Results 121 to 130 of about 1,937,826 (232)
Regioselective Diversification of Aminopyrazoles via Ir‐Catalyzed C─H Borylation
Aminopyrazoles, an important bioactive pharmacophore, are typically accessed inefficiently through de novo syntheses that yield isomeric mixtures of 3‐ and 5‐substituted derivatives. To address this challenge, we have elaborated readily available 3‐ and 5‐aminopyrazole fragments using Ir C─H borylation, regioselectively furnishing boronates for ...
Jay S. Wright +9 more
wiley +1 more source
A series of title compounds was synthesized, with 6e and 6k exhibiting the lowest IC50 values against MCF‐7, HeLa, and HepG2 cancer cell lines. Molecular docking and dynamics revealed strong binding to the adenosine A1 receptor (ΔG = –9.02 and –9.24 kcal/mol).
Bangar Reddy Vancha +9 more
wiley +1 more source
Synthesis and Anti-Trypanosoma cruzi Activity of New Pyrazole-Thiadiazole Scaffolds
Chagas disease, a silent but widespread disease that mainly affects a socioeconomically vulnerable population, lacks innovative safe drug therapy. The available drugs, benznidazole and nifurtimox, are more than fifty years old, have limited efficacy, and
Thamyris Perez de Souza +6 more
doaj +1 more source
Small‐Molecule Kinase Inhibitors Modulating Circadian Rhythms
ABSTRACT The circadian clock mechanism generates 24‐h rhythms crucial for regulating various physiological processes, and its dysregulation has been implicated in numerous diseases. In cells, the circadian clock operates through a transcriptional‐translational feedback loop, where phosphorylation plays a pivotal role in maintaining accurate circadian ...
Irene Castellino +3 more
wiley +1 more source
Three novel pyrazole-dicarboxylate acid derivatives namely 1-(carboxymethyl)-5-methyl-1H-pyrazole-3-carboxylic acid [L1], 1-[(3-carboxy-5-methyl-1H-pyrazol-1-yl) methyl]-5-methyl-1H-pyrazole-3-carboxylic acid [L2] and 1-[3-(3-carboxy-5-methyl-1H-pyrazol ...
Nayarassery Narayanan, Adarsh +6 more
core +1 more source
Synthesis of Heterocyclic Compounds Derived from 2-Mercapto Quinoline
2-Mercapto quinoline was used as precursor for synthesis of new heterocyclic derivatives of quinoline nucleus such as pyrazole (3), pyrazolone (4), 1,3,4-oxadiazole (5) and 1,2,4-triazole (8). New Schiff bases (9a-e) were obtained from the reaction of
A. H. Sharba, H. A. Hassan, D. F. Hassan
doaj
Experimental setup for dsRNA feeding in Brassicogethes aeneus to evaluate the effect of a synthetic polymer nanocarrier on RNAi efficiency. The experiment assessed whether the nanocarrier enhances RNAi after oral dsRNA delivery. (a) Stability of dsRNA–nanocarrier complexes was tested in simulated gut conditions. (b) Gene expression of αCOP and dre4 was
Triin Kallavus +13 more
wiley +1 more source
Pyrazole-3/5-carboxylic acids from 3/5-trifluoromethyl NH-pyrazoles
International audienceWe report here the transformation of 3/5-trifluoromethylpyrazoles derivative into the corresponding NH-pyrazole-3/5-carboxylic acids.
Janin, Yves, Louis +2 more
core +1 more source
Covalent drug discovery: Progress against key targets, emerging strategies and lessons learnt
Abstract Covalent drug discovery is currently experiencing a boom in industrial and academic interest. To date, at least 75 covalent drugs have received regulatory approval, targeting both traditional target classes and more challenging proteins for which other approaches failed. In many cases, unique aspects of covalent targeting are essential for the
Charles P. Brown +2 more
wiley +1 more source
A simple, facile, and high yielding stereoselective approach for the integration of α-methylene-pyrazole-carboxylates at the β-lactam nucleus is described.
Aman Bhalla (3832465) +4 more
core +1 more source

