• Archives of Pharmacal Research
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• 제12권2호
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• pp.68-72
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• 1989

The hydrolysis rates of ester and amide derivatives of 20-dihydroprednisolonic acid were measured in rat serum and liver homogenate. The hydrolysis rate of the esters in serum was found to be faster than that in liver homogenate on the basis of blood volume and liver weight, while the amide derivatives showed much slower change. And it is also found that the size of substituents at C-21 and C-20 configuration expressed considerable effects on the hydrolysis rate of these derivatives.

• Bulletin of the Korean Chemical Society
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• 제31권6호
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• pp.1765-1768
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• 2010

• Bulletin of the Korean Chemical Society
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• 제19권10호
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• pp.1105-1109
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• 1998

A chiral stationary phase derived from (S)-N-(3,5-dinitrobenzoyl)leucine N-phenyl N-alkyl amide (CSP 2) was applied in separating the two enantiomers of various π-basic aromatic derivatives of leucine N-propyl amide in order to evaluate π-basic aromatic groups as an effective derivatizing group for the resolution of a-amino acids. Subsequently N-(3,5-dimethoxybenzoyl) group was found to be very effective as a π-basic aromatic derivatizing group. Based on these results, N-(3,5-dimethoxybenzoyl) derivatives of various a-amino N-propyl amides, N,N-diethyl amides and esters were resolved on the CSP derived from (S)-N-(3,5-dinitrobenzoyl) leucine N-phenyl N-alkyl amide (CSP 2) and the resolution results were compared with those on the CSP derived from (S)-N-(3,5-dinitrobenzoyl)leucine N-alkyl amide (CSP 1). The enantioselectivities exerted by CSP 2 were much greater than those exerted by CSP 1. In addition, racemic N-(3,5-dimethoxybenzoyl)-a-mino N,Ndiethyl amides were resolved much better than the corresponding N-(3,5-dimethoxybenzoyl)-a-mino N-propyl amides and esters on both CSPs. Based on these results, a chiral recognition mechanism utilizing the π-π donor-acceptor interaction and the two hydrogen bondings between the CSP and the analyte was proposed.

• Bulletin of the Korean Chemical Society
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• 제32권3호
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• pp.1022-1026
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• 2011

The syntheses of DTPA-bis(amide) conjugates of phosphonated cyclohexane moieties (5a-d) and their Gd(III) complexes of the type $[Gd(L)(H_2O)]{\cdot}nH_2O$ (6a-d; L = 5a-d) are described. All new compounds have been characterized by microanalysis and spectroscopic techniques. High $r_1$ relaxivities of aqueous solutions of 6a-d are observed to be in the range of $10.7-18.3\;mM^{-1}sec^{-1}$, which compare much better than that of $Omniscan^{(R)}$ ($r_1=3.90\;mM^{-1}sec^{-1}$).

• Animal Bioscience
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• 제34권10호
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• pp.1684-1694
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• 2021

Objective: This study investigated the association between feed efficiency, physicochemical properties, flavor precursors and biomolecules in the thigh meat of Korat (KR) chickens. Methods: The feed intake and body weight of individual male KR chickens were recorded from 1 to 10 weeks old to calculate the individual residual feed intake (RFI) of 75 birds. At 10 weeks of age, chickens with the 10 highest (HRFI) and lowest RFI (LRFI) were slaughtered to provide thigh meat samples. The physicochemical properties (ultimate pH, water holding capacity [WHC], drip loss) and flavor precursors (guanosine monophosphate, inosine monophosphate (IMP), adenosine monophosphate and inosine) were analyzed conventionally, and Fourier transform infrared spectroscopy was used to identify the composition of biomolecules (lipids, ester lipids, amide I, amide II, amide III, and carbohydrates) and the secondary structure of the proteins. A group t-test was used to determine significant differences between mean values and principal component analysis to classify thigh meat samples into LRFI and HRFI KR chickens. Results: The physicochemical properties of thigh meat samples from LRFI and HRFI KR chickens were not significantly different but the IMP content, ratios of lipid, lipid ester, protein (amide I, amide II) were significantly different (p<0.05). The correlation loading results showed that the LRFI group was correlated with high ratios of lipids, lipid esters, collagen content (amide III) and beta sheet protein (rg loading >0.5) while the HRFI group was positively correlated with protein (amide I, amide II), alpha helix protein, IMP content, carbohydrate, ultimate pH and WHC (rg loading >0.5). Conclusion: The thigh meat from chickens with different RFI differed in physiochemical properties affecting meat texture, and in the contents of flavor precursors and biomolecules affecting the nutritional value of meat. This information can help animal breeders to make genetic improvements by taking more account of traits related to RFI.

