• Title, Summary, Keyword: Substituted Thiadiazoles

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Synthesis and Biological Evaluation of Novel 2-[Substituted acetly]-amino-5-alkyl]-amino-5-alkyl-1,3,4-thiadiazoles

  • Shakya, Ashok K.;Mishra, Pradeep;Patnaik, G.K.;Shukla, Rakesh;Srimal, R.C.
    • Archives of Pharmacal Research
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    • v.21 no.6
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    • pp.753-758
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    • 1998
  • Sixteen novel 2-substituted acetyl amino-5-alkyl-1,3,4-thiadiazol were synthesized and screened for their pharmacological activities. A few of the compounds namely 11, 12 and 16 showed anti-inflammatory activities comparable to phenylbutazone. Compound 12 also showed significan non-specific spasmolytic activity. Diuretic activity of compound 15 at a dose level of 90mg/kg p.o. was two fold higher compared to 50mg/kg p.o. of furosemide. Comparable diuresis was aso produced by compounds 9, 10, and 16.

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A One-Step Synthesis and Antimicrobial Activities of New Substituted Dihydro-1,3,4-Thiadiazoles

  • Mahran, Asma M.;Hassan, Nasser A.
    • Archives of Pharmacal Research
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    • v.29 no.1
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    • pp.46-49
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    • 2006
  • In this study, 2-N-arylimino-2,3-dihydro-1,3,4-thiadiazoles derivatives (6a-h) were synthetized. The mechanism of the studied reactions was discussed. The chemical structures of the compounds were elucidated by their IR, $^1H-NMR,\;^{13}C-NMR$, and Mass spectral data and elemental analyses. The compounds were tested for antimicrobial activity using diffusion agar technique.

Electrochemical Studies on Some Substituted Thiadiazoles (몇 가지 치환 Thiadiazole에 대한 전기화학적 연구)

  • El Maghraby, A. A.;Abou-Elenien, G. M.;Abdel-Reheem, N. A.;Abdel-Tawab, H. R.
    • Journal of the Korean Chemical Society
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    • v.50 no.4
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    • pp.307-314
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    • 2006
  • The redox characteristics of 2-ketohydrazono-3-phenyl-5-substituted-2,3-dihydro-1,3,4-thiadiazoles and its derivatives (1a-h) has been investigated in nonaqueous solvents such as 1,2-dichloroethane (DCE), dichloromethane (DCM), acetonitrile (AN), tetrahydrofuran (THF), and dimethylsulfoxide (DMSO) containing 0.1 mol.dm-3 tetra n-butylammonium perchlorate (TBAP) as supporting electrolyte at platinum ectrode. Through controlled potential electrolysis, the oxidation and reduction products of the investigated compounds can be separated and indentified. The redox mechanism is suggested and proved. It was found that all the investigated compounds are oxidized in two irreversible one-electron processes following the well known pattern of EC-mechanism. On the other hand, these compounds are reduced in a single two electron or in a successive two one electron processes following the well known pattern of EEC-mechanism according to the nature of the substituent

Voltammetric Studies on Some Thiadiazoles and Their Derivatives

  • Maghraby, A. A. El;Abou-Elenien, G. M.;Rateb, N. M;Abdel-Tawab, H. R.
    • Journal of the Korean Electrochemical Society
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    • v.12 no.1
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    • pp.54-60
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    • 2009
  • The redox characteristics of 2-arylaldehydehydrazono-3-phenyl-5-substituted-2, 3-dihydro-1, 3, 4-thiadiazoles (1a-h) have been investigated in nonaqueous solvents such as 1, 2-dichloroethane (DCE), dichloromethane (DCM), acetonitrile (AN), Tetrahydrofuran (THF), and dimethylsulfoxide (DMSO) at platinum electrode. Through controlled potential electrolysis, the oxidation and reduction products of the investigated compounds had been separated and indentified. The redox mechanism had been suggested and proved. It had been found that all the investigated compounds were oxidized in two irreversible one-electron processes following the well-known pattern of The EC-mechanism; the first electron loss gives the corresponding cation-radical which is followed by proton removal from the ortho-position in the N-phenyl ring forming the radical. The obtained radical undergoes a second electron uptake from the nitrogen in the N = C group forming the unstable intermediate (di-radical cation) which undergoes ring closure forming the corresponding cation. The formed cation was stabilized in solution through its combination with a perchlorate anion from the medium. On the other hand, these compounds are reduced in a single two-electron process or in a successive two one-electron processes following the well known pattern of the EEC-mechanism according to the nature of the substituent; the first one gives the anion-radical followed by a second electron reduction to give the dianion which is basic enough to abstract protons from the media to saturate the (C = O) bond.

CoMFA on the Antiproliferative Activity of N-Substituted(R) 2-Amino-5-(2,4-dihydroxyphenyl)-1,3,4-thiadiazole Analogues against Bladder and Rectal Cancer Cells (방광암(HCV29T) 및 직장암(SW707) 세포에 대한 N-치환(R)-2-amino-5-(2,4-dihydroxyphenyl)-1,3,4-thiadiazole 유도체의 항증식 활성에 관한 CoMFA 분석)

  • Myung, Pyung-Keun;Kang, Na-Na;Lee, Jae-Hwang;Sung, Nack-Do
    • YAKHAK HOEJI
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    • v.54 no.5
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    • pp.328-333
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    • 2010
  • Comparative molecular field analyses (CoMFA) on the antiproliferative activity of N-substituted (R) 2-amino-5-(2,4-dihydroxyphenyl)-1,3,4-thiadiazole analogues (ADTs: 1-17) against bladder cancer (HCV29T) and rectal cancer (SW707) cells were studied quantitatively. The statistical predictability and fitness of CoMFA A1 model for bladder cancer cells were better than those of CoMFA F1 model for rectal cancer cells and the antiproliferative activity of ADTs depends on steric field (HCV29T: 93.1% & SW707: 83.8%). Also, from the contour maps of optimized CoMFA models, the activity for bladder cancer cells had predicted to increase when sterically favored groups were substituted on meta- and para-position, and sterically disfavored groups were substituted on one ortho-position of phenyl ring. The activity for rectal cancer cells had predicted to increase when sterically favored groups were substituted on para-position, and sterically disfavored groups were substituted on two ortho-position of phenyl ring as R-group.