98%
921
2 minutes
20
Sulfur-containing pyrroles (1-3), tris(2-pyridyl)phosphine(selenide) sulfide (4-5) and 4-benzyl-6-(thiophen-2-yl)pyrimidin-2-amine (6) were synthesized and characterized by elemental analysis, IR and NMR spectra. In this study, the synthesized compounds of nitrogen, phosphorus, selenium and sulfur-containing heterocyclic compounds (1-6) were evaluated against the human erythrocyte carbonic anhydrase I, and II isoenzymes, acetylcholinesterase (AChE), butyrylcholinesterase (BChE), and α-glycosidase enzymes. The synthesized heterocyclic compounds showed IC values in range of 33.32-60.79 nM against hCA I, and 37.05-66.64 nM against hCA II closely associated with various physiological and pathological processes. On the other hand, IC values were found in range of 13.13-22.21 nM against AChE, 0.54-31.22 nM against BChE, and 13.51-26.55 nM against α-glycosidase as a hydrolytic enzyme. As a result, nitrogen, phosphorus, selenium and sulfur-containing heterocyclic compounds (1-6) demonstrated potent inhibition profiles against indicated metabolic enzymes. Therefore, we believe that these results may contribute to the development of new drugs particularly in the treatment of some global disorders including glaucoma, Alzheimer's disease and diabetes.
Download full-text PDF |
Source |
---|---|
http://dx.doi.org/10.1016/j.bioorg.2020.104171 | DOI Listing |
Physiol Plant
September 2025
State Key Laboratory for Conservation and Utilization of Subtropical Agro-Bioresources, College of Agriculture, South China Agricultural University, Guangzhou, China.
The rice root system mediates nutrient uptake while adapting to tillage, management, and environmental changes. While optimized nitrogen (N) supply is known to enhance 2-acetyl-1-pyrroline (2-AP) biosynthesis in fragrant rice, the underlying mechanisms linking nitrogen availability, root development, and their combined effects on physiological processes and aroma formation remain unclear. To address this knowledge gap, we conducted a pot experiment employing two fragrant rice cultivars (Huahangxiangyinzhen and Qingxiangyou19xiang) under three nitrogen regimes (0, 1.
View Article and Find Full Text PDFArch Pharm (Weinheim)
September 2025
Chemistry Department, Faculty of Science, Ain Shams University, Cairo, Egypt.
Through applying the hybridization technique, new coumarin derivatives (2-17) were prepared with substitution at coumarin C-3 utilizing various heterocyclic derivatives, aiming to afford multi-target carbonic anhydrases (CAs) IX/XII and topoisomerase II (Topo II) inhibitors with potent antiproliferative activity. Eight different cell lines were used to evaluate the growth inhibition percentages (GI%) of cancer cells determined by coumarin analogues 1-17. Analogues 16 and 17 had the most substantial cytotoxic effects, achieving mean GI% of 86.
View Article and Find Full Text PDFBrain Behav
September 2025
Department of Neurology, NHO Nishiniigata Chuo Hospital, Niigata, Japan.
Background: Y69H (p.Y89H) variant hereditary transthyretin (ATTRv) amyloidosis causes meningeal amyloidosis, with mutant TTR deposits localized to the leptomeninges and vitreous body.
Methods: The effect of tafamidis meglumine on neurological disorders, such as the frequency of transient focal neurological episodes (TFNEs), magnetic resonance imaging (MRI) findings, and TTR levels in cerebrospinal fluid, was investigated in two patients diagnosed with Y69H ATTRv mutation.
Mycoses
September 2025
Grupo Infección e Inmunidad, Facultad Ciencias de la Salud, Universidad Tecnológica de Pereira, Pereira, Risaralda, Colombia.
Background: Malassezia genus includes lipodependent commensal yeasts of humans and animals' skin and mucous membranes. It can cause dermatological pathologies, and azoles are mainly used for treatment. However, in vitro susceptibility testing has shown decreased sensitivity to these antifungals.
View Article and Find Full Text PDFFuture Med Chem
September 2025
Department of Pharmaceutical Chemistry, Faculty of Pharmacy, Anadolu University, Eskişehir, Turkey.
In this review, the primary aim is to examine non-azole ring systems that have analgesic activity and, where applicable, to establish structure - activity relationships (SARs) with the nine major pathways, prostaglandin synthesis inhibition, opioid receptor modulation, sodium channel blockade, enhancement of serotonin and norepinephrine levels, cannabinoid receptor (CBR) binding, N-methyl-D-aspartate (NMDA) receptor antagonism, transient receptor potential cation channel subfamily V member 1 (TRPV1) antagonism, and P2X purinergic receptor blockade, have been described for pain relief. Analgesic effects have been observed in compounds containing ring systems such as piperidine, piperazine, pyridine, pyridazine, pyrazine, morpholine, thiomorpholine, pyran, thiopyran, indane, benzofuran, benzothiophene, quinoline, quinazoline, and chromene. These ring systems were classified in the whole study, first according to their molecular weights and then by bioisosteric similarity as same as first part.
View Article and Find Full Text PDF