부산대학교 도서관

Assessment of structure–activity relationships for anti-protozoan activity revealed a strategy for preparing potent anisomycin derivatives with reduced host toxicity. Thirteen anisomycin analogs were synthesized by modifying the alcohol, amine, and aromatic functional groups. Examination of anti-protozoal activity against various strains of Leishmania and cytotoxicity against leucocytes with comparison against the parent natural product demonstrated typical losses of activity with modifications of the alcohol, amine, and aromatic meta-positions. On the other hand, the para-phenol moiety of anisomycin proved an effective location for introducing substituents without significant loss of anti-protozoan potency. An entry point for differentiating activity against Leishmania versus host has been uncovered by this systematic study.
Author(s): Anh Minh Thao Nguyen (corresponding author) [1,*]; Moran Shalev-Benami [2]; Chloé Rosa-Teijeiro [3,4]; Ana Victoria Ibarra-Meneses [3,4]; Ada Yonath [2]; Anat Bashan [2]; Charles L. Jaffe [5]; Martin Olivier [...]