Rational utilization of 1,2,3-triazole scaffold in anti-MRSA drug development: Design strategies, structural insights and pharmacological outcomes

Journal of Molecular Structure, Год журнала: 2023, Номер 1295, С. 136557 - 136557

Опубликована: Сен. 2, 2023

Язык: Английский

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Recent Developments in 1,2,3‐Triazole Based α‐Glucosidase Inhibitors: Design Strategies, Structure‐Activity Relationship and Mechanistic Insights

Chemistry & Biodiversity, Год журнала: 2024, Номер 21(9)

Опубликована: Июль 2, 2024

Diabetes mellitus is a chronic and most prevalent metabolic disorder affecting 422 million the people worldwide causing life-threatening associated conditions including disorders of kidney, heart, nervous system as well leg amputation retinopathy. Steadily rising cases from last few decades suggest failure currently available drugs in containment this disease. α-Glucosidase potential target for effectively tackling disease attracting significant interest medicinal chemists around globe. Besides having set side effects, α-glucosidase inhibitors (carbohydrate mimics) offer better tolerability, safety, synergistic pharmacological outcomes with other antidiabetic therefore have working extensively over three developing alternative inhibitors. The 1,2,3-Triazole nucleus energetically used by various research groups globe development posing it an optimum scaffold field drug development. This review systematic analysis developed employing 1,2,3-triazole special focus on design strategies, structure-activity relationships, mechanism inhibitory effect. article will act lantern potent, safer, effective desired properties improved therapeutic efficacy.

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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Design, Synthesis, and Anticancer and Antibacterial Activities of Quinoline-5-Sulfonamides

Molecules, Год журнала: 2024, Номер 29(17), С. 4044 - 4044

Опубликована: Авг. 26, 2024

A series of new unique acetylene derivatives 8-hydroxy- and 8-methoxyquinoline- 5-sulfonamide

Язык: Английский

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Exploring 1,2,3-triazole-Schiff’s base hybrids as innovative EGFR inhibitors for the treatment of breast cancer: In vitro and in silico study

Bioorganic Chemistry, Год журнала: 2025, Номер 155, С. 108106 - 108106

Опубликована: Янв. 4, 2025

Язык: Английский

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Discovery of novel 1,2,3-Triazole hybrids derivatives as vasorelaxant agents: Molecular structure, Hirshfield surface, in-vivo and in-silico investigation by molecular docking simulation

European Journal of Medicinal Chemistry, Год журнала: 2025, Номер unknown, С. 117515 - 117515

Опубликована: Март 1, 2025

Язык: Английский

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Progress and Prospects of Triazoles in Advanced Therapies for Parasitic Diseases

Tropical Medicine and Infectious Disease, Год журнала: 2025, Номер 10(5), С. 142 - 142

Опубликована: Май 20, 2025

Parasitic diseases represent a severe global burden, with current treatments often limited by toxicity, drug resistance, and suboptimal efficacy in chronic infections. This review examines the emerging role of triazole-based compounds, originally developed as antifungals, advanced antiparasitic therapy. Their unique structural properties, particularly those 1,2,3- 1,2,4-triazole isomers, facilitate diverse binding interactions favorable pharmacokinetics. By leveraging innovative synthetic approaches, such click chemistry (copper-catalyzed azide–alkyne cycloaddition) structure-based design, researchers have repurposed optimized triazole scaffolds to target essential parasite pathways, including sterol biosynthesis via CYP51 other novel enzymatic routes. Preclinical studies models Chagas disease, leishmaniasis, malaria, helminth infections demonstrate that derivatives like posaconazole, ravuconazole, DSM265 exhibit potent vitro vivo activity, although their primarily static effects success monotherapies cases. Combination strategies hybrid molecules demonstrated potential enhance mitigate resistance. Despite challenges achieving complete clearance managing interdisciplinary efforts across medicinal chemistry, parasitology, clinical research highlight significant triazoles components next-generation, patient-friendly regimens. These findings support further optimization evaluation agents improve for neglected parasitic diseases.

Язык: Английский

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An overview of synthetic approaches and the potential bioactivity of different 1,2,3-triazole hybrids

Egyptian Pharmaceutical Journal, Год журнала: 2024, Номер 23(2), С. 157 - 183

Опубликована: Фев. 22, 2024

1,2,3-Triazole is considered to be the lead structure for discovery of many drug molecules. has received considerable attention in field due its remarkable widespread biological potential. This work summarizes current synthetic pathways adopted synthesis diverse analogs 1,2,3-triazole. It also introduces an overview latest advances 1,2,3-triazole hybrid models with various pharmacological activities, their chemical structures, structure–activity relationships, and mechanisms action.

Язык: Английский

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Synthesis of 1,2,3-triazole containing compounds as potential antimicrobial agents

PeerJ Organic Chemistry, Год журнала: 2024, Номер 6, С. e10 - e10

Опубликована: Июль 25, 2024

Invasive fungal infections are increasing worldwide due to an expanding number of immunocompromised patients as well increase in drug-resistant fungi. While resistance has increased, this not been accompanied by the development new antifungals. A common class antifungal agents that prescribed azoles, which contain either a triazole or imidazole group. Unfortunately, current like fluconazole, have shown be less effective with resistant pathogens. Therefore, novel azole compounds is urgent need. The objective research was synthesize triazole-containing small molecules potent activity. scaffold synthesized contains moiety and via copper-catalyzed azide-alkyne click reaction (CuAAC) between appropriate alkyne azide intermediates. minimum inhibitory concentrations these were determined using standard broth microdilution assays against opportunistic bacteria fungi associated life-threatening invasive infections. Although possessed no antimicrobial activity, results can used further long-term goal developing optimizing lead vitro

Язык: Английский

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Visible-light-induced photocatalytic iododi(per)fluoroalkylation of 5-amino-N-allyl-1,2,3-triazole-4-carboxamides

Journal of Fluorine Chemistry, Год журнала: 2024, Номер 276, С. 110292 - 110292

Опубликована: Апрель 24, 2024

Язык: Английский

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