Abstract
Fifteen analogues of benzenepropanamine were synthesized and evaluated for their spermicidal as well as microbicidal activities against Trichomonas vaginalis and Candida spp. Several compounds showed appreciable dual activities. Compound 12 exhibited good spermicidal (MEC=0.1%) along with substantial anticandidal (MIC=0.05%) activities, while compounds 3 and 6 showed significant microbicidal activities with moderate spermicidal effect. The SAR of these structures is being discussed here in this communication. It is concluded that suitable structural modifications in this class of compounds at 3-amino position may lead to a potent spermicide with associated microbicidal activity.
Publication types
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Research Support, Non-U.S. Gov't
MeSH terms
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Adult
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Amines / chemistry
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Amines / pharmacology*
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Animals
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Antifungal Agents / chemical synthesis*
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Antifungal Agents / chemistry
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Antifungal Agents / pharmacology*
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Antitrichomonal Agents / chemical synthesis*
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Antitrichomonal Agents / chemistry
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Antitrichomonal Agents / pharmacology*
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Benzene Derivatives / chemistry
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Benzene Derivatives / pharmacology*
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Candida albicans / drug effects
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Cell Survival / drug effects
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Chemical Phenomena
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Chemistry, Physical
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Humans
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In Vitro Techniques
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Male
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Microbial Sensitivity Tests
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Spectroscopy, Fourier Transform Infrared
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Spermatocidal Agents / chemical synthesis*
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Spermatocidal Agents / chemistry
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Spermatocidal Agents / pharmacology*
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Spermatozoa / drug effects
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Structure-Activity Relationship
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Trichomonas vaginalis / drug effects
Substances
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Amines
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Antifungal Agents
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Antitrichomonal Agents
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Benzene Derivatives
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Spermatocidal Agents