• Archives of Pharmacal Research
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• 제8권1호
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• pp.7-14
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• 1985

Membrane-coated tablet of isonicotinic acid hydrazide (INAH) which releases INAH at the zero-order kinetics was deveoped. It consisted of a soluble tablet core surrounded by a porous membrane which controls the diffusion rate. Tablet cores were prepared by compressing granules of INAH and polyvinyl chloride (PVC) dissolved in methyl ethyl ketone in which micronized sucrose were suspended. Diffusion rate of INAH from the tablet through the membrane was constant until the loaded INAH in the core was almost released. The rate was independent of pH of the dissolution medium. Water-soluble sucrose particles behaved as a poreproducing material in the water-insoluble PVC film coat. The pH independency of the rate was probably due to the high solubility of INAH in the water of wide pH range. The diffusion rate of INAH could be controlled by chnaging the composition of the membrane or the coat weight. This membrane-coated INAH tablet seemed to be a powerful candidate for the controlled release drug delivery system (DDS) of INAH or other highly watersoluble drugs.

• 한국미생물·생명공학회지
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• 제30권2호
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• pp.142-150
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• 2002

Cholesterol oxidase(EC 1.1.3.6)는 cholesterol을 산화 또는 이성화시키는 효소로, 혈중 cholesterol 측정 등의 임상진단용 시약에 이용되고 있으며, 여러 종류의 미생물에서 분리, 연구되어 왔다. 현재에는 농업 및 식품 등에도 응용이 기대되고 있는 매우 유용한 효소이다. 본 실험은 공시균인 Streptomyces polychromogenes IFO 13072의 효소 생산 조건과 cholesterol oxidase의 정제 및 효소학적 특성을 조사하였다. 효소 생산 조건을 검토한 결과, 탄소원으로 1% dextrin, 유기 질소원으로는 0.5% casamino acid, 무기 질소원으로는 0.5% sodium nitrate가 효소생산에 우수하였으며, 이들 탄소원, 질소원 이외 0.1% $KH_2$$PO_4$, 0.05% $MgSO_4$ㆍ$7H_2$O가 함유된 배지를 생산 최적 배지로 사용하였다. 본 효소의 정제는 30-80% 포화의 ($NH_4$)$_2$$SO_4$ 침전 및 cholesterol affinity column chromatography를 통하여 23.2%의 수율로 정제되었다. 정제된 효소는 SDS-PAGE에서 단일한 밴드를 보였으며, 분자량은 약 52,000 Da으로 추정되었다. 본 효소의 특성을 검토한 결과, 최적 온도와 최적 pH는 각각 $37^{\circ}C$, pH 7.0이었으며, 효소의 안정성은 온도 $25^{\circ}C$, pH 6.0~7.0의 범위까지 안정한 것으로 나타났다. 또한 본 효소는 금속이온으로 Hg와 Fe 이온의 존재시 크게 저해를 받았고, dithiothreitol과 mercaptoethanol, Isonicotinic acid와 같은 저해제에 의해서 상당히 실활 되었다. 본 cholesterol oxidase의 Michaelis 상수는 cholesterol을 기질로 하여 Lineweaver-Burk plot 분석에서 25 mM로 추산되었다

• 약학회지
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• 제13권1호
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• pp.33-37
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• 1969

A new organic reagent, 1-isonicotynyl-2-furfurylidene hydrazine synthesized from isonicotinic acid hydrazid and furfural, gives yellow liquid with cadmium (II). Cadmium complex of the reagent is soluble in water with yellow coloration. The complex has a maximum absorption at 363 m${\mu}$ and molar ratio of cadmium to reagent was estimated as 1:1 by continuous variation method and slope method. Molecular extinction coefficient and apparent formation constant of this complex was spectrophotometrically determined. K=4.48 $\times$ 10$^{3}$ (Babko's method) K=1.33 $\times$ 10$^{3}$ (Anderson's method)

• 약학회지
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• 제9권1_2호
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• pp.18-22
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• 1965

A new organic reagent, 1-isonicotinoyl-2-furfurylidene hydrazine was synthesized from isonicotinic acid hydrazide and furfural, gives precipitate with copper(II), mercury(II) and argent(I), whereas, it gives a water soluble yellow complex with iron(III). Copper complex of the reagent is soluble in EtOH MtOH, pyridine, dioxane and dimethylformamide with green yellow coloration. The complex has a maximum absorption at 385 m.$\mu$ and molar ratio of copper; reagent was estimated as 1:1 by continuous variation method, slop method and chelate titration method. Molar extinction coefficient (9600) and apparant formation constant of this complex was spectrophotometrically determined. K=1.7 * $10^{7}$ (Babko's method) K=2.1 * $10^{7}$ (Anderson's method). This reagent reacted with copper so sensitive that it would be available for determination of Cu (II).

