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Studies On The Design、Synthesis And Crystal Structure Of New Nicotinic Acid Derivative’s Compounds

Posted on:2010-04-26Degree:MasterType:Thesis
Country:ChinaCandidate:S Y LuoFull Text:PDF
GTID:2234360278468300Subject:Medicinal chemistry
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Thiadiazole derivatives have been attracting widespread attention due to their significant bioactivities, such as antibacterial, fungicidal, insecticidal, herbicidal, plant growth regulating and pharmacological activities.These compounds are known to inhibit the biosynthesis of ergosterol in fungi. On the other hand, nicotinic acid derivatives, are well known to highly active as fungicides, especially for combatting fungus diseases in various crops. In general, pyridine can serve as effective bioisostere of benzene in drug design, and considerable interest has been shown in pyridine derivatives in the field of modern agrochemistry and medicinal chemistry because the substitution of benzene by pyridine may result in the good biological activity and low toxicity of molecules containing pyridyl moiety.With these in mind, we would like to investigate the nicotinamide derivatives incorporating 5-substituted-1,3,4-thiadiazol-2-amine nucleus. So we have synthesized a series of 5-substituted-1,3,4-thiadiazol-2-amine. Some substituted ureas also have been found to display combating bacterium activity. In order to research the substituted groups impact to the activity we also synthesized some ureas compounds.In a word,we have synthesized eight intermediate and ten new compounds which have no reported in anywhere. Through the analytical methods of IR,MS,1H-NMR and others spectral analysis we have determined the molecular structure.we also studyed some physico-chemical property of these compounds,such as color、solubility、melting point and so on . Otherwise,we analysised the crystal structure of the compoundⅠ.The spatial structure and atomic configuration in crystal of this groups have been discovered. Herein, we report the design, preparation, characterization and crystal structure of the 2-Chloro-N-Substituted -nicotinamide derivatives.
Keywords/Search Tags:2-chloronicotinic acid, nicotinamide, nicotinic acid derivatives, 1,3,4- thiadiazole, X-ray single crystal diffraction
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