Sulfur (SⅥ)-containing heterocyclic hybrids as antibacterial agents against methicillin-resistant Staphylococcus aureus (MRSA) and its SAR

Bioorganic Chemistry, Год журнала: 2024, Номер 145, С. 107241 - 107241

Опубликована: Фев. 25, 2024

Язык: Английский

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Sulfoxidation of pyrimidine thioate derivatives and study their biological activities

Scientific Reports, Год журнала: 2025, Номер 15(1)

Опубликована: Янв. 6, 2025

Abstract In a quest to innovate biologically active molecules, the benzoylation of 4,6-dimethylpyrimidine-2-thiol hydrochloride ( 1 ) with benzoyl chloride derivatives was employed produce series pyrimidine benzothioate 2–5 ). Subsequent sulfoxidation these using hydrogen peroxide and glacial acetic acid yielded diverse array sulfonyl methanone 6–9 parallel, sulfonothioates 10–12 pyrimidines 13–15 ), originating from condensation compound derivatives. The newly synthesized compounds underwent characterization via FT-IR, NMR, mass spectrometry, elemental analyses. Biological screenings unveiled interesting properties: 6 exhibited significant antimicrobial potency against S. epidermidis haemolyticus , whereas 11 showed distinct insensitivity. Excitingly, 12 showcased robust antioxidant activity by efficiently scavenging DPPH • radical, underscoring their potential in oxidative stress mitigation. Notably, 10 displayed promising anti-tumor effects, demonstrating superior efficacy MCF-7 breast cancer cell line compared . study revealed spectrum biological activities across derivatives, modifications often resulting diminished bioactivity parent These findings shed light on intricate relationship between chemical properties, offering valuable insights for future drug discovery endeavors.

Язык: Английский

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A Review of Click Chemistry in the Synthesis of Organophosphorus Triazoles and Their Biological Activities

European Journal of Medicinal Chemistry, Год журнала: 2025, Номер 286, С. 117270 - 117270

Опубликована: Янв. 13, 2025

Organophosphorus compounds, characterized by the incorporation of phosphorus into organic molecules, play a critical role in various fields such as medicine, agriculture, and industry. Their unique electronic properties versatility make them essential developing therapeutic agents, pesticides, materials. One prominent class organophosphorus compounds is heterocycles, which combine benefits both cyclic structures. Triazoles, nitrogen-containing heterocyclic are particularly notable for their broad biological activities, including anticancer, antiviral, antibacterial, antioxidant effects. Traditional methods synthesizing triazoles often encounter challenges low yields non-selective products, whereas click chemistry provides more efficient reliable alternative. The copper-catalyzed azide-alkyne [3 + 2] cycloaddition, cornerstone chemistry, allows rapid selective formation under mild conditions. When functionalized with groups, not only retain but enhance improving potency, selectivity, stability. This review covers synthesis organophosphorus-functionalized via explores molecular structure, coordination these compounds. behavior interactions derivatives metal ions also addressed, significantly influence chemical reactivity, stability, bioactivity.

Язык: Английский

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Fluoroquinolones tackling antimicrobial resistance: Rational design, mechanistic insights and comparative analysis of norfloxacin vs ciprofloxacin derivatives

Bioorganic Chemistry, Год журнала: 2024, Номер 153, С. 107773 - 107773

Опубликована: Сен. 3, 2024

Язык: Английский

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Ampyrone linked 1,2,3-triazole based chemosensor for selective detection of Fe(II and III) ions

Inorganic Chemistry Communications, Год журнала: 2024, Номер unknown, С. 113692 - 113692

Опубликована: Дек. 1, 2024

Язык: Английский

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Synthesis of novel Bis-1,2,4-Triazolo[3,4-b][1,3,4]Thiadiazines from natural camphoric acid as potential anti-candidal agents

Results in Chemistry, Год журнала: 2024, Номер 7, С. 101406 - 101406

Опубликована: Янв. 1, 2024

Candida species have long been attributed to various diseases like candidiasis and systemic exacerbate the symptoms of immunocompromised patients. enzymes that could function as drug targets decrease their pathogenicity eradicate fungi. This research aimed investigate potency new bis-triazolothiadiazine derivatives contained in inhibiting important C. albicans an example, through molecular docking simulation. Thus, a novel series bis-triazolo[3,4-b][1,3,4]thiadiazines were designed prepared via reaction most versatile, hitherto unreported 5,5′-(1,2,2-trimethylcyclopentane-1,3-diyl)bis(4-amino-2,4-dihydro-3H-1,2,4-triazole-3-thione) with appropriate hydrazonoyl halides phenacyl bromides. Various spectroscopic techniques used identify structures synthesized derivatives. The tested against different spp. effective compound was 6f followed by 6b, 6d, 6e, where inhibition zone ranged from 45 mm 38 mm. By using docking, which highlighted interactions amino acid residues Lys57, Leu77, Glu116, Gly114, Phe36, Thr58, Glu32 at point binding, it possible determine binding produced fluconazole target interaction energy discovered be −6.494 kcal/mol for fungi candida (PDB ID: 1IA2). demonstrated highest efficacy, displayed significant conserved site fungi, conjunction PDB co-crystal ligand 1IA2. study's results also revealed dG scores bis-triazolo-thiadiazines 6b-f. study shows good acceptable interactions. Finally, studies lowest activity 6e 6c

Язык: Английский

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Targeting EGFR/PI3K/AKT/mTOR signaling in lung and colon cancers: synthesis, antitumor evaluation of new 1,2,4-oxdiazoles tethered 1,2,3-triazoles

RSC Advances, Год журнала: 2024, Номер 14(24), С. 16713 - 16726

Опубликована: Янв. 1, 2024

The EGFR/PI3K/Akt/mTOR pathway is important for metastasis, medication resistance, apoptosis prevention, and malignant transformation.

Язык: Английский

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Discovery of Schiff bases as potent antibacterial and antifungal agents

New Journal of Chemistry, Год журнала: 2024, Номер unknown

Опубликована: Янв. 1, 2024

Schiff bases as potent inhibitors of microorganisms growth.

Язык: Английский

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Novel 1,2,4-triazole-derived Schiff base derivatives: Design, synthesis, and multi-enzyme targeting potential for therapeutic applications

Bioorganic Chemistry, Год журнала: 2025, Номер 157, С. 108246 - 108246

Опубликована: Фев. 5, 2025

Язык: Английский

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Eco-friendly synthesis, structural insights, and antimicrobial potential of 1,3,5-tri-N-substituted hexahydro-1,3,5-triazine derivatives

Analytical Chemistry Letters, Год журнала: 2025, Номер unknown, С. 1 - 23

Опубликована: Март 16, 2025

Язык: Английский

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