122813-74-5Relevant articles and documents
Synthesis, characterization and biological evaluation of novel 1-N-substituted thiocarbomoyl-3-ferrocenyl-2-pyrazoline derivatives
Parveen, Humaira,Alatawi, Raedah Aiyed Suliman,Khan, Salman Ahmad,Al-Ahmdi, Mohammed Issa,Mukhtar, Sayeed,Azam, Amir,Elsayed, Nadia H.
, p. 1835 - 1840 (2016/07/06)
Some novel 1-N-substituted thiocarbomoyl-3-ferrocenyl-2-pyrazoline derivatives were synthesized and evaluated for in vitro antiamoebic activity against HM1:IMSS strain of Entamoeba histolytica. The results showed that most of the compounds exhibited promising activity (IC50 values in the range of 0.050-1.683 μM) than the reference drug metronidazole (IC50 = 1.78 μM). Active compounds were further screened for cytotoxicity against human embryonic kidney-293 (HEK-293) normal cell lines to ensure their toxic effect and the results revealed that active compounds were least toxic in the concentration range of 2.5-50 μM for 48 h and 2.5-25 μM for 72 h. At 100 μM for 48 h and at 50 μM for 72 h only four compounds 2c, 2h, 2k and 2l showed maximum viability and least cytotoxicity, respectively, concluding that all the screened compounds were least cytotoxic against human embryonic kidney-293 (HEK-293) normal cell lines in the concentration range of 2.5-50 and 2.5-25 μM.
New 2-aminothiadiazole derivatives
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Page/Page column 25, (2011/08/03)
The present invention relates to a compound of formula (I), or a pharmaceutically acceptable salt or N-oxide thereof: wherein: ? L represents a direct bond or a -S(O)2- group, ? n is an integer having a value from 0 to 2, ? R1 represents a pyridyl group or an imidazo[1,2-a]pyridinyl group, wherein the pyridyl group is substituted with one or more substituents selected from halogen atoms, a hydroxy group, a C1-4 alkyl group and a C1-4 alkoxy group, or ? R1 represents a group of formula: wherein: o Ra and Rb independently represent a hydrogen atom, halogen atom or a linear or branched C1-4 alkyl group, o Rc represents a hydroxy group, a linear or branched C1-4 alkyl group or C1-4 alkoxy group wherein the alkyl and the alkoxy groups independently are optionally substituted with one or more substituents selected from hydroxy group, cyano group and-NR'R" groups and wherein ■ R' represents a hydrogen atom or a linear or branched C1-4 alkyl group, ■ R" represents a hydrogen atom or a linear or branched C1-4 alkyl group optionally substituted with a hydroxycarbonyl group; or ■ R' and R" together with the nitrogen atom to which they are attached form a 4 to 6 membered, saturated heterocyclic ring optionally substituted with a hydroxycarbonyl group. ? R2 represents a pyridyl group, a C3-6 cycloalkyl group or a phenyl group which is optionally substituted with one or more substituents selected from halogen atoms, cyano group, and C1-4 alkoxy group; and ? R3 represents a C3-6 cycloalkyl group, a C3-6 cycloalkyl-C1-2 alkyl group or a linear or branched C2-4 alkyl group optionally substituted with one or more substituents selected from halogen atoms and C1-2 alkoxy group.
Bis-pyrazolines: Synthesis, characterization and antiamoebic activity as inhibitors of growth of Entamoeba histolytica
Bhat, Abdul R.,Athar, Fareeda,Azam, Amir
scheme or table, p. 426 - 431 (2009/04/18)
The cyclization of chalcone with N-4 substituted thiosemicarbazides under basic condition led to the formation of new compounds, thiocarbamoyl bis-pyrazoline derivatives. The structure of the compounds were elucidated by UV, IR, 1H NMR, 13C NMR and ESI-MS spectral data and thermogravimetric analysis, and their purities were confirmed by elemental analyses. The antiamoebic activity of these complexes was evaluated by microdilution method against HM1:IMSS strain of Entamoeba histolytica and the results were compared with the standard drug, metronidazole. Structure-activity relationship shows that the compound with aromatic substituents at the thiocarbamoyl group was more active than those with the cyclic groups. However, it was clear from the IC50 values that the compounds 15 and 20 are more active and both showed a structural resemblance having an electron withdrawing groups attached to the phenyl ring. MTT assay showed that all the compounds are non-toxic to human kidney epithelial cell line.
