Synthesis and molecular docking analysis of novel hydrazone and thiosemicarbazide derivatives incorporating a pyrimidine ring: exploring neuroprotective activity.

The increasing global prevalence of Alzheimer's disease necessitates the development of novel therapeutic approaches. Neurodegenerative diseases are associated with increased oxidative stress and levels of cholinesterase enzymes. Hence, the development of cholinesterase inhibitors and antioxidants may provide neuroprotective effects.

Synthesis, Biological Evaluation and in Silico Studies of Novel Urea/Thiourea Derivatives of Lenalidomide.

Designing new compounds from existing chemotherapeutic drugs to enhance inhibitory effects on tumor cells while overcoming multidrug resistance is one of the important strategies for new drug discovery in medicinal chemistry. A new series of urea and thiourea derivatives based on Lenalidomide as potential anticancer agents have been designed and synthesized. In vitro anticancer activity assay against Caki cancer cells and HUVEC endothelial cells revealed that 1-(4-methylphenyl)-3-[2-(2,6-dioxopiperidin-3-yl)-1-oxoisoindolin-4-yl]urea (11) exhibited the highest anticancer activity and selectivity in the series with IC values of 9.

Design, synthesis, molecular modeling, in vitro evaluation of novel piperidine-containing hydrazone derivatives as cholinesterase inhibitors.

In an effort to develop new and effective therapeutic agents for Alzheimer's disease, a series of hydrazone derivatives bearing piperidine rings have been designed and synthesized. The chemical structures of the compounds were characterized by various spectroscopic techniques. In vitro antioxidant and cholinesterase activities of the compounds were evaluated.

Insecticidal effect of new synthesized chalcone derivatives on Caribbean fruit fly, .

In this present study, new chalcone derivatives were synthesized from 4-aminoacetophenone, which were confirmed by spectroscopic methods. The toxic risks of chalcones to humans and the environment were investigated by a web-based platform called ADMETlab. With this program, the possible toxic effects of the compounds on liver, respiratory system, and eyes were evaluated.

Synthesis, biological evaluation and molecular docking studies of novel 1,3,4-thiadiazoles as potential anticancer agents and human carbonic anhydrase inhibitors.

Thiosemicarbazide and also 1,3,4-thiadiazole derivatives have been garnering substantial attention from researchers worldwide due to their expansive range of biological activities, encompassing antimicrobial, anti-inflammatory, and anticancer properties. Herein, we embarked on a comprehensive investigation in this study, introducing a novel series of thiosemicarbazides (3a-3i) and their corresponding 1,3,4-thiadiazole (4a-4i) derivatives. The compounds were meticulously designed, synthesized, and subjected to meticulous characterization using various spectroscopic methods such as FT-IR, H-NMR, C-NMR, and elemental analysis.

Morphological and electrophysiological evaluation of median and ulnar nerve in complex regional pain syndrome type 1.

Objective: Complex regional pain syndrome (CRPS) can be distinguished as type I without and type II with electrophysiological evidence of major nerve lesion. The pathophysiology of both subgroups is still under investigation. The aim of this research is to demonstrate the nerve morphology and electrophysiology in CRPS type I patients.

Synthesis of Phthalimide Derivatives and Their Insecticidal Activity against Caribbean Fruit Fly, (Loew).

In this study, thirteen phthalimide derivatives were designed and synthesized. All synthesized compounds were evaluated to determine their potential for inhibitory activities against females of the Caribbean fruit fly, (Loew) (Diptera: Tephritidae). These efforts led to the discovery of three compounds , , and with potent insecticidal activity (LD range from 0.

Synthesis and Biological Evaluation of Some Hydrazide-Hydrazone Derivatives as Anticancer Agents.

In this study, a series of hydrazide-hydrazone derivatives (3a-3u) were synthesized and evaluated for their anticancer activities against prostate cancer cell line (PC-3), breast cancer cell line (MCF-7), colon cancer cell line (HT-29) and human umbilical vein endothelial cells (HUVEC) using MTT assay. In particular, compound 3h having a pyrrole ring was found to be the most potent derivative with IC50 = 1.32, 2.

Design, Synthesis, In Silico ADMET Studies and Anticancer Activity of Some New Pyrazoline and Benzodioxole Derivatives.

A new series of 2-pyrazoline derivatives starting from substituted benzodioxole chalcones were designed and synthesized. IR and 1H NMR spectral data and elemental analysis were used to characterize the structures of the synthesized compounds. The cytotoxic activities on HeLa, MCF-7 cancer cell lines and NIH-3T3 for these compounds were tested by using MTT assay.

N-Substituted Arylidene-3-(Methylsulfonyl)-2-Oxoimidazolidine-1-Carbohydrazide as Cholinesterase Inhibitors: Design, Synthesis, and Molecular Docking Study.

The development of new enzyme inhibitors in degenerative brain diseases has gained more attention. Enzyme inhibitors play an effective role in controlling central nervous system diseases. For this purpose, a novel series of hydrazone derivatives containing imidazolidine ring aimed against Alzheimer's disease (AD), have been designed and synthesized.

Synthesis, Biological Evaluation and in Silico Studies of New Pyrazoline Derivatives Bearing Benzo[d]thiazol-2(3H)-one Moiety as Potential Urease Inhibitors.

Novel pyrazoline derivatives containing benzo[d]thiazol-2(3H)-one moiety were synthesized and screened for their inhibitory properties against urease, a clinically important metabolic enzyme. In vitro enzyme inhibition studies revealed that all pyrazolines (7.21-87.

Synthesis of new hydrazone derivatives and evaluation of their monoamine oxidase inhibitory activity.

