GX Wang, L Wang, ZZ Zhao, T Zhang , PZ Tao, . SYNTHESIS OF S-9-(2,3-DIHYDROXYPROPYL)ADENINE (DHPA) ANALOGS AND THEIR INHIBITION OF S-ADENOSYL-L-HOMOCYSTEINE (SAH) HYDROLASEJ. Acta Pharmaceutica Sinica, 1997, 32(3): 188-192.
Citation: GX Wang, L Wang, ZZ Zhao, T Zhang , PZ Tao, . SYNTHESIS OF S-9-(2,3-DIHYDROXYPROPYL)ADENINE (DHPA) ANALOGS AND THEIR INHIBITION OF S-ADENOSYL-L-HOMOCYSTEINE (SAH) HYDROLASEJ. Acta Pharmaceutica Sinica, 1997, 32(3): 188-192.

SYNTHESIS OF S-9-(2,3-DIHYDROXYPROPYL)ADENINE (DHPA) ANALOGS AND THEIR INHIBITION OF S-ADENOSYL-L-HOMOCYSTEINE (SAH) HYDROLASE

  • In order to search for new antiviral agents with high potency and low toxicity, eleven new acyclonucleosides were synthesized. Nucleic acid bases were condensed with 3-chloro-2-methylpropene to give 5~8a.b, which were oxidized by N-methylmorpholine N-oxide in the presence of OsO4 to give vicinal dihydroxy acyclonucleosides 1~4a.b. Four DHPA analogs have been tested for the inhibitory activities on s adenosyl L homocysteine hydrolase (SAH). Only compound 1 showed some enzyme inhibitory effect with IC 50 of 1.1 mmol·L-1.
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