608531-87-9Relevant academic research and scientific papers
Arylpiperazines for management of benign prostatic hyperplasia: Design, synthesis, quantitative structure-activity relationships, and pharmacokinetic studies
Sarswat, Amit,Kumar, Rajeev,Kumar, Lalit,Lal, Nand,Sharma, Smriti,Prabhakar, Yenamandra S.,Pandey, Shailendra K.,Lal, Jawahar,Verma, Vikas,Jain, Ashish,Maikhuri, Jagdamba P.,Dalela, Diwakar,Kirti,Gupta, Gopal,Sharma, Vishnu L.
experimental part, p. 302 - 311 (2011/03/20)
A series of 27 aryl/heteroaryl/aralkyl/aroyl piperazines were synthesized, and most of these compounds reduced prostate weight of mature rats by 15-47%. Three compounds, 10, 12, and 18, had better activity profile (reduced prostate weight by 47%, 43%, and 39%, respectively) than the standard drug flutamide (24% reduction). QSAR suggested structures with more cyclic and branched moieties, increased topological separation of O and N therein, and reduced solvation connectivity index for better activity. Pharmacokinetic study with compound 10 at an oral dose of 10.0 mg/kg indicated good absorption, negligible extrahepatic elimination, and rapid distribution to the target organ (prostate) but restricted entry through the blood-brain barrier. A 10-fold decrease in PSA and 15-fold increase in ER-β gene expressions of human prostate cancer cells (LNCaP) by compound 10 in vitro indicated AR and ER-β mediated actions. The findings may stimulate further explorations of identified lead for the management of benign prostatic hyperplasia.
Synthesis and biological evaluation of piperazine-based derivatives as inhibitors of plasminogen activator inhibitor-1 (PAI-1)
Ye, Bin,Chou, Yuo-Ling,Karanjawala, Rushad,Lee, Wheeseong,Lu, Shou-Fu,Shaw, Kenneth J.,Jones, Steven,Lentz, Dao,Liang, Amy,Tseng, Jih-Lie,Wu, Qingyu,Zhao, Zuchun
, p. 761 - 765 (2007/10/03)
Compound 2 was identified by high throughput screening as a novel PAI-1 inhibitor. Systematic optimization of the A, B, and C segments of 2 resulted in the identification of a more potent compound 39 with good oral bioavailability. The synthesis and SAR d
