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Bis(1,3,4-thiadiazolo)-1,3,5-triazinium hal.id.es 1 can be converted into various products such as guanidines or bis(azolyl)alkanes. However, they also react with hydroxide ions in aqueous solution to form novel heterocyclic- substituted ureas 2a-i. The yields were increased from, moderate to good or excellent in the presence of excess guanidine 3. The assumption that hydrogen-bonded intermediate encounter complexes EC are formed gives a reasonable explanation for the observed reaction path. The molecular structures of some of the crystalline products 2 were determined by X-ray analysis. Furthermore, with copper(II) a dinuclear complex 8 is formed with the two metal, ions in a distorted octahedral environment; a water molecule acts as a. bridging llgand between the CuII ions.

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Piperidine – Wikipedia,
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Imidazothiadiazoles (ITDs) are a class of potent nonsteroidal ecdysone agonists with larvicidal activity. Previously, we performed the Hansch?Fujita type of quantitative structure?activity relationship (QSAR) analysis for ITD analogs (Yokoi et al., Pestic. Biochem. Physiol. 2015, 120, 40?50). The activity was reasonably explained by hydrophobicity and electronegativity of substituents on the imidazothiadiazole ring system. However, the limited data points (n = 8) hampered the examination of other physicochemical parameters. In the present study, we expanded the library of ITD congeners and evaluated their receptor-binding affinity using intact Sf-9 cells. The QSAR analysis for the expanded set revealed the significance of the third physicochemical parameter, the negative steric effect for long substituents. We also evaluated the larvicidal activity of the synthesized compounds against Spodoptera litura; however, it was not correlated to the binding affinity. The results obtained here suggests that the pharmacokinetic properties must be improved to enhance the larvicidal activity of ITDs.

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Reaction of 5-chloro-3-methyl-1-phenyl-1H-pyrazole-4-carbonyl chloride 4 with substituted benzothiazol-2-ylamine and substituted [1,3,4] thiadiazol-2-ylamine yields 5-chloro-3-methyl-1-phenyl-1H pyrazole-4-carboxylic acid-substituted benzothiazol-2-ylamide 5 and 5-chloro-3-methyl-1-phenyl-1H pyrazole-4-carboxylic acid (5-substituted -[1,3,4] thiadiazol-2-yl)amide 6 respectively in good yields.

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The optimal conditions for obtaining hetarylamides of 4-hydroxy-2-oxo-1,2, 5,6,7,8-hexahydroquinoline-3-carboxylic acid are suggested on the basis of derivatographic investigations. The 1H NMR spectra of the synthesized compounds, their spatial structure, and also the results of a study of their antitubercular properties are discussed.

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Studies in potential organo-fluorine oral hypoglycemic agents. Part 6: Synthesis and biological activities of some fluorinated 2-arylsulfonamido-5-alkyl-1.3.4-thiadiazoles.

Forty new fluorinated 2-arylsulfonamido-5-alkyl-1.3.4-thiadiazoles have been synthesized and a representative number of synthesized compounds have been screened for their hypoglycemic activity and some other types of biological activities.

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Piperidine – Wikipedia,
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