Different modes of inhibition of purified ribonucleic acid directed deoxyribonucleic acid polymerase of avian myeloblastosis virus by rifamycin SV derivatives

Quantitative structure-activity correlations of rifamycins as inhibitors of viral RNA-directed DNA polymerase and mammalian .alpha. and .beta. DNA polymerases

“…23 The elongation of chains initiated before drug addition is continuous, and the elongation of primer molecules added after the drug does not occur. 22 The order of addition described in the DiCloccio and Srivastava paper18 was template, drug, substrates, and enzyme. For this experimental design there is a potential for the formation of a stable enzyme-substrate-template complex before the inhibitory action of rifamycin becomes fully active.…”

“…(13) log P [20] = log P [22] " log PCgHe + log Ppentane = 4.83 -2.13 + 3.11 = 5.81 (14) log P[2ij = log P [22] -/ceH5 + 2/Ch2 -fa + 2/C6h6 + Pb + FGBi = 4.83 -1.90 -1.32 -0.23 + 3.80 + 0.12 -0.22 = 5.08 (13) A. J. Leo, personal communication. (14) The fragment value of a methylene group attached to a tetrahedral nitrogen was reduced to 0.46.…”

Chemotherapy of Viral Infections

“…The derivatives AF-013, AF/DNFI, and C-27, which have major differences in the structure of the side chain component, were compared for their ability to inhibit the enzyme when added during the reaction of polymerization (GURGO and GRANDGENETT 1977). These compounds, which have comparable activity when added prior to the template, can be distinguished on the basis of their behavior when added during the reaction of DNA synthesis.…”