26595-60-8Relevant articles and documents
Synthesis and Physical Properties of Thiol-Ene Networks Utilizing Plant-Derived Phenolic Acids
Yang, Guozhen,Kristufek, Samantha L.,Link, Lauren A.,Wooley, Karen L.,Robertson, Megan L.
, p. 8418 - 8427 (2015)
Elastomeric polymer films synthesized through thiol-ene chemistry, suitable in applications as coatings and adhesives due to their ease of preparation and superior physical properties, are traditionally derived from petroleum sources. Of recent interest i
Synthesis of Albicidin Derivatives: Assessing the Role of N-terminal Acylation on the Antibacterial Activity
Kerwat, Dennis,Gr?tz, Stefan,Kretz, Julian,Seidel, Maria,Kunert, Maria,Weston, John B.,Süssmuth, Roderich D.
supporting information, p. 1899 - 1903 (2016/10/12)
The peptide antibiotic albicidin, which is synthesized by the plant pathogenic bacterium, Xanthomonas albilineans, represents the most prominent member of a new class of antibacterial gyrase inhibitors. It shows remarkable antibacterial activities against Gram-positive and Gram-negative microorganisms. Its unique structure potentially represents a new lead structure for the development of an antibacterial drug. Here we report the synthesis of 14 albicidin derivatives with structural variations at the N-terminus, primarily investigating the effects of variation of cinnamoyl, phenylpropanoyl, and benzoyl residues. Gyrase inhibition in vitro and determination of minimal inhibitory concentrations were assessed in parallel. Activities in a nanomolar range and the importance of N-acylation were demonstrated.
Discovery of benzamide analogs as negative allosteric modulators of human neuronal nicotinic receptors: Pharmacophore modeling and structure-activity relationship studies
Yi, Bitna,Long, Sihui,González-Cestari, Tatiana F.,Henderson, Brandon J.,Pavlovicz, Ryan E.,Werbovetz, Karl,Li, Chenglong,McKay, Dennis B.
, p. 4730 - 4743 (2013/07/26)
The present study describes our ongoing efforts toward the discovery of drugs that selectively target nAChR subtypes. We exploited knowledge on nAChR ligands and their binding site that were previously identified by our laboratory through virtual screenings and identified benzamide analogs as a novel chemical class of neuronal nicotinic receptor (nAChR) ligands. The lead molecule, compound 1 (4-(allyloxy)-N-(6-methylpyridin-2-yl)benzamide) inhibits nAChR activity with an IC50 value of 6.0 (3.4-10.6) μM on human α4β2 nAChRs with a ～5-fold preference against human α3β4 nAChRs. Twenty-six analogs of compound 1 were also either synthesized or purchased for structure-activity relationship (SAR) studies and provided information relating the chemical/structural properties of the molecules to their ability to inhibit nAChR activity. The discovery of subtype-selective ligands of nAChRs described here should contribute significantly to our understanding of the involvement of specific nAChR subtypes in normal and pathophysiological states.
