• Title/Summary/Keyword: thiosemicarbazide

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Synthesis of Some Heterocycles of Potential Biological Activity

  • Ali-Harb, Abd-Elfattah;Mostafa, Fatma-H.;Metwally, Saoud-A.
    • Archives of Pharmacal Research
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    • v.13 no.2
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    • pp.187-191
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    • 1990
  • A convenient method for the preparation of imidazobenzimidazole 3, imidazoimidazole 5, imidazotriazole 6 and pyrano [2, 3-c] oxazole 7 derivatives is described. This depends on interaction of 2-methyl-4-arylidene-2-oxazolin-5-ones 1 with o-diamines, thiosemicarbazide and/or ethylcyanoacetate. The effect of alcoholic potassium cyanide on axazolinone 1 was studied. Antibacterial activity of the obtained products was studied.

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Corrosion Inhibitors For Zinc in 2 M HCI Solution

  • A. S. Fouda;L. H. Madkour;A. A. El-Shafel;S. A. Abd ElMaksoud
    • Bulletin of the Korean Chemical Society
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    • v.16 no.5
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    • pp.454-458
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    • 1995
  • Inhibiting action of semicarbazide, thiosemicarbazide, sym. diphenylcarbazide towards corrosion of zinc in hydrochloric acid has been investigated. The rate of corrosion depends on the nature of the inhibitor and its concentration. The values of inhibition efficiency from, weight loss, thermometric measurements are in good agreement with those obtained from polarization studies. From the polarization studies, the inhibitors used act as mixed absorption type inhibitors, increased adsorption resulting from an increase in the electron density at the reactive C=S and C=O groups and N-atoms. The thermodynamic parameters of adsorption obtained using Bockris-Swinkels adsorption isotherm reveal a strong interaction of these carbazides on zinc surface.

Studies on the synthesis of N,N'-disubstituted thiourea derivatives and their antibacterial, antitubercular and antitumor activities (N,N'-diusbstituted thiourea derivatives의 합성과 항균성, 항인결핵성및 항종양 시험에 관한 연구)

  • 조윤성;이명걸
    • YAKHAK HOEJI
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    • v.14 no.1_2
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    • pp.1-14
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    • 1970
  • Seventeen N,N/sup I/-disubstituted thiourea derivatives were synthesized by the Hugershof reaction and reported. Antitumor activities of the synthesized compounds against ascitic Ehrlich Carcinoma and ascitic sarcoma 180 were reported. It was found that 1,1/sup I/-(p-Phenylene)-3,3/sup I/-bis (2-carboxyphenyl)-2,2/sup I/-dithiourea was considerably active against ascitic Ehrlich Carcinoma and Sarcoma 180 respectively. 1-(2-Carboxyphenyl)-3-(p-ethoxyphenyl)-2 thiourea was active against ascitic Sarcoma 180. 1-Salicyloyl-3-(p-ethoxyphenyl)-2-thiourea and 1,1/sup I/-(p-Phenylene)-3,3/sup I/-bis(2-hydroxyethyl)-2,2/sup I/-dithiourea were active against ascitic Ehrlich Carcinoma. Antitubercular activities of the synthesized compounds against Mycobacterium tuberculosis H/sub 37/ R/sub v/ were also reported. It was found that 1-Isonicotinyl-4-cyclohexyl-3-thiosemicarbazide was considerably active at 100 .mu.g/ml. 1,1/sup I/-(p-Phenylene)-3,3/sup I/-bis(2-hydroxyethyl)-2,2/sup I/-dithiourea and 1-Salicyloyl-3-(p-ethoxyphenyl)-2-thiourea were active at 1000 .mu.g/ml respectively. Antibacterial activities of nine compounds of the synthesized compounds against S. aureus and E. Coli were reported. It was found that 1,1-(p-Phenylene)-4,4/sup I/-bis(isonicotinyl)-2,2/sup I/-dithiosemicarbazide and 1-Isonicotinyl-4-cyclohexyl-3-thiosemicarbazide were considerably active against S. aureus and E. Coli respectively. 1-(6-Methyl-2-benzothiazolyl)-3-(1-naphthyl)-2-thiourea was active against S. aureus. 1,1/sup I/-(p-Phenylene)-3,3/sup I/-bis (2-hydroxyethyl)-2,2/sup I/-dithiourea was active against E. Coli.

