In 2022,Arendse, Lauren B.; Cozier, Gyles E.; Eyermann, Charles J.; Basarab, Gregory S.; Schwager, Sylva L.; Chibale, Kelly; Acharya, K. Ravi; Sturrock, Edward D. published an article in Journal of Medicinal Chemistry. The title of the article was 《Probing the Requirements for Dual Angiotensin-Converting Enzyme C-Domain Selective/Neprilysin Inhibition》.Application of 7524-52-9 The author mentioned the following in the article:
Selective inhibition of the angiotensin-converting enzyme C-domain (cACE) and neprilysin (NEP), leaving the ACE N-domain (nACE) free to degrade bradykinin and other peptides, has the potential to provide the potent antihypertensive and cardioprotective benefits observed for nonselective dual ACE/NEP inhibitors, such as omapatrilat, without the increased risk of adverse effects. We have synthesized three 1-carboxy-3-phenylpropyl dipeptide inhibitors with nanomolar potency based on the previously reported C-domain selective ACE inhibitor lisinopril-tryptophan (LisW) to probe the structural requirements for potent dual cACE/NEP inhibition. Here we report the synthesis, enzyme kinetic data, and high-resolution crystal structures of these inhibitors bound to nACE and cACE, providing valuable insight into the factors driving potency and selectivity. Overall, these results highlight the importance of the interplay between the S1′ and S2′ subsites for ACE domain selectivity, providing guidance for future chem. efforts toward the development of dual cACE/NEP inhibitors. In the part of experimental materials, we found many familiar compounds, such as H-Trp-OMe.HCl(cas: 7524-52-9Application of 7524-52-9)
H-Trp-OMe.HCl(cas:7524-52-9) is one of amino acid derivatives. Amino acid derivatives represent an important category of skin penetration promoters. These compounds possess hydrophobic chains attached to an amino acid headgroup via a biodegradable ester bond. Due to the amphiphilic nature of these derivatives, it is possible for them to enter into the SC lipid barrier and significantly disorganize skin membrane lipids.Application of 7524-52-9
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