70618-87-0Relevant academic research and scientific papers
Thio- and selenosemicarbazones as antiprotozoal agents against Trypanosoma cruzi and Trichomonas vaginalis
álvarez-Márquez, Manuel,Escario, José Antonio,Espinosa-Buitrago, Teresa,Fernández-Bola?os, José G.,Fonseca-Berzal, Cristina,Gómez-Barrio, Alicia,Gómez-Nú?ez, María,Ibá?ez-Escribano, Alexandra,López, óscar,Lacueva-Arnedo, Manuel,Martín-Pérez, Tania,Martínez-Montiel, Mónica,Merino-Montiel, Penélope,Montiel-Smith, Sara
, p. 781 - 791 (2022/03/09)
Herein, we report the preparation of a panel of Schiff bases analogues as antiprotozoal agents by modification of the stereoelectronic effects of the substituents on N-1 and N-4 and the nature of the chalcogen atom (S, Se). These compounds were evaluated towards Trypanosoma cruzi and Trichomonas vaginalis. Thiosemicarbazide 31 showed the best trypanocidal profile (epimastigotes), similar to benznidazole (BZ): IC50 (31)=28.72 μM (CL-B5 strain) and 33.65 μM (Y strain), IC50 (BZ)=25.31 μM (CL-B5) and 22.73 μM (Y); it lacked toxicity over mammalian cells (CC50 > 256 μM). Thiosemicarbazones 49, 51 and 63 showed remarkable trichomonacidal effects (IC50?=16.39, 14.84 and 14.89 μM) and no unspecific cytotoxicity towards Vero cells (CC50 ≥ 275 μM). Selenoisosters 74 and 75 presented a slightly enhanced activity (IC50=11.10 and 11.02 μM, respectively). Hydrogenosome membrane potential and structural changes were analysed to get more insight into the trichomonacidal mechanism.
One-pot two-step facile synthesis of 2,3,4,5-tetra substituted dihydrooxazoles and their antimicrobial activity
Tiwari, Shailendra,Pathak, Poonam,Pratap Singh, Kamal,Sagar, Ram
supporting information, p. 3802 - 3805 (2017/07/27)
New 2,3,4,5-tetra substituted dihydrooxazoles derivatives were efficiently synthesized starting from benzaldehyde, aryl thiosemicarbazide and benzoin using designed synthetic route. Newly synthesized 2,3,4,5-tetra substituted dihydrooxazole derivatives we
One-pot and catalyst-free synthesis of thiosemicarbazones via multicomponent coupling reactions
Cunha, Silvio,Silva, Tiago Lima da
experimental part, p. 2090 - 2093 (2009/09/05)
A novel and efficient procedure for the synthesis of thiosemicarbazones has been achieved via a multicomponent and catalyst-free reaction of phenyl or p-chlorophenyl isothiocyanate, hydrazine, and aldehydes or ketones. The method afforded 20 thiosemicarba
Novel synthesis of new 5,7-disubstituted-2-alkyl/arylamino-4H-pyrazolothiadiazines and 4,6-disubstituted-3-amino/anilino-2-alkyl/aryliminopyrazolothiazolines
Chande, Madhukar S.,Joshi, Rajesh D.
, p. 289 - 301 (2007/10/02)
The title compounds have been prepared by the interaction of substituted 4-bromopyrazolin-5-ones with thiosemicarbazides.An alternate unambiguous synthesis of pyrazolothiazolines has been described.All the compounds have been characterised by spect
2-Acetylpyridine thiosemicarbazones. 1. A new class of potential antimalarial agents
Klayman,Bartosevich,Griffin,Mason,Scovill
, p. 855 - 862 (2007/10/04)
Based on the antimalarial properties observed for 2-acetylpyridine 4-phenyl-3-thiosemicarbazone (1), an extensive series of related thiosemicarbazones was prepared and tested against Plasmodium berghei in mice. Screening results indicated that the presence of the 2-pyridylethylidene group was critical and that certain phenyl, benzyl, phenethyl, or cycloalkyl groups at N4 of the thiosemicarbazone moiety also contribute to antimalarial activity.
