Synthesis and Evaluation of Oxodioxolenylmethyl Carbamate Prodrugs of Pseudomycins

التفاصيل البيبلوغرافية
العنوان: Synthesis and Evaluation of Oxodioxolenylmethyl Carbamate Prodrugs of Pseudomycins
المؤلفون: Sun, X., Rodriguez, M., Zeckner, D., Sachs, B., Current, W., Boyer, R., Paschal, J., McMillian, C., Chen, S.-H.
المصدر: Journal of Medicinal Chemistry; August 2001, Vol. 44 Issue: 16 p2671-2674, 4p
مستخلص: With the aim of increasing therapeutic indexes of novel cyclic depsinonapeptide pseudomycins, we synthesized and evaluated a series of mono-, di-, and trioxodioxolenylmethyl carbamate prodrugs (2 and 4) of pseudomycin B 1 and pseudomycin C‘ 3. It is rather encouraging to note that several members of the newly synthesized prodrugs described herein (e.g., 2a, 2e, and 4e) exhibited comparable in vivo efficacy to that achieved by the parent compounds, yet free of tail vein irritation and histamine induced toxicity in vivo.
قاعدة البيانات: Supplemental Index