2-Amino-5-(heteroarylmethylene)-1,3,4-oxadiazoles/thiadiazoles 7-10 were synthesized by cyclisation of 1-(heteroarylacetyl)semicarbazides/thiosemicarbazides 3-6. 5-(2'-Heteroarylmethylene-5'-aminomethylene-1',3,'4'- oxadiazol-2'-yl/thiadiazol-2'-yl)-2-oxo/thiobarbituric acids 11-18 were synthesized by condensation of compounds 7-10 at the 5th position of 2-oxo/thiobarbituric acids. The newly synthesized compounds showed anticonvulsant activity ranging from 50-90% (seizures protection). Compound 18 (5-(2'-phenothiazinylmethylene-5'-aminomethylene-1',3',4'-thiadiazol-2'- yl)-2-thiobarbituric acid) showed maximum activity being more potent than the reference drug phenytoin sodium (CAS 630-93-3).
Download full-text PDF |
Source |
|---|---|
| http://dx.doi.org/10.1055/s-0031-1297113 | DOI Listing |
Publication Analysis
Top Keywords
Similar Publications
A Narrative Review of the Interplay Between Carbohydrate Intake and Diabetes Medications: Unexplored Connections and Clinical Implications.
Int J Mol Sci
January 2025
Department of Pharmacy, University of Limpopo, Mankweng 0727, South Africa.
This narrative review examines the dynamic interplay between carbohydrate intake and diabetes medications, highlighting their combined molecular and clinical effects on glycemic control. Carbohydrates, a primary energy source, significantly influence postprandial glucose regulation and necessitate careful coordination with pharmacological therapies, including insulin, metformin, glucagon-like peptide (GLP-1) receptor agonists, and sodium-glucose cotransporter-2 (SGLT2) inhibitors. Low-glycemic-index (GI) foods enhance insulin sensitivity, stabilize glycemic variability, and optimize medication efficacy, while high-GI foods exacerbate glycemic excursions and insulin resistance.
View Article and Find Full Text PDFTryptophan Kynurenine Pathway-Based Imaging Agents for Brain Disorders and Oncology-From Bench to Bedside.
Biomolecules
January 2025
Department of Radiology, Nemours Children's Health, Delaware, Wilmington, DE 19803, USA.
Tryptophan (Trp)-based radiotracers have excellent potential for imaging many different types of brain pathology because of their involvement with both the serotonergic and kynurenine (KYN) pathways. However, radiotracers specific to the kynurenine metabolism pathway are limited. In addition, historically Trp-based radiopharmaceuticals were synthesized with the short-lived isotope carbon-11.
View Article and Find Full Text PDFCracking the Code of Calcification: How Presence and Burden among Intracranial Arteries Influence Stroke Incidence and Recurrence.
AJNR Am J Neuroradiol
January 2025
University of Padova (M.C.); University of Bologna (M.O.A.); Department of Radiology (R.C, R.S., L.S.), Azienda Ospedaliero Universitaria (A.O.U.) di Cagliari, Cagliari, Sardegna, Italy; Department of Neurology and Stroke Program (S.C.), University of Maryland School of Medicine, Baltimore, Maryland, United States; CVPath Institute (R.V.), Gaithersburg, Maryland, United States; Department of Radiology (G.DR.), Azienda San Camillo Forlanini, Rome, Lazio, Italy; Department of Epidemiology (D.B.), Erasmus Medical Center, Rotterdam, South Holland, Netherlands; Department of Radiology and Nuclear Medicine (D.B.), Erasmus Medical Center, Rotterdam, South Holland, Netherlands; Mayo Clinic (L.S.), Rochester, Minnesota, United States.
Background: Intracranial atherosclerosis accounts for about 8% of all strokes in Western societies but the influence of arterial calcification on plaque instability is a topic on ongoing debate.
Purpose: Explore the association between the presence and burden of calcium in atherosclerotic plaques among intracranial arteries with the risk of clinical or silent stroke events through a systematic review and meta-analysis.
Data Sources: Adhering to PRISMA guidelines, studies from PubMed and Embase were analyzed up to May 2024.
Unraveling the synthetic strategy, structure activity relationship of azetidinones: Insights into their multidrug and toxin extrusion protein (MATE transporter) inhibition facilitating drug development against MDR.
Bioorg Chem
January 2025
Medicinal Chemistry Research Laboratory, School of Pharmaceutical Sciences, Siksha 'O' Anusandhan (Deemed to be University), Campus-2, Ghatikia, Kalinga Nagar, Bhubaneswar, Odisha 751003, India. Electronic address:
Heterocyclic chemistry gathered a wide audience due to their presence in potential drug candidates and being attractive synthons initiating several retro-syntheses the organic as well as in medicinal chemistry fields. Among them, azetidinones have been a subject of discussion due to their serendipity, curiosity, versatility by Penicillin and Cephalosporins as β-lactam antibiotics. Despite possessing a large margin of biological activities, azetidinones mainly work as antimicrobial, interfering with bacterial cell-wall synthesis blocking transpeptidase.
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!