Imidazoline- and Benzamidine-Based Trypanosome Alternative Oxidase Inhibitors: Synthesis and Structure–Activity Relationship Studies
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DOI: 10.1021/acsmedchemlett.1c00717.s001
Abstract: The trypanosome alternative oxidase (TAO), a mitochondrial enzyme involved in the respiration of the bloodstream form trypomastigotes of Trypanosoma brucei, is a validated drug target against African trypanosomes. Earlier series of TAO inhibitors having a… read more here.
Keywords: alternative oxidase; structure activity; relationship studies; activity relationship ... See more keywords
Stereochemical Structure Activity Relationship Studies (S-SAR) of Tetrahydrolipstatin.
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DOI: 10.1021/acsmedchemlett.8b00050
Abstract: Tetrahydrolipstatin (THL), its enantiomer, and an additional six diastereomers were evaluated as inhibitors of the hydrolysis of p-nitrophenyl butyrate by porcine pancreatic lipase. IC50s were found for all eight stereoisomers ranging from a low of… read more here.
Keywords: relationship studies; stereochemical structure; sar tetrahydrolipstatin; activity relationship ... See more keywords
Structure-activity relationship studies for inhibitors for vancomycin-resistant Enterococcus and human carbonic anhydrases
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DOI: 10.1080/14756366.2022.2092729
Abstract: Abstract Vancomycin-resistant enterococci (VRE), consisting of pathogenic Enterococcus faecalis and E. faecium, is a leading cause of hospital-acquired infections (HAIs). We recently repurposed the FDA-approved human carbonic anhydrase (CA) inhibitor acetazolamide (AZM) against VRE agent… read more here.
Keywords: human carbonic; structure activity; relationship studies; vancomycin resistant ... See more keywords
Medicinal Perspective of Indole Derivatives: Recent Developments and Structure-Activity Relationship Studies.
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DOI: 10.2174/1389450121666200310115327
Abstract: Heterocyclic compounds play significant role in various biological processes of human body and many of them are in clinical use due to their diverse, chemical and biological properties. Among these, indole is one of most… read more here.
Keywords: relationship studies; indole derivatives; activity relationship; structure activity ... See more keywords