当前位置： SCI文献检索 > BIOORGANIC & MEDICINAL CHEMISTRY LETTERS期刊下所有文献 > Development of a new class of potential antiatherosclerosis agents: NO-donor antioxidants.

Development of a new class of potential antiatherosclerosis agents: NO-donor antioxidants.

Abstract：

:A new class of NO-donor phenol derivatives is described. The products were obtained by joining appropriate phenols with either nitrooxy or 3-phenylsulfonylfuroxan-4-yloxy moieties. All the compounds proved to inhibit the ferrous salt/ascorbate induced lipidic peroxidation of membrane lipids of rat hepatocytes. They were also capable of dilating rat aorta strips precontracted with phenylephrine.

journal_name

Bioorg Med Chem Lett

journal_title

Bioorganic & medicinal chemistry letters

authors

Cena C,Boschi D,Tron GC,Chegaev K,Lazzarato L,Di Stilo A,Aragno M,Fruttero R,Gasco A

doi

10.1016/j.bmcl.2004.10.006

subject

Has Abstract

pub_date

2004-12-20 00:00:00

pages

5971-4

issue

24

eissn

0960-894X

issn

1464-3405

pii

S0960-894X(04)01230-2

journal_volume

14

pub_type

杂志文章

相关文献

BIOORGANIC & MEDICINAL CHEMISTRY LETTERS文献大全
  • Shikonin derivatives: synthesis and inhibition of human telomerase.

    abstract：:We synthesized DL-shikonin, shikonin, alkanin, and their cyclo-derivatives and acyl-derivatives. These compounds have low cytotoxicity, as well as inhibitory activity against the telomerase enzyme, except cyclo-derivatives. ...

    journal_title：Bioorganic & medicinal chemistry letters

    pub_type： 杂志文章

    doi：10.1016/s0960-894x(02)00158-0

    authors： Lu Q,Liu W,Ding J,Cai J,Duan W

    更新日期：2002-05-20 00:00:00

  • Synthesis, structural properties and insulin-enhancing potential of bis(quercetinato)oxovanadium(IV) conjugate.

    abstract：:An oxovanadium complex of quercetin (2), exhibits highly potent insulin-enhancing activity in streptozotocin-induced diabetic mice. It also mimics mitogenic potential of insulin as evaluated by [H(3)]thymidine uptake assay making an effective, orally active insulin-enhancing agent for the treatment of both type 1 and ...

    journal_title：Bioorganic & medicinal chemistry letters

    pub_type： 杂志文章

    doi：10.1016/j.bmcl.2004.07.020

    authors： Shukla R,Barve V,Padhye S,Bhonde R

    更新日期：2004-10-04 00:00:00

  • Structure-activity relationships for a novel series of thiazolyl phenyl ether derivatives exhibiting potent and selective acetyl-CoA carboxylase 2 inhibitory activity.

    abstract：:Structure-activity relationships for a recently discovered thiazolyl phenyl ether series of acetyl-CoA carboxylase (ACC) inhibitors were investigated. Preliminary efforts to optimize the series through modification of the distal aryl ether moiety of the lead scaffold resulted in the identification of compounds exhibit...

    journal_title：Bioorganic & medicinal chemistry letters

    pub_type： 杂志文章

    doi：10.1016/j.bmcl.2006.08.100

    authors： Clark RF,Zhang T,Xin Z,Liu G,Wang Y,Hansen TM,Wang X,Wang R,Zhang X,Frevert EU,Camp HS,Beutel BA,Sham HL,Gu YG

    更新日期：2006-12-01 00:00:00

  • Discovery and SAR of a novel series of Natriuretic Peptide Receptor-A (NPR-A) agonists.

    abstract：:Novel thienopyrimidine compounds 2 and 3 were discovered from high-throughput screening as Natriuretic Peptide Receptor A (NPR-A) agonists. Scaffold hopping of a thienopyrimidine ring to a quinazoline ring, introduction of the basic functional group and optimization of the substituent on the 6-position of the benzene ...

    journal_title：Bioorganic & medicinal chemistry letters

    pub_type： 杂志文章

    doi：10.1016/j.bmcl.2017.09.028

    authors： Iwaki T,Nakamura Y,Tanaka T,Ogawa Y,Iwamoto O,Okamura Y,Kawase Y,Furuya M,Oyama Y,Nagayama T

    更新日期：2017-11-01 00:00:00

  • New chemotypes for cathepsin K inhibitors.

