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Publication Details
AFRICAN RESEARCH NEXUS
SHINING A SPOTLIGHT ON AFRICAN RESEARCH
biochemistry, genetics and molecular biology
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
Bioorganic and Medicinal Chemistry Letters, Volume 22, No. 17, Year 2012
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Description
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. © 2012 Elsevier Ltd. All rights reserved.
Authors & Co-Authors
Singh, Girija Shankar
Botswana, Gaborone
University of Botswana
Al-Kahraman, Yasser M.S.A.
Pakistan, Quetta
University of Balochistan
Mpadi, Disah
Botswana, Gaborone
University of Botswana
Yasinzai, Masoom
Pakistan, Islamabad
Quaid-i-azam University
Statistics
Citations: 16
Authors: 4
Affiliations: 3
Identifiers
Doi:
10.1016/j.bmcl.2012.06.081
ISSN:
0960894X
e-ISSN:
14643405