- Synthesis and antimycobacterial activity of new 2-hydroxy-N-(3-oxo-1-thia- 4-azaspiro[4.4]non-4-yl)/(3-oxo-1-thia-4-azaspiro[4.5]dec-4-yl)-2, 2-diphenylacetamide derivatives
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2-Hydroxy-2,2-diphenylacetohydrazide (2), cyclic ketones, and mercaptoalkanoic acids were converted into 2-hydroxy-N-(3-oxo-1-thia-4- azaspiro[4.4]non/[4.5]dec-4-yl)-2,2-diphenylacetamide derivatives (3, 4) in a one pot procedure. Compounds 3 and 4 were tested for in vitro antimycobacterial activity against M. tuberculosis H37Rv. The compounds were found to provide 0-86% inhibition of mycobacterial growth in the primary screen conducted at 6.25 μg/cm3. Springer-Verlag 2006.
- Guezel, Oezlen,Ilhan, Eser,Salman, Aydin
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- Design and Bioevaluation of Novel Hydrazide-Hydrazones Derived from 4-Acetyl-N-Substituted Benzenesulfonamide
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Abstract: In this research, a series of hydrazine-hydrazone derivatives (Ia–g), (IIa–h) were synthesized to discover new antioxidant and anticholinesterase agents. The structures of synthesized compounds were characterized by spectroscopic data using UV, IR, 1H, 13C NMR, mass spectroscopy, and elemental analysis. The bio-evaluation of the synthesized compounds (Ia–g), (IIa–h) were evaluated according to in vitro activity assays. The results of β-carotene/linoleic acid assay showed that among the synthesized compounds, the (Ib), (Ie), (IIb–IIe), and (IIh) compound exhibited higher activity for the lipid peroxidation inhibitory activity. In the DPPH free scavenging activity and the cation radical scavenging activity in ABTS?+ activity, compound (IIb) was found to be more active. In the CUPRAC reduced power assay, the A0.5 values of all synthesized compounds were better than α-TOC. In AChE assay, compound (IIb) exhibited the most activity with IC50 = 11.12 ± 0.74 μM, while the compounds (Ib–g) and (IIb–h), exhibited excellent activity than the positive standard galantamine (IC50 = 46.06 ± 0.10 μM) in the BChE assay.
- ?ztürk, M.,Bozkurt, E.,Iyido?an, A. Karakü?ük,Oru?-Emre, E. E.,S?cak, Y.
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p. 702 - 714
(2020/10/29)
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- Synthesis and antimicrobial evaluation of new 3-alkyl/aryl-2-[((α, α-diphenyl-α-hydroxy)acetyl)hydrazono]-5-methyl-4-thiazolidinones
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New 4-thiazolidinone derivatives of benzilic acid (α,α- diphenyl-α-hydroxyacetic acid) have been synthesized and evaluated for antibacterial and antifungal activities. The reaction of 1- (α,α- diphenyl-α-hydroxy)acetyl-4-alkyl/arylthiosemicarbazides with ethyl 2-bromopropionate gave 3-alkyl/aryl-2-[((α,α-diphenyl-α- hydroxy)acetyl)hydrazono]-5-methyl-4-thiazolidinone derivatives. Their antibacterial and antifungal activities were evaluated against S. aureus ATCC 29213, P. aeruginosa ATCC 27853, E. coli ATCC 25922, C. albicans ATCC 10231, C. parapsilosis ATCC 22019, C. krusei ATCC 6258, T. mentagrophytes var. erinacei NCPF 375, M. gypseum NCPF 580 and T. tonsurans NCPF 245. 3e, 3f, 3g and 3h showed the highest antibacterial activity. Particularly 3a and 3e showed the highest antifungal activities against C. parapsilosis ATCC 22019, T. tonsurans NCPF 245 and M. gypseum NCPF 580.
- Güzeldemirci, Nuray Ulusoy,Ilhan, Eser,Kü?ükbasmaci, ?mer,Satana, Dilek
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p. 17 - 24
(2011/11/29)
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- Kinetics of the hydrolysis of N1-salycilaldehyde-2-hydroxy-2,2-diphenylacethydrazone
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The hydrolysis of N1-salycilaldehyde-2-hydroxy-2,2-diphenylacethydrazone in 30% viv aqueous solution of ethanol was investigated by spectrophotometric method. The investigations were carried out at different pH-values at 296 K. Spectral characteristics were discussed and correlated to the spectral characteristics of several molecules of the same type. According to the proposed mechanism of the reaction, a fast protonation was followed by the rate-determing attack of water on the protonated hydrazone. The observed pseudo first-order rate constants show that the alteration of pH values from 4.09 to 1.13 accelerates the hydrolysis by about 170 times.
- Juranyi, Maria
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p. 443 - 452
(2007/10/03)
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- HYDRAZIDES OF DISUBSTITUTED GLYCOLIC ACIDS
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A method was developed for the production of the unsubstituted hydrazides of diaryl- and dialkylglycolic acids, based on the hydrolysis and transhydrazonization of α-propylbenzylidenehydrazides of disubstituted glycolic acids.
- Berdinskii, I. S.,Maslivets, A. N.
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p. 1609 - 1612
(2007/10/02)
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- Azomethine Imines by Reaction of Diphenylketene with Azodicarboxylates
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The reaction of diphenylketene with azodicarboxylates yields azomethine imines 4 which show 1,3-dipolaric reactivity: addition of diphenylketene yields the 2:1 adduct 8, addition of phenylisocyanate productes 7, and dimerization leads to 5.
- Fahr, Egon,Buettner, Ehrfried,Keil, Karl-Heinz,Markert, Juergen,Scheckenbach, Franz,et al.
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p. 1433 - 1444
(2007/10/02)
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