Synthesis and tuberculostatic activity of podands with a dihydropyrimidine fragment
A method for the preparation of 3-oxobutanoate-containing podands differing in the length of the polyether fragment by acetoacetylation of oligo(ethylene glycols) with 2,2,6-trimethyl-4 H -1,3-dioxin-4-one upon heating in toluene was optimized. A multi-component Biginelli reaction was used for the f...
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Published in | Russian chemical bulletin Vol. 65; no. 5; pp. 1360 - 1364 |
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Main Authors | , , , , , , , |
Format | Journal Article |
Language | English |
Published |
New York
Springer US
01.05.2016
Springer Nature B.V |
Subjects | |
Online Access | Get full text |
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Summary: | A method for the preparation of 3-oxobutanoate-containing podands differing in the length of the polyether fragment by acetoacetylation of oligo(ethylene glycols) with 2,2,6-trimethyl-4
H
-1,3-dioxin-4-one upon heating in toluene was optimized. A multi-component Biginelli reaction was used for the formation of the dihydropyrimidine ring on the ether matrix obtained. Tuberculostatic activity of dihydropyrimidine podands in the
in vitro
experiments against a laboratory strain H
37
Rv was studied. A combination of dihydropyrimidine and podand fragments imparts tuberculostatic activity to the compounds obtained, which noticeably enhances with the increase in the oxyethylene spacer length. |
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ISSN: | 1066-5285 1573-9171 |
DOI: | 10.1007/s11172-016-1462-4 |