Über aliphatische 1,2‐Diamine

Reihlen, Hans; Heßling, G. v.; Hühn, Werner; Weinbrenner, Erwin

doi:10.1002/jlac.19324930103

Cited by 17 publications

(7 citation statements)

References 8 publications

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“…Compounds (1,2,3). N-(1-cyanocyclopentyl)acetamide (1) was synthesized via the method of Reihlen, Hessling, Hühn, and Weinbrenner [14]. e reduction of nitriles (1) gives N-[(1-aminomethyl)cyclopentyl]acetamide (2) by nickel Raney.…”

Section: General Procedures For the Synthesis Of The Intermediatementioning

confidence: 99%

Synthesis and Evaluation of N-[1-(((3,4-Diphenylthiazol-2(3H)-ylidene)amino)methyl)cyclopentyl]acetamide Derivatives for the Treatment of Diseases Belonging to MAOs

Turan-Zitouni

Tabbi

Hussein

et al. 2018

Journal of Chemistry

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A series of N-[1-(((3,4-diphenylthiazol-2(3H)-ylidene)amino)methyl)cyclopentyl]acetamide derivatives (4a-4i) were synthesized in good yield and assayed for their inhibitory potency against monoamine oxidase (MAO) isoforms. Structures of newly synthesized compounds were characterized by IR, 1H-NMR, 13C-NMR, and mass spectroscopic methods. The inhibitory activity of compounds (4a-4i) against hMAO-A and hMAO-B enzymes was elucidated by using in vitro fluorometric method using Amplex Red® reagent. In the hMAO-A inhibition assay, compounds 4a, 4b, 4c, and 4i exhibited similar activity with standard drug moclobemide (IC50 = 6.061 ± 0.262 µM) with IC50 values of 7.06 ± 0.18 µM, 6.56 ± 0.20 µM, 6.78 ± 0.15 µM, and 7.09 ± 0.17 µM, respectively. According to hMAO-B inhibition results, compounds 4a, 4b, and 4c displayed significant activity with IC50 values of 0.42 ± 0.012 µM, 0.36 ± 0.014 µM, and 0.69 ± 0.020 µM, respectively. In the wake of all these results, it was understood that compound 4b was found to be the most potent derivative in the series against both isoforms and selective as MAO-B inhibitor. The cytotoxicity test was performed for compounds 4a, 4b, and 4c, and it was found that these compounds were noncytotoxic at the concentration of their IC50 values. Also, enzyme kinetic and docking studies of compound 4b were performed against MAO-B. It was observed that 4b showed a reversible and noncompetitive inhibition type. The important binding modes of this compound with active site of hMAO-B were shown owing to in silico studies.

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Section: General Procedures For the Synthesis Of The Intermediatementioning

confidence: 99%

Synthesis and Evaluation of N-[1-(((3,4-Diphenylthiazol-2(3H)-ylidene)amino)methyl)cyclopentyl]acetamide Derivatives for the Treatment of Diseases Belonging to MAOs

Turan-Zitouni

Tabbi

Hussein

et al. 2018

Journal of Chemistry

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“…Dehydrohalorubremetine.-This material was prepared as previously described. 10 The m.p. behavior of the crude material depends on the rate of heating and on the temperature at which the sample is introduced into the m.p.…”

Section: Experimental20•21mentioning

confidence: 99%

“…Meanwhile the preparation and catalytic reduction of dehydrohalorubremetine had been repeated in these laboratories on a larger scale than previously employed. 10 The crude dehydrohalorubremetine was found to absorb about 1.8 moles of hydro-(15) A. R. Battersby and . T. Openshaw, Experientia, VI, 378 (1950).…”

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confidence: 99%

Reduction Products of the Rubremetinium Cation¹

Tietz¹,

McEwen²

1953

J. Am. Chem. Soc.

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“…Nutrition, 35, 499 (1948). (11) Rubin, S. H., Scheiner, J., and Hirschberg, E., J. Biol. Chem.. 167, 599 (1947).…”

