β-Amino acids sharing a lipophilic diaromatic side chain were synthesized and characterized pharmacologically on mouse GABA transporter subtypes mGAT1-4. The parent amino acids were also characterized. Compounds 13a, 13b, and 17b displayed more than 6-fold selectivity for mGAT2 over mGAT1. Compound 17b displayed anticonvulsive properties inferring a role of mGAT2 in epileptic disorders. These results provide new neuropharmacological tools and a strategy for designing subtype selective GABA transport inhibitors.
Download full-text PDF |
Source |
|---|---|
| http://dx.doi.org/10.1021/jm301872x | DOI Listing |
Publication Analysis
Top Keywords
Similar Publications
Design and synthesis of novel 2-(2-(4-bromophenyl)quinolin-4-yl)-1,3,4-oxadiazole derivatives as anticancer and antimicrobial candidates: and studies.
RSC Adv
October 2024
Pharmaceutical Chemistry Department, College of Pharmaceutical Sciences and Drug Manufacturing, Misr University for Science and Technology 6th of October City, P.O. Box 77 Giza Egypt.
Cancer is the second leading cause of death globally, surpassed only by heart disease. Moreover, bacterial infections remain a significant global health burden, contributing substantially to morbidity and mortality, especially among hospitalized patients. EGFR has emerged as a prime therapeutic target due to its pivotal role in driving uncontrolled cell growth and survival across numerous cancer types.
View Article and Find Full Text PDFGenetic diversity and genomic epidemiology of SARS-CoV-2 during the first 3 years of the pandemic in Morocco: comprehensive sequence analysis, including the unique lineage B.1.528 in Morocco.
Access Microbiol
October 2024
Laboratory of Physiopathology and Molecular Genetics, Faculty of Sciences Ben M'Sik, Hassan II University of Casablanca (Morocco), Avenue Cdt Driss El Harti, PB 7955 Sidi Othman, Casablanca, Morocco.
During the 3 years following the emergence of the COVID-19 pandemic, the African continent, like other regions of the world, was substantially impacted by COVID-19. In Morocco, the COVID-19 pandemic has been marked by the emergence and spread of several SARS-CoV-2 variants, leading to a substantial increase in the incidence of infections and deaths. Nevertheless, the comprehensive understanding of the genetic diversity, evolution, and epidemiology of several viral lineages remained limited in Morocco.
View Article and Find Full Text PDFA seawater field study of crude and fuel oil depletion in Northern Norway at two different seasons - Chemistry and bacterial communities.
Mar Pollut Bull
October 2024
SINTEF Ocean, Dept. Climate and Environment, Brattørkaia 17b, 7010 Trondheim, Norway. Electronic address:
After marine oil spills, natural processes like photooxidation and biodegradation can remove the oil from the environment. However, these processes are strongly influenced by environmental conditions. To achieve a greater understanding of how seasonal variations in temperature, light exposure and the bacterial community affect oil depletion in the marine environment, we performed two field experiments during the spring and autumn.
View Article and Find Full Text PDFNew substituted benzenesulphonamoyl 'Cys-Gly' dipeptide carboxamide derivatives: Design, synthesis, characterization and pharmacological studies.
Bioorg Chem
November 2024
Department of Pure and Industrial Chemistry, University of Nigeria, Nsukka 410001, Enugu State, Nigeria.
Twelve new sulphonamide (Cys-Gly) dipeptide carboxamide derivatives 17a-17l were designed, prepared and characterized through spectroscopic techniques and their pharmacological properties investigated. The molecular docking analyses revealed good interactions of the derivatives with the desired amino residues active pockets. In vitro antimicrobial, in vivo antimalarial, haematological and other related tests (liver and kidney) were also conducted.
View Article and Find Full Text PDFDifferences in bacterial taxa between treatment-naive patients with major depressive disorder and non-affected controls may be related to a proinflammatory profile.
BMC Psychiatry
January 2024
Centre for Clinical Research, North Denmark Regional Hospital, Bispensgade 37, Hjørring, 9800, Denmark.
Background: Major depressive disorder (MDD) is characterized by sadness and anhedonia, but also physical symptoms such as changes in appetite and weight. Gut microbiota has been hypothesized to be involved in MDD through gut-brain axis signaling. Moreover, antidepressants display antibacterial properties in the gastrointestinal tract.
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!