Synthesis and Antileukemic Activity of N-Phthaloyl-2-Aminoalcohols

Pharmaceutical Chemistry Journal -     

Preparation,Gram-Negative Antibacterial Activity,and Hydrolytic Stability of Novel Siderophore-Conjugated Monocarbam Diols

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抗瘤酮A10类似物的合成及抗肿瘤活性

合成了抗瘤酮Ａ１０类似物。通过元素分析和核磁对这８个席夫碱化合物进行了结构表征。并得到了化合物７ａ的单晶结构。抗肿瘤试验显示这些化合物在 １０~（－４） ｍｏｌ·Ｌ~（－１）浓度下对Ｐ３８８和Ａ－５４９有较好的抑制作用。     

Synthesis and Analgesic Activity of 3,3-Dialkyl-Substituted Drotaverine Analogs

Pharmaceutical Chemistry Journal - Ritter reactions of 3,4-(R1)2-benzylcyanides with 1,1-(R2)2-2-[3,4-(R3)2-phenyl]ethanols synthesized...     

Synthesis and Anti-Inflammatory Activity of Tyrosol and Its Structural Analogs

Pharmaceutical Chemistry Journal - The anti-inflammatory activity of tyrosol and 12 structural analogs including 3 new compounds was determined. Several structure-activity (anti-inflammatory)...     

Acute Cardiotoxicity of Nucleoside Analogs FddA and Fddl in Rats

The acute cardiotoxic potential of single dosages of FddA (2'-fluoro-2',3'-dideoxyadenosine)and FddI (2'-fluoro-2',3'-di-deoxyinosine) was investigatedin 6- to 9-week-old rats. Both nucleoside analogs were administeredorally at 1000 and 2000 mg/kg and intravenously at 500 or 1000mg/kg. For comparative purposes, additional groups of rats received2'-deoxyadeno-sine or the 2-fluororibose moiety common to boththe FddA and Fddl molecules. The effects of two adenosine receptorantagonists, caffeine and theophylline, on the cardiotoxicityinduced by FddA were also investigated. Deaths occurred withina few hours to a few days in FddA-treated rats given 2000 mg/kgorally or 500 mg/kg intravenously and in Fddl-treated rats given1000 mg/kg intravenously. Microscopic examination of the heartsrevealed myocardial degeneration and necrosis for all rats thatdied and myocardial fibrosis for many survivors. No deaths orcardiac lesions were observed after administration of 2'-deoxyadenosineor the 2-fluororibose moiety. FddA was more cardiotoxic thanFddl in rats at equivalent dosages administered either orallyor intravenously. Based on the anatomic findings, all deathswere attributed to cardiac lesions. The administration of high,oral dosages of caffeine and theophylline accentuated the acutecardiotoxicity of FddA in rats.     

Design,Synthesis, and Antileukemic Activity of Stereochemically Defined Constrained Analogues of FTY720 (Gilenya)

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核苷类抗病毒药物研究进展

近年来新的抗病毒药物不断出现,但病毒性感染的发病率仍持续不衰,特别是80年代初艾滋病及其原病毒的出现,对抗病毒药物的研究开发提出了紧迫的要求.由于人类免疫缺陷病毒( HIV)感染病人往往对其他病毒感染很敏感,如单纯疱疹病毒(HSV)、巨细胞病毒(CMV)、水痘带状疱疹病毒(VZV)等等.因此,治疗HIV感染的同时也要给予抗这些病毒的药物,这样就进一步推动了抗病毒药物的发展.     

Cyclic Analogs of Chemotactic Formylpeptides,I.: Synthesis and Biological Activity of For-Cys-Leu-Phe-Cys-OMe

By using the side chain to side chain mode of cyclization the 14-membered disulfide cyclopeptide ( 5 ) has been synthesized as conformationally constrained analog of the prototypical chemotactic tripeptide For-Met-Leu-Phe-OMe. Compound 5 is inactive towards human neutrophils. The lack of biological activity of cyclotetrapeptide 5 is discussed taking into account the backbone folding and the side chain topography.     