Section: Literature Citedmentioning

confidence: 99%

“…samples and semiautomatic operation, an accuracy of ±0.02% absolute can be attained; this furnishes a method of high accuracy requiring relatively small amounts of sample for such difficult problems as the determination of the constitution of high molecular weight compounds. PREGL'S micromethod (10) has undergone development in three directions: The sample size has been decreased (2, 9), the combustion has been made automatic (4,5,11,13,16), and the precision and accuracy have been increased (3, 6-8). In the absence of a practicable ultramicrobalance the first and third are mutually exclusive; higher accuracy requires larger amounts of sample.…”

Section: Literature Citedmentioning

confidence: 99%

Microdetermination of Carbon and Hydrogen

Fischer¹

1949

Anal. Chem.

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genin effect similar to that described by Sprince and Woolley ( 14) and Wright and Skeggs (19) for a variety of other bacteria.Differences in the sensitivity of response to pantoic acid have been observed, however, with different cultures. These variations appear to be associated with the time of incubation required for attainment of suitable levels of growth. As previously noted, a decrease in the growth rate has been observed after repeated serial transfers of the culture from slant to slant. The concomitant increase observed in the relative activity of pantothenic acid as compared to pantoic acid appears to indicate that this effect is due to a decrease in the efficiency of the organism in synthesizing pantothenic acid from the latter.With the present culture carried as directed, the use of a heavy inoculum (G = 15 to' 20), plus the modified medium, has permitted shortening the time of incubation in stationary flasks from 60 to 40 hours. The use of continuous shaking in Evelyn tubes during incubation permits assays in 20 to 24 hours. Inclusion of Tween 80 in bacterial media was reported by Dubos and Davis (4) to enhance the rate and abundance of growth of tubercle bacilli and has been applied extensively with other organisms (6). The stimulatory effect of the lactate is similar to that observed by Tosic ( 15), who attributed it to the buffering effect of the bicarbonate formed from the lactate during growth of Acetobacter turbidans. SUMMARY A microbiological procedure is described which permits assay of panthenol, the biologically active hydroxy analog of pantothenic acid, in the presence of pantoyl lactone as well as pantoic acid. The lactone is removed quantitatively from water solution by continuous extraction with ethyl ether for 1 to 2 hours. Panthenol in the aqueous residue is then hydrolyzed to pantoic acid for microbiological assay with Acetobacter suboxydans. Assay before hydrolysis provides a correction for preformed pantoic acid and a partial correction for pantothenic acid. Hence, small percentages of pantothenic acid (up to 10%) will not seriously affect, the specificity of the panthenol assay. By modification of

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Über aliphatische 1,2‐Diamine

Cited by 17 publications

References 8 publications

Synthesis and Evaluation of N-[1-(((3,4-Diphenylthiazol-2(3H)-ylidene)amino)methyl)cyclopentyl]acetamide Derivatives for the Treatment of Diseases Belonging to MAOs

Synthesis and Evaluation of N-[1-(((3,4-Diphenylthiazol-2(3H)-ylidene)amino)methyl)cyclopentyl]acetamide Derivatives for the Treatment of Diseases Belonging to MAOs

Reduction Products of the Rubremetinium Cation¹

Microdetermination of Carbon and Hydrogen

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Über aliphatische 1,2‐Diamine

Cited by 17 publications

References 8 publications

Synthesis and Evaluation of N-[1-(((3,4-Diphenylthiazol-2(3H)-ylidene)amino)methyl)cyclopentyl]acetamide Derivatives for the Treatment of Diseases Belonging to MAOs

Synthesis and Evaluation of N-[1-(((3,4-Diphenylthiazol-2(3H)-ylidene)amino)methyl)cyclopentyl]acetamide Derivatives for the Treatment of Diseases Belonging to MAOs

Reduction Products of the Rubremetinium Cation1

Microdetermination of Carbon and Hydrogen

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Product

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Reduction Products of the Rubremetinium Cation¹