7283-39-8Relevant articles and documents
Structures of anti,Z-4,4-dimethyl-3-thiosemicarbazide, syn,E,Z-2,4-dimethyl-3-thiosemicarbazide and syn,E-1-cyclopentano-3-thiosemicarbazone
Valente, Edward J.,Zubkowski, Jeffrey D.,Jabalameli, Ali,Mazhari, Sam,Venkatraman, Ramiyer,Sullivan
, p. 27 - 33 (1998)
The structures of three alkyl derivatives of thiosemicarbazide are described: anti,Z-4,4-dimethyl-3-thiosemicarbazide (1), syn,E,Z-2,4-dimethyl-3-thiosemicarbazide (2), and syn,E-1-cyclopentano-3-thiosemicarbazone (3). Crystal data: for 1: triclinic, P-1
Design, synthesis and biochemical evaluation of novel multi-target inhibitors as potential anti-Parkinson agents
Carradori, Simone,Ortuso, Francesco,Petzer, Anél,Bagetta, Donatella,De Monte, Celeste,Secci, Daniela,De Vita, Daniela,Guglielmi, Paolo,Zengin, Gokhan,Aktumsek, Abdurrahman,Alcaro, Stefano,Petzer, Jacobus P.
, p. 1543 - 1552 (2017/11/27)
New 4-(3-nitrophenyl)thiazol-2-ylhydrazone derivatives are proposed as dual-target-directed monoamine oxidase B (MAO-B) and acetylcholinesterase (AChE) inhibitors, as well as antioxidant agents, for the treatment of neurodegenerative disorders such as Parkinson's disease. Rational molecular design, target recognition and predicted pharmacokinetic properties have been evaluated by means of molecular modelling. Based on these properties, compounds were synthesized and evaluated in vitro as MAO-B and AChE inhibitors, and compared to the activities at their corresponding isozymes, monoamine oxidase A (MAO-A) and butyrylcholinesterase (BuChE), respectively. Anti-oxidant properties, potentially useful in the treatment of neurodegenerative disorders, have been also investigated in vitro. Among the evaluated compounds, three inhibitors may be considered as promising dual inhibitors of MAO-B and AChE, in vitro. MAO-B inhibition was also shown to be competitive and reversible for compound 19.
Anti-Candida activity and cytotoxicity of a large library of new N-substituted-1,3-thiazolidin-4-one derivatives
De Monte, Celeste,Carradori, Simone,Bizzarri, Bruna,Bolasco, Adriana,Caprara, Federica,Mollica, Adriano,Rivanera, Daniela,Mari, Emanuela,Zicari, Alessandra,Akdemir, Atilla,Secci, Daniela
, p. 82 - 96 (2015/11/18)
On the basis of the recent findings about the biological properties of thiazolidinones and taking into account the encouraging results about the antifungal activity of some (thiazol-2-yl)hydrazines, new N-substituted heterocyclic derivatives were designed combining the thiazolidinone nucleus with the hydrazonic portion. In details, 1,3-thiazolidin-4-ones bearing (cyclo)aliphatic or (hetero)aromatic moieties linked to the N1-hydrazine at C2 were synthesized and classified into three series according to the aromatic or bicyclic rings connected to the lactam nitrogen of the thiazolidinone. These molecules were assayed for their anti-Candida effects in reference to the biological activity of the conventional topic (clotrimazole, miconazole, tioconazole) and systemic drugs (fluconazole, ketoconazole, amphotericin B). Finally, we investigated the selectivity against fungal cells by testing the compounds endowed with the best MICs on Hep2 cells in order to assess their cell toxicity (CC50) and we noticed that two derivatives were less cytotoxic than the reference drug clotrimazole. Moreover, a preliminary molecular modelling approach has been performed against lanosterol 14-α demethylase (CYP51A1) to rationalize the activity of the tested compounds and to specify the target protein or enzyme.
