Chemistry can be defined as the study of matter and the changes it undergoes. You¡¯ll sometimes hear it called the central science because it is the connection between physics and all the other sciences, starting with biology. 16153-81-4, Name is 4-(4-Methylpiperazin-1-yl)phenylamine, molecular formula is , belongs to piperazines compound. In a document, author is Kalbfleisch, Jacob J., Name: 4-(4-Methylpiperazin-1-yl)phenylamine.
Synthesis and SAR of a series of mGlu(7) NAMs based on an ethyl-8-methoxy-4-(4-phenylpiperazin-1-yl)quinoline carboxylate core
A High-Throughput Screening (HTS) campaign identified a fundamentally new mGlu(7) NAM chemotype, based on an ethyl-8-methoxy-4-(4-phenylpiperazin-1-yl)quinolone carboxylate core. The initial hit, VU0226390, was a potent mGlu(7) NAM (IC50 = 647 nM, 6% L-AP4 min) with selectivity versus the other group III mGlu receptors (> 30 mu M vs. mGlu4 and mGlu8). A multi-dimensional optimization effort surveyed all regions of this new chemotype, and found very steep SAR, reminiscent of allosteric modulators, and unexpected piperazine mimetics (whereas classical bioisosteres failed). While mGlu(7) NAM potency could be improved (IC(50)s similar to 350 nM), the necessity of the ethyl ester moiety and poor physiochemical and DMPK properties precluded optimization towards in vivo tool compounds or clinical candidates. Still, this hit-to-lead campaign afforded key medicinal chemistry insights and new opportunities.
Sometimes chemists are able to propose two or more mechanisms that are consistent with the available data. If a proposed mechanism predicts the wrong experimental rate law, however, the mechanism must be incorrect.Welcome to check out more blogs about 16153-81-4, in my other articles. Name: 4-(4-Methylpiperazin-1-yl)phenylamine.
Reference:
Piperazine – Wikipedia,
,Piperazines – an overview | ScienceDirect Topics