• 약학회지
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• 제13권1호
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• pp.43-46
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• 1969

Five new acyl derivatives of isonicotinic acid hydrazide such as N-(2,4-dichlorophenoxyacetyl)-isoniotinic acid hydrazide (I), N-(p-nitrobenzoyl)-isonicotinic acid hydrazide (II), N-benzoylisonicotinic acid hydrazide (III), N-furoylisonicotinic acid hydrazide (IV) and N-(p-aminobenzoyl)-isonicotinic acid hydrazide (V) were synthesized. They were obtained by the action of 2,4-dichlorophenylacetyl chloride, p-nitrobenzoyl chloride, benzoyl chloride, furoyl chloride and p-aminobenzoyl chloride with isonicotinic acid hydrazide in pyridine solution. Evaluated for their in vitro antitubercular activity against Mycobaterium tuberculosis H$_{37}$ R$_{\upsilon}$ N-furoylisonicotinic acid hydrazide (IV) showed antitubercular activity at 1${\gamma}$/ml.

• Archives of Pharmacal Research
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• 제24권5호
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• pp.377-384
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• 2001

The reaction of either Digitoxin or Digoxin with cyanoacetic acid hydrazide gave the hydrazone derivatives 3a and 3b respectively. The reactivity of the latter products towards chemical reagents was studied to give heterocyclic derivatives with potential biological activities.

• 생약학회지
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• 제29권4호
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• pp.360-364
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• 1998

To develop new elicitors inducing the high productivity of taxane derivatives, plant growth inhibitors, namely, maleic acid hydrazide, N-phosphomethyl glycine and succinic acid 2.2-dimethyl hydrazide, coconut milk and yeast extract were administrated in the cell suspension culture system of Taxus cuspidata, and the production of baccatin III were analysed. The effects of amino acid related with the biosynthesis of baccatin III were also examined in these culture system. As the results, a remarkable enhancement of baccatin III production was observed in the cultivation with coconut water and with maleic acid hydrazide.

• Archives of Pharmacal Research
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• 제25권3호
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• pp.250-257
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• 2002

A series of benzimidazole derivatives carrying different heterocycles such as 1,2,3-thiadiazole, 1,3,4-thiadiazole, thiazolidine, 2,3-dihydro-thiazole, 1,3,4-oxadiazole, semicarbazone and substituted thiosemi-carbazones were synthesized. Also a series of 1-methylbenzimidazole carrying hydroxy ethyl-amide, substituted sulfonyl hydrazide and benzoyl hydrazide from aminobenzoyl group at position 2 of 1-methylbenzimidazole were synthesized. The antimicrobial evaluation of some of the new compounds was carried out.

• Archives of Pharmacal Research
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• 제16권4호
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• pp.318-321
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• 1993

Cyanoaccetic acid hydrazide reacted with some 2-pyrazolin-5-one, isoxazol-5-one and 2-thiazolin-4-one and their ylidene derivatives to yield several new annelated pyran heterocycles. Structures wre established on the basis of elementary analyses and spectral data studies in addition to synthesis via other routes.

• Archives of Pharmacal Research
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• 제13권1호
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• pp.14-18
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• 1990

The carbinols, hydrazide, Schiff's bases and acryloyl derivatives of 2-thiobenzethiazole were prepared. The acid and nitrile of 20thiobenzothiazole were also obtained. The derivatives were tested for their antibacterial activities. Some derivatives showed the highest antifungal and activity.

• 대한화학회지
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• 제54권4호
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• pp.419-428
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• 2010

마이크로웨이브 반응 장치 (Synthos 3000 Aton Paar, GmbH, 1400 W maximum magnetron)를 이용하여, diisopropylcarbodiimide (DIC)/와 1-hydroxybenzotriazoles (HOXt) (X = A or B)를 반응시켜서 amino acid hydrazide를 효율적으로 합성할 수 있는 반응 조건을 개발하였다. 일반적인 가열반응과 마이크로웨이브 반응을 반응 시간, 반응 조건 등을 비교하였을 때에, 마이크로웨이브 반응이 보다 효율적으로 진행되었으며, diisopropylcarbodiimide (DIC)와 1-hydroxybenzotriazole (HOBt) 반응에서보다는 diisopropylcarbodiimide (DIC)와 7-aza-1-hydroxybenzotriazole (HOAt)를 반응시켰을 때에 좋은 수율 (95 - 98%)로 얻어졌다.

• Archives of Pharmacal Research
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• 제26권10호
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• pp.778-784
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• 2003

N'-(1-alkyl-2,3-dihydro-2-oxo-1H-3-indolyliden)-4-pyridinecarboxylic acid hydrazide derivatives, 3(a-g), were synthesized in a trial to overcome the resistance developed with the therapeutic uses of isoniazid (INH). The lipophilicity of the synthesized derivatives supersedes that of the INH as expressed by Clog p values. The synthesized compounds and INH were tested against bovin, human sensitive and human resist strains of Mycobacterium tuberculosis. Compounds 3a, 3d, 3f and 3g with 1-unsubstituted, 1-propyl, 1-propynyl and 1-benzyl groups respectively exhibited equipotent growth inhibitory activity (MIC 10 $\mu$mol) against the tested strains as compared with INH however the later has no activity against human resist strain. Pharmacokinetic study revealed that the rate and extent of absorption of the tested derivatives (3d and 3f) significantly higher than that of INH (p＜0.05). The relative bioavailabilities ($F_R%$) were 183.15 and 443.25 for 3f and 3d respectively as compared to INH. These results preliminary indicate the possible use of the prepared derivatives for treatment of tuberculosis infections in order to overcome the resistance developed with INH.

• 대한화학회지
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• 제58권5호
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• pp.450-455
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• 2014

In the present study, a series of novel N-(1H-benzo[d]imidazol-2-yl)methyl-5-[(hetero)aryl-1,3,4-oxadiazol-2-yl]methanamine (4a-4j) were efficiently synthesized. Condensation of hydrazide derivative 3 with various carboxylic acid derivatives yielded N-[(1H-benzo[d]imidazol-2-yl)methy](5-substituted-1,3,4-oxadiazol-2-yl)methanamine (4a-4j) and compound 5-{[(1H-benzo[d]imidazol-2-yl)methylamino]methyl}-1,3,4-oxadiazole-2-thiol (4k) was obtained on treating hydrazide 3 with carbon disulfide. All the newly synthesized analogues were characterized by IR, $^1H$ NMR, $^{13}C$ NMR and mass spectral data.

• Archives of Pharmacal Research
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• 제11권3호
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• pp.175-180
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• 1988

1-Aryl-4-arylidene-2-oxazoline-5-ones (I) and the corresponding unsaturated amidoesters (II) and arylidene hypuric acid hydrazide (III) were obtained. The hydrazides and 1-aryl-1,3-dithiophenol-2-amidopropan-3-ones derivatives (IV) were also obtained. The derivatives were tested for their antibacterial activities.