Lp-PLA2 inhibitory activities of fatty acid glycerols isolated from Saururus chinensis roots.

Abstract:

:(R)-Glycerol-monolinoleate 4 and (R)-glycerol-monostearate 5 were isolated from the ethyl acetate extracts of Saururus chinensis roots and (R)- or (S)-fatty acid glycerols 4 and 5 were synthesized for confirming their structures and evaluating their inhibitory activities against Lp-PLA(2). The (R)-4 and (S)-4 exhibited Lp-PLA(2) inhibitory activities with IC(50) values of 45.0 and 52.0 microM, respectively.

journal_name

Bioorg Med Chem Lett

authors

Lee WS,Kim MJ,Beck YI,Park YD,Jeong TS

doi

10.1016/j.bmcl.2005.05.056

subject

Has Abstract

pub_date

2005-08-01 00:00:00

pages

3573-5

issue

15

eissn

0960-894X

issn

1464-3405

pii

S0960-894X(05)00666-9

journal_volume

15

pub_type

杂志文章
  • Discovery and optimization of novel constrained pyrrolopyridone BET family inhibitors.

    abstract::Novel conformationally constrained BET bromodomain inhibitors have been developed. These inhibitors were optimized in two similar, yet distinct chemical series, the 6-methyl-1H-pyrrolo[2,3-c]pyridin-7(6H)-ones (A) and the 1-methyl-1H-pyrrolo[2,3-c]pyridin-7(6H)-ones (B). Each series demonstrated excellent activity in ...

    journal_title:Bioorganic & medicinal chemistry letters

    pub_type: 杂志文章

    doi:10.1016/j.bmcl.2018.04.020

    authors: Fidanze SD,Liu D,Mantei RA,Hasvold LA,Pratt JK,Sheppard GS,Wang L,Holms JH,Dai Y,Aguirre A,Bogdan A,Dietrich JD,Marjanovic J,Park CH,Hutchins CW,Lin X,Bui MH,Huang X,Wilcox D,Li L,Wang R,Kovar P,Magoc TJ,Raj

    更新日期:2018-06-01 00:00:00

  • Topological estimation of electronic absorption bands of arene absorption spectra as a tool for modeling their toxicity and environmental pollution.

    abstract::A novel application of distance-based topological indices : Wiener (W)-, Szeged (Sz)-, Padmakar-Ivan (PI)-, and Sadhana (Sd)-indices in modeling electronic absorption bands of arene absorption spectra has been described. It is demonstrated that all these indices correlate linearly with the logarithm of beta and para e...

    journal_title:Bioorganic & medicinal chemistry letters

    pub_type: 杂志文章

    doi:10.1016/j.bmcl.2004.06.094

    authors: Khadikar PV,Singh S,Jaiswal M,Mandloi D

    更新日期:2004-09-20 00:00:00

  • Bioactive new withanolides from the cultured soft coral Sinularia brassica.

    abstract::Continuing study of the ethyl acetate (EtOAc) extract of the cultured soft coral Sinularia brassica afforded five new withanolides, sinubrasolides H-L (1-5). The structures of the new compounds were elucidated on the basis of spectroscopic analysis. The cytotoxicities of new compounds 1-5 and a known compound sinubras...

    journal_title:Bioorganic & medicinal chemistry letters

    pub_type: 杂志文章

    doi:10.1016/j.bmcl.2017.06.029

    authors: Huang CY,Ahmed AF,Su JH,Sung PJ,Hwang TL,Chiang PL,Dai CF,Liaw CC,Sheu JH

    更新日期:2017-08-01 00:00:00

  • Phosphonic acid-containing analogues of mycophenolic acid as inhibitors of IMPDH.

    abstract::The design, synthesis, and IMPDH inhibitory activity of a series of phosphonic acid-containing analogues of mycophenolic acid are described. ...

    journal_title:Bioorganic & medicinal chemistry letters

    pub_type: 杂志文章

    doi:10.1016/j.bmcl.2006.03.097

    authors: Watkins WJ,Chen JM,Cho A,Chong L,Collins N,Fardis M,Huang W,Hung M,Kirschberg T,Lee WA,Liu X,Thomas W,Xu J,Zeynalzadegan A,Zhang J

