• Title/Summary/Keyword: Pharmaceutical Compounds

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Flavonoids of Crotalaria sessiliflora

  • Yoo, Hun-Sung;Lee, Ji-Suk;Kim, Chul-Young;Kim, Jin-Woong
    • Archives of Pharmacal Research
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    • v.27 no.5
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    • pp.544-546
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    • 2004
  • Phytochemical investigation of the whole plants of Grata/aria sessiliflora L. led to the isolation of four flavonoids. The structures of these compounds were identified as 2',4',5,7-tetrahydroxy-isoflavone (1), 2',4',7-trihydroxyisoflavone (2), 4',7-dihydroxyflavone (3), and isovitexin (4) using spectroscopic analysis. Among these, compounds 2, and 3 have not been reported from Crotalaria species, whereas compounds 1, and 4 were reported from this plant for the first time.

Synthesis and Antinociceptive Activity of (5-Chloro-2(3H)-Benzoxazolon-3-yl) Propanamide Derivatives

  • Onkol, Tijen;Sahin, M.Fethi;Yidirim, Engin;Erol, Kevser;Ito, Shigero
    • Archives of Pharmacal Research
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    • v.27 no.11
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    • pp.1086-1092
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    • 2004
  • In this study, (5-chloro-2(3H)-benzoxazolon-3-yl)propanamide derivatives were synthesized. The chemical structures of the compounds were elucidated by their IR and $^1H-NMR$ spectral data and microanalysis. The compounds were tested for anti nociceptive activity by using the tail clip, tail flick, hot plate, and writhing methods. The varying levels of anti nociceptive activity of the compounds were compared with those of dipyrone and aspirin. Among these compounds, compound 5e, 5g, and 5h have been found to be significantly more active than the others and the standards in all the tests.

Synthesis and Antimicrobial Activity of Novel Tetrahydrobenzothienopyrimidines

  • Amal Abdel Haleem Mohamed Eissa;Ashraf Ahmed Moneer
    • Archives of Pharmacal Research
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    • v.27 no.9
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    • pp.885-892
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    • 2004
  • Due to the rapidly growing number of resistant strains of bacteria, the search for antibacterial agents with new modes of action will always remain an important and challenging task. Thus, the reaction of 2-substituted or. unsubstituted-4-(4-acetylanilino)-5,6,7,8-terahydrobenzo[b] thieno[2,3-d]pyrimidine derivatives 1-3 with the hydrazine derivatives, semi and / or thiosemi-carbazides, provided the corresponding hydrazones 4-6 and semi and/or thiosemicarbazones 7-9. Claisen-Schmidt condensation of compounds 1 or 2 with the appropriate aldehyde yielded the chalcones 10, 11 which, when treated with hydroxylamine hydrochloride gave rise to the isoxazoline-containing compounds 12, 13. Furthermore, reacting the respective chalcones 10, 11 with different hydrazines, urea and/or thiourea, furnished compounds 14, 15, 16, and 17 respectively. Representative compounds were tested for their antimicrobial activity against Candida Albicans and certain gram-positive and gram-negative bacteria. Their MICs were then determined. Compound 15e, showed a broad spectrum of activity while most of the other com-pounds showed varying antimicrobial activity.

Phenolic Compounds Isolated from Opuntia ficus-indica Fruits

  • Kim, Jung Wha;Kim, Tae Bum;Yang, Heejung;Sung, Sang Hyun
    • Natural Product Sciences
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    • v.22 no.2
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    • pp.117-121
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    • 2016
  • On the phytochemical investigation of a 70% ethanol extract of the fruits of Opuntia ficus-indica, (Cacataceae), we could result in the isolation of thirteen phenolic compounds including seven flavonoids (1 - 9) and four simple phenolic glycosides (10 - 13) by column chromatographic methods. Among the isolated compounds, picein (11), androsin (12), and $1-O-feruloyl-{\beta}-{\small{D}}-glucopyranoside$ (13) were isolated for the first time from O. ficus-indica; additionally, this is the first report $benzyl-O-{\beta}-{\small{D}}-glucopyranoside$ (10) from the genus Opuntia. The structures of the compounds were determined by spectral data analysis which included 1D, 2D NMR spectrum and ESIMS.

Anti-emetic Principles of Alpinia katsumadai Hayata

  • Yang, Ye;Kinoshita, Kaoru;Koyama, Kiyotaka;Takahashi, Kunio;Tai, Takaaki;Nunoura, Yoshiki;Watanabe, Kazuo
    • Natural Product Sciences
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    • v.5 no.1
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    • pp.20-24
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    • 1999
  • Bioassay-guided fractionation of anti-emetic constituents of Alpinia katsumadai Hayata was performed. Nine compounds including one novel compound, (3R,5S)-trans-3,5-dihydroxy-1,7-diphenyl-1-heptene (9) were isolated from it. Among these compounds, four diarylheptanoids, one sesquiterpenoid and one flavonoid showed anti-emetic activity on copper sulfate induced-emesis in young chicks.

