• Archives of Pharmacal Research
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• 제21권6호
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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.

• Archives of Pharmacal Research
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• 제29권1호
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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.

• 대한화학회지
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• 제50권4호
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• pp.307-314
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• 2006

2-Ketohydrazono-3-phenyl-5-substituted-2,3-dihydro-1,3,4-thiadiazole과 그 유도체들(1a-h)의 산화환원 특성을 백금 전극의 지지전해질로서 0.1 M tetra n-butylammonium perchlorate (TBAP)을 함유한 1,2-dichloroethane (DCE), dichloromethane (DCM), acetonitrile (AN), tetrahydrofuran (THF), and dimethylsulfoxide (DMSO)와 같은 비수용매 속에서 조사하였다. 조사한 화합물들의 산화 및 환원 생성물들을 조절전위 전해법으로 분리 확인하였으며, 산화환원 메커니즘을 제안하고 이를 증명하였다. 조사한 모든 화합물은 잘 알려진 EC 메커니즘에 이은 두 번의 비가역 일전자 과정에 의해 산화되는 반면, 환원의 경우에는 치환기의 성질에 따라, 잘 알려진 EEC 메커니즘에 이은 한번의 이전자 또는 두 번의 연속적인 일전자 과정에 의해 이루어짐을 알았다.

• 전기화학회지
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• 제12권1호
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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.

• 약학회지
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• 제54권5호
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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.