Synthesis and biological evaluation of non-polyene analogs of amphotericin B

Article abstract of DOI:10.1016/S0960-894X(97)10180-9

Synthesis of the first analog of a polyene macrolide antibiotic containing a rigid, non-polyene backbone has been accomplished. The sterol recognition surface of amphotericin B has been modified in an effort to better understand the role of the polyene backbone. Its antifungal activity is reduced significantly compared with amphotericin B.