740-86-3Relevant 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
On the synthesis of fused thiazolo[5,4-d]isoxazoles and a novel rearrangement involving conversion of 5(4H)-isoxazolones to 4(5H)-isoxazolones
Chande,Joshi
, p. 403 - 409 (2007/10/03)
The interaction of 4-bromo-3-substituted-(4H)-isoxazol-5-ones (1) with alkyl/aryl thiocarbamides (2), 4-alkyl/aryl thiosemicarbazides (7) and 2, 4-disubstituted thiosemicarbazides (12) afford 5-alkyl/ arylamino-3-substituted-thiazolo [5, 4-d]isoxazoles (3) and 6-amino/anilino-5-alkyl/arylimino-3-substituted-thiazolo[5, 4-d]isoxazoles respectively. An alternate unambiguous one step synthesis is described. The compounds have been characterised by chemical reactions and spectral data.
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
