Robichaud, Joeel; Bayly, Christopher I.; Black, W. Cameron; Desmarais, Sylvie; Leger, Serge; Masse, Frederic; McKay, Daniel J.; Oballa, Renata M.; Paquet, Julie; Percival, M. David; Truchon, Jean-Francois; Wesolowski, Gregg; Crane, Sheldon N. published the artcile< β-Substituted cyclohexanecarboxamide cathepsin K inhibitors: Modification of the 1,2-disubstituted aromatic core>, Safety of (9Z,12Z)-Methyl octadeca-9,12-dienoate, the main research area is cyclohexanecarboxamide preparation cathepsin K inhibitor SAR.
Further SAR study around the central 1,2-disubstituted Ph of the previously disclosed Cat K inhibitor (-)-1 (I) has demonstrated that the solvent exposed P2-P3 linker can be replaced by various 5- or 6-membered heteroaromatic rings. While some potency loss was observed in the 6-membered heteroaromatic series (IC50 = 1 nM for pyridine-linked 4 vs 0.5 nM for phenyl-linked (±)-1), several inhibitors showed a significantly decreased shift in the bone resorption functional assay (10-fold for pyridine 4 vs 53-fold for (-)-1). Though this shift was not reduced in the 5-membered heteroaromatic series, potency against Cat K was significantly improved for thiazole 9 (IC50 = 0.2 nM) as was the pharmacokinetic profile of N-Me pyrazole 10 over our lead compound (-)-1.
Bioorganic & Medicinal Chemistry Letters published new progress about Bone resorption. 112-63-0 belongs to class esters-buliding-blocks, and the molecular formula is C19H34O2, Safety of (9Z,12Z)-Methyl octadeca-9,12-dienoate.
Referemce:
Ester – Wikipedia,
Ester – an overview | ScienceDirect Topics