A series of N-methyl-N-pyrimidin-2-yl glycines, having the pyrimidine ring fused with a cyclohexane [N-methyl-N-(5,6,7,8-tetrahydroquinazolin-2-yl)glycine], cyclohexene [N-methyl-N-(5,6-dihydroquinazolin-2-yl)glycine], 1,2,3,4-tetrahydronaphthalene [N-methyl-N-(5,6-dihydrobenzo[e]quinazolin-2-yl)glycine], benzopyrane [N-methyl-N-(5-phenyl-5H-[1]benzopyrano[4,3-d]pyrimidin-2-yl)glycine] and benzothiopyrane [N-methyl-N-(5H-[1]benzothiopyrano[4,3-d]pyrimidin-2-yl)glycine] ring, was prepd. and tested for antiinflammatory activity. With the same purpose a no. of N-5H-[1]benzopyrano[4,3-d]pyrimidin-2-yl substituted amino acids, having a different chain length and branching were also synthesized and tested. All the described products showed an appreciable antiphlogistic activity. Structure-activity relations are discussed.
Antiinflammatory agents: new series of N-substituted amino acids with complex pyrimidine structures endowed with antiphlogistic activity
BRUNO, OLGA;SCHENONE, SILVIA;RANISE, ANGELO;BONDAVALLI, FRANCESCO;
1999-01-01
Abstract
A series of N-methyl-N-pyrimidin-2-yl glycines, having the pyrimidine ring fused with a cyclohexane [N-methyl-N-(5,6,7,8-tetrahydroquinazolin-2-yl)glycine], cyclohexene [N-methyl-N-(5,6-dihydroquinazolin-2-yl)glycine], 1,2,3,4-tetrahydronaphthalene [N-methyl-N-(5,6-dihydrobenzo[e]quinazolin-2-yl)glycine], benzopyrane [N-methyl-N-(5-phenyl-5H-[1]benzopyrano[4,3-d]pyrimidin-2-yl)glycine] and benzothiopyrane [N-methyl-N-(5H-[1]benzothiopyrano[4,3-d]pyrimidin-2-yl)glycine] ring, was prepd. and tested for antiinflammatory activity. With the same purpose a no. of N-5H-[1]benzopyrano[4,3-d]pyrimidin-2-yl substituted amino acids, having a different chain length and branching were also synthesized and tested. All the described products showed an appreciable antiphlogistic activity. Structure-activity relations are discussed.
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