Conformationally restricted peptide isosteres. 2.1 Synthesis and in vitro potency of dipeptide renin inhibitors employing a 2-alkylsulfonyl-3-phenylcyclopropane carboxamide as a P3 amino acid replacement☆

Add time:09/07/2019    Source:sciencedirect.com

A series of dipeptide renin inhibitors employing a 2,3-disubstituted cyclopropane carboxamide at the P3 position of the molecule were prepared by coupling racemic(IS,2R,3R) 2-alkylsulfonyl-3-phenyl(or cyclohexyl)cyclopropanecarboxylic acid with the amino acid derivatives 11a–d. The individual diastereomers were separated and tested for in vitro potency. IC50 values ranged from 0.37 to 1.4 nM and 5.8 to 29 nm against purified, pH 6.0 and plasma, pH 7.4 human renin, respectively. In all examples, the more polar diastereomer was the most potent.

We also recommend Trading Suppliers and Manufacturers of O-(N-morpholinocarbonyl)-3-phenyllactic acid (cas 114343-31-6). Pls Click Website Link as below: cas 114343-31-6 suppliers

Prev:Anti-AIDS agents—XXVII. Synthesis and anti-HIV activity of betulinic acid and dihydrobetulinic acid derivatives☆
Next:New substrates of the multispecific bile acid transporter in liver cells: interference of some linear renin inhibiting peptides with transport protein(s) for bile acids)