A5024613157- Synthesis and biological activity
- Synthesis and Biological Evaluation
- Synthesis and Characterization of Heterocyclic Compounds
- Multicomponent Synthesis of Heterocycles
- Inflammatory mediators and NSAID effects
- Quinazolinone synthesis and applications
- Synthesis of heterocyclic compounds
- Synthesis and Reactions of Organic Compounds
- Click Chemistry and Applications
- Synthesis of β-Lactam Compounds
- Bioactive Compounds and Antitumor Agents
- Cancer therapeutics and mechanisms
- Phenothiazines and Benzothiazines Synthesis and Activities
- Synthesis of Organic Compounds
- Computational Drug Discovery Methods
- HER2/EGFR in Cancer Research
- Synthesis and Catalytic Reactions
- Fungal Plant Pathogen Control
- Synthesis and Reactivity of Heterocycles
- Polymer-Based Agricultural Enhancements
- Biochemical and Molecular Research
- Synthesis of Tetrazole Derivatives
- Microtubule and mitosis dynamics
- Photosynthetic Processes and Mechanisms
- Cholinesterase and Neurodegenerative Diseases
Beni-Suef University
2016-2025
Jouf University
2016-2022
In an effort to improve and achieve biologically active anticancer agents, a novel series of 1,2,3-triazole-containing hybrids were designed efficiently synthesized via the Cu-catalyzed azide-alkyne cycloaddition (CuAAC) reaction substituted-arylazides with alkyne-functionalized pyrazole-[1,2,4]-triazole hybrids. The structure geometry these new clicked 1,2,3-triazoles was explored by density functional theory (DFT) using B3LYP/6-311++G(d,p) level; also, potential activity compounds for...
An eco-friendly green bio-organic catalyst and low-cost 3,4-dihydropyrimidin-2(1H)-ones/thione derivatives 4-7 have been synthesized using a high-yield, synthetic method via one-pot, three-component process between 4-formylphenyl-4-methylbenzenesulfonate (1), thiourea, or urea ethyl acetoacetate acetylacetone under microwave irradiation in aqueous media of water ethanol (3:1 ratio) as solvent the presence cysteine new catalyst. The reaction compound 1, 4-(carbamothioylhydrazono)...
Abstract Treatment of p‐ tosyloxybenzaldehyde ( 1 ) with ethyl cyanoacetate afforded 2‐cyano‐3‐(4‐{[(4‐methylphenyl)sulfonyl]oxy}phenyl)acrylate 2 which reacted some active methylene derivatives under microwave irradiation in presence ammonium acetate yielded pyridine 3 – 7 . On the other hand, when treatment compound thiosemicarbazide gave 4‐tosyloxybenzylidenethiosemicarbazone 8 ), allowed to react compounds, such as: bromoacetate, chloroacetonitrile or phenacyl bromide thiazole 9 13 The...
Epidermal growth factor receptor (EGFR) inhibition is an imperative therapeutic approach targeting various types of cancer including colorectal, lung, breast, and pancreatic types. Moreover, cyclooxygenase-2 (COX-2) frequently overexpressed in different cancers has a role the promotion malignancy, apoptosis inhibition, metastasis tumor cells. Combination therapy been emerged to improve benefit against curb intrinsic acquired resistance.Three semi-synthetic series compounds (C1-4, P1-4, G1-4)...
A new group of 1-phenylpyrazolo[3,4-d]pyrimidine derivatives 14a–d–21 were synthesized from 2-(6-methyl-1-phenyl-1H-pyrazolo[3,4-d]pyrimidin-4-yloxy)acetohydrazide (12). All the compounds evaluated for their cyclooxygenase (COX) inhibition, anti-inflammatory activity and ulcerogenic liability. target more potential in inhibiting COX-2 than COX-1. Compounds having pyrazolyl moiety a hybrid structure with pyrazolo[3,4-d]pyrimidine scaffold (14a–d, 16 17) showed higher edema inhibition...
Pyrazolopyrimidine heterocycle and its isosteres represent the main scaffold for many pharmacologically active drugs including anti-inflammatory agents. The COX-2 inhibitors are principal gate design of new safe potent Novel derivatives pyrazolo[1,5-a] pyrimidines were synthesized screened in vivo vitro their potential. Within constructed compounds, compound 11 was most on IL-6 TNF-α (percentage inhibition = 80 89%, respectively). In addition, 12 displayed inhibitory effect towards (IC50...
Novel triazino[4,3‐a]quinolinecarboxylate compounds (4, 6, 8 and 10) were synthesized investigated for their antifungal activity against Candida species. Compound was a standout candidate which displayed impressive anticandidal various species with low minimum inhibitory concentrations (MIC = 32‐45 µg/ml) compared to the reference drug Miconazole 50‐60 µg/ml). Furthermore, induced both morphological ultra‐structural changes by compound on cells are analyzed light transmission electron...
3,6-Dimethyl-1-phenyl-1H-pyrazolo[3,4-d][1,3]oxazin-4-one (3) was prepared by hydrolysis of ethyl 5-amino-3-methyl-1-phenyl-1H-pyrazole-4-carboxylate (1) to afford the corresponding carboxylic acid 2, which reacted with acetic anhydride give 3. The pyrazolo[3,4-d][1,3]oxazin-4-one 3 hydroxylamine hydrochloride, urea, thiourea, thiosemicarbazide, phenylhydrazine and aromatic amines pyrazolo[3,4-d]pyrimidin-4-ones 4, 5a,b, 6, 7, 8a-e, respectively. Condensation pyrazoloxazine derivative 99%...
Because of gastrointestinal irritation and kidney toxicity associated with non-steroidal anti-inflammatory drugs the cardiovascular problems Coxibs use, developing novel agents reduced improved selectivity remains a major challenge. Depending on our previous work, series pyridopyrimidinones IIIa-i has been synthesized via reaction 6-amino-2-thioxo-2,3-dihydro-1H-pyrimidin-4-one (I) phenyldiazenyl aromatic aldehydes (IIa-i). All new constructed compounds were fully characterized by elemental...
NSAIDs represent a mainstay in pain and inflammation suppression, their actions are mainly based on inhibiting COX-1 COX-2 enzymes.Due to the adverse effects of these drugs, especially stomach heart, scientists efforts have been directed manufacture selective without cardiovascular side with minimal stomach. The thought be related chemical composition rather than mechanism action drugs.Novel pyridopyrimidines, 9a-j, were prepared structures confirmed by NMR, mass IR Spectra, elemental...