Design and synthesis of N¹,N⁵-bis[4-(5-alkyl-1,2,4-oxadiazol-3-yl)phenyl]glutaramides as potential antifungal prodrugs

Design and synthesis of N¹,N⁵-bis[4-(5-alkyl-1,2,4-oxadiazol-3-yl)phenyl]glutaramides as potential antifungal prodrugs

A facile three step synthesis of a group of N1,N5-bis[4-(5-alkyl-1,2,4-oxadiazol-3-yl)phenyl]glutaramides, N1,N5-bis[4-(1,2,4-oxadiazol-3-yl)phenyl]glutaramide and N1,N5-bis[4-(5-oxo-4,5-dihydro-1,2,4-oxadiazol-3-yl)phenyl]glutaramide is described. These products are designed to function as masked b...

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Veröffentlicht in:Molecules (Basel, Switzerland) Switzerland), 2013-09, Vol.18 (9), p.11250-11263
Hauptverfasser: Kode, Nageswara Rao, Vanden Eynde, Jean J, Mayence, Annie, Wang, Guangdi, Huang, Tien L
Format: Artikel
Sprache:eng
Schlagworte:
amidoximes
Animals
Antifungal Agents - chemical synthesis
Antifungal Agents - metabolism
Bioavailability
Cytotoxicity
Design
Glutarates - chemical synthesis
Glutarates - metabolism
Microsomes, Liver - metabolism
oxadiazoles
Oxadiazoles - chemical synthesis
Oxadiazoles - metabolism
Oximes - chemical synthesis
Oximes - metabolism
Pneumocystis carinii
prodrugs
Prodrugs - chemical synthesis
Prodrugs - metabolism
Protozoa
Rats
Trypanosoma brucei
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Zusammenfassung:A facile three step synthesis of a group of N1,N5-bis[4-(5-alkyl-1,2,4-oxadiazol-3-yl)phenyl]glutaramides, N1,N5-bis[4-(1,2,4-oxadiazol-3-yl)phenyl]glutaramide and N1,N5-bis[4-(5-oxo-4,5-dihydro-1,2,4-oxadiazol-3-yl)phenyl]glutaramide is described. These products are designed to function as masked bis-amidine prodrugs of a promising N1,N5-bis[4-(N'-(carbamimidoyl)phenyl]glutaramide antifungal lead.
ISSN:1420-3049
1420-3049
DOI:10.3390/molecules180911250