• 제목/요약/키워드: Medicinal chemistry

검색결과 669건 처리시간 0.041초

Phytochemical and Pharmacological Investigations on Moringa peregrina (Forssk) Fiori

  • Elbatran, Seham A.;Abdel-Salam, Omar M.;Abdelshfeek, Khaled A.;Nazif, Naglaa M.;Ismail, Shams I.;Hammouda, Faiza M.
    • Natural Product Sciences
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    • 제11권4호
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    • pp.199-206
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    • 2005
  • Investigation of M. peregrina aerial parts revealed the isolation and identification of 4-flavonoidal compounds, quercetin, quercetin-3-0-rutinoside (rutin), chrysoeriol-7-0-rhamnoside 6,8,3',5'-tetramethoxy apigenin. The compounds were identified by TLC, PC, MS, and $H^1-NMR$. The fatty acids and unsaponifiable matter were studied. The $LD_{50}$ for M. peregrina was 113.4 mg/100g b.wt. Repeated intraperitoneal injection of 1/20 and 1/10 $LD_{50}$ (5.67 mg and 11.34 mg/100g b.wt.) of defatted alcoholic of M. peregrina for 30 days induced significant decrease in serum glucose, liver enzymes and lipid components. M. peregrina administered i.p., 30min prior to carrageenan at the above doses significantly inhibited the rat paw oedema response, In acute pain models, namely, the acetic acid-induced writing and hot-plate assay, M. peregrina exhibited marked analgesic properties. In addition, M. peregrina administered at time of indomethacin injection inhibited the development of gastric lesions in rats.

Two New Diphenylethylenes from Arundina graminifolia and Their Cytotoxicity

  • Li, Yin-Ke;Zhou, Bin;Ye, Yan-Qing;Du, Gang;Niu, De-Yun;Meng, Chun-Yang;Gao, Xue-Mei;Hu, Qiu-Fen
    • Bulletin of the Korean Chemical Society
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    • 제34권11호
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    • pp.3257-3260
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    • 2013
  • Two new diphenylethylenes, gramniphenols H and I (1 and 2), together with six known diphenylethylenes (3-8), were isolated from Arundina graminifolia. The structures of 1-8 were elucidated by spectroscopic methods including extensive 1D- and 2D-NMR techniques. Compounds 1 and 2 were evaluated for their cytotoxicity against five human tumor cell lines. Compound 1 showed cytotoxicity against PC3 cells with $IC_{50}$ value of 3.5 ${\mu}M$. Compound 2 showed cytotoxicity against NB4 and PC3 cells with $IC_{50}$ values of 3.6 and 3.8 ${\mu}M$, respectively.

Synthesis and Antiviral Activity of Novel Exomethylene Cyclopropyl Pyrimidine Nucleosides

  • Kook, Min-Chul;Kim, Gu;Kwak, Eun-Yee;Hong, Joon-Hee;Lee, Chong-Kyo;Choi, Bo-Gil
    • Archives of Pharmacal Research
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    • 제25권6호
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    • pp.790-794
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    • 2002
  • A series of novel exomethylene cyclopropyl nucleosides have been synthesized starting from Feist's acid. Classical nucleophilic substitution conditions ($K_2CO_3$, 18-crown-6) of the tosylate 2 as well as Mitsunobu reaction (DEAD, $PPh_3$) of alcohol 1 with pyrimidine bases afforded a series of novel cyclopropyl nucleosides. Compound 4b displayed moderate anti-HBV activity without any cytotoxicity up to $100{\;}{\mu}M$.

Discovery and Synthesis of Novel N-Cyanopyrazolidine and N-Cyanohexahydropyridazine Derivatives as Cathepsin Inhibitors

  • Song, Jong- Hwan;Kim, Sun-Gi;No, Zae-Sung;Hyun, Young-Lan;Jeon, Dong-Ju;Kim, Ik-Yon
    • Bulletin of the Korean Chemical Society
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    • 제29권8호
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    • pp.1467-1471
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    • 2008
  • The design, synthesis, and biological evaluation of structurally novel N-cyanopyrazolidine and N-cyanohexahydropyridazine derivatives as cathepsin inhibitors are described. In vitro assay reveals that several compounds exhibit highly potent and selective profiles against cathepsins K or S.

