دورية أكاديمية
Total synthesis and antifungal evaluation of cyclic aminohexapeptides.
| العنوان: | Total synthesis and antifungal evaluation of cyclic aminohexapeptides. |
|---|---|
| المؤلفون: | Klein LL; Infectious Disease Research, Abbott Laboratories, Abbott Park, IL 60064-3500, USA. larry.l.klein@abbott.com, Li L, Chen HJ, Curty CB, DeGoey DA, Grampovnik DJ, Leone CL, Thomas SA, Yeung CM, Funk KW, Kishore V, Lundell EO, Wodka D, Meulbroek JA, Alder JD, Nilius AM, Lartey PA, Plattner JJ |
| المصدر: | Bioorganic & medicinal chemistry [Bioorg Med Chem] 2000 Jul; Vol. 8 (7), pp. 1677-96. |
| نوع المنشور: | Comparative Study; Journal Article |
| اللغة: | English |
| بيانات الدورية: | Publisher: Elsevier Science Country of Publication: England NLM ID: 9413298 Publication Model: Print Cited Medium: Print ISSN: 0968-0896 (Print) Linking ISSN: 09680896 NLM ISO Abbreviation: Bioorg Med Chem Subsets: MEDLINE |
| أسماء مطبوعة: | Publication: Oxford : Elsevier Science Original Publication: Oxford : New York : Pergamon Press, c1993- |
| مواضيع طبية MeSH: | Fungal Proteins* , Peptides*, Antifungal Agents/*chemical synthesis , Antifungal Agents/*pharmacology , Peptides, Cyclic/*chemical synthesis , Peptides, Cyclic/*pharmacology, Acute Disease ; Amines/chemical synthesis ; Amines/chemistry ; Amines/pharmacology ; Amphotericin B/pharmacology ; Animals ; Anti-Bacterial Agents/chemical synthesis ; Anti-Bacterial Agents/chemistry ; Anti-Bacterial Agents/pharmacology ; Antifungal Agents/chemistry ; Candida/drug effects ; Candidiasis, Vulvovaginal/drug therapy ; Candidiasis, Vulvovaginal/microbiology ; Disease Models, Animal ; Dose-Response Relationship, Drug ; Echinocandins ; Female ; Mice ; Microbial Sensitivity Tests ; Peptides, Cyclic/chemistry ; Proline/chemistry ; Solubility ; Structure-Activity Relationship ; Yeasts/drug effects |
| مستخلص: | The need for new therapies to treat systemic fungal infections continues to rise. Naturally occurring hexapeptide echinocandin B (1) has shown potent antifungal activity via its inhibition of the synthesis of beta-1,3 glucan, a key fungal cell wall component. Although this series of agents has been limited thus far based on their physicochemical characteristics, we have found that the synthesis of analogues bearing an aminoproline residue in the 'northwest' position imparts greatly improved water solubility (> 5 mg/mL). The synthesis and structure-activity relationships (SAR) based on whole cell and upon in vivo activity of the series of compounds are reported. |
| المشرفين على المادة: | 0 (Amines) 0 (Anti-Bacterial Agents) 0 (Antifungal Agents) 0 (Echinocandins) 0 (Fungal Proteins) 0 (Peptides) 0 (Peptides, Cyclic) 7XU7A7DROE (Amphotericin B) 9DLQ4CIU6V (Proline) CNW0ZW8ZTQ (echinocandin B) |
| تواريخ الأحداث: | Date Created: 20000908 Date Completed: 20010118 Latest Revision: 20190831 |
| رمز التحديث: | 20221213 |
| DOI: | 10.1016/s0968-0896(00)00097-3 |
| PMID: | 10976515 |
| قاعدة البيانات: | MEDLINE |
Full Text Finder | تدمد: | 0968-0896 |
|---|---|
| DOI: | 10.1016/s0968-0896(00)00097-3 |