Several new 6-oxiranyl-, 6-oxiranylmethyluracils, and pyrimidinone derivatives, synthesized by lithiation-alkylation sequence of 1,3,6-trimethyluracil, 1,3-dimethyl-6-chloromethyluracil, and 2-alkoxy-6-methyl-4(3H)-pyrimidinones, showed a potent and selective antiviral activity against Sendai virus (SV) replication. To gain insight into the structural features required for SV inhibition activity, the new compounds were submitted to a pharmacophore generation procedure using the program Catalyst. The resulting pharmacophore model showed high correlation and predictive power. It also rationalized the relationships between structural properties and biological data of these inhibitors of SV replication.

Saladino, R., Crestini, P., Danti, M.C., Manetti, F., Corelli, F., Garaci, E., et al. (2001). Synthesis, biological evaluation and pharmacophore generation of uracil, 4(3H)-pyrimidinone, and uridine derivatives as potent and selective inhibitors of parainfluenza 1 (Sendai) virus. JOURNAL OF MEDICINAL CHEMISTRY, 44(26), 4554-4562 [10.1021/jm010938i].

Synthesis, biological evaluation and pharmacophore generation of uracil, 4(3H)-pyrimidinone, and uridine derivatives as potent and selective inhibitors of parainfluenza 1 (Sendai) virus

MANETTI, FABRIZIO;CORELLI, FEDERICO;BOTTA, MAURIZIO
2001-01-01

Abstract

Several new 6-oxiranyl-, 6-oxiranylmethyluracils, and pyrimidinone derivatives, synthesized by lithiation-alkylation sequence of 1,3,6-trimethyluracil, 1,3-dimethyl-6-chloromethyluracil, and 2-alkoxy-6-methyl-4(3H)-pyrimidinones, showed a potent and selective antiviral activity against Sendai virus (SV) replication. To gain insight into the structural features required for SV inhibition activity, the new compounds were submitted to a pharmacophore generation procedure using the program Catalyst. The resulting pharmacophore model showed high correlation and predictive power. It also rationalized the relationships between structural properties and biological data of these inhibitors of SV replication.
2001
Saladino, R., Crestini, P., Danti, M.C., Manetti, F., Corelli, F., Garaci, E., et al. (2001). Synthesis, biological evaluation and pharmacophore generation of uracil, 4(3H)-pyrimidinone, and uridine derivatives as potent and selective inhibitors of parainfluenza 1 (Sendai) virus. JOURNAL OF MEDICINAL CHEMISTRY, 44(26), 4554-4562 [10.1021/jm010938i].
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Utilizza questo identificativo per citare o creare un link a questo documento: https://hdl.handle.net/11365/21526
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