Pyrimidine-based dual-target inhibitors targeting epidermal growth factor receptor for overcoming drug resistance in cancer therapy(2006-present) DOI

Yufeng An,

Xinya Lv,

Shidi Xu

et al.

European Journal of Medicinal Chemistry, Journal Year: 2025, Volume and Issue: 286, P. 117268 - 117268

Published: Jan. 13, 2025

Language: Английский

Therapeutic potential of pyrrole and pyrrolidine analogs: an update DOI Open Access
N. Jeelan Basha,

S. M. Basavarajaiah,

K. Shyamsunder

et al.

Molecular Diversity, Journal Year: 2022, Volume and Issue: 26(5), P. 2915 - 2937

Published: Jan. 25, 2022

Language: Английский

Citations

119

Chemistry and Pharmacology of Fluorinated Drugs Approved by the FDA (2016–2022) DOI Creative Commons
Ghulam Shabir, Aamer Saeed,

Wajeeha Zahid

et al.

Pharmaceuticals, Journal Year: 2023, Volume and Issue: 16(8), P. 1162 - 1162

Published: Aug. 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

Language: Английский

Citations

48

Fungal Drug Response and Antimicrobial Resistance DOI Creative Commons

Paloma Osset-Trénor,

Amparo Pascual‐Ahuir, Markus Proft

et al.

Journal of Fungi, Journal Year: 2023, Volume and Issue: 9(5), P. 565 - 565

Published: May 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.

Language: Английский

Citations

47

Heterocyclic pyrimidine derivatives as promising antibacterial agents DOI
Kainat Ahmed, M. Iqbal Choudhary, Rahman Shah Zaib Saleem

et al.

European Journal of Medicinal Chemistry, Journal Year: 2023, Volume and Issue: 259, P. 115701 - 115701

Published: Aug. 5, 2023

Language: Английский

Citations

46

Mini-Reviewing the Synthesis of Dihydropyrimidine Derivatives DOI
Dharmesh Katariya,

Amita Vyas,

Ranjan C. Khunt

et al.

Reviews and Advances in Chemistry, Journal Year: 2025, Volume and Issue: unknown

Published: Jan. 8, 2025

Language: Английский

Citations

3

Emerging impact of triazoles as anti-tubercular agent DOI
Anindra Sharma, Anand K. Agrahari, Sanchayita Rajkhowa

et al.

European Journal of Medicinal Chemistry, Journal Year: 2022, Volume and Issue: 238, P. 114454 - 114454

Published: May 13, 2022

Language: Английский

Citations

54

A Search for Heterocycles in GOTHAM Observations of TMC-1 DOI
Timothy Barnum, Mark A. Siebert, Kin Long Kelvin Lee

et al.

The Journal of Physical Chemistry A, Journal Year: 2022, Volume and Issue: 126(17), P. 2716 - 2728

Published: April 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.

Language: Английский

Citations

42

Azolylpyrimidinediols as Novel Structural Scaffolds of DNA-Groove Binders against Intractable Acinetobacter baumannii DOI

Yi-Min Tan,

Ya Wang, Shuo Li

et al.

Journal of Medicinal Chemistry, Journal Year: 2023, Volume and Issue: 66(7), P. 4910 - 4931

Published: March 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.

Language: Английский

Citations

31

Recent medicinal approaches of novel pyrimidine analogs: A review DOI Creative Commons
Sharanabasappa B. Patil

Heliyon, Journal Year: 2023, Volume and Issue: 9(6), P. e16773 - e16773

Published: June 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.

Language: Английский

Citations

30

Synthesis and antibacterial activities of novel hybrid molecules based on benzothiazole, benzimidazole, benzoxazole, and pyrimidine derivatives, each connected to N-arylacetamide and benzoate groups DOI
Ahmed H. M. Elwahy,

Hadeel F. Hammad,

Nada S. Ibrahim

et al.

Journal of Molecular Structure, Journal Year: 2024, Volume and Issue: 1307, P. 137965 - 137965

Published: March 5, 2024

Language: Английский

Citations

9