Described herein is design, synthesis, and biological evaluation of novel series of 2-aryl-7-(3',4'-dialkoxyphenyl)-pyrazolo[1,5-a]pyrimidines acting as inhibitors of type 4 phosphodiesterase (PDE4) which is known as a good target for the treatment of asthma and COPD. For this purpose, structure optimization was conducted with the aid of structure-based drug design using the known X-ray crystallography. Also, biological effects of these compounds on the target enzyme were evaluated by using in vitro assays, leading to the potent and selective PDE-4 inhibitor (IC(50)<10nM).
Download full-text PDF |
Source |
|---|---|
| http://dx.doi.org/10.1016/j.bmcl.2009.12.070 | DOI Listing |
Publication Analysis
Top Keywords
Similar Publications
Nitroglycerine for retained placenta: a meta-analysis of randomized controlled trials.
Am J Obstet Gynecol MFM
January 2025
Division of Maternal-Fetal Medicine, Department of Obstetrics and Gynecology, Sidney Kimmel Medical College of Thomas Jefferson University, Philadelphia, PA, USA. Electronic address:
Objective: To evaluate the effect of nitroglycerine on placenta delivery after retained placenta DESIGN: Systematic review with meta-analysis DATA SOURCES: MEDLINE, PROSPERO, Scopus, ClinicalTrials.gov, EMBASE, Sciencedirect, the Cochrane Library, Scielo were searched from their inception until February 2024.
Eligibility Criteria For Selecting Studies: We included all randomized clinical trials comparing use of nitroglycerine (i.
Current strategies in design and synthesis of antifungals hybrid and chimeric diazine derivatives.
Bioorg Med Chem
January 2025
Alexandru Ioan Cuza University of Iasi, Faculty of Chemistry, Bd. Carol 11, 700506 Iasi, Romania. Electronic address:
In the last decades fungal infections became a major threat to human health having an unacceptably occurrence, a high rate of mortality and the number of patients at risk for these infections continue to increase every year. An effective, modern and very useful strategy in antifungal therapy is represented by the use of chimeric and hybrid drugs, most of them being with azaheterocycle skeleton. In this review, we present an overview from the last five years of the most representative achievements in the field of chimeric and hybrid diazine derivatives with antifungal properties.
View Article and Find Full Text PDFGalactinol synthase 4 influences plant height by affecting phenylpropanoid metabolism and the balance of soluble carbohydrates in tomato.
Plant Physiol Biochem
January 2025
Modern Protected Horticulture Engineering & Technology Center, College of Horticulture, Shenyang Agricultural University, China; National & Local Joint Engineering Research Center of Northern Horticultural Facilities Design & Application Technology (Liaoning), Shenyang, China; Key Laboratory of Protected Horticulture (Shenyang Agricultural University), Ministry of Education, Shenyang, China; Key Laboratory of Horticultural Equipment, Ministry of Agriculture and Rural Affairs, Shenyang, China. Electronic address:
Plant height is a key trait that significantly influences plant architecture, disease resistance, adaptability to mechanical cultivation, and overall economic yield. Galactinol synthase (GolS) is a crucial enzyme involved in the biosynthesis of raffinose family oligosaccharides (RFOs). It plays a significant role in carbohydrate transport and storage, combating abiotic and biotic stresses, and regulating plant growth and development.
View Article and Find Full Text PDFSpatially constrained hyperpolarized 13C MRI pharmacokinetic rate constant map estimation using a digital brain phantom and a U-Net.
J Magn Reson
January 2025
UC Berkeley - UCSF Graduate Program in Bioengineering, 1700 4th St, San Francisco, CA 94158, USA; Radiology and Biomedical Imaging, University of California, San Francisco, 1700 4th St, San Francisco, CA 94158, USA.
Fitting rate constants to Hyperpolarized [1-C]Pyruvate (HP C13) MRI data is a promising approach for quantifying metabolism in vivo. Current methods typically fit each voxel of the dataset using a least-squares objective. With these methods, each voxel is considered independently, and the spatial relationships are not considered during fitting.
View Article and Find Full Text PDFDesign and synthesis of isatin derivative payloaded peptide-drug conjugate as tubulin inhibitor against colorectal cancer.
Eur J Med Chem
January 2025
China International Science and Technology Cooperation Base of Food Nutrition/Safety and Medicinal Chemistry, Tianjin University of Science and Technology, Tianjin, 300457, China. Electronic address:
A series of isatin derivatives which could inhibit colorectal cancer (CRC) were synthesized. Among those compounds, 5B exhibited good inhibitory activity of CRC through the inhibition of tubulin expression, inducing apoptosis, and causing G2/M phase cell cycle arrest pathway, which suggested that 5B could be a potential tubulin inhibitor. Based on that, a novel peptide-drug conjugate (PDC), which employed the CRC cells related receptor CD44 ligand peptide A6 coupling to 5B to accomplish A6-5B.
View Article and Find Full Text PDFWant 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!