    更新日期:2006-07-01 00:00:00

  • Synthesis and pharmacological evaluation of piperidine (piperazine)-substituted benzoxazole derivatives as multi-target antipsychotics.

    abstract::The present study describes the optimization of a series of novel benzoxazole-piperidine (piperazine) derivatives combining high dopamine D2 and serotonin 5-HT1A, 5-HT2A receptor affinities. Of these derivatives, the pharmacological features of compound 29 exhibited high affinities for the DA D2, 5-HT1A and 5-HT2A rec...

    journal_title:Bioorganic & medicinal chemistry letters

    pub_type: 杂志文章

    doi:10.1016/j.bmcl.2015.09.045

    authors: Huang L,Zhang W,Zhang X,Yin L,Chen B,Song J

    更新日期:2015-11-15 00:00:00

  • Design and synthesis of imidazole and triazole derivatives as Lp-PLA₂ inhibitors and the unexpected discovery of highly potent quaternary ammonium salts.

    abstract::New Lp-PLA(2) inhibitors were synthesized by the bioisosteric replacement of the amide group of Darapladib with an imidazole or a triazole. Unfortunately, the inhibitory activities of these derivatives were lower than that of Darapladib. But interestingly, a series of quaternary ammonium salts that were isolated as by...

    journal_title:Bioorganic & medicinal chemistry letters

    pub_type: 杂志文章

    doi:10.1016/j.bmcl.2013.01.029

    authors: Wang K,Xu W,Liu Y,Zhang W,Wang W,Shen J,Wang Y

    更新日期:2013-03-01 00:00:00

  • Discovery and optimization of 2-aminopyridine derivatives as novel and selective JAK2 inhibitors.

    abstract::Janus kinases (JAKs) including JAK1, JAK2, JAK3, and TYK2 are members of a family of intracellular nonreceptor tyrosine kinases, which have been demonstrated to be critical in the cell signaling pathway and involved in inflammatory diseases and cancer. V617F mutation in JAK2 has been implicated in polycythaemia vera (...

    journal_title:Bioorganic & medicinal chemistry letters

    pub_type: 杂志文章

    doi:10.1016/j.bmcl.2020.127048

    authors: Ma X,Diao Y,Ge H,Xu F,Zhu L,Zhao Z,Li H

    更新日期:2020-04-15 00:00:00

  • Syntheses of sphingosine-1-phosphate analogues and their interaction with EDG/S1P receptors.

    abstract::Sphingosine-1-phosphate (S1P) is an important regulator of a wide variety of biological processes acting as an endogenous ligand to EDG/S1P receptors. In an effort to establish structure-activity relationship between EDG/S1P and ligands, we report herein homology modeling study of EDG-1/S1P(1), syntheses of S1P analog...

    journal_title:Bioorganic & medicinal chemistry letters

    pub_type: 杂志文章

    doi:10.1016/j.bmcl.2004.03.001

    authors: Lim HS,Park JJ,Ko K,Lee MH,Chung SK

    更新日期:2004-05-17 00:00:00

  • Selective inactivation of triosephosphate isomerase from Trypanosoma cruzi by brevifolin carboxylate derivatives isolated from Geranium bellum Rose.

    abstract::In the search of molecules that can serve as leads in the design of a new drug for the treatment of Chagas' disease, we found that some brevifolin carboxylate derivatives isolated from Geranium bellum Rose, inactivate triosephosphate isomerase from Trypanosoma cruzi (TcTIM) in a species-specific manner. After spectros...

    journal_title:Bioorganic & medicinal chemistry letters

    pub_type: 杂志文章

    doi:10.1016/j.bmcl.2009.08.055

    authors: Gayosso-De-Lucio J,Torres-Valencia M,Rojo-Domínguez A,Nájera-Peña H,Aguirre-López B,Salas-Pacheco J,Avitia-Domínguez C,Téllez-Valencia A

    更新日期:2009-10-15 00:00:00

  • Camptothecin analogs with bulky, hydrophobic substituents at the 7-position via a Grignard reaction.

