- Application of alicyclic ketone hydrazone thiazole derivative serving as tyrosinase inhibitor
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The invention discloses an alicyclic ketone hydrazone thiazole derivative having tyrosinase inhibiting activity. Screening results of in-vitro inhibition tyrosinase show that the synthesized derivative has the tyrosinase inhibiting activity. The compound
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Paragraph 0010; 0011
(2018/09/11)
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- Synthesis, semipreparative HPLC separation, biological evaluation, and 3D-QSAR of hydrazothiazole derivatives as human monoamine oxidase B inhibitors
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The present study reports on synthesis in high yields (70-99%), HPLC enantioseparation, inhibitory activity against human monoamino oxidases, and molecular modeling including 3D-QSAR studies, of a large series of (4-aryl-thiazol-2-yl)hydrazones (1-45). Most of the synthesized compounds proved to be potent and selective inhibitors of hMAO-B isoform in the micromolar or nanomolar range, thus demonstrating that hydrazothiazole could be considered a good pharmacophore to design new hMAO-B inhibitors. Due to the presence in some derivatives of a chiral center, we also performed a semipreparative chromatographic enantioseparation of these compounds obtained by a stereoconservative pattern. The separated enantiomers were submitted to in vitro biological evaluation to point out the stereorecognition of the active site of the enzyme towards these structures. Finally, a 3D-QSAR study was carried out using Comparative Molecular Field Analysis (CoMFA), aiming to deduce rational guidelines for the further structural modification of these lead compounds.
- Chimenti, Franco,Secci, Daniela,Bolasco, Adriana,Chimenti, Paola,Granese, Arianna,Carradori, Simone,MacCioni, Elias,Cardia, M. Cristina,Yanez, Matilde,Orallo, Francisco,Alcaro, Stefano,Ortuso, Francesco,Cirilli, Roberto,Ferretti, Rosella,Distinto, Simona,Kirchmair, Johannes,Langer, Thierry
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experimental part
p. 5063 - 5070
(2010/09/08)
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- Synthesis and in vitro activity of 2-thiazolylhydrazone derivatives compared with the activity of clotrimazole against clinical isolates of Candida spp.
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In this paper, we report on the synthesis of a novel series of 2-thiazolylhydrazone derivatives and the influence of the substituents on the thiazole ring on antifungal activity. All synthesized compounds were screened for their in vitro activities agains
- Chimenti, Franco,Bizzarri, Bruna,Maccioni, Elias,Secci, Daniela,Bolasco, Adriana,Fioravanti, Rossella,Chimenti, Paola,Granese, Arianna,Carradori, Simone,Rivanera, Daniela,Lilli, Daniela,Zicari, Alessandra,Distinto, Simona
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p. 4635 - 4640
(2008/12/20)
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