20069-28-7Relevant articles and documents
Ensembling three multicomponent reactions for the synthesis of a novel category of pseudo-peptides containing dithiocarbamate and N,X-heterocylic groups
Khalesi, Maryam,Halimehjani, Azim Ziyaei,Franz, Max,Schmidtmann, Marc,Martens, Jürgen
, p. 263 - 272 (2019)
Consecutive multicomponent reactions have been applied for the synthesis of novel pseudo-peptides bearing dithiocarbamate and N,X-heterocyclic groups (X = S, O) in only one structure. The first multicomponent reaction includes the synthesis of dithiocarbamates using an amine or amino acid, CS2 and an electrophile. The second MCR is synthesis of Asinger imines using 2-chloroisobutyraldehyde, NaXH (X = S, O), ketone and ammonia. The final MCR is Ugi reaction to afford the corresponding three-dimensional pseudo-peptides. Various Asinger imines, carboxylic acids and isocyanides were applied in this protocol to provide diversities of pseudo-peptides in high to excellent yields.
Synthesis and reactivity of 2-pyrrolidino-, 2-N-methylpiperazino-, 2-piperidino-, and 2-morpholino-1,3,4-thiadiazines
Knak, Stefanie,Pfeiffer, Wolf-Diethard,Dollinger, Horst,Langer, Peter
, p. 450 - 462 (2015/03/30)
A variety of 2-pyrrolidino-, 2-N-methylpiperazino-, 2-piperidino-, and 2-morpholino-1,3,4-thiadiazines were prepared by cyclocondensation of phenacyl halides with thiosemicarbazides. Heating of the products resulted in desulfurization and formation of pyrazoles. The rate of this process strongly depends on the substitution pattern of the 1,3,4-thiadiazines.
Synthesis, spectral studies and antiamoebic activity of new 1-N-substituted thiocarbamoyl-3-phenyl-2-pyrazolines
Abid, Mohammad,Bhat, Abdul Roouf,Athar, Fareeda,Azam, Amir
scheme or table, p. 417 - 425 (2009/04/18)
Thirty new pyrazoline derivatives were synthesized by cyclization of Mannich bases with thiosemicarbazides being substituted by different cyclic and aromatic amines. The structures of the compounds were elucidated by elemental analyses, UV, IR, 1H and 13C NMR and ESI-MS spectral data. The in vitro antiamoebic activity was evaluated against Entamoeba histolytica in comparison with metronidazole used as reference substance. Out of the 30 compounds screened for antiamoebic activity, 10 (5, 6, 15, 18, 25-30) were found to be better inhibitors of E. histolytica since they showed lesser IC50 values than metronidazole. The preliminary results indicated that the presence of 3-chloro or 3-bromo substituent on the phenyl ring at position 3 of the pyrazoline ring enhanced the antiamoebic activity as compared to unsubstituted phenyl ring. The study suggests that the preliminary activity of these compounds may further be explored for the development of new targets for amoebiasis.