4750-57-6Relevant articles and documents
Nitroimidazoles. IX. Synthesis of 2-acetyl-1-methyl-5-nitroimidazole
Shafiee,Pirouzzadeh,Ghasemian,Parang
, p. 1021 - 1023 (1992)
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Design, Synthesis, and Trypanocidal Activity of Novel 5-Nitroimidazolyl O-Benzyloxime Ethers
Carvalho, Samir Aquino,Osorio, Luis Felipe Baumotte,Salom?o, Kelly,de Castro, Solange Lisboa,Wardell, Solange M. S. V.,Wardell, James Lewis,da Silva, Edson Ferreira,Fraga, Carlos Alberto Manssour
, p. 3626 - 3631 (2017)
In this paper, we describe the synthesis and the action against of the trypomastigote form of Trypanosoma cruzi of a new class of nitroimidazole-2-carbaldehyde O-benzyloximes. These derivatives were designed through the application of molecular hybridization concept between two potent antiprotozoal compounds, the 5-nitrothiophene-2-carbaldehyde O-oxime 6 and the trypanocidal piperidinyl-4-carbaldehyde O-benzyloxime 7 with the intention of reaching two distinct molecular targets of T.?cruzi. The activity of these benzyl ether derivatives was tested against the infective trypomastigote forms of T.?cruzi, and the derivative (E)-1-methyl-5-nitro-1H-imidazole-2-carbaldehyde O-(4-nitrobenzyl) oxime (1) presented moderate trypanocidal activity (IC50?=?12.7?μM) when compared with the standard drug benznidazole, which showed to be a good starting point for the design of more effective trypanocide agents.
Compound and its as L-type calcium channel blocker or/and application of acetylcholine esterase inhibitors
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Paragraph 0179; 0181-0182, (2016/10/07)
Disclosed in this invention are compounds and the uses as L-type calcium channel blocker and/or acetylcholinesterase inhibitor thereof. The uses of said compounds in the manufactures of a medicament for the treatment of cardiovascular diseases, apoplexy or senile dementia are also disclosed in the present invention.
5-Nitroimidazole-based 1,3,4-Thiadiazoles: Heterocyclic analogs of metronidazole as anti-helicobacter pylori agents
Moshafi, Mohammad Hassan,Sorkhi, Maedeh,Emami, Saeed,Nakhjiri, Maryam,Yahya-Meymandi, Azadeh,Negahbani, Amir Soheil,Siavoshi, Farideh,Omrani, Maryam,Alipour, Eskandar,Vosooghi, Mohsen,Shafiee, Abbas,Foroumadi, Alireza
scheme or table, p. 178 - 183 (2011/10/08)
A series of 5-nitroimidazole-based 1,3,4-thiadiazoles were prepared and tested for antibacterial activity against Helicobacter pylori. The anti-H. pylori activity of target compounds along with the commercially available antimicrobial metronidazole was evaluated by comparing the inhibition-zone diameters determined by the paper disc diffusion bioassay. From our bioassay results against 20 clinical isolates it is evident that piperazinyl, 4-methylpiperazinyl, 3-methylpiperazinyl, and 3,5-dimethylpiperazinyl analogs (6a, 6b, 6e, and 6f, respectively) and pyrrolidine derivative 7 had strong activity at 0.5 μg/disc (average of inhibition zone >20 mm) while metronidazole had no activity at this dose. Compound 6f containing the 3,5-dimethylpiperazinyl moiety at the 2-position of the 5-(1-methyl-5-nitro-1H- imidazol-2-yl)-1,3,4-thiadiazole skeleton was the most potent compound tested at low concentrations.