A5088211625- Synthesis and biological activity
- Cancer therapeutics and mechanisms
- Synthesis and Biological Evaluation
- Computational Drug Discovery Methods
- Synthesis and Reactivity of Heterocycles
- Click Chemistry and Applications
- Synthesis and Characterization of Heterocyclic Compounds
- Synthesis and Reactions of Organic Compounds
- Inflammatory mediators and NSAID effects
- Multicomponent Synthesis of Heterocycles
- Quinazolinone synthesis and applications
- Phenothiazines and Benzothiazines Synthesis and Activities
- Peroxisome Proliferator-Activated Receptors
- X-ray Diffraction in Crystallography
- Crystallization and Solubility Studies
- Synthesis and bioactivity of alkaloids
- Insect Pest Control Strategies
- Advanced Drug Delivery Systems
- Advancements in Transdermal Drug Delivery
- Bioactive Compounds and Antitumor Agents
- Nanoparticles: synthesis and applications
- Synthesis and Biological Activity
- Enzyme function and inhibition
- Nanoparticle-Based Drug Delivery
- Synthesis and pharmacology of benzodiazepine derivatives
King Faisal University
2016-2025
Umm al-Qura University
2012
Laboratoire de Chimie et Biochimie Pharmacologiques et Toxicologiques
2001-2003
Centre National de la Recherche Scientifique
2001-2003
Université Paris Cité
2001-2003
Herein, we report computational and experimental evaluations of the antimicrobial activity twenty one 2,3-diaryl-thiazolidin-4-ones. All synthesized compounds exhibited an antibacterial against six Gram-positive Gram-negative bacteria to different extents. Thus, MIC was in range 0.008–0.24 mg/mL, while MBC 0.0016–0.48 mg/mL. The most sensitive bacterium S. Typhimurium, whereas aureus resistant. best observed for compound 5 (MIC at 0.008–0.06 mg/mL). three active 5, 8, 15, as well 6, which...
Thiazole and benzothiazole derivatives, as well thiazolidinones are very important scaffolds in medicinal chemistry. Literature has revealed that they possess a wide spectrum of biological activities including antimicrobial activity.The goal this paper is the designing new based evaluation their activities.The designed compounds were synthesized using classical organic synthesis methods. The activity was evaluated method microdilution.The twelve newly showed properties. All appeared to be...
A series of ethyl 1-(substituted benzoyl)-5-methylpyrrolo[1,2-a]quinoline-3-carboxylates 4a–f and dimethyl benzoyl)-5-methylpyrrolo[1,2-a]quinoline-2,3-dicarboxylates 4g–k have been synthesized evaluated for their anti-tubercular (TB) activities against H37Rv (American Type Culture Collection (ATCC) strain 25177) multidrug-resistant (MDR) strains Mycobacterium tuberculosis by resazurin microplate assay (REMA). Molecular target identification these compounds was also carried out a...
A series of 1,2,3-trisubstituted indolizines (2a–2f, 3a–3d, and 4a–4c) were screened for in vitro whole-cell anti-tubercular activity against the susceptible H37Rv multidrug-resistant (MDR) Mycobacterium tuberculosis (MTB) strains. Compounds 2b–2d, 4a–4c active H37Rv-MTB strain with minimum inhibitory concentration (MIC) ranging from 4 to 32 µg/mL, whereas 4a–4c, ethyl ester group at 4-position benzoyl ring also exhibited anti-MDR-MTB (MIC = 16–64 µg/mL). In silico docking study revealed...
Novel series of diversely substituted indolizines were designed, synthesized, and evaluated for their in vitro anti-mycobacterial activity against H37Rv multi-drug-resistant (MDR) strains Mycobacterium tuberculosis (MTB). Many compounds exhibited significant inhibitory MTB strains. Indolizines 2d, 2e, 4 also found to be active clinical isolates with multi-resistance rifampicin isoniazid. Indolizine was identified as the most promising agent, displaying minimum concentration (MIC) values 32...
Tuberculosis has been reported to be the worldwide leading cause of death resulting from a sole infectious agent. The emergence multidrug-resistant tuberculosis and extensively drug-resistant made battle against infection more difficult since most currently available therapeutic options are ineffective these resistant strains. Therefore, novel molecules need developed effectively treat disease. Preliminary docking studies revealed that tetrahydropyrimidinone derivatives have favorable...
Novel indolizine scaffolds as COX-2 inhibiting agents.
As a part of our ongoing project on the design and synthesis new thiazole derivatives with antimicrobial activity, fourteen ethyl 2-(2-((E)-((Z)-5-(4-benzyliden)- 4-oxothiazolidin-2-yliden)amino-4-yl)acetates, carrying halogens, methoxy other groups were synthesized. Compounds tested against eight Gram positive negative bacteria as well yeasts mold by microdilution assay. All compounds showed good activity all MIC ranging between 2.3-39.8 µmol/ml x 10-2 MBC 9.2-79.6 10-2. reference drugs...
