Fluorocontaining D-cycloserines. Synthesis and in vitro evaluation of antimicrobial and antiviral activities.
Some fluoroacylderivatives at the side chain NH2 of D-cycloserine were synthesized and evaluated in vitro for antimicrobial activity against bacteria and tubercular or non-tubercular mycobacteria. Against the used Gram-positive and Gram-negative strains only trifluoroacetamide 1 exhibited comparable MIC values and lower MBC values than those of parent antibiotic. Other fluoroacycloserines, inactive at all on these bacteria, were found to inhibit the growth of mycobacteria when tested in liquid media. The in vitro anti-Herpex Simplex virus type-2 (HSV-2) activity was also investigated on HEp-2 and Vero cells. The obtained results demonstrated an antiviral activity of the compounds 1 and 3 when tested on Vero cell-lines, whereas the same cycloserine is inactive.
Vigorita
M G
MG
Dipartimento Farmaco-Chimico, Università di Messina, Italy.
Donato Alessi
G
G
Previtera
T
T
Gabbrielli
G
G
Bisignano
G
G
Arena
A
A
Merendino
R A
RA
Bonina
L
L
D000818:Animals; D000900:Anti-Bacterial Agents; D000890:Anti-Infective Agents / Q000138:chemical synthesis* / Q000494:pharmacology; D000995:Antitubercular Agents / Q000138:chemical synthesis / Q000494:pharmacology; D000998:Antiviral Agents / Q000138:chemical synthesis* / Q000494:pharmacology; D002478:Cells, Cultured; D003523:Cycloserine / Q000138:chemical synthesis* / Q000494:pharmacology; D003588:Cytopathogenic Effect, Viral; D006801:Humans; D008826:Microbial Sensitivity Tests; D009161:Mycobacterium / Q000187:drug effects; D014709:Vero Cells; D014779:Virus Replication / Q000187:drug effects
D000900:Anti-Bacterial Agents; D000890:Anti-Infective Agents; D000995:Antitubercular Agents; D000998:Antiviral Agents; D003523:Cycloserine