Tsuboi S, Takeda M, Okada Y, Nagamatsu Y, Yamamoto J
Faculty of Pharmaceutical Sciences, Kobe-Gakuin University, Japan.
Chem Pharm Bull (Tokyo). 1991 Jan;39(1):184-6. doi: 10.1248/cpb.39.184.
H-Ser-Pro-Val-Thr-Leu-Asp-Leu-Arg-Tyr-OH and H-Thr-Asn-Val-Val-OH, which correspond to the sequences 41-49 and 60-63 of eglin c, respectively, were synthesized by a conventional solution approach using the newly developed 6-chloro-2-pyridyl ester method. The inhibitory activities of the above two peptides against human leukocyte elastase, cathepsin G, porcine pancreatic elastase and alpha-chymotrypsin were examined in comparison with those of the corresponding methyl esters.
采用新开发的6-氯-2-吡啶酯法,通过传统溶液法合成了分别对应于抗凝血酶c序列41 - 49和60 - 63的H-Ser-Pro-Val-Thr-Leu-Asp-Leu-Arg-Tyr-OH和H-Thr-Asn-Val-Val-OH。与相应甲酯相比,检测了上述两种肽对人白细胞弹性蛋白酶、组织蛋白酶G、猪胰弹性蛋白酶和α-胰凝乳蛋白酶的抑制活性。