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In a SAR study, we have synthesized a few 1H-pyrazole carboxylate related microbicides using Vilsmeier reagent. The anti-microbial screening results of 1H-pyrazole-3-carboxylate are reported here for the first time. The effect of 1H-pyrazole carboxylates on the mycelial growth of plant pathogenic fungi is revealed. The first X-ray structure in the family of microbicidal 1H-pyrazole-4-carboxylates is presented.
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http://dx.doi.org/10.1016/j.bmcl.2004.09.066 | DOI Listing |
ACS Med Chem Lett
August 2025
Medicinal Chemistry, Institute of Pharmacy and Molecular Biotechnology IPMB, Heidelberg University, Im Neuenheimer Feld 364, D-69120 Heidelberg, Germany.
We present the discovery of pyrazole-3-carboxylic acid derivatives as novel dengue virus (DENV) NS2B-NS3 protease inhibitors. The discovery was triggered by omission of the phenylglycine scaffold of previous lead structures. We established a robust, regioselective synthetic route toward pyrazole-3-carboxylic acid derivatives.
View Article and Find Full Text PDFChemistryOpen
August 2025
Department of Uzhhorod national university, 3 Narodna Sq, Uzhhorod, Ukraine.
The efficient synthesis of terminal N-alkenyl and N-alkynyl derivatives of pyrazole-4-carboxylic acids and their methyl esters as substrates for studying electrophilic heterocyclization has been reported. The regiochemistry and stereoselectivity of the tellurium-induced heterocyclization of 1-pentynyl (butynyl, butenyl) substituted pyrazole-4-carboxylic acids and their methyl esters under the action of tellurium (IV) oxide in hydrohalic acid were determined. This electrophilic heterocyclization leads to the formation of tetrahydropyrazolo[1,2-a]pyridazinium and dihydropyrazolo[1,2-a]pyrazolium intramolecular salts, as confirmed by X-ray diffraction (XRD) and comprehensive spectral analysis.
View Article and Find Full Text PDFChemistry
August 2025
Department of Applied Chemistry, College of Life Sciences, Ritsumeikan University, 1-1-1 Noji-higashi, Kusatsu, Shiga, 525-8577, Japan.
Bifunctional iridium complexes having a β-protic C-N chelating pyrazole ligand catalyze the carboxylative cyclization of 1-methylamino-2-butyne under atmospheric CO. This reaction affords a five-membered cyclic urethane, along with a six-membered regioisomer. Alkenyliridium(III) complexes as catalytic intermediate models are formed by stoichiometric reaction of related nonprotic pyrazole complexes with 1-methylamino-2-butyne and CO in the presence of AgO, although the protic pyrazole analog is too unstable to be detected.
View Article and Find Full Text PDFRSC Adv
July 2025
Department of Chemistry, Basic of Sciences Faculty, Ilam University 69315-516 Ilam Iran
In this study, we successfully utilized natural asphalt as a natural carbon substrate for the synthesis of a novel heterogeneous Brønsted acid nanocatalyst, Re-NA-CHCOH. The -COOH functional groups present on the surface of Reduced Natural Asphalt Oxide (Re-NA-oxide) serve as catalytic sites for Brønsted acid. This arrangement, in addition to increasing acidity, also expands the surface area accessible for catalytic activity, positioning Re-NA-oxide as a viable option for a range of acid-catalyzed reactions.
View Article and Find Full Text PDFStroke
September 2025
Graduate Institute of Biomedical Science (Y.-P.C., H.-R.J., C.-D.C.), China Medical University, Taichung, Taiwan.
Background: In the aftermath of intracerebral hemorrhage (ICH), the clearance of harmful substances from the hematoma helps to mitigate brain edema and reduce the risk of subsequent neurological damage. This study aimed to investigate the mechanism underlying early hematoma processing following ICH and to explore the potential of modulating this process via astrocyte regulation.
Methods: ICH was induced by intrastriatal injection of bacterial collagenase.