• 한국환경과학회지
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• 제14권7호
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• pp.711-717
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• 2005

A magenta azomethine dye(D) was synthesized from the reaction of 3-methyl-1-phenyl-2-pyrazoline-5-one with N,N-diethyl-1,4-phenylenediamine. The magenta azomethine dye was identified on the basis of elemental analysis, $^{13}C-NMR$, infrared, and GC/MS studies. The magenta azomethine dye was decomposed in a basic solution. Rate constants of the fading reaction of magenta azomethine dye in ethanol-water solvent were measured spectrophoto­metrically at 540 nm. Reaction rate was increased with the increase of $[OH\^{-}]\;and\;[H\_{2}O]$ in the region of $[H_{2}O]=11\~40\;M$. The reaction was governed by the following rate law. -d[D]/dt = $\{k_o\;+\;k_{OH}[OH^-][H_{2O}]\}[D]$ A possible mechanism consistent with the empirical rate law has been proposed.

• 대한화학회지
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• 제57권5호
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• pp.599-605
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• 2013

Some N-acetyl pyrazoles including 1-(3-(3,4-dichlorophenyl)-5-(substituted phenyl)-4,5-dihydro-$^1H$-pyrazole- 1-yl) ethanones have been synthesised by solvent free cyclization cum acetylation of chalcones like substituted styryl 3,4- dichlorophenyl ketones using hydrazine hydrate and acetic anhydride in presence of catalytic amount of fly-ash: $H_2SO_4$ catalyst. The yield of these N-acetyl pyrazole derivatives are more than 75%. The synthesised N-acetyl pyrazoline derivatives were characterized by their physical constants and spectral data.

• Archives of Pharmacal Research
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• 제20권6호
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• pp.610-619
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• 1997

Some new 9H-thioxanthen-9-one incorporated into heterocyclic systems such as pyridone 8, pyrazoline 9, pyranone 11, iminopyrane 12, furopyrimidine 17, imidazothiazole 19, thiazole 21, triazine 24 and other related compounds through a para imminophenyl grouping at position-1 of the thioxanthenone ring were synthesized and tested as antitumor agents against L1210 leukemia in mice. Some of the new compounds showed considerable antitumor activity.

• Archives of Pharmacal Research
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• 제13권2호
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• pp.126-131
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• 1990

The novel N-phenyl-2-furohydrazonyl chloride 4A and its p-nitro analog 4B have been prepared and identified. The cycloaddition reactions of nitrilimines 5A and 5B, derived by base catalyzed dehydrochlorination of 4A and 4B respectively, to a variety of dipolarophiles were investigated. The results showed that 4A and 4B are usuful precursors for synthesis of differently substituted 3-(2-furyl)-2-pyrazoline derivatives and their pyrazoles and analogs.

• 대한화학회지
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• 제58권1호
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• pp.49-56
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• 2014

Different pyrazoline derivatives (6a-h and 7a-h) were synthesized by cyclization of substituted chalcones with hydrazine hydrate in acidic as well as basic conditions. Both the reactions were performed under conventional heating and microwave irradiation and percentage yields were compared. All the reactions were accelerated in acidic and basic conditions under microwave irradiation, with higher yields. All the synthesized compounds were characterized by their spectral study (IR, MS, $^1H$ and $^{13}C$ NMR) and were tested for their antibacterial and antifungal activity. The compounds 6g and 7g exhibited significant activity against S. aureu, 7g against E. faecalis, 6b and 7b against E. coli and 6b, 6c, 7b, 7c against S. typhi. The compounds 6d and 7d exhibited significant activity against C. albicans and 6c against M. luteus. Rest of the synthesized compounds showed moderate to poor activity against tested species with compared to standard.

• Bulletin of the Korean Chemical Society
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• 제33권6호
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• pp.2012-2016
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• 2012

A convenient synthetic route has been developed to synthesize 5-(4-((2-phenylthiazol-4-yl) methoxy)phenyl)-3-(4-sustituted phenyl)pyrazolines (5a-f) and 5-(4-((2-phenylthiazol-4-yl)methoxy)phenyl)-3-(4-substituted phenyl)isoxazolines (6a-f) starting from 2-phenyl-4-chloromethylthiazole (1). The chloromethylthiazole (1) was first condensed with 4-hydroxy benzaldehyde (2) for obtaining 4-((2-phenylthiazol-4-yl)methoxy)benzaldehyde (3). Claisen-Smidth condensation of 4-((2-phenylthiazol-4-yl)methoxy)benzaldehyde (3) and acetophenones has been carried in alkaline alcohol and obtained 3-(4-((2-phenylthiazol-4-yl)methoxy)phenyl)-1-(4-substituted phenyl)prop-2-en-1-ones (4a-f). The cyclocondensation of 2-propen-1-ones has been first time carried separately with hydrazine hydrate and hydroxylamine hydrochloride in aqueous micellar tetradecyltrimethylammonium bromide (TTAB) medium for getting the titled heterocycles with good to excellent yields.

