Synthesis of galactopyranosyl amino alcohols as a new class of antitubercular and antifungal agents

The galactopyranosyl amino alcohols ( 3– 16) were synthesised by regioselective oxirane ring opening of compound 2 with variety of amines and screened for antitubercular and antifungal activities. One of the compounds ( 16) showed potent activity against Mycobacterium tuberculosis H37 Rv in vitro an...

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Veröffentlicht in:Bioorganic & medicinal chemistry letters 2004-01, Vol.14 (2), p.329-332
Hauptverfasser: Tewari, Neetu, Tiwari, V.K., Tripathi, R.P., Chaturvedi, V., Srivastava, A., Srivastava, R., Shukla, P.K., Chaturvedi, A.K., Gaikwad, A., Sinha, S., Srivastava, B.S.
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Sprache:eng
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Zusammenfassung:The galactopyranosyl amino alcohols ( 3– 16) were synthesised by regioselective oxirane ring opening of compound 2 with variety of amines and screened for antitubercular and antifungal activities. One of the compounds ( 16) showed potent activity against Mycobacterium tuberculosis H37 Rv in vitro and also displayed activity in MDR TB. The compound ( 16) was found to be superior to ethambutol clinically used anti TB drug in in vitro screen. A series of glactopyranosyl amino alcohols have been synthesised and evaluated against Mycobacterium tuberculosis and one of them was found to be superior to ethambutol.
ISSN:0960-894X
1464-3405
DOI:10.1016/j.bmcl.2003.11.020