    abstract：:Cyano pyrimidine acetylene and cyano pyrimidine t-amine, which belong to a new chemical class, were prepared and tested for inhibitory activities against cathepsin K and the highly homologous cathepsins L and S. The use of novel chemotypes in the development of cathepsin K inhibitors has been demonstrated by derivativ...

    journal_title：Bioorganic & medicinal chemistry letters

    pub_type： 杂志文章

    doi：10.1016/j.bmcl.2008.03.036

    authors： Teno N,Irie O,Miyake T,Gohda K,Horiuchi M,Tada S,Nonomura K,Kometani M,Iwasaki G,Betschart C

    更新日期：2008-04-15 00:00:00

  • Design and synthesis of conformationally constrained 3-(N-alkylamino)propylphosphonic acids as potent agonists of sphingosine-1-phosphate (S1P) receptors.

    abstract：:A series of conformationally constrained 3-(N-alkylamino)propylphosphonic acids were systematically synthesized and their activities as S1P receptor agonists were evaluated. Several pyrrolidine and cyclohexane analogs had S1P receptor profiles comparable to the acyclic lead compound, 3-(N-tetradecylamino)propylphospho...

    journal_title：Bioorganic & medicinal chemistry letters

    pub_type： 杂志文章

    doi：10.1016/j.bmcl.2004.07.049

    authors： Yan L,Hale JJ,Lynch CL,Budhu R,Gentry A,Mills SG,Hajdu R,Keohane CA,Rosenbach MJ,Milligan JA,Shei GJ,Chrebet G,Bergstrom J,Card D,Rosen H,Mandala SM

    更新日期：2004-10-04 00:00:00

  • Synthesis and SAR of 4-carboxy-2-azetidinone mechanism-based tryptase inhibitors.

    abstract：:A series of N1-activated C4-carboxy azetidinones was prepared and tested as inhibitors of human tryptase. The key stereochemical and functional features required for potency, serine protease specificity and aqueous stability were determined. From these studies compound 2, BMS-262084, was identified as a potent and sel...

    journal_title：Bioorganic & medicinal chemistry letters

    pub_type： 杂志文章

    doi：10.1016/s0960-894x(02)00688-1

    authors： Sutton JC,Bolton SA,Hartl KS,Huang MH,Jacobs G,Meng W,Ogletree ML,Pi Z,Schumacher WA,Seiler SM,Slusarchyk WA,Treuner U,Zahler R,Zhao G,Bisacchi GS

    更新日期：2002-11-04 00:00:00

  • Bis-azaaromatic quaternary ammonium salts as antagonists at nicotinic receptors mediating nicotine-evoked dopamine release: An investigation of binding conformation.

    abstract：:A series of conformationally restricted bis-azaaromatic quaternary ammonium salts (3 and 4) have been designed and synthesized in order to investigate the possible binding conformations of N,N'-dodecane-1,12-diyl-bis-3-picolinium dibromide (bPiDDB; 2), a compound which potently inhibits neuronal nicotinic acetylcholin...

    journal_title：Bioorganic & medicinal chemistry letters

    pub_type： 杂志文章

    doi：10.1016/j.bmcl.2007.10.052

    authors： Zheng G,Zhang Z,Pivavarchyk M,Deaciuc AG,Dwoskin LP,Crooks PA

    更新日期：2007-12-15 00:00:00

  • Radical-scavenging properties of ferrocenyl chalcones.

    abstract：:The radical-scavenging capacities of ferrocenyl group and phenolic hydroxyl group in ferrocenyl chalcone were identified in this work. 1,1'-Diacetylferrocene was applied to condense with benzaldehyde, vanillin, and protocatechualdehyde to produce ferrocenyl chalcones, which were employed to interact with 2,2'-azinobis...

    journal_title：Bioorganic & medicinal chemistry letters

    pub_type： 杂志文章

    doi：10.1016/j.bmcl.2010.12.051

    authors： Nabi G,Liu ZQ

    更新日期：2011-02-01 00:00:00

  • Modified 3-alkyl-1,8-dibenzylxanthines as GTP-competitive inhibitors of phosphoenolpyruvate carboxykinase.

    abstract：:The first non-substrate like inhibitors of human cytosolic phosphoenolpyruvate carboxykinase (PEPCK) competitive with GTP are reported. An effort to discover orally active compounds that improve glucose homeostasis in Type 2 diabetics by reversibly inhibiting PEPCK led to the discovery of 1-allyl-3-butyl-8-methylxanth...

    journal_title：Bioorganic & medicinal chemistry letters

    pub_type： 杂志文章

    doi：10.1016/s0960-894x(03)00722-4

    authors： Foley LH,Wang P,Dunten P,Ramsey G,Gubler ML,Wertheimer SJ

    更新日期：2003-10-20 00:00:00

  • Synthesis and preliminary evaluation of a new fluorine-18 labelled triazine derivative for PET imaging of cannabinoid CB2 receptor.

