Synthesis of N-(1-methyl-1H-indol-3-yl)methyleneamines and 3,3-diaryl-4-(1-methyl-1H-indol-3-yl)azetidin-2-ones as potential antileishmanial agents

Journal article

Authors / Editors

Mpadi, Disah

Research Areas

ENGINEERING AND TECHNOLOGY (Frascati classification)

Publication Details

Subtitle: Synthesis of N-(1-methyl-1H-indol-3-yl)methyleneamines and 3,3-diaryl-4-(1-methyl-1H-indol-3-yl)azetidin-2-ones as potential antileishmanial agents

Author list: Mpadi, Disah

Publisher: Elsevier

Publication year: 2012

Journal: Bioorganic & Medicinal Chemistry Letters (0960-894X)

Volume number: 22

Issue number: 17

Start page: 5704

End page: 5706

Number of pages: 3

ISSN: 0960-894X

URL: https://www.sciencedirect.com/science/article/pii/S0960894X12008414

Languages: English-United States (EN-US)

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Abstract

A series of N-(1-methyl-1H-indol-3-yl)methyleneamines and eight new 3,3-diaryl-4-(1-methyl-1H-indol-3-yl)azetidin-2-ones have been synthesized and screened for their antileishmanial activity against Leishmania major. 3,3-Diaryl-4-(1-methyl-1H-indol-3-yl)azetidin-2-ones have been synthesized by the Staudinger's ketene-imine cycloaddition employing two 2-diazo-1,2- diarylethanones as the precursors of diarylketenes. A marked improvement in anti-parasitic activity is observed by transformation of the methyleneamines to azetidin-2-ones in seven out of eight compounds. Two compounds displayed antileishmanial activity comparable to that of the clinically used antileshmanial drug, amphotericine B.

Keywords

AzomethinesAzetidin-2-ones1-Methyl-1H-indoleAntileishmanial

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