Abstract
A series of aryloxy alkyl/aryl alkyl imidazoles were synthesized and evaluated in vitro as antileishmanials against Leishmania donovani. All the 19 compounds exhibited 94-100% inhibition at 10microg/mL against promastigotes and 12 compounds exhibited high inhibition with an IC(50) in the range of 0.47-4.85microg/mL against amastigotes. Promising compounds were tested further in vivo. Among all, compounds 4 and 23 with 4-CF(3) aryloxy moiety exhibited medium in vivo inhibition of 58-60%, thus providing new structural lead for antileishmanials.
Copyright 2009 Elsevier Ltd. All rights reserved.
Publication types
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Research Support, Non-U.S. Gov't
MeSH terms
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Antigens, Protozoan / metabolism
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Antigens, Surface / metabolism
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Antiprotozoal Agents / chemical synthesis*
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Antiprotozoal Agents / chemistry
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Antiprotozoal Agents / pharmacology
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Cyclohexanes / chemistry
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Imidazoles / chemical synthesis*
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Imidazoles / chemistry
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Imidazoles / pharmacology
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Leishmania donovani / drug effects
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Membrane Proteins / antagonists & inhibitors
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Membrane Proteins / metabolism
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Neuraminidase / antagonists & inhibitors
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Neuraminidase / metabolism
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Protozoan Proteins / antagonists & inhibitors
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Protozoan Proteins / metabolism
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Structure-Activity Relationship
Substances
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Antigens, Protozoan
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Antigens, Surface
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Antiprotozoal Agents
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Cyclohexanes
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Imidazoles
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Membrane Proteins
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Protozoan Proteins
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surface antigen P2, Leishmania
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Cyclohexane
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amastigote surface protein-1
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Neuraminidase