共查询到20条相似文献,搜索用时 31 毫秒
1.
Beaulieu C Wang Z Denis D Greig G Lamontagne S O'Neill G Slipetz D Wang J 《Bioorganic & medicinal chemistry letters》2004,14(12):3195-3199
A series of 2-substituted N-benzyl benzimidazole containing molecules has been synthesized and its structure-activity relationship for the human DP receptor has been evaluated. Selective DP antagonists with nanomolar potency for the DP receptor were identified in this novel series of benzimidazoles. 相似文献
2.
Karen Aknin Alexis Bontemps Amaury Farce Eric Merlet Philippe Belmont Philippe Helissey Philippe Chavatte Marie-Agns Sari Sylviane Giorgi-Renault Stphanie Desbne-Finck 《Journal of enzyme inhibition and medicinal chemistry》2022,37(1):252
New polycyclic heterocycles were synthesised and evaluated as potential inhibitors of thymidine phosphorylase (TP). Inspired by the pharmacophoric pyrimidinedione core of the natural substrate, four series have been designed in order to interact with large empty pockets of the active site: pyrimidoquinoline-2,4-diones (series A), pyrimidinedione linked to a pyrroloquinoline-1,3-diones (series B and C), the polycyclic heterocycle has been replaced by a pyrimidopyridopyrrolidinetetraone (series D). In each series, the tricyclic nitrogen heterocyclic moiety has been synthesised by a one-pot multicomponent reaction. Compared to 7-DX used as control, 2d, 2l, 2p (series A), 28a (series D), and the open intermediate 30 showed modest to good activities. A kinetic study confirmed that the most active compounds 2d, 2p are competitive inhibitors. Molecular docking analysis confirmed the interaction of these new compounds at the active binding site of TP and highlighted a plausible specific interaction in a pocket that had not yet been explored. 相似文献
3.
Zhu B Marinelli BA Abbanat D Foleno BD Bush K Macielag MJ 《Bioorganic & medicinal chemistry letters》2007,17(14):3900-3904
A series of 3-keto-6-O-carbamoyl-11,12-cyclic thiocarbamate erythromycin A derivatives has been synthesized. The best compounds in this series possess potent in vitro antibacterial activity against erythromycin-susceptible and erythromycin-resistant bacteria. 相似文献
4.
Dai Y Guo Y Guo J Pease LJ Li J Marcotte PA Glaser KB Tapang P Albert DH Richardson PL Davidsen SK Michaelides MR 《Bioorganic & medicinal chemistry letters》2003,13(11):1897-1901
A series of hydroxamic acid-based HDAC inhibitors with an indole amide residue at the terminus have been synthesized and evaluated. Compounds with a 2-indole amide moiety have been found as the most active inhibitors among the different regioisomers. Introduction of substituents on the indole ring further improved the potency and generated a series of very potent inhibitors with significant antiproliferative activity. A representative compound in the series, 7b, has been found to be orally active in tumor growth inhibition model. 相似文献
5.
W H Miller W E Bondinell R D Cousins K F Erhard D R Jakas R M Keenan T W Ku K A Newlander S T Ross R C Haltiwanger J Bradbeer F H Drake M Gowen S J Hoffman S M Hwang I E James M W Lark B Lechowska D J Rieman G B Stroup J A Vasko-Moser D L Zembryki L M Azzarano P C Adams W F Huffman 《Bioorganic & medicinal chemistry letters》1999,9(13):1807-1812
A new series of potent nonpeptide vitronectin receptor antagonists, based on a novel carbocyclic Gly-Asp mimetic, has been discovered. A representative of this series, SB 265123 (4), has 100% oral bioavailability in rats, and is orally active in vivo in the ovariectomized rat model of osteoporosis. 相似文献
6.
Fractal dimension of birds population sizes time series 总被引:1,自引:0,他引:1
Information about fractal dimension is collected so that it can be applied to time series interpreting Hurst coefficient. The population size of a species is modelled as a dynamic system. The Hurst coefficient is calculated for these times series. A computer programme has been elaborated to compute the Hurst exponent of time series using the algorithms of range increment, second order moment increment and local second order moment increment. It has been applied to time series of birds' populations. 相似文献
7.
Synthesis and antibacterial activity of 3-O-acyl-6-O-carbamoyl erythromycin A derivatives 总被引:1,自引:0,他引:1
Zhu B Marinelli BA Abbanat D Foleno BD Henninger TC Bush K Macielag MJ 《Bioorganic & medicinal chemistry letters》2006,16(4):1054-1059
A series of 3-O-acyl-6-O-carbamoyl erythromycin A derivatives has been synthesized. Several functional groups were identified as the optimal C3-substituents, and the best compounds in this series possess potent in vitro antibacterial activity against erythromycin-susceptible and erythromycin-resistant bacteria. 相似文献
8.
《Bioorganic & medicinal chemistry》2014,22(22):6459-6470
A novel series of 8-amino imidazo[1,2-a]pyrazine derivatives has been developed as inhibitors of the VirB11 ATPase HP0525, a key component of the bacterial type IV secretion system. A flexible synthetic route to both 2- and 3-aryl substituted regioisomers has been developed. The resulting series of imidazo[1,2-a]pyrazines has been used to probe the structure–activity relationships of these inhibitors, which show potential as antibacterial agents. 相似文献
9.
Fink BE Vite GD Mastalerz H Kadow JF Kim SH Leavitt KJ Du K Crews D Mitt T Wong TW Hunt JT Vyas DM Tokarski JS 《Bioorganic & medicinal chemistry letters》2005,15(21):4774-4779
A novel series of dual EGFR and HER2 inhibitors based on the pyrrolo[2,1-f][1,2,4]triazine nucleus is described. A general route toward their synthesis, which enables functionalization at multiple sites, has been developed. Biological evaluation in enzymatic and cell-based assays has identified a series of C-6 carbamates with potent biochemical and cellular activities. 相似文献
10.
