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 | Zendy

Surwase Santosh M. | Zendy; Mane Yogesh D. | Zendy; Surwase Mahesh M. | Zendy; Khade Bhimrao C. | Zendy

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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 .

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