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

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BIOORGANIC & MEDICINAL CHEMISTRY LETTERS
卷 14, 期 2, 页码 329-332

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PERGAMON-ELSEVIER SCIENCE LTD
DOI: 10.1016/j.bmcl.2003.11.020

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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. (C) 2003 Elsevier Ltd. All rights reserved.

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