• 제목/요약/키워드: Heterocyclic compounds

검색결과 142건 처리시간 0.019초

Synthesis and In-vitro Activity of Some New Class of Thiazolidinone and Their Arylidene Derivatives

  • Seelam, Nareshvarma;Shrivastava, S.P.
    • Bulletin of the Korean Chemical Society
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    • 제32권11호
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    • pp.3996-4000
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    • 2011
  • In an attempt to find a new class of anti microbial agents, a series of thiazolidinone and their 5-arylidene derivatives containing 4-(4-methyl benzamido)-benzoyl moiety were synthesized via the reaction of benzocaine with appropriate chemical reagents. These compounds were screened for their antibacterial activity against Gram-positive bacteria (Bacillus subtilis and Bacillus thuringiensis), Gram-negative bacteria (Escherichia coli, Pseudomonas aeruginosa) and antifungal activity against Botrytis fabae, Fusarium oxysporan and Candida albicans. On the other hand the synthesized compounds were also screened for their anti tubercular activity. IR, $^1H$ NMR, $^{13}C$ NMR and MS spectral analyses established the structures of the newly synthesized compounds. The results revealed that some of these compounds have shown promising antimicrobial and anti tubercular activity in comparison with standard drugs.

Volatile Flavor Components in Boiled Snow Crab (Chionoecetes japonicus) and Its Concentrated Cooker Effluent

  • Park, Sung-Hee;Kim, Young-Man;Hyun, Sook-Kyung
    • Preventive Nutrition and Food Science
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    • 제6권2호
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    • pp.87-90
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    • 2001
  • The volatile flavor components of snow crabs from the Young-duk coast of Korea and their concentrated cooker effluent were isolated by a modified method from Likens and Nickerson, using a simultaneous distillation and extraction apparatus. The concentrated extract was analyzed and identified by gas chromatography and GC-MS. The flavor profile of boiled crab demonstrated that the favorable flavor characteristic of crab involved a seafood-like note, and that of concentrated cooker effluent demonstrated that the weak boiled crab flavor involved a fishy note. The main flavor components of boiled crab were heterocyclic compounds including alkylpyrazines, thizoles and thiolanes, aliphatic ketones including 2-heptanone and nonanone. On the other hand, the main flavor components of cooker effluent were aldehydes including 3-methylbutanal, alipatic ketones including 2-heptanone and alkanes including 2,6,10,14-tetramethyl-pentadecane. Almost all of heterocyclic compounds, which seem to be important contributors to the flavor of boiled crab, were not identified in concentrated cooker effluent. As a result, there may be a need to add the crab flavor components formed through model experiments of Maillard reactions to the concentrated cooker effluent for human consumption.

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Simultaneous degradation of nitrogenous heterocyclic compounds by catalytic wet-peroxidation process using box-behnken design

  • Gosu, Vijayalakshmi;Arora, Shivali;Subbaramaiah, Verraboina
    • Environmental Engineering Research
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    • 제25권4호
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    • pp.488-497
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    • 2020
  • The present study investigates the feasibility of nitrogenous heterocyclic compounds (NHCs) (Pyridine-Quinoline) degradation by catalytic wet peroxidation (CWPO) in the presence of nanoscale zerovalent iron supported on granular activated carbon (nFe0/GAC) using statistical optimization technique. Response surface methodology (RSM) in combination with Box-Behnken design (BBD) was used to optimize the process parameters of CWPO process such as initial pH, catalyst dose, hydrogen peroxide dose, initial concentration of pyridine (Py) and quinolone (Qn) were chosen as the main variables, and total organic carbon (TOC) removal and total Fe leaching were selected as the investigated response. The optimization of process parameters by desirability function showed the ~85% of TOC removal with process condition of initial solution pH 3.5, catalyst dose of 0.55 g/L, hydrogen peroxide concentration of 0.34 mmol, initial concentration of Py 200 mg/L and initial concentration of Qn 200 mg/L. Further, for TOC removal the analysis of variance results of the RSM revealed that all parameter i.e. initial pH, catalyst dose, hydrogen peroxide dose, initial concentration of Py and initial concentration of Qn were highly significant according to the p values (p < 0.05). The quadratic model was found to be the best fit for experimental data. The present study revealed that BBD was reliable and effective for the determination of the optimum conditions for CWPO of NHCs (Py-Qn).