Synthesis,Antibacterial and Antitumor Activity of Semisynthetic Penicillins and Cephalosporins Based on New Sarcomycin Analogs

A series of new semisynthetic penicillins and cephalosporins containing structural fragments of the well-known antitumor antibiotic sarcomycin have been synthesized and their antitumor and antibacterial properties have been studied. The synthesized compounds showed substantial antitumor and antibacterial activities.__________Translated from Khimiko-Farmatsevticheskii Zhurnal, Vol. 39, No. 2, pp. 13 – 15, February, 2005.     

Synthesis,Antiproliferative Activity,and Effect on Carcinoma A549 Cell Microtubules of New Tubuloclustin Analogs

Pharmaceutical Chemistry Journal - Combretastatin analogs of the antitumor agent tubuloclustin {N-[7-(adamant-2-yloxy)-7-oxoheptanoyl]-Ndeacetylcolchicine} were prepared via esterification of...     

Design,Synthesis and Antifungal Activity of a Series of Novel Analogs Based on Diphenyl Ketones

To find potent fungicides, 35 analogs of diphenyl ketones were synthesized and evaluated for their antifungal activity. These compounds possessed a furyl–carbonyl–phenyl skeleton. Bioassay results showed that the synthesized compounds were effective in promoting the antifungal activity of diphenyl ketones. Compound 3 showed the best activity against the four tested fungi (100%, 100%, 100% and 96.4%) and could be used as potent fungicide for further research.     

Synthesis,Properties, and Applications of Diazotrifluropropanoyl-Containing Photoactive Analogs of Farnesyl Diphosphate Containing Modified Linkages for Enhanced Stability

Photoactive analogs of farnesyl diphosphate (FPP) are useful probes in studies of enzymes that employ this molecule as a substrate. Here, we describe the preparation and properties of two new FPP analogs that contain diazotrifluoropropanoyl photophores linked to geranyl diphosphate via amide or ester linkages. The amide-linked analog ( 3 ) was synthesized in ³²P-labeled form from geraniol in seven steps. Experiments with Saccharomyces cerevisiae protein farnesyltransferase (ScPFTase) showed that 3 is an alternative substrate for the enzyme. Photolysis experiments with [³²P]3 demonstrate that this compound labels the β-subunits of both farnesyltransferase and geranylgeranyltransferase (types 1 and 2). However, the amide-linked probe 3 undergoes a rearrangement to a photochemically unreactive isomeric triazolone upon long term storage making it inconvenient to use. To address this stability issue, the ester-linked analog 4 was prepared in six steps from geraniol. Computational analysis and X-ray crystallographic studies suggest that 4 binds to protein farnesyl transferase (PFTase) in a similar fashion as FPP. Compound 4 is also an alternative substrate for PFTase, and a ³²P-labeled form selectively photocrosslinks the β-subunit of ScPFTase as well as E. coli farnesyldiphosphate synthase and a germacrene-producing sesquiterpene synthase from Nostoc sp. strain PCC7120 (a cyanobacterial source). Finally, nearly exclusive labeling of ScPFTase in crude E. coli extract was observed, suggesting that [³²P]4 manifests significant selectivity and should hence be useful for identifying novel FPP-utilizing enzymes in crude protein preparations.     

Hydrolytic Stability of Alkyl 1H-Benzotriazolecarboxylates

Hydrolysis of 1H-benzotriazolecarboxylates was studied in 0.1 M NaOH, phosphate buffer pH 7.4 and using a microsomal esterase preparation. Results obtained for the alkaline hydrolysis qualitatively resembled those of enzymatic hydrolysis. In phosphate buffer pH 7.4 the esters were sufficiently stable concerning their use as potential substrates for in vitro biotransformation studies.