Synthesis and studies of new 6-[halo(diphenyl)methyl]- and 6-(thiophen-2-ylmethyl)pyrimidin-4(3H)-ones as possible HIV-1 reverse transcriptase inhibitors
Six new 6-[halo(diphenyl)methyl]- and 6-(thiophen-2-ylmethyl)pyrimidin- 4(3H)-one derivatives were synthesized and studied for biological activity. The studies showed that the 6-(thiophen-2-ylmethyl)pyrimidin-4(3H)-one derivatives inhibited activity of the HIV-1 recombinant reverse transcriptase in the micromolar range of concentrations. The 6-[halo-(diphenyl)methyl]pyrimidin-4(3H) -one derivative showed no activity in the concentrations up to 200 μmol mL-1.
Characteristics of the halogenation of 2-substituted 6-benzhydryl-4(3H)- pyrimidinones
The halogenation of 2-substituted 6-benzhydryl-4(3H)-pyrimidinones has been investigated. Bromination with Py?Br2 and iodination with I2 solution in alkali occurs exclusively at the CH hydrogen of the benzhydryl group. Springer Scien
Novakov,Orlinson,Nawrozkij
p. 1233 - 1235
(2008/09/20)
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