The results from the synthesis of peptides by Fmoc/SPPS on a 2-CTC resin and then lactamization in solution or solid phase for the preparation of cyclopeptides are presented. Both procedures allow the synthesis of the desired compounds in good to very good yield and with high cyclization efficiency for on-resin macrocyclization. In addition, the activities of the corresponding cyclopeptides against the chloroquine-resistant K1 strain of Plasmodium falciparum were evaluated. Cyclo-Cys(Trt)-Gly-Thr(^tBu)-Gly-Cys(Trt)-Gly showed potent in vitro and selective activity against this parasite, EC₅₀ = 28 nM.

中文翻译：

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环肽的合成作为潜在的抗疟疾药物

呈现了以下结果：在2-CTC树脂上通过Fmoc / SPPS合成肽，然后在溶液或固相中内酰胺化以制备环肽。两种方法都允许以良好的收率和非常高的收率合成所需的化合物，并且对于树脂上的大环化反应具有高的环化效率。此外，评估了相应的环肽对恶性疟原虫抗氯喹K1菌株的活性。Cyclo -Cys（Trt）-Gly-Thr（^t Bu）-Gly-Cys（Trt）-Gly显示出强大的体外活性和对这种寄生虫的选择性活性，EC ₅₀ = 28 nM。