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porter recognition since the Leishmania promastigotes are known to
References and notes
possess a pyrimidine/purine transporter as mentioned in our previ-
ous Letter16 and to the affinity of the compoundstowards their intra-
cellular target. It was also observed from these preliminary results
that keeping the –NH moiety on the 2-pyridone ring intact is crucial
to maintain activity since the replacement of –NH in 6f with either –
NMe (6e), –NEt (6g) or –O (6h) resulted in significant decrease of
activity. In addition, hybrid 7e also showed moderate activity with
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In conclusion, a novel, green and efficient preparation of pyr-
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We are grateful to the National Natural Science Foundation of
China (Nos. 20772025, 20972042 and 20911140238), the Program
for Science & Technology Innovation Talents in Universities of
Henan Province (No. 2008HASTIT006) and the Natural Science
Foundation of Henan Province (Nos. 092300410192 and
094300510054). The authors sincerely thank Professor Dr. Paul F
Torrence, Department of Chemistry, Northern Arizona University,
USA, for his kind help and excellent instructions.
Supplementary data
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2006, 16, 5047; (b) Peyron, C.; Benhida, R.; Bories, C.; Loiseau, P. M. Bioorg.
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Supplementary data associated with this article can be found, in
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