Structure-activity relationship studies of tolfenpyrad reveal subnanomolar inhibitors of Haemonchus contortus development was written by Le, Thuy G.;Kundu, Abhijit;Ghoshal, Atanu;Nguyen, Nghi H.;Preston, Sarah;Jiao, Yaqing;Ruan, Banfeng;Xue, Lian;Huang, Fei;Keiser, Jennifer;Hofmann, Andreas;Chang, Bill C. H.;Garcia-Bustos, Jose;Wells, Timothy N. C.;Palmer, Michael J.;Jabbar, Abdul;Gasser, Robin B.;Baell, Jonathan B.. And the article was included in Journal of Medicinal Chemistry in 2019.Quality Control of 5-Methoxybenzo[d]oxazole This article mentions the following:
Recently, we have discovered that the registered pesticide, tolfenpyrad, unexpectedly and potently inhibits the development of the L4 larval stage of the parasitic nematode Haemonchus contortus with an IC50 value of 0.03 μM while displaying good selectivity, with an IC50 of 37.9 μM for cytotoxicity. As a promising mol. template for medicinal chem. optimization, we undertook anthelmintic structure-activity relationships for this chem. Modifications of the left-hand side (LHS), right-hand side (RHS), and middle section of the scaffold were explored to produce a set of 57 analogs. Analogs I, II, and III were shown to be the most potent compounds of the series, with IC50 values at a subnanomolar level of potency against the chemotherapeutically relevant fourth larval (L4) stage of H. contortus. Selected compounds from the series also showed promising activity against a panel of other different parasitic nematodes, such as hookworms and whipworms. In the experiment, the researchers used many compounds, for example, 5-Methoxybenzo[d]oxazole (cas: 132227-03-3Quality Control of 5-Methoxybenzo[d]oxazole).
5-Methoxybenzo[d]oxazole (cas: 132227-03-3) belongs to benzoxazole derivatives. Being a heterocyclic compound, benzoxazole finds use in research as a starting material for the synthesis of larger, usually bioactive structures. Due to its versatile biological properties, benzoxazole has been incorporated as an essential pharmacophore and substructure in many medicinal compounds.Quality Control of 5-Methoxybenzo[d]oxazole
Referemce:
Benzoxazole – Wikipedia,
Benzoxazole | C7H5NO – PubChem