73286-33-6Relevant academic research and scientific papers
Synthesis, characterization, and antibacterial activities of some novel N,N'-disubstituted thiourea, 2-Amino thiazole, and imidazole-2-thione derivatives
Kalhor, Mehdi,Salehifar, Mina,Nikokar, Iraj
, p. 2947 - 2954 (2014/05/06)
In the search of bioactive molecules, a series of novel N-substituted thiourea derivatives 3(a-d) are prepared by reaction of the α-Amino pyridyl ketone hydrochloride (2a) with the corresponding aryl isothiocyanates. The synthesis of some new 2-Amino thiazoles 4(a-d) and imidazole-2-thiones 6(a-d) were attempted by intramolecular cyclization reaction of the N,N'-disubstituted thioureas 3(a-d) and their intermediate ketals 5(a-d) in diluted aqueous acidic and strong acidic mediums. The structure of all newly synthesized compounds was established by analytical and spectral data. The antibacterial studies to all of the synthesized compounds against Bacillus cereus, Escherichia coli, Pseudomonas aeruginosa, Staphylococcus aureus, and Enterococcus faecalis bacteria with Gram-positive and negative strains, as MIC values are reported. Some of these compounds such as 3a,b,d and 4b,d exhibited a good to significant antibacterial activity. Also, all of new synthesized compounds 3,4,6(a-d) were active against Gram-positive S. aureus bacterium. Thus, some of these compounds can emerge as a promising tool for further research work.
COMPOUNDS FOR TREATING RESPIRATORY SYNCYTIAL VIRUS INFECTIONS
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Page/Page column 127, (2011/09/14)
The present invention relates to compounds of formula (I), its salts, isomers or prodrugs thereof useful in the treatment of viral infections, in particular respiratory syncytial virus (RSV) infections. The present invention also relates to processes for preparing the compounds and intermediates used in their preparation.
NICOTINIC ACETYCHOLINE RECEPTOR LIGANDS
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Page/Page column 26, (2010/11/08)
Acetylcholine receptor ligands of formula I (I) wherein D, E and G are as described in the specification, diastereoisomers, enantiomers, pharmaceutically-acceptable salts, methods of making, pharmaceutical compositions containing, and methods for using th
NICOTINIC ACETYLCHOLINE RECEPTOR LIGANDS
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Page/Page column 27, (2010/02/12)
Acetylcholine receptor ligands of formula (I), wherein D, Ar1, E and Ar2 are as described in the specification, diastereoisomers, enantiomers, pharmaceutically-acceptable salts, methods of making, pharmaceutical compositions containing and methods for usi
Design of potent non-thiourea H3-receptor histamine antagonists
Ganellin,Hosseini,Khalaf,Tertiuk,Arrang,Garbarg,Ligneau,Schwartz
, p. 3342 - 3350 (2007/10/02)
Starting from thioperamide, the first potent and selective H3-receptor histamine antagonist, analogues have been synthesized and tested in vitro on rat cerebral cortex to explore structure-activity relationships. The aim has been to design potent compounds which do not possess the thiourea group of thioperamide and which may have improved brain penetration. In a short series of open chain thiourea analogues, the optimum chain length for H3- antagonist potency was found to be (CH2)3. Compounds derived from histamine and possessing an aromatic nitrogen-containing heterocycle on the side chain amino group in place of thiourea show H3-antagonist activity. Furthermore, when the heterocycle is 2-pyridyl, electron-withdrawing substituents (e.g. NO2, CF3, CO2Me) in the pyridine 5-position increased potency. The synthesis of 4-[4(5)-imidazolyl]piperidine and its conversion into the (trifluoromethyl)pyridyl analogue 5b of thioperamide is described; however, 5b is not as potent as thioperamide. Replacing imidazole by pyridine or substituting imidazole on the remote N considerably reduced potency. Replacing the side-chain NH by S increased potency still further and the most potent compound is 2-{[2-[4(5)-imidazolyl]ethyl]thio}-5-nitropyridine (UCL 1199) which has K(i) = 4.8 nM.
