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Synthesis of diverse (E)‐2‐((1 H ‐imidazol‐1‐yl)methyl)‐2‐((benzyloxy)methyl)‐2,3‐dihydro‐1 H ‐inden‐1‐one O‐benzyl oxime derivatives as potent antileishmanial agents
Author(s) -
Surwase Santosh M.,
Mane Yogesh D.,
Surwase Mahesh M.,
Khade Bhimrao C.
Publication year - 2020
Publication title -
journal of heterocyclic chemistry
Language(s) - English
Resource type - Journals
SCImago Journal Rank - 0.321
H-Index - 59
eISSN - 1943-5193
pISSN - 0022-152X
DOI - 10.1002/jhet.3812
Subject(s) - chemistry , amastigote , potency , oxime , leishmania donovani , stereochemistry , in vitro , leishmania major , leishmania , medicinal chemistry , biochemistry , parasite hosting , world wide web , computer science
A series of (E)‐2‐((1 H ‐imidazol‐1‐yl)methyl)‐2‐((benzyloxy)methyl)‐2,3‐dihydro‐1 H ‐inden‐1‐one O‐benzyl oximes ( 6a‐j ) were prepared and evaluated for their in vitro antileishmanial potency against Leishmania donovani (in promastigote and amastigote models). At a concentration of 05‐μg/mL, compounds 3a‐d , 4a‐d , 5a , 5b , 6a‐d, and 7a‐d exhibited 97% to 100% and 87% to 100% inhibition against promastigotes and amastigotes, respectively. Compounds 6a , 6d‐6j and 6a , 6i , 6j exhibited equal antileishmanial potency to that of SSG and Pentamidin at lower values of IC 50 .