CYP3A4 drug metabolism considerations in pediatric pharmacotherapy DOI Creative Commons

Marin Vander Schaaf,

Kyrle Luth,

Danyelle M. Townsend

и другие.

Medicinal Chemistry Research, Год журнала: 2024, Номер unknown

Опубликована: Дек. 5, 2024

Abstract Cytochrome P450 3A4 (CYP3A4) is a crucial enzyme involved in the Phase I metabolism of numerous medications used clinical practice. Its potential significance pediatric pharmacotherapy underscored by unique metabolic profile children, which differs markedly from adults, especially neonates, infants, and young children due to developmental changes activity. This review explores critical role CYP3A4 drugs population, with particular focus on combination drug therapies. Given high for drug-drug interactions therapies, understanding modulation activity essential optimizing therapeutic outcomes minimizing adverse effects. paper further examines structural similarities between these bergamottin, known inhibitor found citric fruits such as grapefruit. Variability activity, influenced genetic polymorphisms, stage, external factors, necessitates careful consideration prescribing management children. corroborates need personalized medicine approaches enhanced pharmacovigilance ensure safe effective use CYP3A4-metabolized population. Graphical

Язык: Английский

Triazination/IEDDA Cascade Modular Strategy Installing Pyridines/Pyrimidines onto Tyrosine Enables Peptide Screening and Optimization DOI
Quan Zuo,

Xinyi Song,

Jie Yan

и другие.

Journal of the American Chemical Society, Год журнала: 2025, Номер unknown

Опубликована: Янв. 30, 2025

Modular chemical postmodification of peptides is a promising strategy that supports the optimization and innovation hit peptide therapeutics by enabling rapid derivatization. However, current methods are primarily limited to traditional bio-orthogonal strategies ligation techniques, which require preintroduction non-natural amino acids impose fixed limit diversity. Here, we developed Tyrosine-1,2,3-Triazine Ligation (YTL) strategy, constructs novel linkages (pyridine pyrimidine) through "one-pot, two-step" process combining SNAr IEDDA reactions, promoting modular post modification Tyr-containing peptides. After optimizing YTL establishing standard procedures, successfully applied it solid-phase various biorelated peptides, such as synthesis dual-mode imaging probes long-acting GLP-1 analogs. As proof concept, library 384 amphipathic was constructed using based on 96-well microfiltration plates. modifications were then performed screened template tripeptide RYR, leading generation 20 derivatives. The antibacterial activity these derivatives systematically characterized, identifying Z8 potential candidate.

Язык: Английский

Процитировано

2

The Liebeskind–Srogl Cross-Coupling Reaction Towards the Synthesis of Biologically Active Compounds DOI

Jan Chasák,

Ignacy Janicki, Lucie Brulíková

и другие.

European Journal of Medicinal Chemistry, Год журнала: 2025, Номер unknown, С. 117526 - 117526

Опубликована: Март 1, 2025

Язык: Английский

Процитировано

0

Ionic Liquid-Assisted Approaches in the Synthesis of Nitrogen-Containing Heterocycles: A Focus on 3- to 6-Membered Rings DOI Creative Commons

P. K. Maity,

Amrit Krishna Mitra

Journal of Ionic Liquids, Год журнала: 2025, Номер unknown, С. 100146 - 100146

Опубликована: Март 1, 2025

Язык: Английский

Процитировано

0

Iodine-Catalyzed Room-Temperature Aerobic Oxidation of C(sp3)–H Bonds and Its Application in the Synthesis of Quinoxaline Derivatives DOI

Hanyu Xiong,

Longxing Wang,

Yuanyang Mu

и другие.

The Journal of Organic Chemistry, Год журнала: 2025, Номер unknown

Опубликована: Май 1, 2025

An iodine-catalyzed aerobic oxidation reaction of C(sp3)-H bonds was established at room temperature. In this transformation, iodine acts as a Lewis acid catalyst, and the pyridine moiety in substrate plays crucial role. Under optimum conditions, picolyl ketone substrates were smoothly transformed into corresponding 1,2-dicarbonyl compounds, subsequent introduction 1,2-diaminobenzenes mixture led to formation various quinoxaline derivatives. This synthetic process does not use transition metals also features mild operational simplicity, gram-scale synthesis.

Язык: Английский

Процитировано

0

Design and Synthesis of New Pyridine-Thiazole Hybrids as Potential Antibacterial Agents: Spectral, Antimicrobial, and in silico Molecular Docking Studies DOI
Sagar Ramdas Shrimandilkar, Pravin Tryambake,

Seema Borgave

и другие.

Journal of Molecular Structure, Год журнала: 2025, Номер unknown, С. 142612 - 142612

Опубликована: Май 1, 2025

Язык: Английский

Процитировано

0

Unraveling Structural and Anticancer Properties of Pyridine-Oxadiazole Derivatives: Single-Crystal XRD, Hirshfeld Analysis, and Cytotoxicity against A549 Cells DOI Creative Commons
Yogeesha N. Nayak, Deepika Dwarakanath,

Keerthana Suresh Kizhakkanoodan

и другие.

ACS Omega, Год журнала: 2025, Номер unknown

Опубликована: Июнь 1, 2025

Язык: Английский

Процитировано

0

CYP3A4 drug metabolism considerations in pediatric pharmacotherapy DOI Creative Commons

Marin Vander Schaaf,

Kyrle Luth,

Danyelle M. Townsend

и другие.

Medicinal Chemistry Research, Год журнала: 2024, Номер unknown

Опубликована: Дек. 5, 2024

Abstract Cytochrome P450 3A4 (CYP3A4) is a crucial enzyme involved in the Phase I metabolism of numerous medications used clinical practice. Its potential significance pediatric pharmacotherapy underscored by unique metabolic profile children, which differs markedly from adults, especially neonates, infants, and young children due to developmental changes activity. This review explores critical role CYP3A4 drugs population, with particular focus on combination drug therapies. Given high for drug-drug interactions therapies, understanding modulation activity essential optimizing therapeutic outcomes minimizing adverse effects. paper further examines structural similarities between these bergamottin, known inhibitor found citric fruits such as grapefruit. Variability activity, influenced genetic polymorphisms, stage, external factors, necessitates careful consideration prescribing management children. corroborates need personalized medicine approaches enhanced pharmacovigilance ensure safe effective use CYP3A4-metabolized population. Graphical

Язык: Английский

Процитировано

2