Abstract: >Background: Several promising compounds against multi-drug-resistant Mycobacterium tuberculosis (MTB) are currently in the drug discovery and development pipeline. While it has yet to establish candidature this pipeline, early results have been for putative anti-mycobacterial potency of indolizine scaffold. Methods: The molecular properties, as well Absorption, Disruption, Metabolism, Excretion Toxicity (ADMET) indolizines were assessed using Accelry's Discovery Studio 4.0 client...
The cyclooxygenase-2 (COX-2) enzyme is considered to be an important target for developing novel anti-inflammatory agents. Selective COX-2 inhibitors offer the advantage of lower adverse effects that are commonly associated with non-selective COX inhibitors. In this work, a series methyl 3-(substituted benzoyl)-7-substituted-2-phenylindolizine-1-carboxylates was synthesized and evaluated inhibitory activity. Compound 4e identified as most active compound IC50 6.71 M, which comparable...
Thiazole derivates as well chalcones, are very important scaffold for medicinal chemistry. Literature survey revealed that they possess wide spectrum of biological activities among which anti-inflammatory and antimicrobial.The current studies describe the synthesis evaluation antimicrobial activity twenty eight novel thiazole-based chalcones.The designed compounds were synthesized using classical methods organic synthesis. The in vivo was performed by microdilution method.All have shown...
As a part of our ongoing studies in developing new derivatives as antimicrobial agents we describe the synthesis novel substituted 5-benzylideno-2-adamantylthiazol[3,2-b][1,2,4]triazol-6(5H)ones.The twenty-five newly synthesized compounds were tested for their and antifungal activity. All have shown antibacterial properties with 1–9 showing lowest activity, followed by 10–14 while 15–25 highest Specific appeared to be more active than ampicillin most studied strains some cases streptomycin....
Background: HIV-1 RT inhibitors were the first drugs approved to treat AIDS and remain key components of highly active antiretroviral therapy (HAART). While HAART effectively suppresses viral replication slows disease progression, it has limitations, including long-term side effects emergence drug-resistant strains, highlighting need for new treatments. Objectives: Based on our previous experience, insights from existing RNase H, we aim design synthesize safer, multifunctional molecules....
Background.: Inflammation is a multifactorial process reflecting the response of organism to various stimuli and associated with number disorders such as arthritis, asthma psoriasis, which require long-lasting or repeated treatment. Objective.: The aim this paper evaluate anti-inflammatory activity previous synthesized thiazole-based chalcone derivatives. Methods: Chalcones were via Cliazen-Schmidt condensation1-(4-methyl-2- alkylamino)thiazol-5-yl) ethanone corresponding aromatic aldehyde....
Malaria, affecting all continents, remains one of the life-threatening diseases introduced by parasites that are transmitted to humans through bites infected Anopheles mosquitoes. Although insecticides currently used reduce malaria transmission, their safety concern for living systems, as well environment, is a growing problem. Therefore, discovery novel, less toxic, and environmentally safe molecules effectively combat control these vectors in high demand. In order identify new potential...
In this study, we report the design, synthesis, computational and experimental evaluation of antimicrobial activity, as well docking studies new 5-methylthiazole based thiazolidinones. All compounds demonstrated antibacterial efficacy, some which (1, 4, 10 13) exhibited good activity against E. coli B. cereus. The three resistant strains, MRSA, P. aeruginosa coli, revealed that compound 12 showed best higher than reference drugs ampicillin streptomycin, were inactive or only bacteriostatic...
Background: Inflammation is a complex response to noxious stimuli promoted by the release of chemical mediators from damaged cells. Metabolic products arachidonic acid, produced action cyclooxygenase and lipoxygenase, play important roles in this process. Several non-steroidal anti-inflammatory drugs act as inhibitors. However, almost all them have undesired side effects. Methods: Prediction compounds was performed using PASS Program. The activity evaluated carrageenan paw edema test. COX...
Considering the importance of benzothiazepine pharmacophore, an attempt was carried out to synthesize novel 1,5-benzothiazepine derivatives using polyethylene glycol-400 (PEG-400)-mediated pathways. Initially, different chalcones were synthesized and then subjected a cyclization step with in presence bleaching clay PEG-400. PEG-400-mediated synthesis resulted yield more than 95% less hour reaction time. Synthesized compounds 2a-2j investigated for their vitro cytotoxic activity. Moreover,...
Despite the greatest achievement in development of anti-inflammatory agents last two decades, current clinical drugs suffer from a variety complications community settings and hospital. There is still an urgent need to design novel molecules with better safety profile different molecular targets those use. The aim this research was discover series benzothiazole-based thiazolidinones lipoxygenase (LOX) inhibitory activity as mechanism action. Carrageenan-induced mouse foot paw oedema assay...
Major obstacles faced by the use of nonsteroidal anti-inflammatory drugs (NSAID) are their gastrointestinal toxicity induced non-selective inhibition both cyclooxygenases (COX) 1 and 2 cardiotoxicity associated with a certain class COX-2 selective inhibitors. Recent studies have demonstrated that COX-1 generates compounds no gastric damage. The aim current study is to develop novel agents better profile. In our previous paper, we investigated activity 4-methylthiazole-based thiazolidinones....