European Journal of Medicinal Chemistry, Год журнала: 2025, Номер 286, С. 117268 - 117268
Опубликована: Янв. 13, 2025
Язык: Английский
Molecular Diversity, Год журнала: 2022, Номер 26(5), С. 2915 - 2937
Опубликована: Янв. 25, 2022
Язык: Английский
Процитировано
119
Pharmaceuticals, Год журнала: 2023, Номер 16(8), С. 1162 - 1162
Опубликована: Авг. 15, 2023
Fluorine is characterized by high electronegativity and small atomic size, which provide this molecule with the unique property of augmenting potency, selectivity, metabolic stability, pharmacokinetics drugs. (F) substitution has been extensively explored in drug research as a means improving biological activity enhancing chemical or stability. Selective F onto therapeutic diagnostic candidate can enhance several pharmacokinetic physicochemical properties such stability membrane permeation. The increased binding ability fluorinated target proteins also reported some cases. An emerging line on addressed using 18F radiolabel tracer atom extremely sensitive methodology positron emission tomography (PET) imaging. This review aims to report drugs approved US Food Drug Administration (FDA) from 2016 2022. It cites selected examples variety FDA-approved period have heterocyclic cores, including pyrrole, pyrazole, imidazole, triazole, pyridine, pyridone, pyridazine, pyrazine, pyrimidine, triazine, purine, indole, benzimidazole, isoquinoline, quinoline appended either F-18 F-19. Some oligonucleotides were authorized FDA between 2019
Язык: Английский
Процитировано
48
Journal of Fungi, Год журнала: 2023, Номер 9(5), С. 565 - 565
Опубликована: Май 12, 2023
Antifungal resistance is a growing concern as it poses significant threat to public health. Fungal infections are cause of morbidity and mortality, especially in immunocompromised individuals. The limited number antifungal agents the emergence have led critical need understand mechanisms drug resistance. This review provides an overview importance resistance, classes agents, their mode action. It highlights molecular including alterations modification, activation, availability. In addition, discusses response drugs via regulation multidrug efflux systems drug–target interactions. We emphasize understanding develop effective strategies combat highlight for continued research identify new targets development explore alternative therapeutic options overcome Overall, its will be indispensable field clinical management fungal infections.
Язык: Английский
Процитировано
47
European Journal of Medicinal Chemistry, Год журнала: 2023, Номер 259, С. 115701 - 115701
Опубликована: Авг. 5, 2023
Язык: Английский
Процитировано
46
Reviews and Advances in Chemistry, Год журнала: 2025, Номер unknown
Опубликована: Янв. 8, 2025
Язык: Английский
Процитировано
3
European Journal of Medicinal Chemistry, Год журнала: 2022, Номер 238, С. 114454 - 114454
Опубликована: Май 13, 2022
Язык: Английский
Процитировано
54
The Journal of Physical Chemistry A, Год журнала: 2022, Номер 126(17), С. 2716 - 2728
Опубликована: Апрель 20, 2022
We have conducted an extensive search for nitrogen-, oxygen-, and sulfur-bearing heterocycles toward Taurus Molecular Cloud 1 (TMC-1) using the deep, broadband centimeter-wavelength spectral line survey of region from GOTHAM large project on Green Bank Telescope. Despite their ubiquity in terrestrial chemistry, confirmed presence a number cyclic polycyclic hydrocarbon species source, we find no evidence any heterocyclic species. Here, report derived upper limits column densities these molecules obtained by Markov Chain Monte Carlo (MCMC) analysis compare this approach to traditional single-line limit measurements. further hypothesize why are absent our data, how they might form interstellar space, nature observations that would be needed secure detection.
Язык: Английский
Процитировано
42
Journal of Medicinal Chemistry, Год журнала: 2023, Номер 66(7), С. 4910 - 4931
Опубликована: Март 23, 2023
A unique class of antibacterial azolylpyrimidinediols (APDs) and their analogues were developed. Some synthesized compounds showed excellent bacteriostatic potency; especially, triazolylpyrimidinediol (triazolyl PD) 7a exhibited good anti-Acinetobacter baumannii potential with a low MIC 0.002 mmol/L. Triazolyl PD inconspicuous cytotoxicity hemolytic activity could eradicate the established biofilm, resistance, favorable drug-likeness. Mechanistic explorations revealed that compound without membrane-targeting ability decrease metabolic activity, interact DNA through groove binding action to block replication rather than intercalate into cleave DNA, thus inhibit bacterial growth. Further computations displayed EHOMO large energy gap might help triazolyl biological targets more easily. Moreover, gave appreciable in vivo pharmacokinetic properties pharmacodynamics. These findings as novel structural scaffolds DNA-groove binders imply promise for treatments Acinetobacter infection.
Язык: Английский
Процитировано
31
Heliyon, Год журнала: 2023, Номер 9(6), С. e16773 - e16773
Опубликована: Июнь 1, 2023
Pyrimidine derivatives attract researchers due to their versatile scaffold & medicinal significance. associated analogs are majorly contributed the field of chemistry. In this review article, recent new structural design and development active agent studies biological approaches highlighted. addition, potency structure-activity relationship pyrimidines such as antimicrobial, anticancer, anti-inflammatory, analgesic, anti-diabetic, anti-HIV, anthelmintic, CNS depressants, cardiac agents discussed. Finally, article may for novel pyrimidine scaffolds with more less harmful.
Язык: Английский
Процитировано
30
Journal of Molecular Structure, Год журнала: 2024, Номер 1307, С. 137965 - 137965
Опубликована: Март 5, 2024
Язык: Английский
Процитировано
9