Pyrazole scaffold‐based derivatives: A glimpse of α‐glucosidase inhibitory activity, SAR, and route of synthesis
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DOI: 10.1002/ardp.202200421
Abstract: The α‐glucosidase is a validated target to develop drugs for treating type 2 diabetes mellitus. The existing α‐glucosidase inhibitors have certain shortcomings related to side effects and route of synthesis. Accordingly, it is inevitable to… read more here.
Keywords: glucosidase; synthesis; glucosidase inhibitors; activity ... See more keywords
Remarkable colorimetric sensing behavior of pyrazole-based chemosensor towards Cu(II) ion detection: synthesis, characterization and theoretical investigations
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DOI: 10.1039/c8ra02905a
Abstract: We report the synthesis of a new imine based ligand, 3-((3-methoxybenzylidene)amino)-1H-pyrazol-5-ol (HL) and its Cu(II) complexes in 2 : 1 (HL : metal) and 1 : 1 : 1 (HL : metal : HQ) stoichiometric ratio using 8-hydroxyquinoline (HQ) as an additional bidentate ligand. The synthesized ligand… read more here.
Keywords: remarkable colorimetric; behavior pyrazole; sensing behavior; ligand ... See more keywords
Supramolecular polymerization of BODIPY dyes extended with rationally designed pyrazole-based motifs
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DOI: 10.1039/d1py00963j
Abstract: Two distinct aggregation pathways during the supramolecular polymerization of BODIPY dyes functionalized with rationally designed pyrazole-based motifs have been investigated. read more here.
Keywords: supramolecular polymerization; designed pyrazole; polymerization bodipy; bodipy dyes ... See more keywords
Enantioselective synthesis of C–C and C–N axially chiral pyrazole-based heterobiaryls
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DOI: 10.1039/d5sc06841j
Abstract: Axially chiral five-membered heteroaryls are prevalent in bioactive molecules. Their catalytic asymmetric synthesis remains challenging due to their relatively low rotational energy barriers. We developed a chiral nickel(ii) complex-catalyzed asymmetric cycloaddition/oxidation sequential reaction of hydrazonoyl… read more here.
Keywords: based heterobiaryls; enantioselective synthesis; pyrazole based; axially chiral ... See more keywords
Pyrazole-based photoinitiator with antibacterial activity
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DOI: 10.14314/polimery.2024.3.3
Abstract: 1-(naphthalen-2-yl)-2-(1H-pyrazol-1-yl) ethanone (MPPY) was synthesized. The structure was characterized by spectral analysis (1H-NMR, FTIR). The molar absorptivity of MPPY is high enough, similarly to acetonaphthone derivatives, to be used as an efficient type I photoinitiator.… read more here.
Keywords: photoinitiator antibacterial; based photoinitiator; pyrazole based; antibacterial activity ... See more keywords
Discovery of 3-Amino-1H-pyrazole-Based Kinase Inhibitors to Illuminate the Understudied PCTAIRE Family
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DOI: 10.3390/ijms232314834
Abstract: The PCTAIRE subfamily belongs to the CDK (cyclin-dependent kinase) family and represents an understudied class of kinases of the dark kinome. They exhibit a highly conserved binding pocket and are activated by cyclin Y binding.… read more here.
Keywords: family; kinase; amino pyrazole; discovery amino ... See more keywords
Synthesis of Pyrazole-Based Inhibitors of the Bacterial Enzyme N-Succinyl-l,l-2,6-Diaminopimelic Acid Desuccinylase (DapE) as Potential Antibiotics
Sign Up to like & getrecommendations! Published in 2024 at "International Journal of Molecular Sciences"
DOI: 10.3390/ijms26010022
Abstract: Based on the inhibitory potencies from earlier reported tetrazole thioether analogs, we now describe the synthesis and inhibition of pyrazole-based inhibitors of N-succinyl-l,l-2,6-diaminopimelic acid desuccinylase (DapE) from Haemophilus influenzae (HiDapE). The most potent pyrazole analog… read more here.
Keywords: acid desuccinylase; diaminopimelic acid; pyrazole based; succinyl diaminopimelic ... See more keywords
New Benzofuran–Pyrazole-Based Compounds as Promising Antimicrobial Agents: Design, Synthesis, DNA Gyrase B Inhibition, and In Silico Studies
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DOI: 10.3390/ph17121664
Abstract: Background/Objectives: The alarming rise in antibiotic resistance necessitates the discovery of novel antimicrobial agents. This study aims to design, synthesize, and evaluate new benzofuran–pyrazole-based compounds for their antimicrobial, antioxidant, and anti-inflammatory properties. Methods: New benzofuran–pyrazole… read more here.
Keywords: benzofuran pyrazole; pyrazole based; dna gyrase; antimicrobial agents ... See more keywords
Microbiological Screening of 5-Functionalized Pyrazoles for the Future Development of Optimized Pyrazole-Based Delivery Systems
Sign Up to like & getrecommendations! Published in 2022 at "Pharmaceutics"
DOI: 10.3390/pharmaceutics14091770
Abstract: The pyrazole ring represents a widely applied chemical scaffold in medicinal chemistry research and we have observed that the physicochemical and biological features of highly substituted pyrazoles can be successfully improved by their encapsulation in… read more here.
Keywords: microbiological screening; future development; delivery systems; delivery ... See more keywords