Synthesis and evaluation of (S,S)-N,N′-bis-[3-(2,2′,6,6′-tetramethylbenzhydryloxy)-2-hydroxy-propyl]-ethylenediamine (S2824) analogs with anti-tuberculosis activity

Xuelian Zhang, Yanwei Hu, Shudan Chen, Rusong Luo, Jun Yue, Ying Zhang, Wenhu Duan, Honghai Wang

Research output: Contribution to journalArticlepeer-review

Abstract

In order to identify new and potent candidate drugs to treat tuberculosis, a library of compounds was screened, and (S,S)-N,N′-bis-[3-(2,2′,6,6′-tetramethylbenzhydryloxy)-2-hydroxy-propyl]-ethylenediamine (S2824) was identified as a hit in the screen. This research discusses our efforts to synthesize and test 30 analogs of this hit for activity against Mycobacterium tuberculosis. Two compounds with homopiperazine ring possess high in vitro activity against drug sensitive and resistant M. tuberculosis with MICs 0.78-3.13 μg/mL (or 1.22-4.88 μM).

Original languageEnglish (US)
Pages (from-to)6074-6077
Number of pages4
JournalBioorganic and Medicinal Chemistry Letters
Volume19
Issue number21
DOIs
StatePublished - Nov 1 2009

Keywords

  • Antitubercular drug
  • MIC
  • Resistance

ASJC Scopus subject areas

  • Biochemistry
  • Molecular Medicine
  • Molecular Biology
  • Pharmaceutical Science
  • Drug Discovery
  • Clinical Biochemistry
  • Organic Chemistry

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