A series of new 1,2,4‐triazole‐3‐one derivatives bearing the salicyl moiety were synthesized by using microwave irradiation, and their chemical structures identified IR, 1 H NMR, 13 C elemental analysis, LC‐MS. The anticonvulsant activities compounds 4a – c , 4e 5a e evaluated Anticonvulsant Screening Program National Institute Health, USA. had moderate in maximum electroshock‐induced seizure minimal clonic models mice, without any neurotoxic effects.

A chiral lipidomics approach was established for comprehensive profiling of regio- and stereoisomeric monoepoxy monohydroxy metabolites long-chain PUFAs as generated enzymatically by cytochromes P450 (CYPs), lipoxygenases (LOXs), cyclooxygenases (COXs) and, in part, also unspecific oxidations. The method relies on reversed-phase chiral-LC coupled with ESI/MS/MS. Applications revealed partially opposing enantioselectivities soluble microsomal epoxide hydrolases (mEHs). Ablation the hydrolase...

Epoxides derived from arachidonic acid (AA) are released during exercise and may contribute to vasodilation. However, also affect circulating levels of other epoxides cytochromes P450 (CYP) monooxygenase lipoxygenase (LOX) pathways, many whose exhibit cardiovascular activity in vitro. The effects on their have not been documented. We tested the hypothesis that acute, maximal would influence plasma concentrations these vasoactive substances. measured CYP LOX mediators both n − 3 6 fatty (FA)...

Abstract Azole antifungal drugs are commonly used in chemotherapy. Antibacterial effects of some topical antifungals, such as miconazole and econazole, have lately been revealed, which suggests a promising venue antimicrobial In this study, we tested an in‐house azole collection with properties for their antibacterial activity to identify dual‐acting hits using the broth microdilution method. The vitro screen yielded number potent derivatives against gram‐positive bacteria, Enterococcus...

In this study, hydroxy benzoin ( 1-7 ), benzil 8-14 and benzoin/benzil-O-β-D-glucosides 15-25 ) were synthesized to investigate their biological activities. An efficient method for synthesizing compounds 1 - 7 was prepared from four different benzaldehydes using an ultrasonic bath. Then, antioxidant (FRAP, CUPRAC, DPPH), antimicrobial (3 Gram (-), 4/6 (+), one tuberculosis fungus), enzyme inhibition (acetylcholinesterase, butyrylcholine esterase, tyrosinase, α-amylase, α- glucosidase) the...

Fatty acid (FA)-derived lipid products generated by cytochrome P450 (CYP), lipoxygenase (LOX), and cyclo-oxygenase (COX) influence cardiovascular function. However, plasma measurements invariably ignore 40% of the blood specimen, namely erythrocytes. These red cells (RBCs) represent a cell mass about 3 kg. RBCs are potential reservoir for epoxy fatty acids, which on release could regulate vascular capacity. We tested hypothesis that maximal physical activity would status in RBCs. used...

Factors causing the increased cardiovascular morbidity and mortality in hemodialysis (HD) patients are largely unknown. Oxylipins a superclass of lipid mediators with potent bioactivities produced from oxygenation polyunsaturated fatty acids. We previously assessed impact HD on oxylipins arterial blood plasma found that increases several oxylipins. To study phenomenon further, we now evaluated differences venous undergoing HD. collected samples upper extremities 12 end-stage renal disease...

Novel 2‐substitutedbenzyl‐4(7)‐phenyl‐1 H ‐benzo[d]imidazole compounds were synthesized and characterized. Although 2a 2b reported previously in the literature, 11 (nine of them newly synthesized) tyrosinase inhibitory effects antioxidant activities these studied for first time. All displayed certain on tyrosinase, with IC 50 values ranging from 37.86 ± 0.24 to 75.81 2.49 μM. Among compounds, 2j exhibited similar effect (IC = µM) positive control, kojic acid 21.93 0.11 µM). Kinetic studies...

Omega-3 fatty acids have long been ascribed a positive cardiovascular function. However, the plasma measurements invariably ignore 40% of blood specimen, cells that engage in continuous exchange with their environment. In our study, we included all components circulating blood. Erythrocyte or red-blood-cell (RBC) n-3 acid status has linked to disease and death. A low omega-3 index is an independent risk factor for mortality. We tested hypothesis acute, maximal exercise would influence...

