The synthesis of R-(+) and S-(-) isomers of O-[3-tert-butylamino)-2-hydroxypropyl] cyclopropyl methyl ketone oxime (falintolol) is described. The syn and anti isomers of falintolol were obtained in two different ways from cyclopropyl methyl ketoxime or from falintolol. For comparison purposes, the enantiomers of the dicyclopropyl ketone oxime derivatives were also prepared. Structure-activity relationships are described.
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http://dx.doi.org/10.1021/jm00145a008 | DOI Listing |
J Phys Chem A
January 2025
Department of Chemistry, University of California, Davis, One Shields Ave., Davis, California 95616, United States.
Combustion and pyrolysis processes of allene and propyne are known to involve radicals with the structural formula CH, the most stable of which is the classic resonance-stabilized allyl radical. In addition to allyl, four other isomers of CH are possible: the propene derivatives -1-propenyl, -1-propenyl, and 2-propenyl, as well as the cyclopropane derivative cyclopropyl. Among these 5 species, the allyl radical has been extensively studied both theoretically and spectroscopically; however, little is known about the spectroscopy of the cyclopropyl radical, and virtually no experimental spectroscopic data are available for the remaining three.
View Article and Find Full Text PDFArch Biochem Biophys
January 2025
Department of Biosciences Grand Asian University of Sialkot, Pakistan.
Acyl thiourea scaffolds are frequently employed in drug development to discern unique and essential therapies for the eradication of the most challenging diseases. Hence, we developed a library of novel cyclopropyl incorporating acyl thiourea derivatives (4a-j) and evaluated their antimicrobial, α-amylase, and proteinase K inhibition potential. Compound (4h) (4-methoxy) demonstrated the strongest α-amylase inhibition (IC = 1.
View Article and Find Full Text PDFEnviron Sci Pollut Res Int
January 2025
Laboratório de Química Analítica E Ecotoxicologia (LAEC), Federal University of Maranhão (UFMA), Av. Dos Portugueses, 1966, São Luís, Maranhão, 65080-805, Brazil.
Pesticide contamination remains a significant environmental concern globally, with important implications for aquatic ecosystems. Despite being one of the world's largest pesticide consumers, monitoring and assessment of pesticide pollution are limited in Brazil, especially in sensitive regions like the Amazon. In this study, the occurrence and environmental risks of 8 pesticides of different classes, namely alachlor, atrazine, chlorfenvinphos, isoproturon, irgarol, simazine, diuron, and its transformation product DCPMU (1-(3,4-dichlorophenyl)-3-methyl urea) were analysed in surface water of the São Marcos Estuarine Complex (SMEC) in two consecutive years.
View Article and Find Full Text PDFLiver Int
January 2025
Phase I Clinical Trial Center, the First Hospital of Jilin University, Jilin, China.
Background And Aims: Freethiadine is a novel hepatitis B virus capsid assembly modulator. Herein, we report the safety, tolerability, pharmacokinetics and 28-day antiviral activities of freethiadine.
Methods: The study consisted of two parts.
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