mg.mL-1 and EC50 = 0.3243 mg.mL-1, resp. So, this compound was selected to preparation of a nanostructured formulation to be orally administered to Santa Ines sheep. In general, from the fecal egg count reduction test (FECRT), it was observed that the product kept the parasitic load in the digestive tract of the hosts stable, with eggs per g of faeces (EPG) counts having a mean value < 3,000 (EPGmean = 2167.1, efficacy = 36,45%), thus protecting the animals from health risks caused by a massive nematode infestation. To better understand the mode of action of this thiophene derivative, in silico mol. modeling studies were carried out with the glutamate-activated chloride channel (GluCl), a well-known mol. target of anthelmintic compounds Based on the affinity score (GlideScore = -5.7 kcal.mol-1) and the proposed binding mode, Thio1 could be classified as a potential GluCl ligand, justifying the promising results observed in the anthelmintic assays. Acta Tropica published new progress about Anthelmintics. 3480-11-3 belongs to class bromides-buliding-blocks, and the molecular formula is C8H5BrS2, Product Details of C8H5BrS2.
Referemce:
Bromide – Wikipedia,
bromide – Wiktionary