A novel series of hydrazone derivatives were designed and synthesized. Their structures were characterized by IR, H NMR, C NMR and HR-MS spectroscopic methods. The newly synthesized compounds were evaluated for their inhibitory activity against monoamine oxidase enzymes (MAO-A and MAO-B).

Induction of Divergent Cell Death Pathways by Urea and Carbohydrazide Derivatives.

Background: The complexity of cancer biology and the development of chemotherapy resistance are two main obstacles to cancer treatment and necessitate novel anticancer molecules that target different cell death pathways. Modulation of Endoplasmic Reticulum (ER) stress and subsequent activation of the Unfolded Protein Response (UPR) has been proposed as a potential chemotherapeutic target, as prolonged ER stress can lead to cell death via apoptosis or necrosis.

Objective: The present study aims to evaluate the molecular mechanism underlying the cytotoxic activity of selected urea and carbohydrazide derivatives.

Novel 2,5-disubstituted-1,3,4-oxadiazole derivatives as MAO-B inhibitors: Synthesis, biological evaluation and molecular modeling studies.

Thirty novel 2,5-disubstituted-1,3,4-oxadiazole derivatives bearing urea moiety were designed and synthesized. IR, H-NMR, C-NMR and mass spectroscopic methods and elemental analysis were used to confirm the structures of the compounds. Their monoamine oxidase inhibitory activity was determined against the MAO-A and MAO-B isoforms.

Design, Synthesis and Biological Screening of Novel 1,5-Diphenyl-3-(4-(trifluoromethyl)phenyl)-2-pyrazoline Derivatives.

1-Phenyl-5-substituted-3-(4-(trifluoromethyl)phenyl)-4,5-dihydro-1H-pyrazole derivatives were synthesized from chalcone derivatives. The structures of compounds were characterized by IR, 1H NMR spectroscopic methods and elemental analysis. All compounds were evaluated for their in vitro antioxidant activity using DPPH and ABTS methods, anti-inflammatory activity using lipoxygenase inhibitory method and antidiabetic activity using the ?-glucosidase inhibitory method.

Design, synthesis and biological evaluation of some new 2-Pyrazoline derivatives as potential anticancer agents.

A new series of N-(4-(1-Phenyl-5-aryl-4,5-dihydro-1H-pyrazol-3-yl)phenyl)-4-substitutedbenzamide derivatives were designed and synthesized from new chalcone derivatives. All newly synthesized compounds were determined by using IR, H-NMR, C-NMR spectroscopic methods, elemental analysis and evaluated for their in vitro antiproliferative activities on HeLa, MCF-7, MKN-45 cancer cell lines and NIH-3T3 cell line using MTT assay. Expression of Bax and Bcl-2 proteins was detected by Western-blot analysis and caspase-3 enzyme activity was measured.

Design, Synthesis and Evaluation of the Biological Activities of Some New Carbohydrazide and Urea Derivatives.

Objectives: Urea and carbohydrazide derivatives are important compounds exhibiting cytotoxic activities. In this study, a series of new urea and carbohydrazide derivatives containing an pyridine ring were synthesized and evaluated for cytotoxic activity.

Materials And Methods: The proposed structures of the synthesized compounds were confirmed using elemental analysis, IR, and H-NMR spectroscopic techniques.

Synthesis and biological evaluation of new pyrazolone Schiff bases as monoamine oxidase and cholinesterase inhibitors.

In the current work, Schiff base derivatives of antipyrine were synthesized. The chemical characterization of the compounds was confirmed using IR, H NMR, C NMR and mass spectroscopies. The inhibitory potency of synthesized compounds was investigated towards acetylcholinesterase (AChE), butyrylcholinesterase (BuChE), and monoamine oxidases A and B (MAO-A and MAO-B) enzymes.

Synthesis and structure-activity relationships of carbohydrazides and 1,3,4-oxadiazole derivatives bearing an imidazolidine moiety against the yellow fever and dengue vector, Aedes aegypti.

Background: 1,3,4-Oxadiazole and imidazolidine rings are important heterocyclic compounds exhibiting a variety of biological activities. In this study, novel compounds with oxadiazole and imidazolidine rings were synthesized from 3-(methylsulfonyl)-2-oxoimidazolidine-1-carbonyl chloride and screened for insecticidal activities. The proposed structures of the 17 synthesized compounds were confirmed using elemental analysis, infrared (IR), proton nuclear magnetic resonance ( H-NMR), and mass spectroscopy.

The investigation of the role of the facet joint angle in the development of L5-S1 spondylolysis in young men.

Objectives: This study aims to evaluate facet tropism in younger patients with lumbar spondylolysis and to investigate the role of facet tropism in the development of spondylolysis.

Patients And Methods: Between February 2013 and December 2015, a total of 102 male patients with bilateral L5 pars defect including 53 with spondylolysis and 49 control subjects were included in this case-control study. The facet joint angles were measured bilaterally and axially at the level of L3-4, L4-5, L5-S1 using computed tomography (CT).

Ultrasonographic Assessment of Femoral Cartilage Thickness in Patients With Cerebral Palsy.

Background: Cerebral palsy (CP) is one of the most disabling syndromes in children. To our knowledge, there has not yet been any reported evaluation by ultrasonography of the effect of CP on distal femoral cartilage. The value of understanding this effect on cartilage is that sonographic evaluation of cartilage thickness may help physicians to predict the joint health of these children.

Sonographic guide for botulinum toxin injections of the lower limb: EUROMUSCULUS/USPRM spasticity approach.

The pertinent literature lacks overt technical data for optimal lower limb muscle botulinum toxin injections using ultrasound (US) imaging. Therefore, this guide is prepared for the commonly injected muscles of the lower limb and the pelvic girdle mainly in spasticity. It includes clinical information, anatomical description and explanation regarding the US imaging of several muscles.