    abstract：:Cannabinoid CB2 PET tracers are considered as a promising alternative to PBR/TSPO tracers for the in-vivo imaging of neuroinflammation. We describe here the synthesis and characterization of compound 3, a new potent and brain penetrating CB2 ligand based on an original triazine template. The PET tracer [(18)F]-dideute...

    journal_title：Bioorganic & medicinal chemistry letters

    pub_type： 杂志文章

    doi：10.1016/j.bmcl.2013.11.023

    authors： Hortala L,Arnaud J,Roux P,Oustric D,Boulu L,Oury-Donat F,Avenet P,Rooney T,Alagille D,Barret O,Tamagnan G,Barth F

    更新日期：2014-01-01 00:00:00

  • Synthesis of OSW saponin analogs with modified sugar residues and their antiproliferative activities.

    abstract：:Eight monosaccharide analogs of the potent antitumor OSW saponins (2-9) were synthesized. One analog, 2-O-acetyl-alpha-l-arabinopyranoside 3, showed antiproliferative activity against the Jurkat cells (IC(50)=0.078microM) comparable to that of the disaccharide derivative (1). ...

    journal_title：Bioorganic & medicinal chemistry letters

    pub_type： 杂志文章

    doi：10.1016/j.bmcl.2006.11.032

    authors： Tang P,Mamdani F,Hu X,Liu JO,Yu B

    更新日期：2007-02-15 00:00:00

  • Evaluation of hadacidin analogues.

    abstract：:Several derivatives of hadacidin have been developed and evaluated for activity against adenylosuccinate synthetase. ...

    journal_title：Bioorganic & medicinal chemistry letters

    pub_type： 杂志文章

    doi：10.1016/j.bmcl.2010.10.088

    authors： Tibrewal N,Elliott GI

    更新日期：2011-01-01 00:00:00

  • The development of benzo- and naphtho-fused quinoline-2,4-dicarboxylic acids as vesicular glutamate transporter (VGLUT) inhibitors reveals a possible role for neuroactive steroids.

    abstract：:Substituted quinoline-2,4-dicarboxylates (QDCs) are conformationally-restricted mimics of glutamate that were previously reported to selectively block the glutamate vesicular transporters (VGLUTs). We find that expanding the QDC scaffold to benzoquinoline dicarboxylic acids (BQDC) and naphthoquinoline dicarboxylic aci...

    journal_title：Bioorganic & medicinal chemistry letters

    pub_type： 杂志文章

    doi：10.1016/j.bmcl.2013.12.086

    authors： Carrigan CN,Patel SA,Cox HD,Bolstad ES,Gerdes JM,Smith WE,Bridges RJ,Thompson CM

    更新日期：2014-02-01 00:00:00

  • Silanediol-based inhibitor of thermolysin.

    abstract：:The first silanediol inhibitor of thermolysin is reported, prepared by analogy with the Grobelny/Bartlett phosphinate inhibitor. A Cbz group on nitrogen proved to be unstable to the triflic acid mediated silanediol deprotection and was replaced with a dihydrocinnamoyl group. The silanediol was prepared in high purity ...

    journal_title：Bioorganic & medicinal chemistry letters

    pub_type： 杂志文章

    doi：10.1016/s0960-894x(02)00804-1

    authors： Kim J,Glekas A,McN Sieburth S

    更新日期：2002-12-16 00:00:00

  • The sulfamide moiety affords higher inhibitory activity and oral bioavailability to a series of coumarin dual selective RAF/MEK inhibitors.

    abstract：:Introducing a sulfamide moiety to our coumarin derivatives afforded enhanced Raf/MEK inhibitory activity concomitantly with an acceptable PK profile. Novel sulfamide 17 showed potent HCT116 cell growth inhibition (IC50=8 nM) and good PK profile (bioavailability of 51% in mouse), resulting in high in vivo antitumor eff...

    journal_title：Bioorganic & medicinal chemistry letters

    pub_type： 杂志文章

    doi：10.1016/j.bmcl.2013.10.001

    authors： Aoki T,Hyohdoh I,Furuichi N,Ozawa S,Watanabe F,Matsushita M,Sakaitani M,Ori K,Takanashi K,Harada N,Tomii Y,Tabo M,Yoshinari K,Aoki Y,Shimma N,Iikura H

