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.

Download full-text PDF

Source
http://dx.doi.org/10.1021/jm00145a008DOI Listing

Publication Analysis

Top Keywords

cyclopropyl methyl
8
ketone oxime
8
chiral isomeric
4
isomeric cyclopropyl
4
cyclopropyl ketoxime
4
ketoxime propanolamine
4
propanolamine derivatives
4
derivatives potent
4
potent beta-adrenergic
4
beta-adrenergic blocking
4

Similar Publications

Ab Initio Rotational and Vibrational Spectroscopy of CH Radicals at the Coupled Cluster Level.

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 PDF

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 PDF

Pesticide contamination and associated ecological risks in estuarine waters of Brazil's Legal Amazon.

Environ 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 PDF

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.

View Article and Find Full Text PDF

Want AI Summaries of new PubMed Abstracts delivered to your In-box?

Enter search terms and have AI summaries delivered each week - change queries or unsubscribe any time!