Novel and High Affinity 2-[(Diphenylmethyl)sulfinyl]acetamide (Modafinil) Analogues as Atypical Dopamine Transporter Inhibitors was written by Cao, Jianjing;Slack, Rachel D.;Bakare, Oluyomi M.;Burzynski, Caitlin;Rais, Rana;Slusher, Barbara S.;Kopajtic, Theresa;Bonifazi, Alessandro;Ellenberger, Michael P.;Yano, Hideaki;He, Yi;Bi, Guo-Hua;Xi, Zheng-Xiong;Loland, Claus J.;Newman, Amy Hauck. And the article was included in Journal of Medicinal Chemistry in 2016.Safety of 1-Propylpiperazine This article mentions the following:
The development of pharmacotherapeutic treatments of psychostimulant abuse has remained a challenge, despite significant efforts made toward relevant mechanistic targets, such as the dopamine transporter (DAT). The atypical DAT inhibitors have received attention due to their promising pharmacol. profiles in animal models of cocaine and methamphetamine abuse. Herein the authors report a series of modafinil analogs that have an atypical DAT inhibitor profile. The authors extended SAR by chem. manipulating the oxidation states of the sulfoxide and the amide functional groups, halogenating the Ph rings, and/or functionalizing the terminal nitrogen with substituted piperazines, resulting in several novel leads such as 1-(4-(2-((bis(4-fluorophenyl)methyl)sulfinyl)ethyl)piperazin-1-yl)-3-phenylpropan-2-ol (compound 11b), which demonstrated high DAT affinity (Ki = 2.5 nM) and selectivity without producing concomitant locomotor stimulation in mice, as compared to cocaine. These results are consistent with an atypical DAT inhibitor profile and suggest that 11b may be a potential lead for development as a psychostimulant abuse medication. In the experiment, the researchers used many compounds, for example, 1-Propylpiperazine (cas: 21867-64-1Safety of 1-Propylpiperazine).
1-Propylpiperazine (cas: 21867-64-1) belongs to piperazine derivatives. Industrial applications of piperazine include the manufacture of plastics, resins, pesticides and brake fluids. Although many piperazine derivatives occur naturally, piperazine itself can be synthesized by reacting alcoholic ammonia with 1,2-dichloroethane, by the action of sodium and ethylene glycol on ethylene diamine hydrochloride, or by reduction of pyrazine with sodium in ethanol.Safety of 1-Propylpiperazine
Referemce:
Piperazine – Wikipedia,
Piperazines – an overview | ScienceDirect Topics