Facile Synthesis and Biological Evaluation of Heterocyclic Compounds Containing Diazepam

  • Berghot, M.A.
    • Archives of Pharmacal Research
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    • 제24권4호
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    • pp.263-269
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    • 2001
  • Diazepamoxadiazoles 4,5,6,12,14 and 22 were prepared with the binary form system. Diazepamthiadiazoles 15,20 and Diazepamtriazoles 7,8,9,17,18,19 and 21 were also shapely synthesized. Some of these compounds were screened to test their antibacterial activity against E. coli and B. subtilis compounds 15 and 20 show potent activity against these bacteria.

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Preparation of Boronated Heterocyclic Compounds Using Intramolecular Cyclization Reaction

  • Lee, Chai-Ho;Jin, Guofan;Kim, Hyo-Suk;Nakamura, Hiroyuki;Chung, Yong-Seog;Lee, Jongdae
    • Bulletin of the Korean Chemical Society
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    • 제29권2호
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    • pp.357-362
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    • 2008
  • A method for synthesizing o-carborane substituted tetrahydroisoquinolines containing a polar functional group such as sulfamide, sulfonic, or phosphoric acid on the nitrogen atom of the piperidine ring, starting from arylethylamine, N-(2-arylethyl)sulfamide, N-(2-arylethyl)sulfamic acid or 2-arylethylamidophosphate, is described. In vitro studies showed the desired compounds 10, 15, 19, and 25 synthesized accumulate to high levels in B-16 melanoma cells with low cytotoxicity.

Antimicrobial Activity of Garlic Heated under Different Conditions, Time of Heating, and pH

  • Kim, Eun-Hee;Kang, Seung-Sik;Kang, Dong-Hee;Kyung, Kyu-Hang
    • Food Science and Biotechnology
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    • 제18권3호
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    • pp.771-775
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    • 2009
  • Antimicrobial activity of garlic (pH 6.0) heated at $120^{\circ}C$ reached its maximum at 45 min of heating and maintained the level for the rest of heating time (300 min) when tested against Candida utilis ATCC42416. The principal antimicrobial compound was allyl alcohol (AA), a highly volatile compound without sulfur in its molecule. The concentration of AA in heated garlic gradually increased to over 2,000 ppm for the first 90 min and stayed at the level without appreciable changes in spite of further heating. Other antimicrobial compounds secondary to AA were lowly volatile sulfur compounds including diallyl polysulfides (diallyl trisulfide, diallyl tetrasulfide, and diallyl pentasulfide) and heterocyclic sulfur compounds (4-methyl-1,2,3-trithiolane, 5-methyl-1,2,3,4-tetrathiane, and 6-methyl-1,2,3,4,5-pentathiepane). When the pH of the garlic extract was lowered before heating, considerably more secondary antimicrobial sulfur compounds were formed and the antimicrobial activity was stronger than the pH unadjusted garlic. Lowly volatile sulfur compounds contributed a significant part of antimicrobial activity of heated garlic only during the early period (45-120 min) of heating regardless of pH treatment.

Synthesis of Novel Benzofuran and Related Benzimidazole Derivatives for Evaluation of In Vitro Anti-HIV-1, Anticancer and Antimicrobial Activities

  • Rida, Samia M.;El-Hawash, Soad A.M.;Fahmy, Hesham T.Y.;Hazzaa, Aly A.;El-Meligy, Mostafa M.M.
    • Archives of Pharmacal Research
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    • 제29권10호
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    • pp.826-833
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    • 2006
  • Previously, we synthesized and evaluated several benzofuran derivatives containing heterocyclic ring substituents linked to the benzofuran nucleus at C-2 by a two- to four-atom spacer as potential anti-HIV-1, anticancer and antimicrobial agents. Among these derivatives, NSC 725612 and NSC 725716 exhibited interesting anti-HIV-1 activity. To further investigate the structure-activity relationship, we synthesized several new benzofuran derivatives derived from 2-acetylbenzofuran (2, 3a-c) and 2-bromoacetylbenzofuran (6; 7a,b; 8a,b). The compounds were designed to comprise the heterocyclic substituents directly linked to the benzofuran nucleus at C-2. Moreover, various related benzimidazoles derived from 2-acetylbenzimidazole and from 2-cyanomethylbenzimidazole (12a,b; 13a,b; 15; 16a,b) were also prepared as isosteres. The synthesized compounds were preliminarily evaluated for their in vitro anti-HIV-1, anticancer and antimicrobial activity. Compounds 2, 3a, 3b, and 12b showed weak anti-HIV-1 activity. Compound 6 exhibited mild activity against S. aureus, while compound 15 had mild activity towards S. aureus and C. albicans. However, no significant anticancer activity was observed with any of the tested compounds. From these results, we conclude that the presence of the spacer between the heterocyclic substituent and the benzofuran nucleus may be essential for the biological activity.