Evaluation of Quinazolin-2,4-Dione Derivatives as Promising Antibacterial Agents: Synthesis, In Vitro, In Silico ADMET and Molecular Docking Approaches.

A series of new quinazolin-2,4-dione derivatives incorporating amide/eight-membered nitrogen-heterocycles -, in addition, acylthiourea/amide/dithiolan-4-one and/or phenylthiazolidin-4-one - and -. The starting compound was prepared by reaction of 4-(2,4-dioxo-1,4-dihydro-2-quinazolin-3-yl)-benzoyl chloride with ammonium thiocyanate and cyanoacetic acid hydrazide. The reaction of with strong electrophiles, namely, -aminophenol, -amino thiophenol, and/or -phenylene diamine, resulted in corresponding quinazolin-2,4-dione derivatives incorporating eight-membered nitrogen-heterocycles -.

New quinazolin-2,4-dione derivatives incorporating acylthiourea, pyrazole and/or oxazole moieties as antibacterial agents DNA gyrase inhibition.

This article contributes to the search for new therapeutic agents for treatment of diseases caused by bacterial pathogens. In this study, a new series of compounds incorporating numerous bioactive moieties such as quinazolin-2,4-dione, acylthiourea linkage, and/or five membered nitrogen heterocycles (pyrazole and oxazole) 2-5a-c was described to identify new antibacterial drug candidates inhibition of DNA gyrase enzyme. The precursor -['-(2-cyano-acetyl)-hydrazinocarbothioyl]-4-(2,4-dioxo-1,4-dihydro-2-quinazolin-3-yl)-benzamide 2 was prepared by treatment of compound 1 with ammonium thiocyanate and cyanoacetic acid hydrazide through multicomponent reaction (MCR).

Novel 3-phenylquinazolin-2,4(1H,3H)-diones as dual VEGFR-2/c-Met-TK inhibitors: design, synthesis, and biological evaluation.

Multitarget anticancer drugs are more superior than single target drugs regarding patient compliance, drug adverse effects, drug-drug interactions, drug resistance as well as pharmaceutical industry economics. Dysregulation of both VEGFR-2 and c-Met tyrosine kinases (TKs) could result in development and progression of different human cancers. Herein, we reported a novel series of 3-phenylquinazolin-2,4(1H,3H)-diones with thiourea moiety as dual VEGFR-2/c-Met TKs.

Comparing the Efficacy of Local Corticosteroid Injection, Platelet-Rich Plasma, and Extracorporeal Shockwave Therapy in the Treatment of Pes Anserine Bursitis: A Prospective, Randomized, Comparative Study.

Background: Pes anserine bursitis (PAB) is one of the most common causes of painful knee syndromes. This study aimed at examining the efficacy of local corticosteroid injection, platelet-rich plasma (PRP) injection, and extracorporeal shock wave therapy (ESWT) as different modalities to alleviate pain and enhance function in patients with pes anserine bursitis (PAB).

Methods: A prospective, randomized, comparative study was conducted on 180 patients diagnosed with chronic PAB.

Evaluating the Effect of Delayed Diagnosis on Disease Outcome in Fibromyalgia: A Multi-Center Cross-Sectional Study.

Background: The impact of delayed diagnosis (DD) on fibromyalgia (FM) patients' symptomatology and disease outcome has not yet been systematically studied.

Objective: To analyze the predictors of DD and the influence of DD on FM aggravation and disease evaluation measures.

Methods: 370 FM patients were interviewed prospectively for this study.

Design and biological evaluation of 3-substituted quinazoline-2,4(1,3)-dione derivatives as dual c-Met/VEGFR-2-TK inhibitors.

The dual c-Met/vascular endothelial growth factor receptor 2 (VEGFR-2) TK inhibition is a good strategy to overcome therapeutic resistance to small molecules VEGFR-2 inhibitors. In this study, we designed 3-substituted quinazoline-2,4(1,3)-dione derivatives as dual c-Met/VEGFR-2 TK inhibitors. We introduced new synthetic methods for reported derivatives of 3-substituted quinazoline-2,4(1,3)-dione -, in addition to the preparation of some new derivatives namely, and -.

Synthesis, Characterization, Antibacterial Activity, and Computer-Aided Design of Novel Quinazolin-2,4-dione Derivatives as Potential Inhibitors Against .

Cholera is a bacterial disease featured by dehydration and severe diarrhea. It is mainly caused by alimentary infection with . Due to the wide applicability of quinazolin-2,4-dione compounds in medicinal and pharmaceutical chemistry, a new series of -containing heterocyclic compounds was synthesized.

Subclinical enthesopathy in patients with psoriasis and its association with other disease parameters: a power Doppler ultrasonographic study.

Objective: This study aimed to determine the prevalence of subclinical enthesopathy in patients with psoriasis using power Doppler ultrasonography (PDUS) and its association with other disease parameters.

Material And Methods: A total of 50 patients with psoriasis (31 females) aged 19-70 years underwent a thorough clinical examination that included assessment of body mass index (BMI) and psoriasis area and severity index (PASI) score. Measurements of inflammatory markers, C-reactive protein (CRP), erythrocyte sedimentation rate (ESR), serum uric acid, and plain radiography of the heels, knees, and sacroiliac joints were performed for all patients.

Organobase-catalyzed three-component reactions for the synthesis of 4H-2-aminopyrans, condensed pyrans and polysubstituted benzenes.

Novel routes for the preparation of 2-amino-4H-pyran-3-carbonitrile 9, amino-arylbenzoic acid ester derivatives 13a,b, 2-aminotetrahydro-4H-chromene-3-carbonitrile 18, 3-amino-4-cyanotetrahydronaphthalene-2-carboxylic acid ester 26 and 4-amino-3,5-dicyanophthalic acid ester derivatives 37a-c were developed. The synthetic methods utilize one-pot reactions of acetylene carboxylic acid esters, α,β-unsaturated nitriles and/or active methylenenitriles in the presence of L-proline or DABCO. Plausible mechanisms are suggested for the formation of the products.