• Journal of Pharmaceutical Investigation
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• 제8권2호
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• pp.26-34
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• 1978

Isoniazid(INH)는 체내(體內)에서 신속(迅速)히 흡수(吸收)되어 일부(一部)는 치료효과(治療?果)가 있는 유리(遊離) INH로 변(變)하고 일부(一部)는 치료효과(治療?果)가 없는 acetylisoniazid, isonicotinic acid, isonicotinuric acid등(等)으로 대사(代謝)되어 불활성화(不活性化)된다. 가토(家兎)의 뇨(尿) 및 혈장중(血?中)에서 총(總) INH에 대(對)한 유리(遊離) INH의 비(比)를 정색적(呈色的)으로 정량(定量) 산출(算出)함으로써 INH의 불활성화(不活性化)에 미치는 Ethambutol(EMB)의 영향(影響)을 실험(實驗)하였다. 가토(家兎)에 INH를 경구투여(經口投與)한 결과(結果) 그 대사(代謝)에 의(依)한 불활성화비(不活性化比)는 같은 가토(家兎)에서는 비교적(比較的) 일정(一定)하고 개체간(個體間)의 차이(差異)는 현저하였다. INH에 EMB를 배합투여(配合投與)하거나 분자화합물(分子化合物)을 투여(投與)했을 경우 EMB에 의(依)해 INH의 대사(代謝)가 억제(抑制)되어 INH 단독투여시(單獨投與時)보다 유리(遊離) INH가 뇨(尿) 및 혈장중(血漿中)에서 증가(增加)하였다. EMB에 의(依)한 유리(遊離) INH의 상승(上昇)은 INH단독투여(單獨投與)보다 평균(平均) 1.5배(倍)이며 EMB분자화합물(分子化合物)이 EMB배합물(配合物)보다 혈장중(血?中)에서 1.3배(倍) 높게 나타났다.

• 한국응용과학기술학회지
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• 제7권2호
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• pp.11-18
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• 1990

N-alkyl carboxy pyridinium chlorides such as N-lauryl carboxy-pyridinium chloride, N-myristyl carboxy pyridinium chloride, N-cetyl carboxy pyridinium chloride and N-stearyl carboxy pyridinium chloride were synthesized by the reaction of nicotinic acid and isonicotinic acid with long chain alkyl chlorides, and N-alkyl pyrinium carboxylates such as N-lauryl pyridinium carboxylate, N-myristyl pyridinium carboxylate. N-cetyl pyridinium carboxylate and N-stearyl pyridinium carboxylate were prepared from N-alkyl carboxy pyridinium chlorides. These reaction products could be separated by both column chromatogrphy, and paper chromatography, and there dissociation constants of N-alkyl pyridinium carboxylates were found to pKa $1.0{\times}10^{13}{\sim}6,31{\times}10^{14}$.

• 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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• 제55권6호
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• pp.960-968
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• 2011

A series of isonicotinyl hydrazones and their 4-thiazolidinones have been synthesized by condensation of isonicotinic acid hydrazide with various aromatic aldehydes to yield Schiff's bases, followed by the cyclocondensation of Schiff's bases with 2-mercaptoacetic acid to yield their 4-thiazolidinones. The synthesized compounds have been characterized by their elemental, analytical and spectral studies. All these compounds were evaluated for their invitro antimicrobial activity against a spectrum of non-resistant and resistant microbial organisms. These studies proved that compounds 5e,i against B. subtilis; 5e,f,h against B. anthracis; 5g,i against S. aureus showed good activity at lower concentrations. Compounds 5d-5i displayed significant activity against resistant strain of K. pneumonia with minimum inhibitory potency in the concentration range of 2-16 ug/ml.

• The Plant Pathology Journal
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• 제39권2호
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• pp.159-170
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• 2023

Spot blotch disease of wheat caused by Bipolaris sorokiniana (Sacc.) Shoem is considered as an economically important disease which affects all the growing stages of wheat crop. Therefore, it is important to search some effective management strategies against the spot blotch pathogen. Some synthetic elicitor compounds (salicylic acid, isonicotinic acid, and chitosan) and nano-particles (silver and aluminum) were tested against the pathogen to observe the change in biochemical activity and defense action of wheat plant against spot blotch disease. All the tested elicitor compounds and nano-particles showed a significant increase in activity of peroxidase, polyphenol oxidase (PPO), and total phenol over control. The highest increase in activity of peroxidase was recorded at 72 h from chitosan at 2 mM and 96 h from silver nano-particle at 100 ppm. Maximum PPO and total phenol activity were recorded from chitosan at 2 mM and silver nano-particle at 100 ppm as compared to pathogen-treated and healthy control. The lowest percent disease index, lowest no. of spots/leaf, and no. of infected leaves/plant were found in silver nano-particle at 100 ppm and chitosan at 2 mM, respectively. The use of defense inducer compounds results in significantly up-regulated enzymatic activity and reduced spot blotch disease. Therefore, chitosan and silver nano-particle could be used as alternative methods for the management of spot blotch disease.

• 한국연초학회지
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• 제31권1호
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• pp.39-44
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• 2009

Hydrogen cyanide (HCN) is present in both the particulate and vapor phase of cigarette mainstream smoke. It is one of the 44 harmful substances on Hoffmann's list and is known to be a major ciliatoxic agent in cigarette mainstream smoke. Typically the determination of HCN in cigarette mainstream smoke has been done through colorimetric and electrochemical techniques, such as UV-spectrophotometry (UV), continuous flow analyzer (CFA), ion chromatography (IC) and capillary GC-ECD. In particular, CFA commonly has been using analysis hydrogen cyanide in cigarette smoke and the basic principle is pyridine-pyrazolone reaction. In this study, the more optimized analytical method is suggested isonicotinic acid-pyrazolone reaction method than previous pyridine-pyrazolone reaction method, a commonly used method for the determination of cyanide in water and air, by CFA. Sample collection was optimized by trapping particulate and vapor phase of smoke separately. The optimum NaOH concentration of the trapping solution was shown to be 0.2 M. HCN was stable up to 6 hours in this concentration but only 3 hours in 0.1 M solution. The sensitivity of this method was fairly good and it might be used in analysis of HCN in cigarette mainstream smoke.