A series of inhibitors of the enzyme trypanothione reductase has been identified using directed solid-phase chemistry. The compounds were based on a series of polyamine scaffolds and used the natural product kukoamine A as the lead structure. A compound with a Ki of 76 nM was identified, although somewhat surprisingly the compound appeared to be noncompetitive in nature. 相似文献
11.
Synthesis and antibacterial activity of novel 6-O-substituted erythromycin A derivatives 总被引:1,自引:0,他引:1
Clark RF Ma Z Wang S Griesgraber G Tufano M Yong H Li L Zhang X Nilius AM Chu DT Or YS 《Bioorganic & medicinal chemistry letters》2000,10(8):815-819
A series of novel 6-O-substituted erythromycin A derivatives has been synthesized. Good in vitro antibacterial activity has been demonstrated for analogues incorporating a variety of structural features. The methodology disclosed is expected to find application in the design of future macrolide antibiotics that target the prevalent bacterial resistance problem. 相似文献
12.
A quantitative structure-activity relationship (QSAR) study has been made on eight different series of Clostridium histolyticum collegenase (ChC) inhibitors. These series are comprised of four different groups of sulfonylated amino acids and their corresponding hydroxamates. In each series, the inhibition potency of the compounds has been found to be significantly correlated with the electrotopological state (E-state) indices of nitrogen and sulfur atoms of the sulfonylated amino group in the molecules, showing the importance of the electronic characterstics of these atoms in controlling the inhibition potency of the compounds. 相似文献
13.
Maosheng Duan Christopher Aquino George F. Dorsey Robert Ferris Wieslaw M. Kazmierski 《Bioorganic & medicinal chemistry letters》2009,19(17):4988-4992
A series of 4,4-disubstituted cyclohexylamine based CCR5 antagonists has been designed and synthesized. Their antiviral structure–activity relationship has been extensively explored. 相似文献
14.
Timothy J. Leeney Peter R. Marsham Graham A.F. Ritchie Michael W. Senior 《Prostaglandins & other lipid mediators》1976,11(6):953-960
A series of bicycloheptene prostaglandin analogues has been prepared as potential inhibitors of prostaglandin biosynthesis. Their inhibitory effect has been examined using a ram seminal vesicle preparation. 相似文献
15.
A series of cycloSal-BVDUMP phosphate triesters has been prepared. The prototype compound was 3-methyl-cycloSal-BVDUMP 2. Furthermore, a series of 3'-O-acyl-modified derivatives having carboxylic acids with different lipophilicity or a L-configurated alpha-amino acid (phenylalanine) was prepared. The hydrolysis properties in phosphate buffer PBS as well as in PBS containing pig liver esterase (PLE) will be described. Finally, the biological activity against EBV has been determined. 相似文献
16.
Michael B. Wallace Mark E. Adams Toufike Kanouni Clifford D. Mol Douglas R. Dougan Victoria A. Feher Shawn M. O’Connell Lihong Shi Petro Halkowycz Qing Dong 《Bioorganic & medicinal chemistry letters》2010,20(14):4156-4158
A novel series of pyrrole inhibitors of MEK kinase has been developed using structure-based drug design. Optimization of the series led to the identification of potent inhibitors with good pharmaceutical properties. 相似文献
17.
Miller ML Roller EE Wu X Leece BA Goldmacher VS Chari RV Ojima I 《Bioorganic & medicinal chemistry letters》2004,14(15):4079-4082
The targeted delivery of taxoids, in the form of taxane-antibody immunoconjugates, requires the preparation of taxoids containing moieties suitable for their conjugation to monoclonal antibodies. A series of taxoids incorporating a disulfide-containing linker at various positions of the taxoid framework have been prepared to investigate the most suitable position for conjugation. A second series of taxoids modified at the C-2 position aimed at increasing the potency of these taxanes has also been prepared. 相似文献
18.
Marialessandra Contino Laura Zinzi Mariangela Cantore Maria Grazia Perrone Marcello Leopoldo Francesco Berardi Roberto Perrone Nicola Antonio Colabufo 《Bioorganic & medicinal chemistry letters》2013,23(13):3728-3731
A series of alkyloxyquinoline derivatives has been developed to evaluate the relationship between P-gp potency and lipophilicity. The results show a satisfactory lipophilicity-activity correlation although a series of derivatives showing higher P-gp potency is needed in order to confirm this hypothesis. 相似文献
19.
Liddle J Allen MJ Borthwick AD Brooks DP Davies DE Edwards RM Exall AM Hamlett C Irving WR Mason AM McCafferty GP Nerozzi F Peace S Philp J Pollard D Pullen MA Shabbir SS Sollis SL Westfall TD Woollard PM Wu C Hickey DM 《Bioorganic & medicinal chemistry letters》2008,18(1):90-94
Optimisation of a series of oxazole diketopiperazines has led to the discovery of a very potent and selective oxytocin antagonist GSK221149A. GSK221149A has been shown to inhibit oxytocin-induced uterine contractions in the anaesthetised rat. 相似文献
20.
Malikova R. N. Sakhautdinov I. M. Maksimova M. A. Kuzmina U. Sh. Vakhitova Yu. V. Yunusov M. S. 《Russian Journal of Bioorganic Chemistry》2020,46(1):115-119
Russian Journal of Bioorganic Chemistry - A series of new functionalized allenoates has been synthesized, and their cytotoxic effect has been studied against the tumor cell line (HepG2 and Jurkat)... 相似文献