    abstract::By developing a new synthetic procedure for introduction of side chains onto the camptothecin ring system, we were able to achieve the preparation of a number of analogs bearing bulky, hydrophobic groups directly attached to the 7-position. These include 7-tert-butylcamptothecin, 7-benzylcamptothecin and the correspon...

    journal_title:Bioorganic & medicinal chemistry letters

    pub_type: 杂志文章

    doi:10.1016/j.bmcl.2004.08.010

    authors: Manikumar G,Wadkins RM,Bearss D,Von Hoff DD,Wani MC,Wall ME

    更新日期:2004-11-01 00:00:00

  • Novel antifungals based on 4-substituted imidazole: solid-phase synthesis of substituted aryl sulfonamides towards optimization of in vitro activity.

    abstract::The in vitro activity of novel 4-substituted imidazole antifungals was optimized by solid-phase chemistry and parallel synthesis. Potent yeast-selective as well as broad-spectrum antifungal compounds (32 and 20) were discovered. ...

    journal_title:Bioorganic & medicinal chemistry letters

    pub_type: 杂志文章

    doi:10.1016/s0960-894x(00)00551-5

    authors: Saha AK,Liu L,Marichal P,Odds F

    更新日期:2000-12-18 00:00:00

  • Nonbenzamidine acylsulfonamide tissue factor-factor VIIa inhibitors.

    abstract::Aminoisoquinoline and isoquinoline groups have successfully replaced the more basic P1 benzamidine group of an acylsulfonamide factor VIIa inhibitor. Inhibitory activity was optimized by the identification of additional hydrophobic and hydrophilic P' binding interactions. The molecular details of these interactions we...

    journal_title:Bioorganic & medicinal chemistry letters

    pub_type: 杂志文章

    doi:10.1016/j.bmcl.2013.06.027

    authors: Glunz PW,Zhang X,Zou Y,Delucca I,Nirschl AH,Cheng X,Weigelt CA,Cheney DL,Wei A,Anumula R,Luettgen JM,Rendina AR,Harpel M,Luo G,Knabb R,Wong PC,Wexler RR,Priestley ES

    更新日期:2013-09-15 00:00:00

  • Synthesis and biological evaluation of pyrrolo[2,1-c][1,4]benzodiazepine (PBD) C8 cyclic amine conjugates.

    abstract::We report examples of a series of novel pyrrolo[2,1-c][1,4]benzodiazepine (PBD) analogues 12-15 prepared from a common functionalized building block 11 that can be conveniently synthesized on a large scale and in optically pure form. Isoindoline analogue 15 is the most cytotoxic agent in this series, has the highest D...

    journal_title:Bioorganic & medicinal chemistry letters

    pub_type: 杂志文章

    doi:10.1016/j.bmcl.2003.12.017

    authors: Masterson LA,Croker SJ,Jenkins TC,Howard PW,Thurston DE

    更新日期:2004-02-23 00:00:00

  • Structure based evolution of a novel series of positive modulators of the AMPA receptor.

    abstract::Starting from compound 1, we utilized biostructural data to successfully evolve an existing series into a new chemotype with a promising overall profile, exemplified by 19. ...

    journal_title:Bioorganic & medicinal chemistry letters

    pub_type: 杂志文章

    doi:10.1016/j.bmcl.2010.11.098

    authors: Jamieson C,Maclean JK,Brown CI,Campbell RA,Gillen KJ,Gillespie J,Kazemier B,Kiczun M,Lamont Y,Lyons AJ,Moir EM,Morrow JA,Pantling J,Rankovic Z,Smith L

    更新日期:2011-01-15 00:00:00

  • Synthesis and evaluation of furoxan-based nitric oxide-releasing derivatives of tetrahydroisoquinoline as anticancer and multidrug resistance reversal agents.

    abstract::Multidrug resistance in tumor cells poses a major obstacle to efficient chemotherapy. Several types of agents have been recognized as multidrug resistance inhibitors, among which the tetrahydroisoquinolines is the most studied. In current study 16 furoxan-based nitric oxide-releasing derivatives of tetrahydroisoquinol...

