Results 41 to 50 of about 46,711 (243)

Search for antibacterial activity in a number of new S-derivatives (1,2,4-triazole-3(2H)-yl)methyl)thiopyrimidines

Aktualʹnì Pitannâ Farmacevtičnoï ì Medičnoï Nauki ta Praktiki, 2021
The relevance of the study of 1,2,4-triazole derivatives with pyrimidine fragment is due to the synthesis of potential broad-spectrum antibacterial drugs, low molecular weight inducers of interferon, and antitumor agents, search for molecular descriptors
Yu. V. Karpenko, O. I. Panasenko
doaj   +1 more source

A New Recruitable E3 Ligase UHRF1 Supporting Targeted Protein Degradation: A Minimal Azide as a Recruitment Ligand

Advanced Science, EarlyView.
Targeted protein degradation is often limited by the scarcity of usable E3 ligases. Herein, we report the first small‐molecule GPX4 degraders that incorporate either electrophilic warheads or a minimal azide group as an E3 recruitment ligand. The azide‐based degrader DK‐5070 effectively drives potent GPX4 degradation; mechanistic studies reveal that ...
Zehong Lin, Kang Duan, Rui Wan, Tao Jiang, Jinzhe Wei, Miao Sun, Mariia A. Skryl'nikova, Maxim A. Gureev, Zhi‐Min Zhang, Zhang Zhang, Ke Ding, Nan Ma, Tongzheng Liu, Yi Tan, Zhengqiu Li   +14 more
wiley   +1 more source

Unveiling the Complete Biosynthetic Pathway of Azacitidine: A Rare 1,3,5‐Triazine Nucleoside Derived From GTP

Angewandte Chemie, EarlyView.
The azacitidine biosynthetic gene cluster (aza BGC) was identified by the resistance‐gene‐guided comparative genomics method in Streptomyces mobaraensis IPIO2. The complete biosynthetic pathway of azacitidine, which follows a “base‐first‐then‐glycosylation” logic, was elucidated through in vivo and in vitro experiments.
Dan Wang, Qingxu Meng, Lingqi Hua, Mengjun Sun, Qianjin Kang, Min‐Juan Xu, Linquan Bai   +6 more
wiley   +2 more sources

Regioselectivity in the Thermal Rearrangement of Unsymmetrical 4-Methyl-4H-1,2,4-triazoles to 1-Methyl-1H-1,2,4-triazoles

Molecules, 2001
The rearrangement of 4-methyl-3,5-diaryl-4H-1,2,4-triazoles to the corresponding 1-methyl-3,5-diaryl-1H-1,2,4-triazoles showed regioselectivity comparable to that observed for the alkylation of 3,5-diaryl-1H-1,2,4-triazoles.
Per H.J. Carlsen, Odd R. Gautun
doaj   +1 more source

AS‐TLC‐Based High‐Throughput Screening Integrated with CuAAC Optimization Strategy Facilitates the Rapid Discovery of YTHDC1 Inhibitor

Advanced Science, EarlyView.
We developed Affinity Selection Thin‐Layer Chromatography (AS‐TLC) as a method for high‐throughput screening (HTS) of compound mixtures. Furthermore, we integrated activity assays with AS‐TLC and identified a YTH domain‐containing protein 1 (YTHDC1) inhibitor. Building on this hit, we applied copper(I)‐catalyzed azide–alkyne cycloaddition (CuAAC) click
Mingchen Wang, Shuiping Fu, Ye Xu, Jia Gao, Jiwei Ren, Xu Yang, Hesong Xu, Ge Sun, Yanjie Li, Yanlin Wang, Lu Jin, Peijuan Chen, Ying Xu, Jianhao Li, Hua Lin, Chujiao Hu, Kaixian Chen, Huan Xiong, Cheng Luo, Shijie Chen   +19 more
wiley   +1 more source

Site‐Specific Protein Bioconjugation Through Cellular Incorporation of Noncanonical Amino Acids

Angewandte Chemie, EarlyView.
Genetic code expansion (GCE) enables site‐specific installation of noncanonical amino acids containing bioorthogonal conjugation handles, allowing precise, homogeneous protein modification. This review examines the principles of orthogonal translation, surveys the chemistries available for chemoselective labeling, and highlights emerging multi‐site ...
Rahul Sarkar, Manas Joshi, Abhishek Chatterjee   +2 more
wiley   +2 more sources

Sequential Patterning of Photoresponsive Hydrogels Directs Crypt Fission and Reveals the Role of Epithelial Curvature on Fission Symmetry

Advanced Science, EarlyView.
Deterministic crypt fission is achieved in intestinal organoids using photopatternable hydrogels with spatiotemporal control. Daughter‐crypt symmetry is shown to depend on parent‐crypt geometry and epithelial curvature, while myosin‐dependent mechanosensing links tissue shape to regenerative outcomes.
Delaney L. McNally, Kaustav Bera, Nolan R. Petrich, Alex Khang, Marilyne Coulombe, David Castillo‐Azofeifa, Ophir D. Klein, Peter J. Dempsey, Kristi S. Anseth   +8 more
wiley   +1 more source

SOLiD‐MaP: A Photoproximity Labeling Platform for Small Molecule Binding Site Mapping on RNA

Angewandte Chemie, EarlyView.
SOLiD‐MaP is a ligand‐directed photoproximity labeling strategy developed for RNA binding‐site analysis. Singlet oxygen‐mediated labeling creates a proximity‐dependent chemical footprint of bound small molecules on RNA. Coupling this chemistry with mutational profiling enables identification of the ligand‐binding region at nucleotide resolution ...
Lin L. Rietveld, Wei Wu, Filip M. Zawisza, Danny Incarnato, Zeshi Li   +4 more
wiley   +2 more sources

Anticonvulsant activity 2-((5-(3-(4-fluorophenyl)-4-R2-1,2,4-triazole-3-yl)-thio)-1-arylethanone

Aktualʹnì Pitannâ Farmacevtičnoï ì Medičnoï Nauki ta Praktiki, 2019
The aim of work is to study of the anticonvulsant activity of 2-((5-(3-,4-fluorophenyl)-4-R2-1,2,4-triazole-3-yl)thio)-1-aryletanones, the establishment of some laws between the structure of compounds and their activity. Materials and methods.
O. A. Bihdan
doaj   +1 more source

Synthesis and properties of S-alkyl 4-amino-5-(5-(3-fluorophenyl)-pyrazol-3-yl)-1,2,4-triazole-3-thiol derivatives

Aktualʹnì Pitannâ Farmacevtičnoï ì Medičnoï Nauki ta Praktiki, 2023
An important direction of modern pharmaceutical science is the creation of promising biologically active compounds, which in the hands of scientists can be transformed into effective medicinal products. Heterocyclic compounds are the undisputed leader in
S. O. Fedotov, A. S. Hotsulia
doaj   +1 more source