Five series of tetrahydrobenzothieno[2,3
-d]pyrimidine and tetrahydrobenzothienotriazolopyrimidine derivatives have been synthesized namely: 4-(substituted amino)-5,6,7,8-tetrahydro[1]benzothieno[2,3
-d]pyrimidines
4a–d, 4-substituted (methylidenehydrazino)-5,6,7,8-tetrahydro[1]benzothieno- [2,3
-d]pyrimidines
6a–c, 4-(3,5-disubstituted pyrazol-1-yl)-5,6,7,8-tetrahydro- [1]benzothieno[2,3
-d]pyrimidines
7a,b, 3-substituted-8,9,10,11-tetrahydro- [1]benzothieno[3,2
-e][1,2,4]triazolo[4,3
-c]pyrimidines
8a,b, N-(phenyl or
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Five series of tetrahydrobenzothieno[2,3
-d]pyrimidine and tetrahydrobenzothienotriazolopyrimidine derivatives have been synthesized namely: 4-(substituted amino)-5,6,7,8-tetrahydro[1]benzothieno[2,3
-d]pyrimidines
4a–d, 4-substituted (methylidenehydrazino)-5,6,7,8-tetrahydro[1]benzothieno- [2,3
-d]pyrimidines
6a–c, 4-(3,5-disubstituted pyrazol-1-yl)-5,6,7,8-tetrahydro- [1]benzothieno[2,3
-d]pyrimidines
7a,b, 3-substituted-8,9,10,11-tetrahydro- [1]benzothieno[3,2
-e][1,2,4]triazolo[4,3
-c]pyrimidines
8a,b, N-(phenyl or 4-substituted phenyl)-2-(8,9,10,11-tetrahydro[1]benzothieno[3,2
-e][1,2,4]- triazolo[4,3
-c]pyrimidin-3-ylsulfanyl)acetamides
10a–c. Preliminary antimicrobial testing revealed that compounds
4a and
10b were the most active among the tested compounds against
C. albicans showing IZ = 22 mm and MIC = MBC = 31.25 μg/ml, with no significant antibacterial activity. Compounds
6b and
6c showed the highest antibacterial activity against
S. aureus (IZ = 21 mm, MIC = 62.5 μg/ml, MBC = 125 μg/ml for
6b; IZ = 21 mm, MIC = MBC = 125 μg/ml for
6c). Compounds
4c and
6c showed the highest antibacterial potency against
P. aeruginosa among the tested compounds (IZ = 19–20 mm, MIC = MBC = 62.5 μg/ml). None of the tested compounds showed significant antibacterial activity against E.
coli.
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