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Synthesis of Pyrazolo [4,5]pyridazine and Isoxazolo [3,4d]pyridazine Derivatives

  • Abbass, Iklass-M.;Sharaf, Mohyee-A.F.;EI-damaty, Alia-A.
    • Archives of Pharmacal Research
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    • v.15 no.3
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    • pp.224-228
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    • 1992
  • Arylhydrazones of diethylacetondicarboxylate 3 was treated with formaldehyde to give 1 aryl-4, 5, 6-trihydropyridaine derivatives 4a-f Cyclization of compound 4a-f by hydroxylamine afforded [3, 4d] 1, 3, 4, 5-tetrahydropyridazine derivatives 5a-f. Also cyclization of compound 4c with semicarbazide gave 1-amidopyrazolo-5-one-1-aryl-3-carboxypyridazine 6. On the other hand compounds 3 reacted with ethylorthoformate to give diethyl-1, 4-dihydro-1-arylpyridazine-4one-2.5 dicarboxylate 7, which on treatment with hydrazine. Semicarbazide and thiosemicarbazide gave pyridazine, amido and thioamido derivatives. The spectral and antimicrobial data of these compounds 1-8 were studied.

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Rhodamine 6G Based New Fluorophore Chemosensor Toward Hg2+

  • Son, Young-A;Park, June-Min
    • Textile Coloration and Finishing
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    • v.24 no.3
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    • pp.158-164
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    • 2012
  • Rhodamine dyes belong to xanthene family has excellent photostability and photophysical properties. In rhodamine dyes, Rhodamine 6G and its precursors also have xanthene chromophore and it shows high fluorescent quantum yield. Rhodamine 6G derivates are simple to synthesis and its high sensitivity and water solubility are suitable as good chemosensor. In this regard, Rhodamine 6G derivates which have selectivity to specific metal cation can used to detect various heavy metal ions. In this study, rhodamine 6G derivatives were synthesized by reaction of rhodamine 6G hydrazide and glyoxal and 4-phenyl thiosemicarbazide and it showed colorimetric and fluorescence sensing toward $Hg^{2+}$ ion. This novel chemosensor was analyzed and measured on UV-Vis and fluorescence spectrophotometer. HOMO/LUMO values were also calculated by computational calculation.

Synthesis, Spectroscopic Studies of Binuclear Ruthenium(II) Carbonyl Thiosemicarba-zone Complexes Containing PPh3/AsPh3 as Co-ligands: DNA Binding/Cleavage

  • Sampath, K.;Sathiyaraj, S.;Jayabalakrishnan, C.
    • Bulletin of the Korean Chemical Society
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    • v.34 no.2
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    • pp.367-373
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    • 2013
  • The ruthenium(II) ferrocenyl heterocyclic thiosemicarbazone complexes of the type $[RuCl(CO)(EPh_3)]_2L$ (where E = P/As; L = binucleating monobasic tridendate thiosemicarbazone ligand) have been investigated. Strutural features were determined by analytical and spectral techniques. Binding of these complexes with CT-DNA by absorption spectral study indicates that the ruthenium(II) complexes form adducts with DNA and has intrinsic binding constant in the range of $3.3{\times}10^4-1.2{\times}10^5M^{-1}$. The complexes exhibit a remarkable DNA cleavage activity with CT-DNA in the presence of hydrogen oxide and the cleavage activity depends on dosage.

Synthesis of Pyrazolo [4,3-c]Pyridazine and Isoxazolo [3,4-d]Pyridazine Derivatives

  • Abbass, Ikhlass-M.;Sharaf, Mohye-A.F.;El-damaty, Alia-A.
    • Archives of Pharmacal Research
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    • v.16 no.2
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    • pp.164-167
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    • 1993
  • Arylhydrazones of diethyl acetonedicarboxylate 3 was treated with fomaldehyde to 1-aryl-1, 4, 5, 6-tetrahyeheypyridazine derivatives 4a-f Cyclization of compound 4a-f by hydroxy-lamine afforded [3, 4-d] 1, 4, 5, 6-tetrahydropyridazine derivative 5a-f. Also, cyclization of compound 4c with semicarbazide gave pyrazolote [4, 3-c] pyridazine 6. On the other hand compound 3 reacted with ethylothofomate to give diethyl-1, 4-dihydro-1-arypyridazine-4-one-3, 5 dicaboxylate 7, which on treatment with hydrazine, semicarbazide and thiosemicarbazide gave pyridazine, amido and thioamido derivatives. The spectrl and antimicrobial data of these compounds 1-8 were studied.

