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

Neetu Tewari; V K Tiwari; R P Tripathi; V Chaturvedi; A Srivastava; R Srivastava; P K Shukla; A K Chaturvedi; A Gaikwad; S Sinha; B S Srivastava

doi:10.1016/j.bmcl.2003.11.020

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

Bioorg Med Chem Lett. 2004 Jan 19;14(2):329-32. doi: 10.1016/j.bmcl.2003.11.020.

Authors

Neetu Tewari¹, V K Tiwari, R P Tripathi, V Chaturvedi, A Srivastava, R Srivastava, P K Shukla, A K Chaturvedi, A Gaikwad, S Sinha, B S Srivastava

Affiliation

¹ Division of Medicinal Chemistry, Central Drug Research Institute, -226001, Lucknow, India.

PMID: 14698152
DOI: 10.1016/j.bmcl.2003.11.020

Abstract

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.

Publication types

Comparative Study
Research Support, Non-U.S. Gov't

MeSH terms

Amino Alcohols / chemical synthesis*
Amino Alcohols / pharmacology
Animals
Antifungal Agents / chemical synthesis*
Antifungal Agents / pharmacology
Antitubercular Agents / chemical synthesis*
Antitubercular Agents / pharmacology
Galactose / chemical synthesis*
Galactose / pharmacology
Humans
Mice
Microbial Sensitivity Tests / statistics & numerical data
Mycobacterium tuberculosis / drug effects
Mycobacterium tuberculosis / growth & development

Substances

Amino Alcohols
Antifungal Agents
Antitubercular Agents
Galactose