The objective of this research was the preparation new 8-nitrofluoroquinolone models and investigation their antibacterial properties. work initially involved large scale synthon 7-chloro-1-cyclopropyl-6-fluoro-8-nitro-4-oxo-1,4-dihydroquinoline-3-carboxylic acid (3), followed by introduction substituted primary amine appendages at C-7 position to give derivatives 9a-g, in which amino group is appended benzenes or aromatic heterocycles, part a α-amino just simple aliphatic amine. This...

This work presents a new synthetic approach to aromatic and aliphatic polycarbonates by melt polycondensation of bisphenol A diacetates with alkylene- arylenediphenyl dicarbonates. The diphenyl dicarbonates were prepared from phenyl chloroformate the corresponding dihydroxy compounds. process involved precondensation step under slow stream dry argon elimination acetate, followed at high temperature vacuum. potential this reaction is demonstrated successful synthesis series aromatic-aromatic...

The study aimed to examine rutin micelles of advanced superlative dual cytotoxicity-antiinflammtion bioefficacies in substantially novel submicro-nanoaffinities vs. both the raw and reference proapoptotic cisplatin.Antiproliferative capabilities rutin, benzoic acid (BA) triazolofluoroqunolone (TFQ) derivatives were reported; hence chemosensitizing effects or its polymeric (of improved solubility bioavailability via direct dissolution using amphiphilic copolymer Pluronic P123) co-incubations...

Background: This study aims to enhance the delivery of polyphenols using nanotechnology. Objective: To develop and evaluate liposomal formulations for improved stability polyphenols, specifically focusing on Rutin. Methods: Liposomal were meticulously prepared via Thin-Film Hydration method. Comprehensive physical characterization was conducted, including assessments Dynamic Light Scattering (DLS) Thermogravimetric Analysis (TGA). The free radical scavenging activity measured DPPH• assay,...

Abstract The repurposing of safe therapeutic drugs has emerged as an alternative approach to rapidly identify effective, safe, and conveniently available therapeutics treat/prevent cancer. Therefore, it was hypothesized that acidic chelator could have a genuine potential antiproliferative agents. Based on their pKa, the selected 15 eight classes—namely sulfonylureas, proton pump inhibitors, fluoroquinolones, nonsteroidal anti‐inflammatory agents, thiazolidinediones, thienopyridines, statins,...

Fluoroquinolones (FQs) have been identified recently as potent inhibitors of pancreatic lipase (PL). The aim this study was to synthesize novel FQs and triazolofluoroquinolones (TFQs) evaluate them in vitro with respect their antilipolytic efficacy potency properties. PL-IC50 values 12 TFQs (3 (a-c)-6 (a-c)) were the range 12.5-189.1 μm. These are further supported by docking studies. suggested association between obesity colorectal cancer initiated evaluation antiproliferative activity new...

The heterocyclic system is a promising core nucleus in many bioactive compounds. This work describes our effort to synthesize and characterize set of new biphenyl, benzofuran benzothiophene carboxamide derivatives. Our biological studies showed that compounds 10 17 have antifungal activity against C. galabrate more potent than fluconazole 9, 10, exerted cytotoxic activities immortalized embryonic mouse fibroblast cells (3T3) human cervical cancer cell line (HeLa); particular, the cyclic...

Paramount efforts by pharmaceutical industry to identify new targets for obesity-diabetes (Diabesity) pharmacologicalintervention have led a number of agents developed and directed at DPP IV [dipeptidyl peptidase IV] enzymeinhibition thereby enhancing endogenous insulinotropic incretins. Besides antioxidative-antiinflammtory moleculesthat inhibit accumulation advanced glycation end products (AGEs) can be good candidates ameliorating diabeticcomplications. Fluoroquinolones (FQs) been...

Capsaicin micelles were prepared by the direct dissolution using amphiphilic copolymer Pluronic P123 and advanced for substantially novel submicro-nanocytotoxicity.Superior cytotoxicity of capsaicin loaded nanomicelles vs. both raw reference cisplatin in pancreatic PANC1, breast MCF7, colorectal resistant CACO2, skin A375, lung A549 prostate PC3 cancer cell lines delineated. Nicotinic acid (NA) derivative 39 (2-Amino IsoNA) had antiinflammatory potential but consistently lacked...

Using Triton WR-1339-induced hyperlipidemic rats as an experimental model, we investigated whether compound 4 [N-(9,10-dihydro-9,10-dioxoanthracen-2-yl)bezofuran-2-carboxamide] and 5 [N-(4-benzoylphenyl)benzofuran-2-carboxamide], two novel anti-hyperlipidemic agents, have any effect on plasma triglyceride (TG), total cholesterol (TC), high-density lipoprotein levels (HDL-C) levels. The tested animals were divided into control (CG), (HG), compounds 4, 5, bezafibrate (BF) treated groups. At a...

In this work, 9 lipophilic-acid chelating FQs (fluoroquinolones) comprising groups have been prepared, characterized and screened for in vitro cytotoxicity, radical scavenging antiinflammation propensities.Using sulforhodamine B colorimetric bioassay vs. cisplatin; FQs-inflicted reductions' of viability against breast T47D MCF7, Pancreatic PANC-1, colorectal HT29, HCT116, SW620, CACO2, SW480 Leukaemia K562 cancer cell lines were examined quadruplicates/dose/cell line. Parameters including...

Abstract In this study, 15 commercial acidic drugs have been evaluated for pancreatic lipase (PL) inhibitory activity using an in vitro spectrophotometric method. The acidity was the basis of selection, since most PL inhibitors exhibit groups and high lipophilicity. Orlistat robust reference agent potency efficacy determinations. comparison to cisplatin, evaluation antineoplastic activities selected a panel colorectal cancer cell lines (HT‐29, HCT‐116, SW620, CACO‐2, SW480) normal...

Dyslipidemia is a major risk factor for the development of cardiovascular diseases. Many dyslipidemic patients do not achieve their target lipid levels with currently available medications, and most them may experience many side effects.The present work aimed toward identifying new class novel nicotinic acid-carboxamide derivatives as promising antihyperlipidemic compounds.Six N-(benzoylphenyl)pyridine-3-carboxamide were synthesized using acid chloride pathways. All structures confirmed...

Glycation is implicated in the pathophysiology of many diseases, including diabetes, cancer, neurodegenerative and aging. Several natural synthetic compounds were investigated for their antiglycation activity. We evaluated effect vanillic acid (VA) using vitro vivo experimental models.In vitro, bovine serum albumin (BSA) (50 mg/ml) was incubated with glucose mM) or without VA at 1.0-100 mM 1 week 37°C, then, excitation/emission fluorescence measured 370/440 nm to determine glycation...

One of the major therapeutic approaches to preventing relapse and accelerating healing duodenal gastric ulcers is eradication Helicobacter pylori. Due emergence antibiotic resistance among clinical strains H. pylori, alternative using newly discovered antimicrobial agents in combination with standard regimens for treatment pylori are increasingly needed. The purpose present study was investigate effect synthesized 8-nitroflouroqunolone derivatives when used either alone or combined...

Background: We hypothesized that superlative dual cytotoxicity-antiinflammtion bioefficacies of 9 selected lipophilic statins correlate to their chelation effect 3,5-dihydroxyheptanoic acid. Methodology: Lipophilic-acid chelating have been screened for in vitro duality proliferation inhibition and NO-radical scavenging capacities. Results: Their spectrum selectivity indices safety PDL fibroblasts -based 72h incubations was reported. Surprisingly despite its lack on macrophages LPS-triggered...