A group of hydrazide and semicarbazide derivatives containing isopropylidene, benzylidene, cyclohexylidene, and phospholidene groups was synthesized and characterized by spectroscopic techniques. These compounds were tested for DNA interaction studies monitored by UV-Vis and IR data as well as molecular docking. Investigations on interactions of these compounds with DNA revealed an intercalative mode of binding between them. It is interesting to note that semicarbazide derivatives with aliphatic substituents showed better DNA binding than the aromatic substituents.
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http://dx.doi.org/10.1007/s12010-014-0868-4 | DOI Listing |
Sci Rep
December 2024
Department of Pharmaceutical Chemistry, Amrita School of Pharmacy, Amrita Vishwa Vidyapeetham, AIMS Health Sciences Campus, Kochi, 682041, India.
Sixteen thio/semicarbazide-based benzyloxy derivatives (BT1-BT16) were synthesized and evaluated for their inhibitory activities against monoamine oxidases (MAOs). Most compounds showed better inhibitory activity against MAO-B than against MAO-A. BT1, BT3, and BT5 showed the greatest inhibitory activity with an identical IC value of 0.
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December 2024
Endocrinology and Metabolism Research Center, Endocrinology and Metabolism Clinical Sciences Institute, Tehran University of Medical Sciences, Tehran, Iran.
In this work, a novel series of quinoline-thiosemicarbazone-1,2,3-triazole-aceamide derivatives 10a-n as new potent α-glucosidase inhibitors was designed, synthesized, and evaluated. All the synthesized derivatives 10a-n were more potent than acarbose (positive control). Representatively, (E)-2-(4-(((3-((2-Carbamothioylhydrazineylidene)methyl)quinolin-2-yl)thio)methyl)-1H-1,2,3-triazol-1-yl)-N-phenethylacetamide (10n), as the most potent entry, with IC = 48.
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November 2024
Department of Chemical and Geological Sciences, University of Cagliari, S.S. 554 Bivio Sestu, Monserrato, 09042 Cagliari, Italy.
Tyrosinase, a key protein in the biosynthesis of melanin pigments, is crucial in determining skin pigmentation. Inhibiting tyrosinase activity is a promising approach for treating conditions related to excessive pigmentation. For the synthesis of more potent tyrosinase inhibitors, we combined two approaches, para-substitution and lipophilicity, to enhance the inhibitory properties of ()-2-(4-hydroxybenzylidene)hydrazine-1-carbotiamide, whose enzyme inhibitory properties have been previously demonstrated.
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November 2024
Applied Organic Chemistry Department, National Research Centre, Dokki, 12622, Cairo, Egypt.
Eur J Med Chem
January 2025
Institute of Chemistry, Universidade Federal Rural do Rio de Janeiro, Seropédica, 23897-000, Brazil. Electronic address:
Inhibition of cholinesterases, combined with antioxidant activity, metal-chelating capacity, and neuroprotection, is recognized as an effective multitarget therapy for the treatment of Alzheimer's disease (AD). Based on our in-house thiosemicarbazone-acridine compounds, this study recognized these derivatives as possible multi-target-directed ligand (MTDL). Initial screening against cholinesterases identified CL-01, which exhibited a promising IC value of 0.
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