Products Cited in Publications Worldwide 6-Phenoxyl-4-aminoquinoline: synthesis and preliminary antitubercular-structure activity relationship analyses

6-Phenoxyl-4-aminoquinoline: synthesis and preliminary antitubercular-structure activity relationship analyses

Beteck, Richard M; Legoabe, Lesetja J; Dube, Phelelisiwe S; Jordaan, Audrey; Warner, Digby F

DOI:

Abstract

and quinoline based compounds have been reported to show activity. Against Mycobacterium tuberculosis, drug targets inhibited by compounds are reportedly different from those perturbed by quinoline based antitubercular hits/drugs. Herein, we conceptualized and synthesized novel molecules incorporating quinoline and moieties. The antitubercular property of the synthesized compounds were measured in vitro using Tween 80 and Tyloxapol supplemented growth media. Compounds in this study generally showed sub micromolar antitubercular activity in tween 80/ albumin supplemented growth medium, and moderate to poor activity in tyloxapol/casitone supplemented growth medium. Compound 4e, havin a trimethylenediamine moiety and low melting point of 68°C, emerged as the hit compound, possessing MIC90 value of 0.2 µM. 4e is non-cytotoxic when tested against normal human cell line, exhibiting CC50 value > 20 µM.

Keywords

Quinoline ; Diphenyl ether ; Tuberculosis ; Cytotoxicity ; Antitubercular

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4-Phenoxyaniline

A1003174139-59-397%

4-Phenoxyaniline

38.0/100g

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Potassium carbonate

A1457891584-08-720% in Deionized water

Potassium carbonate

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