Kong, Haiyan; Meng, Xianshe; Hou, Rui; Yang, Xiaoxiao; Han, Jihong; Xie, Zhouling; Duan, Yajun; Liao, Chenzhong published the artcile< Novel 1-(prop-2-yn-1-ylamino)-2,3-dihydro-1H-indene-4-thiol derivatives as potent selective human monoamine oxidase B inhibitors: Design, SAR development, and biological evaluation>, Formula: C8H8BrCl, the main research area is propynylamino dihydro indene thiol preparation hMAO B inhibitor; antiParkinson agent structure activity relationship; Fragment-based drug design; HMAO-B; Isoform selectivity; Structure activity relationship.
Successes have been achieved in developing human monoamine oxidase B (hMAO-B) inhibitors as anti-Parkinson’s disease (PD) drugs. However, low efficiency and unwanted side effects of the marketed hMAO-B inhibitors hamper their medical applications, therefore, novel potent selective hMAO-B inhibitors are still of great interest. Herein we report 1-(prop-2-yn-1-ylamino)-2,3-dihydro-1H-indene-4-thiol derivatives as hMAO-B inhibitors, which were designed by employing a fragment-based drug design strategy to link rasagiline to hydrophobic fragments. Among the synthesized 31 compounds, I and II demonstrated very encouraging hMAO-B inhibitory activities and selectivity over hMAO-A, better than rasagiline and safinamide. In vitro studies indicated that K8 and K24 are nontoxic to nervous tissue cells and they have considerable effects against ROS formation and potential neuroprotective activity. Further mice behavioral tests demonstrated these two compounds have good therapeutic effects on MPTP-induced PD model mice. All these experiment results suggest that compounds K8 and K24 can be promising candidates for further research for treatment of PD.
Bioorganic & Medicinal Chemistry Letters published new progress about Antiparkinsonian agents. 16799-05-6 belongs to class chlorides-buliding-blocks, and the molecular formula is C8H8BrCl, Formula: C8H8BrCl.
Referemce:
Chloride – Wikipedia,
Chlorides – an overview | ScienceDirect Topics