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Transferrin conjugates of antitubercular drug isoniazid: Synthesis and in vitro efficacy.

Abstract：

:Tuberculosis (TB) caused by Mycobacterium tuberculosis (Mtb) has become the world's leading killer disease due to a single infectious agent which survives in the host macrophage for the indefinite period. Hence, it is necessary to enhance the efficacy of the clinically existing antitubercular agents or to discover new anti antitubercular agents. Here, we report the synthesis, characterization and antimycobacterial evaluation of protein-drug conjugates. A carrier protein, Transferrin (Tf) was covalently conjugated to isoniazid (INH) utilizing hydrazone and amide linkers. The purity of the reactions was confirmed by SDS-PAGE while conjugation was confirmed by UV-visible spectrophotometry, MALDI-TOF analysis, and FTIR spectrophotometry. The in vitro antitubercular assay result showed that the inhibitory activity of the parent drug was conserved in both the conjugates. The conjugates were effective against intracellular Mtb H37Rv and were devoid of cytotoxic effect at therapeutic concentration.

journal_name

Eur J Med Chem

journal_title

European journal of medicinal chemistry

authors

Sutar YB,Mali JK,Telvekar VN,Rajmani RS,Singh A

doi

10.1016/j.ejmech.2019.111713

subject

Has Abstract

pub_date

2019-12-01 00:00:00

pages

111713

eissn

0223-5234

issn

1768-3254

pii

S0223-5234(19)30865-7

journal_volume

183

pub_type

杂志文章

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