87639-84-7Relevant academic research and scientific papers
Discovery of non-peptidic P2-P3 butanediamide renin inhibitors with high oral efficacy
Simoneau, Bruno,Lavallee, Pierre,Anderson, Paul C.,Bailey, Murray,Bantle, Gary,Berthiaume, Sylvie,Chabot, Catherine,Fazal, Gulrez,Halmos, Ted,Ogilvie, William W.,Poupart, Marc-Andre,Thavonekham, Bounkham,Xin, Zhili,Thibeault, Diane,Boelger, Gordon,Panzenbeck, Maret,Winquist, Raymond,Jung, Grace L.
, p. 489 - 508 (2007/10/03)
A new series of non-peptidic renin inhibitors having a 2-substituted butanediamide moiety at the P2 and P3 positions has been identified. The optimized inhibitors have IC50 values of 0.8 to 1.4nM and 2.5 to 7.6nM in plasma renin assays at pH 6.0 and 7.4, respectively. When evaluated in the normotensive cynomolgus monkey model, two of the most potent inhibitors were orally active at a dose as low as 3mg/kg. These potent renin inhibitors are characterized by oral bioavailabilities of 40 and 89% in the cynomolgus monkey. Inhibitor 3z (BILA 2157 BS) was selected as candidate for pre-development. Copyright (C) 1999 Elsevier Science Ltd.
General Method for the Synthesis of Selectively N-Alkylated Polyamines
Nordlander, J. Eric,Payne, Mark J.,Balk, Michael A.,Gress, Julia L.,Harris, Frederick D.,et al.
, p. 133 - 138 (2007/10/02)
A versatile method is presented for the synthesis of linear polyamines-in particular, the naturally ubiquitous putrescine, spermidine, and spermine-regiospecifically N-alkylated or N-polyalkylated.The new approach is based on the acylation of amines with