    journal_title:Bioorganic & medicinal chemistry letters

    pub_type: 杂志文章

    doi:10.1016/j.bmcl.2011.07.077

    authors: Zou ZH,Lan XB,Qian H,Huang WL,Li YM

    更新日期:2011-10-01 00:00:00

  • Phosphinic acid-based inhibitors of tubulin polyglutamylases.

    abstract::Tubulin is subject to a reversible post-translational modification involving polyglutamylation and deglutamylation of glutamate residues in its C-terminal tail. This process plays key roles in regulating the function of microtubule associated proteins, neuronal development, and metastatic progression. This study descr...

    journal_title:Bioorganic & medicinal chemistry letters

    pub_type: 杂志文章

    doi:10.1016/j.bmcl.2013.05.069

    authors: Liu Y,Garnham CP,Roll-Mecak A,Tanner ME

    更新日期:2013-08-01 00:00:00

  • Synthesis and biological evaluation of substituted 4-(thiophen-2-ylmethyl)-2H-phthalazin-1-ones as potent PARP-1 inhibitors.

    abstract::We have developed a series of substituted 4-(thiophen-2-ylmethyl)-2H-phthalazin-1-ones as potent PARP-1 inhibitors. Preliminary biological evaluation indicated that most compounds possessed inhibitory potencies comparable to, or higher than AZD-2281. Among these compounds, 18q appeared to be the most notable one, whic...

    journal_title:Bioorganic & medicinal chemistry letters

    pub_type: 杂志文章

    doi:10.1016/j.bmcl.2014.07.001

    authors: Wang LX,Zhou XB,Xiao ML,Jiang N,Liu F,Zhou WX,Wang XK,Zheng ZB,Li S

    更新日期:2014-08-15 00:00:00

  • Design and synthesis of 4-morpholino-6-(1,2,3,6-tetrahydropyridin-4-yl)-N-(3,4,5-trimethoxyphenyl)-1,3,5-triazin-2-amine analogues as tubulin polymerization inhibitors.

    abstract::A series of thirty-seven 1,3,5-triazine analogues have been synthesized, characterized and evaluated for their antiproliferative activity against a panel of four different human cancer cell lines such as HeLa, HepG2, A549 and MCF-7. Most of the 1,3,5-triazine analogues exhibited promising antiproliferative activity ag...

    journal_title:Bioorganic & medicinal chemistry letters

    pub_type: 杂志文章

    doi:10.1016/j.bmcl.2017.06.060

    authors: Narva S,Chitti S,Amaroju S,Bhattacharjee D,Rao BB,Jain N,Alvala M,Sekhar KVGC

    更新日期:2017-08-15 00:00:00

  • Design, synthesis and antitumor activity of non-camptothecin topoisomerase I inhibitors.

    abstract::Three groups of non-camptothecin compounds with four to five fused rings have been designed and synthesized. Their in vitro anti-proliferative activity has been evaluated with five different cancer cell lines (HCT116, PC3, U87MG, HepG2, SK-OV-3). Compounds B-2 and B-3 showed the most potent cell growth inhibition with...

    journal_title:Bioorganic & medicinal chemistry letters

    pub_type: 杂志文章

    doi:10.1016/j.bmcl.2015.06.042

    authors: Zhang C,Li S,Ji L,Liu S,Li Z,Li S,Meng X

    更新日期:2015-10-15 00:00:00

  • Selectivity profiling of novel indene H(1)-antihistamines for the treatment of insomnia.

    abstract::A series of indene analogs of the H(1)-antihistamine (-)-R-dimethindene was evaluated for selectivity in the search for potentially improved sedative-hypnotics. Variation of the 6-substitutent in the indene core in combination with a pendant electron rich heterocycle led to the identification of several potent H(1)-an...

    journal_title:Bioorganic & medicinal chemistry letters

    pub_type: 杂志文章

    doi:10.1016/j.bmcl.2010.02.055

    authors: Li BF,Moree WJ,Yu J,Coon T,Zamani-Kord S,Malany S,Jalali K,Wen J,Wang H,Yang C,Hoare SR,Petroski RE,Madan A,Crowe PD,Beaton G

