- Synthesis of novel isothiazolopyridines and their in vitro evaluation against Mycobacterium and Propionibacterium acnes
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In this paper we describe synthesis, structures and some physicochemical properties of 20 isothiazolopyridines 8-13 substituted differently into an isothiazole ring as well as their in vitro antibacterial assays against Mycobacterium tuberculosis H37Rv, Mycobacterium fortuitum PCM 672 and Propionibacterium acnes PCM 2400. Compound 13a was found to be the most active derivative against M. tuberculosis H37Rv, demonstrating 100% growth inhibition of microorganisms in the primary screen (minimum inhibitory concentration [MIC] 6.25 μg/mL). Nineteen of the prepared compounds were evaluated against M. fortuitum PCM 672 and P. acnes PCM 2400 and only compounds 9 and 12d exhibited excellent activity against individual strains of microorganisms with MIC 90 1 μg/mL. The inhibitory action of the remaining isothiazolopyridines towards the tested strains of the microorganism was low, absent, or a non-linear correlation prohibited accurate determination of MIC values. Unexpectedly, seven of the remaining isothiazolopyridines tested against M. fortuitum and P. acnes stimulated growth of the microorganisms in the range 10-50% or even more (10b) under experimental conditions.
- Malinka, Wies?aw,?wia?tek, Piotr,?liwińska, Ma?gorzata,Szponar, Bogumi?a,Gamian, Andrzej,Karczmarzyk, Zbigniew,Fruziński, Andrzej
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p. 5282 - 5291
(2013/09/02)
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- Diazotisation of aromatic amines and solvolysis of diazonium salts in ethylene glycol ethers
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Aniline and unhindered alkyl-substituted anilines undergo solvolysis in dioxane and DME saturated with dry hydrogen chloride on diazotisation with isoamyl nitrite to give 2-(2-chloroethoxy)ethyl aryl ethers and 2-methoxyethyl aryl ethers respectively in 36-47% yields. 2,6-Dialkyl-substituted anilines give the corresponding chloro compounds as the major product along with the aryl ethers in lower yields. Diazotisation of aniline in ethylene glycol and monomethyl ethers of ethylene glycol and diethylene glycol gave the corresponding alcoholysis products in low yields. The solvolysis of aniline did not occur on diazotisation in diethyl ether or THF.
- Ram, Ram N.,Singh, Virinder
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p. 800 - 803
(2007/10/03)
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- 1H NMR Studies on the Interactions of Acyclic Polyethers with Dimethyltin Dichloride in Aromatic Solvents
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The interactions between various acyclic polyethers, RO(CH2CH2O)nR'(R, R'=CH3, Ph), and dimethyltin dichloride (DMTC) in aromatic solvents have been studied by means of 1H NMR spectroscopy.On the basis of a continuous variation method, the formation of the 1:1 complexes between glymes, CH3O(CH2CH2O)nCH3 (n=2, 3, 4), and DMTC was revealed in benzene.The 2J(119Sn-CH3) values suggested distorted trans-octahedral configurations for these complexes.From the statistical consideration of stability constants, it was found that the coordination occurred virtually through neighboring two oxygen atoms in these complexes.DMTC gave the complexes of both 1:1 and 1:2 glyme/DMTC stoichiometry with glymes (n=5, 6) in benzene and with all glymes employed here in toluene and 1-chloronaphthalene.Coexistence of 1:1 and 1:2 species was also encountered for PhO(CH2CH2O)nCH3 (n=3, 4, 5), whereas no appreciable interaction was observed between PhO(CH2CH2O)nPh (n=2, 3, 4) and DMTC.On the basis of these observations, the additional formation of the 1:2 complexes was assumed to be caused by the bulkiness of polyethers.
- Otera, Junzo,Shiomi, Tadashi,Murakami, Kazuhiko,Kawasaki, Yoshikane
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p. 2964 - 2967
(2007/10/02)
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