Synthesis and Antibacterial Activity of 1β-Methyl-2-[5-(1,2-disubstituted ethyl)-pyrrolidin-3-ylthio]carbapenem Derivatives. Part III

  • Cho, Jung-Hyuck;Ahn, Soo-Hyun;Jeon, Hee-chol;Kim, So-Young;Oh, Chang-Hyun
    • Bulletin of the Korean Chemical Society
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    • 제27권5호
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    • pp.705-712
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    • 2006
  • The synthesis of a new series of 1 $\beta$-methylcarbapenems having 5-(1,2-disubstituted ethyl)pyrrolidine moiety are described. Their in vitro antibacterial activities against both Gram-positive and Gram-negative bacteria were tested and the effect of substituents on the pyrrolidine ring was investigated. Among them, compound (IIIc) having 1-methoxyimino-2-hydroxyethyl moiety showed the most potent antibacterial activity.

Deuteromethylactin B from a Freshwater-derived Streptomyces sp.

  • Shaikh, Anam F.;Elfeki, Maryam;Landolfa, Samantha;Tanouye, Urszula;Green, Stefan J.;Murphy, Brian T.
    • Natural Product Sciences
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    • 제21권4호
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    • pp.261-267
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    • 2015
  • Compared to their terrestrial and marine counterparts, little is known about the capacity of freshwater-derived actinomycete bacteria to produce novel secondary metabolites. In the current study, we highlight the disparities that exist between cultivation-independent and -dependent analyses of actinomycete communities from four locations in Lake Michigan sediment. Furthermore, through phylogenetic analysis of strains isolated from these locations, we identified a Streptomyces sp., strain B025, as being distinct from other Streptomyces spp. isolated from sediment. Upon fermentation this strain produced a rare class of eight-membered lactone secondary metabolites, which have been for their antitumor properties. We used spectroscopic and chemical derivitization techniques to characterize octalactin B (1) in addition to its corresponding novel, unnatural degradation product (2).

Synthesis of Certain Mercapto and Aminopyrimidine Derivatives as Potential Antimicrobial Agents

  • El-Kerdawy, M.M.;Eisa, H.M.;El-Emam, A.A.;Massoud, M.A.;Nasr, M.N.
    • Archives of Pharmacal Research
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    • 제13권2호
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    • pp.142-146
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    • 1990
  • Reaction of ethyl 4-chloro-2-phenylpyrimidine-4-carboxylate (4) with 5-chloro-2-methylthiophenol or 3-aryl-4-phenyl-1, 2, 4-triazole-5 thiol yielded the corresponding thioethers (5) and (8a, b), respectively. Careful alkaline hydrolysis of (5) yielded the corresponding carboxylic acid (6). Reaction of (4) with p-aminoacetophenone yielded compound (10) which was reacted with certain aromatic aldehyde to afford the$\alpha,\beta$-unsaturated ketones (11a-d). Condensation of (11a-d) with malononitrile or phenylhydrazine yielded the 2-amino-3-cyanopyridines (12a-f) or the 2-pyrazolines (13a, b) respectively. Seven representative compounds were tested for their in vitro antimicrobial activity against some pathogenic micro-organisms, some of them were proved to be active.

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Highly Enantioselective Addition of Diethylzinc to Aldehydes Catalyzed by Novel Chiral tert-Amino Alcohols

  • Zhang, Cong-Hai;Yan, Sheng-Jiao;Pan, Sheng-Qiang;Huang, Rong;Lin, Jun
    • Bulletin of the Korean Chemical Society
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    • 제31권4호
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    • pp.869-873
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    • 2010
  • A series of novel chiral tert-amino alcohols 4a-h derived from enantiomerically pure phenylalanine were synthesized efficiently and used as chiral ligands in the catalytic enantioselective ethylation of aldehydes with diethylzinc (diethylzinc-to-aldehyde addition). The use of 10 mol % of the amino alcohols led to the corresponding sec-alcohols with excellent enantioselectivities (up to 100% ee) and high yields.