Document Detail


Synthesis of paromomycin derivatives modified at C(5'') to selectively target bacterial rRNA.
MedLine Citation:
PMID:  17049499     Owner:  NLM     Status:  MEDLINE    
Abstract/OtherAbstract:
The furanosyl moiety (ring III) of C(6')-deoxyparomomycin and paromomycin was modified in search of aminoglycoside antibiotics with altered selectivity. The key intermediates were the N-Boc-protected derivative of C(6')-deoxyparomomycin and the benzylidene-protected paromomycin. Their H(2)C(5'')-OH group was oxidised with trichlorocyanuric acid or [bis(acetoxy)iodo]benzene in the presence of catalytic amounts of TEMPO to yield the corresponding aldehydes and acids, which were transformed into the protected alkoxy imines, amides and the amine. Standard deprotection gave the title compounds derived from C(6')-deoxyparomomycin and derived from paromomycin that proved less active than paromomycin and its C(6')-deoxy analogue.
Authors:
Iwona Kudyba; Déborah Perez Fernandez; Erik C Böttger; Andrea Vasella
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Publication Detail:
Type:  Journal Article     Date:  2006-10-17
Journal Detail:
Title:  Carbohydrate research     Volume:  342     ISSN:  0008-6215     ISO Abbreviation:  Carbohydr. Res.     Publication Date:  2007 Feb 
Date Detail:
Created Date:  2007-02-02     Completed Date:  2007-04-13     Revised Date:  -    
Medline Journal Info:
Nlm Unique ID:  0043535     Medline TA:  Carbohydr Res     Country:  Netherlands    
Other Details:
Languages:  eng     Pagination:  499-519     Citation Subset:  IM    
Affiliation:
Laboratorium für Organische Chemie, ETH Zürich, HCI, CH-8093 Zürich, Switzerland.
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MeSH Terms
Descriptor/Qualifier:
Mycobacterium smegmatis / drug effects
Oxidation-Reduction
Paromomycin / analogs & derivatives*,  chemical synthesis*,  pharmacology
RNA, Bacterial / chemistry*
RNA, Ribosomal / chemistry*
Ribosomes / drug effects
Structure-Activity Relationship
Chemical
Reg. No./Substance:
0/RNA, Bacterial; 0/RNA, Ribosomal; 7542-37-2/Paromomycin

From MEDLINE®/PubMed®, a database of the U.S. National Library of Medicine


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