Leishmanicidal activity of phenylene bridged C2 symmetric glycosyl ureides

A series of phenylene bridged C 2 symmetric glycosyl ureides were synthesised and evaluated against Leishmania donovani and two of them reduced the dose of standard drug SSG. A number of phenylene bridged C 2 symmetric glycosyl uerides with ester ( 3a– f), alcohol ( 4a– c) and acid ( 5a– d) function...

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Veröffentlicht in:Bioorganic & medicinal chemistry letters 2004-08, Vol.14 (15), p.4055-4059
Hauptverfasser: Tewari, Neetu, Ramesh, Mishra, R.C, Tripathi, R.P, Srivastava, V.M.L, Gupta, Suman
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Sprache:eng
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Zusammenfassung:A series of phenylene bridged C 2 symmetric glycosyl ureides were synthesised and evaluated against Leishmania donovani and two of them reduced the dose of standard drug SSG. A number of phenylene bridged C 2 symmetric glycosyl uerides with ester ( 3a– f), alcohol ( 4a– c) and acid ( 5a– d) functionalities were prepared by addition of glycosyl amino esters with phenyl diisocyanates and their further reaction with LiAlH 4 or hydrolysis with LiOH. All the compounds were screened for their in vitro and in vivo antileishmanial activity. Most of the compounds exhibited good activity while two of the compounds 3e and 3f reduced the clinical dose of standard drug SSG.
ISSN:0960-894X
1464-3405
DOI:10.1016/j.bmcl.2004.05.035