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Synthesis and Antimicrobial Activity of Some New 1-Alkyl-2-alkylthio-1,2,4-triazolobenzimidazole Derivatives

  • Mohamed, Bahaa Gamal;Hussein, Mostafa Ahmed;Abdel-Alim, Abdel-Alim Mohamed;Hashem, Mohammed
    • Archives of Pharmacal Research
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    • v.29 no.1
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    • pp.26-33
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    • 2006
  • Some new derivatives of 1,2,4-triazolo[2,3-a]benzimidazoles were synthesized through the reaction of 1,2-diaminobenzimidazole with carbon disulfide. The resulting 1,2,4-triazolo-[2,3a]benzimidazole-2-thione intermediate was reacted with one equivalent of alkyl halides to give the corresponding 2-alkylthio derivatives, which were further alkylated through the reaction with another one equivalent of different alkyl halides to afford the target compounds; 1-alkyl-2alkylthio-1,2,4-traizolo[2,3-a]benzimidazoles. On the other hand, the 1,2-disubstituted derivatives with two identical alkyl substituents were prepared by the reaction of 1,2,4-triazolo[2,3-a]benzimidazole-2-thione with two equivalents of the alkyl halides. The structures of the new compounds were assigned by spectral and elemental methods of analyses. The synthesized compounds were tested for their antibacterial and antifungal activities. Most of the tested compounds proved comparable results with those of ampicillin and fluconazole reference drugs. The study indicated that, the antibacterial as well as the antifungal activities of the test compounds were improved with increase in the bulkiness of the introduced alkyl groups. Also, some active antibacterial compounds were tested for their antimycobacterial activity. All the test compounds showed equipotent antitubercular activity as that of INH as a reference drug.

Pharmaceutical Applications of Bismuth (III) Compounds (비스마스 화합물의 약제학적 응용)

  • Rhee, Gye-Ju
    • Journal of Pharmaceutical Investigation
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    • v.16 no.4
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    • pp.158-170
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    • 1986
  • This is the article on the uses, methods of elaboration, qualitative, and quantitative evaluations, of organic and inorganic bismuth trivalent compounds. The obvious accent appears to be on the therapeutic uses. However, their interest will relate to all, for the reader looking beyond that first impression will be treated to an amazingly rich compendium of historical applications that can only prompt new questions and open up unsuspected horizons in seemingly unrelated area.

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Bioactive Fabaceous Saponins and Structure-Activity Relationship

  • Kinjo, Junei;Nohara, Toshihiro
    • Proceedings of the PSK Conference
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    • 2002.10a
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    • pp.143-146
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    • 2002
  • Saponins are glycosidic compounds present in many edible and inedible plants. Structurally, they are composed of a lipid-soluble aglycone consisting of either a sterol or, more commonly, a triterpenoid and water-soluble sugar residues differing in type and amount of sugars [1]. Because of their amphiphilic nature, they are highly surface-active. Their biological activity is closely related to the chemical structures that determine the polarity, hydrophobicith and acidity of compounds [1]. (omitted)

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Asymmetric Synthesis in Pharmaceutical Manufacturing Chemistry

  • Jew, Sang-Sup
    • Proceedings of the PSK Conference
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    • 2003.10b
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    • pp.59-61
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    • 2003
  • Organic compounds play an important role in the area of pharmaceutical, agrochemical, and other materials, which possess useful biological activities. Generally, such biological activities are come from the interaction of the organic compounds with the receptors in biological system, such as enzymes. Such receptors are composed of the chiral building blocks such as amino acid or carbohydrate, which means the biological active sites of receptors are chiral. (omiited)

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Fluorescence of 2-(substituted anilino)benzoic acids and their metal chelate compounds

  • Lee, Kang-Choon;Lee, Yoon-Joong;Min, Shin-Hong
    • Archives of Pharmacal Research
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    • v.4 no.2
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    • pp.91-98
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    • 1981
  • The substituent effects on the fluorescence of 2-(substituted anilino)benzoic acids and their aluminum chelate compounds were examined and satisfactory linear relationships between Hammett substitute constants, .sigma. and the lowest excited singlet energy levels were obtained. But fluorescence intensity only made a qualitative relationship with .sigma. values of substituent groups. Effects of solvents and metal ions on the native and metal chelate fluorescence of the above derivatives were also investigated.

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