- Synthesis of new 3-aryl-4,5-dihydropyrazole-1-carbothioamide derivatives. An investigation on their ability to inhibit monoamine oxidase
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Some differently substituted 3-aryl-4,5-dihydropyrazoles-1-carbothioamides have been synthesised with the aim to investigate their monoamine oxidase inhibitory activity. The chemical structures of the compounds have been characterized by means of their IR, 1H NMR, 13C NMR spectroscopic data and elemental analyses. All the active compounds showed a selective activity towards the B isoform of the enzyme, regardless of the substitution on the heterocyclic ring. The inhibition of the enzymatic activity was measured on human recombinant MAO isoforms, expressed in baculovirus infected BTI insect cells. Docking experiments were carried out with the aim to rationalize the mechanism of inhibition of the most active and selective compound.
- MacCioni,Alcaro,Orallo,Cardia,Distinto,Costa,Yanez,Sanna,Vigo,Meleddu,Secci
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experimental part
p. 4490 - 4498
(2010/10/19)
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- Synthesis, structure characterization, and biological evaluation of some new 1,2,3-benzotriazole derivatives
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Ten novel benzotriazole compounds were synthesized. Their chemical structures were confirmed by 1H NMR, IR, and elemental analyses, coupled with three selected single-crystal structures (compounds A2, B3, and B5). Their antimycotic and antitumor activities were also investigated. The title compounds showed some antitumor activities, especially in the case of A3 and A4, which showed the most potent activity of propagation inhibition in liver and galactophore cancer cells. Birkhaueser Boston 2009.
- Wan, Jun,Yan, Xia,Ma, Cuiping,Bi, Sai,Zhu, Hai-Liang
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scheme or table
p. 970 - 983
(2011/12/04)
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- Synthesis of Heterocyclic Compounds: Part XXVIII - Potential Antileukemic Agents from 3,4-Dihydro-1,3,2-oxazaphosphorin-2-oxides
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Some 3,6-diaryl-2-chloro-3,4-dihydro-1,3,2-oxazaphosphorin-2-oxides (4a-q, 6a-e and 7a, b) have been synthesised and tested for their anti-leukemic activity.
- Sahasrabudhe, S. D.,Tilak, B. D.
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p. 914 - 917
(2007/10/02)
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