Kalaba, Predrag published the artcileHeterocyclic Analogues of Modafinil as Novel, Atypical Dopamine Transporter Inhibitors, Quality Control of 75341-23-0, the publication is Journal of Medicinal Chemistry (2017), 60(22), 9330-9348, database is CAplus and MEDLINE.
Modafinil is a wake promoting compound with high potential for cognitive enhancement. It is targeting the dopamine transporter (DAT) with moderate selectivity, thereby leading to reuptake inhibition and increased dopamine levels in the synaptic cleft. A series of modafinil analogs have been reported so far, but more target-specific analogs remain to be discovered. It was the aim of this study to synthesize and characterize such analogs and, indeed, a series of compounds were showing higher activities on the DAT and a higher selectivity toward DAT vs. serotonin and norepinephrine transporters than modafinil. This was achieved by substituting the amide moiety by five- and six-membered aromatic heterocycles. In vitro studies indicated binding to the cocaine pocket on DAT, although mol. dynamics revealed binding different from that of cocaine. Moreover, no release of dopamine was observed, ruling out amphetamine-like effects. The absence of neurotoxicity of a representative analog may encourage further preclin. studies of the above-mentioned compounds
Journal of Medicinal Chemistry published new progress about 75341-23-0. 75341-23-0 belongs to chlorides-buliding-blocks, auxiliary class Thiadiazole,Chloride, name is 2-(Chloromethyl)-5-methyl-1,3,4-thiadiazole, and the molecular formula is C4H5ClN2S, Quality Control of 75341-23-0.
Referemce:
https://en.wikipedia.org/wiki/Chloride,
Chlorides – an overview | ScienceDirect Topics