Two types of P1-P3-linked macrocyclic renin inhibitors containing the hydroxyethylene isostere (HE) scaffold just outside the macrocyclic ring have been synthesized. An aromatic or aliphatic substituent (P3sp) was introduced in the macrocyclic ring aiming at the S3 subpocket (S3sp) in order to optim
Design and synthesis of potent, isoxazole-containing renin inhibitors
✍ Scribed by Pierre-André Fournier; Mélissa Arbour; Elizabeth Cauchon; Austin Chen; Amandine Chefson; Yves Ducharme; Jean-Pierre Falgueyret; Sébastien Gagné; Erich Grimm; Yongxin Han; Robert Houle; Patrick Lacombe; Jean-François Lévesque; Dwight MacDonald; Bruce Mackay; Dan McKay; M. David Percival; Yeeman Ramtohul; René St-Jacques; Sylvie Toulmond
- Book ID
- 113496776
- Publisher
- Elsevier Science
- Year
- 2012
- Tongue
- English
- Weight
- 460 KB
- Volume
- 22
- Category
- Article
- ISSN
- 0960-894X
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## An eflcient synthesis of a novel class of potent macrocyclic renin inhibitors exemplified by compounds 1 and 2, which involves the macrocvclization of 8 to 9 as the key step, is described. The macrocyclic design of renin inhibitors 1 and2 disclosed here incorporates (2R,3S)-3-a&o-&yclohe~l-2-hydr