Identification of a 5-HT4 receptor antagonist clinical candidate through side-chain modification was written by Clark, Robin D.;Jahangir, Alam;Alam, Muzaffar;Rocha, Cynthia;Lin, Lin;Bjorner, Bodil;Nguyen, Khanh;Grady, Carole;Williams, Timothy J.;Stepan, George;Tang, Hai Ming;Ford, Anthony P. D. W.. And the article was included in Bioorganic & Medicinal Chemistry Letters in 2005.Quality Control of 1-Propylpiperazine This article mentions the following:
Replacement of the N-Bu side-chain of lead 5-HT4 receptor antagonist 2 with propanesulfonylpiperidinyl, morpholinyl, and piperazinyl groups led to higher affinity analogs 4-6. In vitro drug metabolism screens and cassette pharmacokinetic studies in the dog led to identification of the N-methylpiperazinyl analog (I), which displayed pharmacokinetic, selectivity, and safety parameters sufficient for advancement to the clinic for the treatment of urinary incontinence. In the experiment, the researchers used many compounds, for example, 1-Propylpiperazine (cas: 21867-64-1Quality Control of 1-Propylpiperazine).
1-Propylpiperazine (cas: 21867-64-1) belongs to piperazine derivatives. Piperazine causes primary dermal irritation and skin burns at high concentrations. Piperazine also causes eye irritation in humans. Piperazine is an anthelminthic especially useful in the treatment of partial intestinal obstruction caused by Ascaris worms, which is a condition primarily seen in children. Piperazine hydrate and piperazine citrate are the main anthelminthic piperazines.Quality Control of 1-Propylpiperazine
Referemce:
Piperazine – Wikipedia,
Piperazines – an overview | ScienceDirect Topics