    更新日期:2010-04-15 00:00:00

  • Monocyclic thiophenes as protein tyrosine phosphatase 1B inhibitors: capturing interactions with Asp48.

    abstract::A series of monocyclic thiophenes was designed and synthesized as PTP1B inhibitors. Guided by X-ray co-crystal structural information and computational modeling, rational design led to key interactions with Asp48 and improved inhibitory potency against PTP1B. ...

    journal_title:Bioorganic & medicinal chemistry letters

    pub_type: 杂志文章

    doi:10.1016/j.bmcl.2006.06.051

    authors: Wan ZK,Lee J,Xu W,Erbe DV,Joseph-McCarthy D,Follows BC,Zhang YL

    更新日期:2006-09-15 00:00:00

  • Synthesis of VS-105: A novel and potent vitamin D receptor agonist with reduced hypercalcemic effects.

    abstract::We have synthesized a novel vitamin D receptor agonist VS-105 ((1R,3R)-5-((E)-2-((3αS,7αS)-1-((R)-1-((S)-3-hydroxy-2,3-dimethylbutoxy)ethyl)-7α-methyldihydro-1H-inden-4(2H,5H,6H,7H,7αH)-ylidene)ethylidene)-2-methylenecyclohexane-1,3-diol). Preparation of a-ring phenylphosphine oxide 11, followed by Wittig-Horner coupl...

    journal_title:Bioorganic & medicinal chemistry letters

    pub_type: 杂志文章

    doi:10.1016/j.bmcl.2013.08.076

    authors: Chen B,Kawai M,Wu-Wong JR

    更新日期:2013-11-01 00:00:00

  • Enzymatic syntheses of 6-(4H-selenolo[3,2-b]pyrrolyl)-L-alanine, 4-(6H-selenolo[2,3-b]pyrrolyl)-L-alanine, and 6-(4H-furo[3,2-b]pyrrolyl-L-alanine.

    abstract::6-(4H-Selenolo[3,2-b]pyrrolyl)-L-alanine 1, 4-(6H-selenolo[2,3-b]pyrrolyl)-L-alanine 2, and 6-(4H-furo[3,2-b]pyrrolyl)-L-alanine 3 have been synthesized via reactions of selenolo[3,2-b]pyrrole, selenolo[2,3-b]pyrrole, and furo[3,2-b]pyrrole, respectively, with L-serine. The reactions are catalyzed by Salmonella typhim...

    journal_title:Bioorganic & medicinal chemistry letters

    pub_type: 杂志文章

    doi:10.1016/s0960-894x(99)00067-0

    authors: Welch M,Phillips RS

    更新日期:1999-03-08 00:00:00

  • Discovery of functionalized bisimidazoles bearing cyclic aliphatic-phenyl motifs as HCV NS5A inhibitors.

    abstract::This Letter describes the discovery of a number of functionalized bisimidazoles bearing a cyclohexylphenyl, piperidylphenyl, or bicyclo[2,2,2]octylphenyl motif as HCV NS5A inhibitors. Compounds 2c, 4b and 6 have demonstrated low single-digit nM potency in gt-1a replicon and double-digit pM potency in gt-1b replicon, r...

    journal_title:Bioorganic & medicinal chemistry letters

    pub_type: 杂志文章

    doi:10.1016/j.bmcl.2014.10.057

    authors: Zhong M,Peng E,Huang N,Huang Q,Huq A,Lau M,Colonno R,Li L

    更新日期:2014-12-15 00:00:00

  • Design, synthesis and biological evaluation of potent NAD+-dependent DNA ligase inhibitors as potential antibacterial agents. Part 2: 4-amino-pyrido[2,3-d]pyrimidin-5(8H)-ones.

    abstract::A series of 4-amino-pyrido[2,3-d]pyrimidin-5(8H)-ones were designed and synthesized as a novel class of inhibitors of NAD(+)-dependent DNA ligase that possess potency against Gram-positive bacteria. ...

