Glycosidopyrroles. Part 2. Acyclic derivatives: 1-(1,3-dihydroxy-2-propoxy)methylpyrroles as potential antiviral agents.
The series of 1-(1,3-dihydroxy-2-propoxy)methylpyrroles 2a-o were prepared in good overall yields according to Scheme I. When evaluated for antiviral activity against HIV-1, only compounds of the triphenyl series (R3 = NH2, N3, Br) were found to inhibit the HIV-1 replication at concentrations that were very not cytotoxic for MT-4 cells, with selectivity index 1.5-9.3. None of these compounds showed antibacterial or antifungal activity.
Almerico
A M
AM
Istituto Farmacochimico, Università degli Studi, Palermo, Italy.
Diana
P
P
Barraja
P
P
Dattolo
G
G
Mingoia
F
F
Putzolu
M
M
Perra
G
G
Milia
C
C
Musiu
C
C
Marongiu
M E
ME
D000818:Animals; D019380:Anti-HIV Agents / Q000138:chemical synthesis / Q000737:chemistry / Q000494:pharmacology*; D002522:Chlorocebus aethiops; D015497:HIV-1 / Q000187:drug effects / Q000502:physiology; D006801:Humans; D011758:Pyrroles / Q000138:chemical synthesis / Q000737:chemistry / Q000494:pharmacology*; D014709:Vero Cells; D014779:Virus Replication / Q000187:drug effects
D019380:Anti-HIV Agents; D011758:Pyrroles