Johnson, Mark published the artcileStructure-Activity Relationship Study of N6-(2-(4-(1H-Indol-5-yl)piperazin-1-yl)ethyl)-N6-propyl-4,5,6,7-tetrahydrobenzo[d]thiazole-2,6-diamine Analogues: Development of Highly Selective D3 Dopamine Receptor Agonists along with a Highly Potent D2/D3 Agonist and Their Pharmacological Characterization, SDS of cas: 945953-41-3, the publication is Journal of Medicinal Chemistry (2012), 55(12), 5826-5840, database is CAplus and MEDLINE.
In our effort to develop multifunctional drugs against Parkinson’s disease, a structure-activity-relationship study was carried out based on our hybrid mol. template targeting D2/D3 receptors. Competitive binding with [3H]spiroperidol was used to evaluate affinity (Ki) of test compounds Functional activity of selected compounds in stimulating [35S]GTPγS binding was assessed in CHO cells expressing either human D2 or D3 receptors. Our results demonstrated development of highly selective compounds for D3 receptor (for (-)-40 (I) Ki, D3 = 1.84 nM, D2/D3 = 583.2; for (-)-45Ki, D3 = 1.09 nM, D2/D3 = 827.5). Functional data identified (-)-40 (EC50, D2 = 114 nM, D3 = 0.26 nM, D2/D3 = 438) as one of the highest D3 selective agonists known to date. In addition, high affinity, nonselective D3 agonist (-)-19 (EC50, D2 = 2.96 nM and D3 = 1.26 nM) was also developed. Lead compounds with antioxidant activity were evaluated using an in vivo PD animal model.
Journal of Medicinal Chemistry published new progress about 945953-41-3. 945953-41-3 belongs to piperazines, auxiliary class Piperazine,Amide,Aldehyde, name is tert-Butyl 4-(2-oxoethyl)piperazine-1-carboxylate, and the molecular formula is C11H20N2O3, SDS of cas: 945953-41-3.
Referemce:
https://en.wikipedia.org/wiki/Piperazine,
Piperazines – an overview | ScienceDirect Topics