Total synthesis of the antiviral peptide antibiotic feglymycin.

نویسندگان

  • Frank Dettner
  • Anne Hänchen
  • Dominique Schols
  • Luigi Toti
  • Antje Nusser
  • Roderich D Süssmuth
چکیده

An adaptable approach: The first highly convergent stereoselective synthesis of feglymycin (see structure) and its enantiomer is based on the coupling of repeating peptide fragments. The use of weakly basic conditions throughout the synthesis suppressed the epimerization of sensitive aryl glycine units. Feglymycin has strong anti-HIV activity as well as potent (previously identified as weak) antibacterial activity against Staphylococcus aureus.

برای دانلود رایگان متن کامل این مقاله و بیش از 32 میلیون مقاله دیگر ابتدا ثبت نام کنید

ثبت نام

اگر عضو سایت هستید لطفا وارد حساب کاربری خود شوید

منابع مشابه

Total synthesis of feglymycin based on a linear/convergent hybrid approach using micro-flow amide bond formation

Feglymycin is a naturally occurring, anti-HIV and antimicrobial 13-mer peptide that includes highly racemizable 3,5-dihydroxyphenylglycines (Dpgs). Here we describe the total synthesis of feglymycin based on a linear/convergent hybrid approach. Our originally developed micro-flow amide bond formation enabled highly racemizable peptide chain elongation based on a linear approach that was previou...

متن کامل

Evaluating the Antiviral Activities of Human Cathelicidin LL-37 Peptide Against Rotavirus in Vitro

Background Rotavirus is the most prevalent cause of severe gastroenteritis, hospitalizations, and deaths among infants and young children, globally. No specific antiviral drug is available against rotavirus infection.  Objective The current study aimed to assess the antiviral effect of human cathelicidin antimicrobial peptide LL-37 on rotavirus infection in vitro.  Methods  This study was con...

متن کامل

Design, synthesis and biological evaluation of Ciprofloxacin- peptide conjugates as anticancer agents

Cancer has emerged as a leading cause of death throughout the world. Peptides are a novel class of anticancer agents that can specifically target cancer cells with low toxicity to normal tissues and thus, offer new opportunities for future cancer treatment. On the other hand, Ciprofloxacin, an antibiotic, also known to its anticancer property for enabling cell cycle arrest and creating double s...

متن کامل

Design, synthesis and biological evaluation of Ciprofloxacin- peptide conjugates as anticancer agents

Cancer has emerged as a leading cause of death throughout the world. Peptides are a novel class of anticancer agents that can specifically target cancer cells with low toxicity to normal tissues and thus, offer new opportunities for future cancer treatment. On the other hand, Ciprofloxacin, an antibiotic, also known to its anticancer property for enabling cell cycle arrest and creating double s...

متن کامل

Effect of Different Levels of Cottonseed Meal Bioactive Peptides on Production Efficiency and Serum Antioxidant Activity of Broiler Chickens

Cottonseed meal was hydrolyzed using five types of enzymes: alkalase, chymotrypsin, pepsin, trypsin, and pancreatin. The experiment was carried out using 240 male broilers of Ross 308 strain in a completely randomized design with 4 treatments and 5 replications from 1 to 35 days of age and during the starter (1-15 days) and grower (16-35 days) phases. The experimental diets were the control die...

متن کامل

ذخیره در منابع من


  با ذخیره ی این منبع در منابع من، دسترسی به آن را برای استفاده های بعدی آسان تر کنید

عنوان ژورنال:
  • Angewandte Chemie

دوره 48 10  شماره 

صفحات  -

تاریخ انتشار 2009