Benbow, John W. published the artcilePiperidinyl-2-phenethylamino inhibitors of DPP-IV for the treatment of Type 2 diabetes, SDS of cas: 243139-71-1, the publication is Bioorganic & Medicinal Chemistry Letters (2009), 19(8), 2220-2223, database is CAplus and MEDLINE.
A highly ligand efficient lead mol. was rapidly developed into a DPP-IV selective candidate series using focused small library synthesis. A significant hurdle for series advancement was genetic safety since some agents in this series impaired chromosome division that was detected using the in vitro micronucleus assay. A recently developed high-throughput imaging-based in vitro micronucleus assay enabled the identification of chem. space with a low probability of micronucleus activity. Advanced profiling of a subset within this space identified a compound with a clean safety profile, an acceptable human DPP-IV inhibition profile based on the rat PK/PD model and a projected human dose that was suitable for clin. development.
Bioorganic & Medicinal Chemistry Letters published new progress about 243139-71-1. 243139-71-1 belongs to chlorides-buliding-blocks, auxiliary class Fluoride,Chloride,Benzyl chloride,Benzene, name is 2,4,5-Trifluorobenzyl chloride, and the molecular formula is C7H4ClF3, SDS of cas: 243139-71-1.
Referemce:
https://en.wikipedia.org/wiki/Chloride,
Chlorides – an overview | ScienceDirect Topics