• 대한화학회지
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• 제64권1호
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• pp.7-18
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• 2020

An efficient and facile procedure has been developed for the synthesis of novel bichalcone derivatives (4a, 4b). The key step contains the solvent-free aldol synthesis of bichalcones based on quinones. Bichalcones (4a, 4b) were used as precursors for the synthesis of some interesting heterocyclic compounds like, diazepines (5a, 5b), pyrazolo-pyrimidines (7a, 7b), and pyrazoline derivatives (8a, 8b). Moreover, new thioxopyrimidine derivatives (9a, 9b) were furnished and used as a functionalizing agent to produce the triazole-pyrimidines (11, 12) and the carbonitrile derivative (14). All the synthesized compounds were fully characterized using physical and spectral data like, FT-IR, ¹H NMR, ¹³C NMR, and MS. Bichalcones (4a, 4b) and diazepines (5a, 5b) were screened for their anticonvulsant activity, where compounds (4a, 5a, and 5b) revealed potent anticonvulsant activity compared to diazepam. On the other hand, some of the prepared compounds were screened for their antiproliferative activity and they showed significant cytotoxic effects on most of the cancer cell lines with regard to broad spectrum antitumor activity.

• Archives of Pharmacal Research
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• 제23권2호
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• pp.128-138
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• 2000

In continuation of the previous work (Fathalla, 1992) on the synthesis of some heterocycles containing uracil moiety, we report herein the incorporation of uracil moiety into cyan-opyridine thione, thiosemecarbazone, semicarbazone, cyanopyridine, ami nocyano pyridine, isoxazoline, pyrazoline, pyrimidine, triazolo pyrimidine, pyran, selena and thiazole derivatives which might modify their biological activities. The biological studies revealed that the chemical compound III f showed high molluscicdal activity than other compounds. The profile of the nucleoprotein extracted from chemically (compound IIIc, e, f and g) treated or UV-irradiated B.alexandrina snails did not show appreciable differences when compared to non-treated (native) snails by using SDS-PAGE, where no obvious qualitative or quantitative differences were observed. Immunization of experimental animals with the nucleoprotein extracted from native, chemically (compound III f ＆ g) treated or physically treated B.alexandrina snails induced significant protection against challenge with normal S.mansoni cercariae, as compared to the non-immunized challenged control. As well as , a decrease in the number of granuloma formation and the size range of granuloma was also observed in immunized animals. It is concluded that, compounds III f and g have a potent molluscicidal activity. They also induced chemical modification comparable to that induced by physical treatment in the snail's nucleoprotein, which could possibly be used in immunization against S. mansoni infection.

• Archives of Pharmacal Research
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• 제28권11호
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• pp.1205-1212
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• 2005

2-Thiouracil-5-sulphonic acid N-(4-acetylphenyl) Amide (1) was reacted with a series of aromatic aldehydes giving chalcones 2 (Claisen-Schemidt reaction), some of these chalcones were reacted with urea and thiourea giving pyrimidine-2-one and pyrimidine-2 thione derivatives respectively of the type 3a,b and 4a,b. In addition many chalcones were reacted with hydroxylamine hydrochloride giving isoxazoline derivatives 5a,b. They could also reacted with phenylhydrazine to give pyrazoline derivatives 5a,b, chalcones also were reacted withethylcyano acetate and/or malononitryl in pyridine giving pyran derivatives 7a,c and 8a,c. In another pathway chalcones were epoxidised by $H_{2}O_{2}$ giving epoxides 9a,c which in turn were reacted with phenylhydrazine giving 4-hydroxypyrazoline derivatives 10a,c. In another reaction chalcones were reacted with ethylcyanoacetate in presence of amm.acetate giving pyridone derivatives 11a,d which could be prepared also in exellent yield from compound 1 by its reaction with certain aromatic aldehydes and ethylcyanoacetate in presence of ammonium acetate. Finally, compound 1 was reacted with semicarbazide giving semicarbazone intermediate 12 which in turn was reacted with thionyl chloride giving thiadiazole derivative 13. The biological effects of some of the new synthesized compounds were also investigated.

• 한국식품위생안전성학회지
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• 제39권2호
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• pp.72-82
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• 2024

본 연구는 자일로올리고당의 과학적이고 체계적인 표준화된 시험법을 마련하여 다양한 제형의 제품에 적용하고자 하였다. 최적화된 시험법을 마련하기 위해 초음파 처리 시간, 산 가수분해 시간 및 농도를 검토하여 전처리 방법을 비교 평가하였으며, HPLC-UVD를 이용하여 시료 중의 자일로올리고당을 분석하였다. 분석 시 1-phenyl-3-methyl-5-pyrazoline (PMP)으로 유도체화하고, photo diode array (PDA)가 장착된 high performance liquid chromatography (HPLC) (Nanospace SI-2)를 사용하였으며, 칼럼은 Cadenza C₁₈ (4.6 × 250 mm, 3 ㎛)이었으며, 이동상은 pH를 6.0으로 맞춘 20 mM 인산완충용액과 아세토니트릴을 78:22 비율로 혼합하여 사용하였고, 0.5 mL/min 유속으로 254 nm로 하여 분석하였다. 건강기능식품 등 시험법 마련 표준절차에 관한 가이드라인에 따라 밸리데이션을 수행하고, 표준화된 시험법을 이용하여 유통 중인 건강기능식품 대상 품목에 대해 시험법 적용 여부를 확인하였다. 표준화된 시험법은 자일로올리고당을 함유한 건강기능식품 품질관리에 대한 신뢰성을 더 높일 것으로 본다.