NOC chemistry for tuberculosis - Further investigations on the structure-activity relationships of antitubercular isoxazole-3-carboxylic acid ester derivatives

Marco Pieroni; Annamaria Lilienkampf; Yuehong Wang; Baojie Wan; Sanghyun Cho; Scott G. Franzblau; Alan P. Kozikowski

doi:10.1002/cmdc.201000169

NOC chemistry for tuberculosis - Further investigations on the structure-activity relationships of antitubercular isoxazole-3-carboxylic acid ester derivatives

Marco Pieroni, Annamaria Lilienkampf, Yuehong Wang, Baojie Wan, Sanghyun Cho, Scott G. Franzblau, Alan P. Kozikowski

Research output: Contribution to journal › Article › peer-review

12 Scopus citations

Abstract

NOC, NOC! Who's there? We have expanded the body of structure-activity relationships (SAR) regarding the 3-isoxazolecarboxylic acid ethyl esters by the design and synthesis of 5-aryl- and 5-[(N-aryl)amino]methyl analogues. Compounds were active against Mycobacterium tuberculosis (Mtb) at sub-micromolar concentrations and, for selected compounds, no toxicity was observed on Vero cells.

Original language	English (US)
Pages (from-to)	1667-1672
Number of pages	6
Journal	ChemMedChem
Volume	5
Issue number	10
DOIs	https://doi.org/10.1002/cmdc.201000169
State	Published - Oct 4 2010
Externally published	Yes

Keywords

Drug design
Drug discovery
Isoxazole derivatives
Tuberculosis

ASJC Scopus subject areas

Biochemistry
Molecular Medicine
Pharmacology
Drug Discovery
Pharmacology, Toxicology and Pharmaceutics(all)
Organic Chemistry

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10.1002/cmdc.201000169

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abstract = "NOC, NOC! Who's there? We have expanded the body of structure-activity relationships (SAR) regarding the 3-isoxazolecarboxylic acid ethyl esters by the design and synthesis of 5-aryl- and 5-[(N-aryl)amino]methyl analogues. Compounds were active against Mycobacterium tuberculosis (Mtb) at sub-micromolar concentrations and, for selected compounds, no toxicity was observed on Vero cells.",

keywords = "Drug design, Drug discovery, Isoxazole derivatives, Tuberculosis",

author = "Marco Pieroni and Annamaria Lilienkampf and Yuehong Wang and Baojie Wan and Sanghyun Cho and Franzblau, {Scott G.} and Kozikowski, {Alan P.}",

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AU - Pieroni, Marco

AU - Lilienkampf, Annamaria

AU - Wang, Yuehong

AU - Wan, Baojie

AU - Cho, Sanghyun

AU - Franzblau, Scott G.

AU - Kozikowski, Alan P.

PY - 2010/10/4

Y1 - 2010/10/4

N2 - NOC, NOC! Who's there? We have expanded the body of structure-activity relationships (SAR) regarding the 3-isoxazolecarboxylic acid ethyl esters by the design and synthesis of 5-aryl- and 5-[(N-aryl)amino]methyl analogues. Compounds were active against Mycobacterium tuberculosis (Mtb) at sub-micromolar concentrations and, for selected compounds, no toxicity was observed on Vero cells.

AB - NOC, NOC! Who's there? We have expanded the body of structure-activity relationships (SAR) regarding the 3-isoxazolecarboxylic acid ethyl esters by the design and synthesis of 5-aryl- and 5-[(N-aryl)amino]methyl analogues. Compounds were active against Mycobacterium tuberculosis (Mtb) at sub-micromolar concentrations and, for selected compounds, no toxicity was observed on Vero cells.

KW - Drug design

KW - Drug discovery

KW - Isoxazole derivatives

KW - Tuberculosis

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NOC chemistry for tuberculosis - Further investigations on the structure-activity relationships of antitubercular isoxazole-3-carboxylic acid ester derivatives

Abstract

Keywords

ASJC Scopus subject areas

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