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Studies on the Synthesis and Antibacterial Activity of 2-Ethoxymethyl-3-(5-nitro-2-furyl)acrylamide Derivatives (2-Ethoxymethyl-3-(5-nitro-2-furyl)acrylamide 유도체(誘導體)의 합성(合成) 및 항균작용(抗菌作用)에 관(關)한 연구(硏究))

  • Ko, Ok-Hyun
    • Journal of Pharmaceutical Investigation
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    • v.10 no.4
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    • pp.8-22
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    • 1980
  • In order obtain some new antibacterial agents, seven new 2-ethoxymethyl-3-(5-nitro-2-furyl) acrylamide derivatives were synthesized by condensing 2-ethoxymethyl-3-(5-nitro-2-furyl) acyloyl chloride with amino compounds namely 5-amino-3, 4-dimethyl isoxazole, sulfamonomethoxazole, d-2-amino-1-butanol, hydroxylamine hydrochloride, semicarbazide hydrochloride, thiosemicarbazide, and p, p'-diaminodiphenylsulfone, respectively. The seven synthesized compounds were 2-ethoxymethyl-3-(5-nitro-2-furyl) acryl-5-amino-3, 4-dimethylisoxazoleamide [VII], $N^4-[2-ethoxymethyl\;3-methyl\;(5-nitro-2-furyl)\;acryl]-N^1-(5-methyl-3-isoxazolyl)$ sulfanilamide [VIII], 2-ethoxyl-3-(5-nitro-2-furyl) acrylsemicarbazide [X], 2-ethoxymethyl-3-(5-nitro-2-furyl) acrylthiosemicarbazide [XI], 2-ethoxymethyl-3-(5-nitro-2-furyl) acryl-d-2-amino-1-butanolamide [XII], and 4, 4'-di[2-ethoxymethyl-3-(5-nitro-2-furyl) acryl-amido] diphenylsulfone [XIII]. These compounds, with exception of the compound XIII, showed generally effective antibacterial activity, especially in the following instances. Compound VII was shown to be effective against Bacillus subtilis ATCC 6633 compound VIII, against Bacillus cereus var. Mycoides ATCC 1778, and compound XII, against both Proteus vuglaris and Saccharomyces cerevisiae ATCC 9763.

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STUDIES ON THE EXTRACELLULAR POLYSACCHARIDES PRODUCED BY ISOLATED DENTAL PLAQUE STREPTOCOCCI (Dental Plaque Streptococci가 생산하는 세포외 다당류에 관한 연구)

  • Chung, Tai-Young
    • The Journal of the Korean dental association
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    • v.9 no.12
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    • pp.819-822
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    • 1971
  • For this investigation, author isolated Streptococcus mitis strain SD-9 from the bacterial flora in the human dental plaque, which was incubated in brain-heart infusion media containing 5% sucrose at 37℃ for 24 hours. For the cytochemical demonstration of polysaccharide produced by this strain, a modified thiosemicarbazide osmium method (Critchley et al., 1967) was used. After fixation with this reagent, the harvested cells was suspended in 1% agar for the higher concentration of cells(Kellenberger et al., 1964). And they were dehydrated in the various concentration of ethanol, and embedded in Epon 812(Luft, 1961). Sectioning was done with the Sorvall MT-2 Porter Blum ultramicrotome by means of a glass knife, and the sections were stained with saturated uranyl acetate and lead citrate (Raynolds, 1963). All preparations were examined in a electron microscope, Hitachi HU-ll E-1 type. The morphological features of extracellular polysaccharide produced by Streptococcus mitis strain SD-9 were appeared in 3 structurally different forms, those are, electron dense fibrillar material linearly arranged adjacent to the outer surface of cell wall, highly electron dense globular material adjacent to the outer surface of cell wall, and strutureless fluffy meshwork of possible very fine filament.

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Synthesis of Asymmetric Pyrazoline Derivatives from Phenylthiophenechalcones; DFT Mechanistic Study

  • Aboelnaga, Asmaa;Mansour, Eman;Ahmed, Hoda. A.;Hagar, Mohamed
    • Journal of the Korean Chemical Society
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    • v.65 no.2
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    • pp.113-120
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    • 2021
  • New phenylthiophenechalcones,1-(biphenyl-4-yl)-3-(5-phenylthiophen-2-yl)prop-2-en-1-one (3a) and 3-(5-phenylthiophen-2-yl)-1-(4-(piperidin-1-yl) phenyl) prop-2-en-1-one (3b) were synthesized, next, their treatment with thiosemicarbazide in ethanol afforded their pyrazoline derivatives (4a) and (4b), respectively. The molecular structures of the synthesized compounds were confirmed via elemental analysis, FT-IR, 1H, 13C NMR and mass spectroscopy. The geometrical elucidation of four suggested conformers has been studied for these compounds. DFT calculations have been performed to study the stability and the structural parameters of the predicted conformers and revealed that orientation of the biphenyl and the phenylthiophene moieties affect the stability of the estimated conformers of the synthesized chalcones and pyrazoline. Moreover, two reaction mechanisms have been proposed to illustrate the reaction products and the DFT calculations have been used to confirm the reaction mechanism of the pyrazoline compounds.