    journal_title:Bioorganic & medicinal chemistry letters

    pub_type: 杂志文章

    doi:10.1016/j.bmcl.2012.04.038

    authors: Wang T,Duncan L,Gu W,O'Dowd H,Wei Y,Perola E,Parsons J,Gross CH,Moody CS,Arends SJ,Charifson PS

    更新日期:2012-06-01 00:00:00

  • Enhanced radical scavenging activity of a procyanidin B3 analogue comprised of a dimer of planar catechin.

    abstract::Proanthocyanidins are oligomers of catechins that exhibit potent antioxidative activity and inhibit binding of oxidized low-density lipoprotein (OxLDL) to the lectin-like oxidized LDL receptor (LOX-1), which is involved in the onset and development of arteriosclerosis. Previous attempts aimed at developing proanthocya...

    journal_title:Bioorganic & medicinal chemistry letters

    pub_type: 杂志文章

    doi:10.1016/j.bmcl.2017.10.007

    authors: Mizuno M,Nakanishi I,Matsumoto KI,Fukuhara K

    更新日期:2017-11-15 00:00:00

  • Mariannamides A and B, new cyclic octapeptides isolated from Mariannaea elegans NBRC102301.

    abstract::Two new cyclic octapeptides, mariannamides A (1) and B (2), have been isolated from Mariannaea elegans NBRC102301, a Pinus densiflora-derived filamentous fungus. Their structures were elucidated to be cyclo-(l-Leu1-l-Pro1-l-Pro2-l-Leu2-l-Ile1-l-Pro3-l-Val1-l-Ile2) and cyclo-(l-Leu1-l-Pro1-l-Pro2-l-Leu2-l-Ile1-l-Pro3-l...

    journal_title:Bioorganic & medicinal chemistry letters

    pub_type: 杂志文章

    doi:10.1016/j.bmcl.2019.126946

    authors: Ishiuchi K,Hirose D,Kondo T,Watanabe K,Terasaka K,Makino T

    更新日期:2020-02-15 00:00:00

  • Synthesis and structural assignment of two major metabolites of the LTA4H inhibitor DG-051.

    abstract::The same two major CYP mediated metabolites of DG-051 were produced in the presence of rat, dog, monkey and human liver microsomes. Their respective structures were hypothesized based on mass spectrometry data correlated with the parent structure and confirmed by comparison with authentic synthetic samples. The number...

    journal_title:Bioorganic & medicinal chemistry letters

    pub_type: 杂志文章

    doi:10.1016/j.bmcl.2009.09.097

    authors: Enache LA,Zhang J,Sullins DW,Kennedy I,Onua E,Zembower DE,Muellner FW,Singh J,Kiselyov AS

    更新日期:2009-11-15 00:00:00

  • Design, synthesis and biological evaluation of 2-indolinone derivatives as PAK1 inhibitors in MDA-MB-231 cells.

    abstract::P21-activated kinase 1 (PAK1) plays a vital role in the proliferation, survival and migration of cancer cells, which has emerged as a promising drug target for cancer therapy. In this study, a series of 2-indolinone derivatives were designed and synthesized through a structure-based strategy. A potent PAK1 inhibitor (...

    journal_title:Bioorganic & medicinal chemistry letters

    pub_type: 杂志文章

    doi:10.1016/j.bmcl.2020.127355

    authors: Yao D,Ruhan A,Jiang J,Huang J,Wang J,Han W

    更新日期:2020-09-01 00:00:00

  • Synthesis and activity in enhancing long-term potentiation (LTP) of clausenamide stereoisomers.

    abstract::Clausenamide, isolated from aqueous extract of dry leaves of Clausena lansium, a Chinese folk medicine, was found to have potent activity in enhancing LTP and show nootropic activity in animal tests. In order to discovery more potent stereoisomers and to analyze the relationship of structure-activity, the synthesis of...

    journal_title:Bioorganic & medicinal chemistry letters

    pub_type: 杂志文章

    doi:10.1016/j.bmcl.2009.03.018

    authors: Feng Z,Li X,Zheng G,Huang L

    更新日期:2009-04-15 00:00:00