- Synthesis of oxazolyl- and furanyl-substituted imidazole hydrochlorides and methiodides
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Oxazolyl-5- and furanyl-2-substituted imidazoles have been synthesized by coupling the two ring systems via the dipolar cycloadditon of tosyl methyl isocyanide to the corresponding oxazolyl and furanyl aldimines in basic media. These substitute oxazolyl and furanylimidazole bases obtained in this manner were then subjected to hydrogen chloride gas and to methyl iodide to form the corresponding hydrochlorides and methyliodides, respectively. All compounds were purified, characterized and then tested for muscarinic binding affinity. Biological test results revealed low muscarinic receptor affinity and selectivity.
- Boulos, John,Schulman, Jerome
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p. 859 - 863
(2007/10/03)
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- 1-cyclopropyl-4-pyridyl-quinolinones
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Compounds of formula STR1 wherein R1 is hydrogen, lower-alkyl, or trifluoromethyl; R2 is lower-alkyl, trifluoromethyl or CH2 Z where Z is hydroxy, chloro, lower-alkylamino or dilower-alkylamino; R3 and R4 are each individually hydrogen or fluoro; and Ar is phenyl, an aromatic 5- or 6-membered heterocycle or any of these substituted at one or more positions with lower-alkyl, fluoro, chloro, hydroxy, amino, lower-alkylamino, dilower-alkylamino, carboxy, sulfonamido, lower alkylsulfonamido, methylenedioxy, trifluoroacetamido, lower-alkanoylamino, or carbamoyl; and their pharmaceutically acceptable acid addition salts are useful as anticancer agents.
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