344620-89-9Relevant academic research and scientific papers
8-amido-bearing pseudomycin B (PSB) analogue: Novel antifungal agents
Zhang, Yan-Zhi,Sun, Xicheng,Zeckner, Douglas J.,Sachs, Roberta K.,Current, William L.,Chen, Shu-Hui
, p. 123 - 126 (2007/10/03)
During the course of a structure-activity relationship (SAR) study on novel depsinonapeptide pseudomycin B, we synthesized a total of 12 8-amidopseudomycin analogues via standard two-step sequence from either ZPSB 2 or AllocPSB 3. A number of these amides exhibited good in vitro antifungal activities.
Syntheses and antifungal activities of novel 3-amido bearing pseudomycin analogues
Zhang, Yan-Zhi,Sun, Xicheng,Zeckner, Douglas J.,Sachs, Roberta K.,Current, William L.,Gidda, Jaswant,Rodriguez, Michael,Chen, Shu-Hui
, p. 903 - 907 (2007/10/03)
As a result of our core SAR effort, we discovered a large number of 3-amido pseudomycin B (PSB) analogues (e.g., 4e LY448212 and 5b LY448731) that retain good in vitro and in vivo (IP) activities against Candida and Cryptococcus without inherent tail vein irritation. Several dimethylamino termini bearing 3-amides (e.g., 5b) also exhibited improved potency against Aspergillus in vitro. When evaluated in a two-week rat toxicology study, it was found that all animals receiving 4e (up to 75 mg/kg) were found to be normal. On the basis of these observations, we are convinced that it is possible to broaden the antifungal spectrum and improve the safety profile of pseudomycin analogues at the same time.
