61043-10-5Relevant articles and documents
Elucidation of the structure of the antineoplastic agents, 2 formylpyridine and 1 formylisoquinoline thiosemicarbazones
Antonini,Claudi,Franchetti,Grifantini,Martelli
, p. 447 - 449 (1977)
The geometrical isomers of the antineoplastic agents 2 formylpyridine and 1 formylisoquinoline thiosemicarbazones were synthesized and their structure was studied by spectroscopic methods. It was found that the compounds previously described in the litera
4-(3-Nitrophenyl)thiazol-2-ylhydrazone derivatives as antioxidants and selective hMAO-B inhibitors: synthesis, biological activity and computational analysis
Secci, Daniela,Carradori, Simone,Petzer, Anél,Guglielmi, Paolo,D’Ascenzio, Melissa,Chimenti, Paola,Bagetta, Donatella,Alcaro, Stefano,Zengin, Gokhan,Petzer, Jacobus P.,Ortuso, Francesco
, p. 597 - 612 (2019/02/14)
A new series of 4-(3-nitrophenyl)thiazol-2-ylhydrazone derivatives were designed, synthesised, and evaluated to assess their inhibitory effect on the human monoamine oxidase (hMAO) A and B isoforms. Different (un)substituted (hetero)aromatic substituents were linked to N1 of the hydrazone in order to establish robust structure–activity relationships. The results of the biological testing demonstrated that the presence of the hydrazothiazole nucleus bearing at C4 a phenyl ring functionalised at the meta position with a nitro group represents an important pharmacophoric feature to obtain selective and reversible human MAO-B inhibition for the treatment of neurodegenerative disorders. In addition, the most potent and selective MAO-B inhibitors were evaluated in silico as potential cholinesterase (AChE/BuChE) inhibitors and in vitro for antioxidant activities. The results obtained from molecular modelling studies provided insight into the multiple interactions and structural requirements for the reported MAO inhibitory properties.
2-Pyridyl thiazoles as novel anti-Trypanosoma cruzi agents: Structural design, synthesis and pharmacological evaluation
Cardoso, Marcos Veríssimo De Oliveira,Siqueira, Lucianna Rabelo Pessoa De,Silva, Elany Barbosa Da,Costa, Lívia Bandeira,Hernandes, Marcelo Zaldini,Rabello, Marcelo Montenegro,Ferreira, Rafaela Salgado,Da Cruz, Luana Faria,Magalh?es Moreira, Diogo Rodrigo,Pereira, Valéria Rêgo Alves,De Castro, Maria Carolina Accioly Brelaz,Bernhardt, Paul V.,Leite, Ana Cristina Lima
, p. 48 - 59 (2014/10/15)
The present work reports on the synthesis, anti-Trypanosoma cruzi activities and docking studies of a novel series of 2-(pyridin-2-yl)-1,3- thiazoles derived from 2-pyridine thiosemicarbazone. The majority of these compounds are potent cruzain inhibitors