BMS-299897 / BMS - LARVOL DELTA

Switchable Deep Eutectic Solvents for Sustainable Sulfonamide Synthesis. (PubMed, Chemistry) - "In ChCl/glycerol (1:2 mol mol-1) and ChCl/urea (1:2 mol mol-1), these reactions yield up to 97% under aerobic conditions at ambient temperature within 2-12 h. The practicality of the method is exemplified by the sustainable synthesis of an FFA4 agonist and a key building block en route to anti-Alzheimer drug BMS-299897. A subtle interplay of electronic effects and the solubility characteristics of the starting materials in the aforementioned DESs seem to be responsible for driving the reaction successfully over the hydrolysis of sulfonyl chlorides. The procedure's eco-friendliness is validated  by quantitative metrics like the E-factor and the EcoScale, with products isolated by extraction or filtration after decantation."

Journal • Alzheimer's Disease • CNS Disorders

Gamma secretase activity modulates BMP-7-induced dendritic growth in primary rat sympathetic neurons. (PubMed, Auton Neurosci) - "BMP-7-induced dendritic growth was inhibited by siRNA knockdown of PSEN1 and by three γ-secretase inhibitors, γ-secretase inhibitor IX (DAPT), LY-411575 and BMS-299897. In summary, our results indicate that γ-secretase activity enhances BMP-7 induced dendritic growth in sympathetic neurons. These findings provide insight into the normal cellular role of the γ-secretase complex in sympathetic neurons."

Journal • Preclinical • Alzheimer's Disease • CNS Disorders • APH1A