An efficient synthesis in 10 steps and overall yields up to 27% of NEtXaa(4
)-cyclosporin A derivatives (Xaa = Leu, Val, Ile, Thr) starting from cyclos
porin A is described. Biological activities of the new analogues show promi
sing results for the design of cyclosporin derivatives exhibiting non-immun
osuppressive and anti-HIV activity. (C) 2000 Elsevier Science Ltd. All righ
ts reserved.