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; Jabbar, Abdul; Wells, Timothy N. C.; Palmer, Michael J.; Gasser, Robin B.; Baell, Jonathan B. published the artcile< Optimization of Novel 1-Methyl-1H-Pyrazole-5-carboxamides Leads to High Potency Larval Development Inhibitors of the Barber's Pole Worm>, HPLC of Formula: 887266-99-1, the main research area is methylpyrazolecarboxamide larva development inhibitor Barber pole worm.
A phenotypic screen of a diverse library of small mols. for inhibition of the development of larvae of the parasitic nematode Haemonchus contortus led to the identification of a 1-methyl-1H-pyrazole-5-carboxamide derivative with an IC50 of 0.29 μM. Medicinal chem. optimization targeted modifications on the left-hand side (LHS), middle section, and right-hand side (RHS) of the scaffold to elucidate the structure-activity relation (SAR). Strong SAR allowed for the iterative and directed assembly of a focus set of 64 analogs, from which compound 60 was identified as the most potent compound, inhibiting the development of the fourth larval (L4) stage with an IC50 of 0.01 μM. In contrast, only 18% inhibition of the mammary epithelial cell line MCF10A viability was observed, even at concentrations as high as 50 μM.
Journal of Medicinal Chemistry published new progress about Haemonchus contortus. 887266-99-1 belongs to class iodides-buliding-blocks, and the molecular formula is C7H3FIN, HPLC of Formula: 887266-99-1.
Referemce:
Iodide – Wikipedia,
Iodide – an overview | ScienceDirect Topics – ScienceDirect.com