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
The design and synthesis of cyclic renin inhibitors
β Scribed by Steven J. Wittenberger; William R. Baker; B.Gregory Donner; Charles W. Hutchins
- Book ID
- 103399075
- Publisher
- Elsevier Science
- Year
- 1991
- Tongue
- French
- Weight
- 240 KB
- Volume
- 32
- Category
- Article
- ISSN
- 0040-4039
No coin nor oath required. For personal study only.
π SIMILAR VOLUMES
## 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
## Abstract In the search for a radioactive form of the peptidomimetic renin inhibitor, ditekiren, with a metabolically suitable radiolabel for conducting drug disposition studies, we prepared [^3^H]ditekiren with tritium labels in the Nβmethylβhistidine moiety and in the leuβval alcohol transition
In 1962 "azapeptides" were described for the first time'). In these peptide analogs the a-CH group of one or more amino acid residues of a peptide chain is replaced with nitrogen.