51146-60-2Relevant academic research and scientific papers
Inhibitions of monoamine oxidases and acetylcholinesterase by 1-methyl, 5-phenyl substituted thiosemicarbazones: Synthesis, biochemical, and computational investigations
Jayanthi, Sivaraman,Kim, Hoon,Kumar, Kumudhavalli Suresh,Mathew, Bijo,Mathew, Githa Elizabeth,Mohan, Kumar,Oh, Jong Min
, p. 246 - 253 (2020/10/02)
A series of eleven 1-methyl, 5-phenyl substituted thiosemicarbazones (MT1–MT11) with the phenyl ring substitutions were prepared and investigated for their inhibitory activities against monoamine oxidases (MAOs) and acetylcholinesterase (AChE). [4-(dimeth
Unexpected ring enlargement of 2-hydrazono-2,3-dihydro-1,3-thiazoles to 1,3,4-thiadiazines
Pfeiffer, Wolf-Diethard,Ahlers, Klaus-Dieter,Saghyan, Ashot S.,Villinger, Alexander,Langer, Peter
, p. 76 - 87 (2014/02/14)
The cyclization of thiosemicarbazide with α-bromoacetophenone can result in the formation of isomeric 1,3,4-thiadiazines and two different thiazoles. We studied the use of 4-methyl- and 4-ethylthiosemicarbazide as dinucleophilic building blocks. In this c
Coordination of nitro-thiosemicarbazones to ruthenium(II) as a strategy for anti-trypanosomal activity improvement
Rodrigues, Claudia,Batista, Alzir A.,Ellena, Javier,Castellano, Eduardo E.,Benítez, Diego,Cerecetto, Hugo,González, Mercedes,Teixeira, Letícia R.,Beraldo, Heloisa
experimental part, p. 2847 - 2853 (2010/08/20)
Complexes [RuCl(H4NO2Fo4M)(bipy)(dppb)]PF6 (1), [RuCl(H4NO2Fo4M)(Mebipy)(dppb)]PF6 (2), [RuCl(H4NO 2Fo4M)(phen)(dppb)]PF6 (3), [RuCl(H4NO2Ac4M) (bipy)(dppb)]PF6 (4), [RuCl(H4NO2Ac4M)(Mebipy)(dppb)] PF6 (5) and [RuCl(H4NO2Ac4M)(phen)(dppb)]PF6 (6) with N4-methyl-4-nitrobenzaldehyde thiosemicarbazone (H4NO 2Fo4M) and N4-methyl-4-nitroacetophenone thiosemicarbazone (H4NO2Ac4M) were obtained from [RuCl2(bipy)(dppb)], [RuCl2(Mebipy)(dppb)], and [RuCl2(phen)(dppb)], (dppb = 1,4-bis(diphenylphospine)butane; bipy = 2,2′-bipyridine; Mebipy = 4,4′-dimethyl-2,2′-bipyridine; phen = 1,10-phenanthroline). In all cases the thiosemicarbazone is attached to the metal center through the sulfur atom. Complexes (1-6), together with the corresponding ligands and the Ru precursors were evaluated for their ability to in vitro suppress the growth of Trypanosoma cruzi. All complexes were more active than their corresponding ligands and precursors. Complexes (1-3) and (5) revealed to be the most active among all studied compounds with ID50 = 0.6-0.8 μM. In all cases the association of the thiosemicarbazone with ruthenium, dppb and bipyridine or phenanthroline in one same complex proved to be an excellent strategy for activity improvement.
Manganese(II) complexes with N4-methyl-4-nitrobenzaldehyde, N4-methyl-4-nitroacetofenone, and N4-methyl-4- nitrobenzophenone thiosemicarbazone: Investigation of in vitro activity against Trypanosoma cruzi
Batista, Denise Da Gama Jaén,Da Silva, Patrícia Bernardino,Lachter, Daniela R.,Silva, Renata S.,Aucelio, Ricardo Q.,Louro, Sonia R.W.,Beraldo, Heloisa,Soeiro, Maria De Nazaré C.,Teixeira, Letícia R.
experimental part, p. 2232 - 2238 (2011/01/05)
Thiosemicarbazones are known to be active against different pathogenic microorganisms including Trypanosoma cruzi, the etiological agent of Chagas disease. In the search for new therapeutic drugs against this illness, the complexes [Mn(H4NO2Fo4M)2Cl2] (1), [Mn(H4NO2Ac4M)2Cl2] (2) and [Mn(H4NO 2Bz4M)2Cl2] (3) of N4-methyl-4- nitrobenzaldehyde thiosemicarbazone (H4NO2Fo4M), N 4-methyl-4-nitroacetophenone thiosemicarbazone (H4NO2Ac4M) and N4-methyl-4-nitrobenzophenone thiosemicarbazone (H4NO 2Bz4M) were obtained and screened in vitro against bloodstream and intracellular forms of T. cruzi. H4NO2Fo4M, H4NO2Ac4M and their Mn(II) complexes displayed poor effect on bloodstream trypomastigotes, with IC50 values ranging from 68 to >200 μM. However, although H4NO2Bz4M was also not active, its corresponding Mn(II) complex presented high effect on this T. cruzi form, with an IC50 value of 19 μM. The effect of complex (3), against trypomastigotes of T. cruzi supports further in vitro as well as in vivo studies.
