Piperidine, pyrrolidine, and azetidine sulfonamides were examined as linkers in designing novel human beta(3) adrenergic receptor (beta(3)-AR) agonists. The azetidine derivative 37, and piperidine derivatives 7, 8, and 13 were found to be potent beta(3)-AR agonists and have good selectivity against beta(1)- and beta(2)-AR.

Download full-text PDF

Source
http://dx.doi.org/10.1016/s0960-894x(03)00387-1DOI Listing

Publication Analysis

Top Keywords

novel human
8
human beta3
8
beta3 adrenergic
8
adrenergic receptor
8
beta3-ar agonists
8
cyclic amine
4
amine sulfonamides
4
sulfonamides linkers
4
linkers design
4
design synthesis
4

Similar Publications

Objectives: Acute T-cell lymphoblastic leukemia (T-ALL) is a severe hematologic malignancy with limited treatment options and poor long-term survival. This study explores the role of IKZF1 in regulating BCL-2 expression in T-ALL.

Methods: CUT&Tag and CUT&Run assays were employed to assess IKZF1 binding to the BCL-2 promoter.

View Article and Find Full Text PDF

Background: The burden of hospital-acquired infections (HAIs) equates to 3.5 million cases, resulting in more than 90 000 deaths and 2.5 million disability-adjusted life years (DALYs) across Europe.

View Article and Find Full Text PDF

Municipal waste classification is significant for effective recycling and waste management processes that involve the classification of diverse municipal waste materials such as paper, glass, plastic, and organic matter using diverse techniques. Yet, this municipal waste classification process faces several challenges, such as high computational complexity, more time consumption, and high variability in the appearance of waste caused by variations in color, type, and degradation level, which makes an inaccurate waste classification process. To overcome these challenges, this research proposes a novel Channel and Spatial Attention-Based Multiblock Convolutional Network for accurately classifying municipal waste that utilizes a unique attention mechanism for enhancing feature learning and waste classification accuracy.

View Article and Find Full Text PDF

Novel Surgical Initiatives in Gastroenteropancreatic Neuroendocrine Tumours.

Curr Oncol Rep

January 2025

Department of General, Visceral and Thoracic Surgery, University Medical Center Hamburg- Eppendorf, Martinistraße 52, D-20246, Hamburg, Germany.

Purpose Of Review: Neuroendocrine tumours (NET) are rare entities arising from hormone producing cells in the gastroentero-pancreatic (GEP) tract. Surgery is the most common treatment of GEP-NETs.

Recent Findings: Improvements in surgical techniques allow for more locally advanced and metastasised GEP-NETs to be resected.

View Article and Find Full Text PDF

Disruption of the mycobacterial redox homeostasis leads to irreversible stress induction and cell death. Hydroquinone scaffolds, as a new type of redox cycling anti-tuberculosis chemotypes, exhibit potent bactericidal activity against non-replicating, nutrient-deprived phenotypically drug-resistant bacteria. Evidences from microbiological, biochemical, and genetic studies indicate that the redox-driven mode of action relies on the reduction of quinones by type II NADH dehydrogenase (NDH2), generating reactive oxygen species (ROS) of bactericidal level.

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!