New thiopyrazolo[3,4-d]pyrimidine derivatives as anti-mycobacterial agents

Lluis Ballell; Robert A. Field; Gavin A. C. Chung; Robert J. Young

doi:10.1016/j.bmcl.2006.12.066

New thiopyrazolo[3,4-d]pyrimidine derivatives as anti-mycobacterial agents

Lluis Ballell, Robert A. Field, Gavin A. C. Chung, Robert J. Young

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

116 Citations (Scopus)

Abstract

The multiple parallel synthesis of a series of N,S-bis-alkylated thiopyrazolo[3,4-d]pyrimidines, based on sequential S- then N-alkylation, is reported. These compounds showed significant anti-mycobacterial activity (MICs down to ≤2 μg/ml) and their potential as significant drug-like leads is substantiated through cytotoxicity evaluation and in silico profiling.

Original language	English
Pages (from-to)	1736-1740
Number of pages	5
Journal	Bioorganic and Medicinal Chemistry Letters
Volume	17
Issue number	6
DOIs	https://doi.org/10.1016/j.bmcl.2006.12.066
Publication status	Published - 15 Mar 2007

Keywords

Anti-mycobacterial
Anti-tubercular
SAR
Thiopyrazolopyrimidines

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10.1016/j.bmcl.2006.12.066

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title = "New thiopyrazolo[3,4-d]pyrimidine derivatives as anti-mycobacterial agents",

abstract = "The multiple parallel synthesis of a series of N,S-bis-alkylated thiopyrazolo[3,4-d]pyrimidines, based on sequential S- then N-alkylation, is reported. These compounds showed significant anti-mycobacterial activity (MICs down to ≤2 μg/ml) and their potential as significant drug-like leads is substantiated through cytotoxicity evaluation and in silico profiling.",

keywords = "Anti-mycobacterial, Anti-tubercular, SAR, Thiopyrazolopyrimidines",

author = "Lluis Ballell and Field, {Robert A.} and Chung, {Gavin A. C.} and Young, {Robert J.}",

note = "Funding Information: We thank the GlaxoSmithKline Action TB Initiative for financial support and Mar{\'i}a Jes{\'u}s Almela for generating the cytotoxicity data. ",

year = "2007",

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doi = "10.1016/j.bmcl.2006.12.066",

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T1 - New thiopyrazolo[3,4-d]pyrimidine derivatives as anti-mycobacterial agents

AU - Ballell, Lluis

AU - Field, Robert A.

AU - Chung, Gavin A. C.

AU - Young, Robert J.

N1 - Funding Information: We thank the GlaxoSmithKline Action TB Initiative for financial support and María Jesús Almela for generating the cytotoxicity data.

PY - 2007/3/15

Y1 - 2007/3/15

N2 - The multiple parallel synthesis of a series of N,S-bis-alkylated thiopyrazolo[3,4-d]pyrimidines, based on sequential S- then N-alkylation, is reported. These compounds showed significant anti-mycobacterial activity (MICs down to ≤2 μg/ml) and their potential as significant drug-like leads is substantiated through cytotoxicity evaluation and in silico profiling.

AB - The multiple parallel synthesis of a series of N,S-bis-alkylated thiopyrazolo[3,4-d]pyrimidines, based on sequential S- then N-alkylation, is reported. These compounds showed significant anti-mycobacterial activity (MICs down to ≤2 μg/ml) and their potential as significant drug-like leads is substantiated through cytotoxicity evaluation and in silico profiling.

KW - Anti-mycobacterial

KW - Anti-tubercular

KW - SAR

KW - Thiopyrazolopyrimidines

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AN - SCOPUS:33847055385

SN - 0960-894X

VL - 17

SP - 1736

EP - 1740

JO - Bioorganic and Medicinal Chemistry Letters

JF - Bioorganic and Medicinal Chemistry Letters

IS - 6

ER -

New thiopyrazolo[3,4-d]pyrimidine derivatives as anti-mycobacterial agents

Abstract

Keywords

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