• Journal of Pharmaceutical Investigation
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• 제10권3호
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• pp.46-50
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• 1980

This study was performed to compare the activities of sulfate esters and sulfonate salts. (comparison of activities such as detergency, forming, permeation and patient of hard water). The one of the method is the combined use of nonionics and the other is the use of anionics alone. The results obtained are as follows: 1. The sulfonate salts are better soluble than the sulfate esters. 2. The lauryl system is better soluble than the sulfate esters. 3. The alkylol sulfate(CONH-OSO3H)that is induced amide radical to the fatty acid shows the excellent foaming power and detergency.

• Bulletin of the Korean Chemical Society
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• 제18권10호
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• pp.1085-1089
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• 1997

A new HPLC chiral stationary phase (CSP 3) has been prepared by connecting N-phenyl N-propyl amide of (S)-naproxen to silica gel through the 6-methoxy-2-naphthyl group of (S)-naproxen. The new CSP has been applied in resolving a homologous series of N-(3,5-dinitrobenzoyl)-α-amino acid esters and a homologous series of N-(3,5-dinitrobenzoyl)-α-(4-alkylphenyl)alkylamines. The separation factors, α, for resolving a homologous series of N-(3,5-dinitrobenzoyl)-α-amino esters and a homologous series of N-(3,5-dinitrobenzoyl)-α-(4-alkylphenyl)alkylamines on the new CSP have been found to remain almost constant throughout the wide range of the length of the alkyl substituent of the analytes while those on the previously reported CSPs (CSP 1 and 2) which were prepared by connecting N-phenyl N-propyl amide of (S)-naproxen to silica gel through the N-propyl group increase or decrease continuously. These results are concluded to support the chiral recognition models which utilize the intercalation of the alkyl substituent of the racemic analytes between the adjacent strands of CSP 1 or 2 to rationalize the increasing or decreasing trends of separation factors.

• Bulletin of the Korean Chemical Society
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• 제25권2호
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• pp.207-212
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• 2004

In this study, we attempted to prepare compounds with heterocyclic replacements for metabolically unstable esters of benzopyranyl indole-2-carboxylic esters, which showed good in vitro and in vivo cardioprotective efficacies possibly through the opening of mitochondrial ATP-sensitive potassium channel ($K_{ATP}$). Initially, we tried to construct indolin-2-yl-heterocycles using unprotected indoline-2-carboxylic acid, but the cyclization was proceeded with oxidation of the indoline ring to the indole, which didn't react with benzopyranyl epoxide. Thus we introduced N-Boc group to deplete the electron density of the indoline ring. We successfully prepared various indolin-2-yl-heterocycles by the cyclization of the building blocks including carboxamide, ${\beta}$-hydroxy amide, hydrazide, nitrile starting from N-Boc-indoline-2-carboxylic acid.

• 공업화학
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• 제23권4호
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• pp.421-427
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• 2012

초저유황 경유의 윤활성능을 향상시킬 목적으로 식물유 기반 알칸올 아마이드 유도체를 합성하여 윤활성능을 평가하였다. 알칸올 아마이드 유도체는 폐식물유(다크오일), 팜유, 코코넛유를 메탄올과의 연속 전이에스테르화 반응을 통하여 합성한 지방산 메틸에스테르와 디에탄올아민(DEA)의 아마이드화 반응을 행하여 합성하였다. 합성한 알칸올 아마이드 유도체는 1 wt% 범위 내에서 초저유황 경유에 잘 용해되었으며, 이 유도체를 120 ppm 포함한 초저유황 경유의 윤활성능을 HFRR법으로 측정하였다. 그 결과, 초저유황 경유의 마모흔의 직경이 581 ${\mu}m$에서 아마이드 첨가 후 305~323 ${\mu}m$으로 현저히 작아져 초저유황 경유의 윤활성능을 향상하는 것으로 확인되었다. 한편, 식물유의 종류에 따른 마모흔의 차이는 크지 않아 알칸올 아마이드 유도체의 알킬기의 구조에 따른 윤활성능의 차이는 크게 나타나지 않았다. 알칸올 아마이드 한 종류를 선정하여 첨가 농도에 따른 윤활성능을 평가한 결과, 농도에 따라 마모흔의 직경이 현저히 작아지는 결과를 얻었는데 이는 윤활성능이 첨가 농도에 따라 향상되는 것을 의미한다.

• Archives of Pharmacal Research
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• 제28권6호
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• pp.637-647
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• 2005

This work includes the synthesis of 15 final compounds (6a-h and 7b-h) as prod rugs of 5-ASA in the form of the acid itself, esters and amides linked by an amide linkage through a spacer to the endocyclic ring N of nicotinamide. Also, 15 new intermediate compounds were prepared. The target compounds (6b, 6f, 7b, and 7e-h) revealed potent analgesic and anti-inflammatory activities in comparison to sulfasalazine and 5-ASA. In addition, ulcerogenicity, $LD_{50}$, in vivo and in vitro metabolism of compound 7f were determined.