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
β¦ LIBER β¦
Design of potent substrate-analogue inhibitors of canine renin
β Scribed by HUI, K.Y. ;SIRAGY, H.M. ;HABER, E.
- Book ID
- 115099398
- Publisher
- Wiley (Blackwell Publishing)
- Year
- 2009
- Tongue
- English
- Weight
- 805 KB
- Volume
- 40
- Category
- Article
- ISSN
- 0367-8377
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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