Rifamycins as inhibitors of retroviral reverse transcriptase from M-MuLV, RAV-2, and HIV-1.
29 Rifamycins were tested for inhibition of Reverse Transcriptase (RT) as potential anti HIV drugs. Two purified commercial enzymes from M-MuLV and RAV-2 were used. Anti-RT activity was also measured on a crude lysate of HIV-1. The results show that some derivatives have interesting levels of activity on isolated M-MuLV and RAV-2 RTs, while they are less active on the RT in the crude HIV-1 lysate. The active derivatives include oximes and hydrazones, alkylaminoderivatives, open ansa-chain derivatives and derivatives carrying a modified nucleoside.
Bartolucci
C
C
Istituto di Strutturistica Chimica, G. Giacomello, CNR C.P. 10 00016, Roma, Italy.
Cellai
L
L
Di Filippo
P
P
Segre
A
A
Brufani
M
M
Filocamo
L
L
Bianco
A D
AD
Guiso
M
M
Brizzi
V
V
Benedetto
A
A
D054303:HIV Reverse Transcriptase; D015497:HIV-1 / Q000201:enzymology; D009052:Leukemia Virus, Murine / Q000201:enzymology; D008970:Molecular Weight; D012190:Retroviridae / Q000201:enzymology*; D018894:Reverse Transcriptase Inhibitors; D012294:Rifamycins / Q000138:chemical synthesis / Q000494:pharmacology*
D018894:Reverse Transcriptase Inhibitors; D012294:Rifamycins; D054303:HIV Reverse Transcriptase