Replacement of the core beta-amino acid in our previously reported piperidine acetic acid and beta-phenylalanine-based Bradykinin B1 antagonists by dihydroquinoxalinone acetic acid increases the in vitro potency and metabolic stability. The most potent compounds from this series have IC(50)s<0.2 nM in a human B1 receptor functional assay. A molecular modeling study of the binding modes of key compounds, based on a B1 homology model, explains the structure-activity relationship (SAR) for these analogs.
Download full-text PDF |
Source |
|---|---|
| http://dx.doi.org/10.1016/j.bmcl.2008.07.055 | DOI Listing |
Publication Analysis
Top Keywords
Similar Publications
Reproductive Health Among School Employees in Vijayapura, Karnataka.
Cureus
December 2024
Obstetrics and Gynecology, Shri B M Patil Medical College Hospital and Research Centre, BLDE (Deemed to be University), Vijayapura, IND.
Background Cervical cancer typically progresses over 10-20 years, making it a preventable disease and underscoring the importance of screening. In low-resource settings, Papanicolaou (Pap) smears and visual inspection with acetic acid (VIA) serve as primary screening tools. This study was conducted as part of the noncommunicable disease camps organized by the government of Karnataka, India.
View Article and Find Full Text PDFEffect of hempseed meal on health, growth performance, ruminal fermentation, and carcass traits of intact male goats.
Transl Anim Sci
December 2024
Department of Agricultural and Environmental Sciences, College of Agriculture, Environment and Nutrition Sciences, Tuskegee University, Tuskegee, AL 36088, USA.
Hempseed meal (HSM) is a potential alternative feedstuff for livestock due to its high protein content, but it has not been approved for animal feed in the United States due to safety concerns. This study was conducted to determine the effects of HSM on feed intake, growth performance, serum biochemistry, ruminal papillae morphology, ruminal fermentation profiles, and carcass characteristics of intact male goats. Thirty-six Boer × Spanish intact male goats were randomly assigned to one of four experimental diets ( = 9 goats/diet): 0%, 10%, 20%, and 30% HSM on as-fed basis.
View Article and Find Full Text PDFIntegrated role of biochar and PGPR (Leclercia adecarboxylata HW04) in enhancing cadmium phytoremediation and stress tolerance in Glycine max L.
Plant Physiol Biochem
January 2025
Department of Applied Biosciences, Kyungpook National University, 41566, Daegu, Republic of Korea. Electronic address:
Plant growth-promoting rhizobacteria (PGPR) and biochar (BC) are recognized as effective biological agents for enhancing stress tolerance and mitigating heavy metal toxicity in crops. Therefore, this study aims to investigate the effects of the cadmium (Cd)-resistant PGPR strain Leclercia adecarboxylata HW04 (>4 mM Cd resistance) on soybean plants exposed to 300 μM Cd. HW04 was observed to possess the innate ability to synthesize indole-3-acetic acid and exopolysaccharides, which facilitated the absorption of Cd in the medium.
View Article and Find Full Text PDFComplex transcription regulation of acidic chitinase suggests fine-tuning of digestive processes in Drosera binata.
Planta
January 2025
Institute of Plant Genetics and Biotechnology, Plant Science and Biodiversity Center, Slovak Academy of Sciences, Akademicka 2, P. O. Box 39A, 950 07, Nitra, Slovak Republic.
DbChitI-3, Drosera binata's acidic chitinase, peaks at pH 2.5 from 15 °C to 30 °C. Gene expression is stimulated by polysaccharides and suppressed by monosaccharide digestion, implying a feedback loop in its transcriptional regulation.
View Article and Find Full Text PDFEvaluation of the anti-cholelithiasis activity of vinegar-soaked Ficus carica fruit in adults: A randomized controlled trial.
Pak J Pharm Sci
January 2025
Department of Pathobiology and Biomedical Sciences, Muhammad Nawaz Sharif University of Agriculture, Multan, Pakistan/Ali-Ul-Murtaza Department of Rehabilitation Sciences, Muhammad Institute of Medical and Allied Sciences, Multan, Pakistan.
This study aimed to evaluate the efficacy of vinegar-soaked Ficus carica fruits (VSFCF) for managing cholelithiasis in adults. A parallel-group, single-blinded, randomized controlled trial at Noreen Nishat Welfare Hospital, Khanewal, Pakistan, was conducted from December 2023 to February 2024. Fifty adults with ultrasound-confirmed cholelithiasis were randomly assigned to receive either VSFCF (1 g/kg/day) or ursodiol (600 mg/day).
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!