Omega-3 (n-3) fatty acids have beneficial cardiovascular effects, perhaps also in chronic kidney disease (CKD) patients. A low omega-3 index is an independent risk factor end-stage renal (ESRD) dialysis However, the plasma measurements invariably ignore circulating blood cells, including preponderant erythrocytes (RBCs). We measured (HPLC-MS lipidomics) all components of blood, since RBC n-3 acid status has been linked to and mortality. studied 15 healthy persons CKD patients undergoing...

Abstract Systemic Candida infections pose a serious public health problem with high morbidity and mortality. C. albicans is the major pathogen identified in candidiasis; however, non‐ spp. antifungal resistance are now more prevalent. Azoles first‐choice drugs for they ineffective certain caused by resistant strains. block ergosterol synthesis inhibiting fungal CYP 51, which leads to disruption of membrane permeability. In this study, we screened activity an in‐house azole library 65...

A series of eleven hydroxy and methoxy by the condensation chalcone (1asynthesized compounds were characterized using NMR (1D; ROESY), FT-IR, UV, LC-MS spectral data elemental analysis.These synthetic ( screened for their α-glucosidase inhibition.Th 2a 2b with in range 1.61 (IC 50 , 13,34 µM).IC values other synthesized which more or as active acarbose, but, IC geometric isomers 2a-2k showed that cisoid 1E,2E is most stable geometrical isomer all.

Chronic kidney disease (CKD) is an important risk factor for cardiovascular and all-cause mortality. Survival rates among end-stage renal (ESRD) hemodialysis patients are poor most deaths related to disease. Oxylipins constitute a family of oxygenated natural products, formed from fatty acid by pathways involving at least one step dioxygen-dependent oxidation. They derived polyunsaturated acids (PUFAs) cyclooxygenase (COX) enzymes, lipoxygenases (LOX) or cytochrome P450 epoxygenase. have...

Long-chain fatty acids (LCFAs) serve as energy sources, components of cell membranes, and precursors for signaling molecules. Uremia alters LCFA metabolism so that the risk cardiovascular events in chronic kidney disease (CKD) is increased. End-stage renal (ESRD) patients undergoing dialysis are particularly affected their hemodialysis (HD) treatment could influence blood bioaccumulation transformation. We investigated HD studied profiles vivo by analyzing arterio-venous (A-V) LFCA...

Polyunsaturated fatty acids (PUFA) are precursors of bioactive metabolites and mediators. In this study, the profile hydroxyeicosatetraenoic (HETE), hydroxyeicosapentaenoic (HEPE) hydroxydocosahexaenoic (HDHA) derived from arachidonic acid (AA), eicosapentaenoic (EPA) docosahexaenoic (DHA) in colon, liver, lung, spleen, muscle, heart kidney tissue healthy wildtype mice were characterized, compared to profiles organs transgenic fat-1 engineered express Caenorhabditis elegans gene encoding an...

Nineteen tosylated acyl hydrazone derivatives were synthesized, and their inhibitory activities against monoamine oxidases (MAOs), acetylcholinesterase (AChE), butyrylcholinesterase (BChE), β-secretase (BACE-1) evaluated. Compound 3o was the most potent inhibitor of MAO-A, with an IC50 value 1.54 µM, followed by 3a (IC50 = 3.35 µM). A structural comparison indicated that 3-F group in increased its activity MAO-A. 3s MAO-B, 3.64 3t 5.69 The MAO-B order 3- > 4- 2-NO2 groups 3s, 3t, 3r,...

Abstract In this work, a series of phenyl‐derivatives spirofuran‐triazolo[1,5‐ ]pyrimidine ( 5 – i ) were evaluated for their anti‐inflammatory and analgesic activities, including SAR molecular docking studies. The cytotoxicity compounds was studied in RAW 264.7 murine macrophage cell line by MTT assay. Then, those with viability higher than 70 % tested activity at non‐toxic doses evaluating the nitrite level supernatants Griess reagent. Compounds b , d e, g demonstrated significant...

Metabolic stability, a key parameter in drug development, refers to substance's resistance metabolism. The failure rate can be significantly reduced by conducting metabolism studies for the candidate compound from early stages. These are primarily carried out on vitro microsomal enzymes, which play crucial role process. Various analytical methods, predominantly liquid chromatography, used analysis. In this context, we conducted metabolic stability of hydrazone-sulfonate derivative previously...