    更新日期：2013-12-01 00:00:00

  • First hydroxamate inhibitors for carboxypeptidase A. N-acyl-N-hydroxy-beta-phenylalanines.

    abstract：:A series of N-acyl-N-hydroxy-beta-Phe were designed, synthesized, and shown to have potent inhibitory activity for carboxypeptidase A (CPA). They are the first examples of CPA inhibitors having a hydroxamate functionality. ...

    journal_title：Bioorganic & medicinal chemistry letters

    pub_type： 杂志文章

    doi：10.1016/s0960-894x(99)00055-4

    authors： Kim DH,Jin Y

    更新日期：1999-03-08 00:00:00

  • Synthesis and antiproliferative activity of benzocyclobutacarbazol derivatives. A new class of potential antitumor agents.

    abstract：:Several benzocyclobutacarbazol derivatives were synthesized and evaluated for their potential cytotoxic properties. A number of these compounds exhibited significant antiproliferative activity with concomitant interaction with the cell cycle and represent a new class of potential anticancer agents. ...

    journal_title：Bioorganic & medicinal chemistry letters

    pub_type： 杂志文章

    doi：10.1016/s0960-894x(00)00532-1

    authors： Graf-Christophe S,Kuehm-Caubère C,Renard P,Pfeiffer B,Pierré A,Léonce S,Caubère P

    更新日期：2000-12-04 00:00:00

  • Optimization of alpha-acylaminoketone ecdysone agonists for control of gene expression.

    abstract：:Fifteen new alpha-acylaminoketones were prepared by four different routes in an initial effort to optimize the potency of these compounds as ecdysone agonists. The compounds were assayed in mammalian cells expressing the ecdysone receptors from Bombyx mori (BmEcR) and Choristoneura fumiferana (CfEcR) for their ability...

    journal_title：Bioorganic & medicinal chemistry letters

    pub_type： 杂志文章

    doi：10.1016/s0960-894x(03)00315-9

    authors： Tice CM,Hormann RE,Thompson CS,Friz JL,Cavanaugh CK,Saggers JA

    更新日期：2003-06-02 00:00:00

  • The discovery of a series of N-substituted 3-(4-piperidinyl)-1,3-benzoxazolinones and oxindoles as highly brain penetrant, selective muscarinic M1 agonists.

    abstract：:A series of N-substituted 3-(4-piperidinyl)-1,3-benzoxazolinones and oxindoles are reported which were found to be potent and selective muscarinic M1 agonists. By control of the physicochemical characteristics of the series, particularly the lipophilicity, compounds with good metabolic stability and excellent brain pe...

    journal_title：Bioorganic & medicinal chemistry letters

    pub_type： 杂志文章

    doi：10.1016/j.bmcl.2010.07.097

    authors： Johnson DJ,Forbes IT,Watson SP,Garzya V,Stevenson GI,Walker GR,Mudhar HS,Flynn ST,Wyman PA,Smith PW,Murkitt GS,Lucas AJ,Mookherjee CR,Watson JM,Gartlon JE,Bradford AM,Brown F

    更新日期：2010-09-15 00:00:00

  • The discovery of potent, selective, and orally bioavailable PDE9 inhibitors as potential hypoglycemic agents.

    abstract：:Starting from a non-selective pyrazolo-pyrimidone lead, the sequential use of parallel medicinal chemistry and directed synthesis led to the discovery of potent, highly selective, and orally bioavailable PDE9 inhibitors. The availability of these tools allowed for a thorough evaluation of the therapeutic potential of ...

    journal_title：Bioorganic & medicinal chemistry letters

    pub_type： 杂志文章

    doi：10.1016/j.bmcl.2009.03.024

    authors： Deninno MP,Andrews M,Bell AS,Chen Y,Eller-Zarbo C,Eshelby N,Etienne JB,Moore DE,Palmer MJ,Visser MS,Yu LJ,Zavadoski WJ,Michael Gibbs E

    更新日期：2009-05-01 00:00:00

  • Synthesis and biological evaluation of 1-(2,4,5-trisubstituted phenyl)-3-(5-cyanopyrazin-2-yl)ureas as potent Chk1 kinase inhibitors.

    abstract：:Based on the X-ray crystallography of our lead compound 1-(5-chloro-2,4-dimethoxyphenyl)-3-(5-cyanopyrazin-2-yl)urea in the checkpoint kinase 1 (Chk1) enzyme, we modified R4, and to a lesser extent, R2, and R5 of the phenyl ring, and made a variety of N-aryl-N'-pyrazinylurea Chk1 inhibitors. Enzymatic activity less th...

    journal_title：Bioorganic & medicinal chemistry letters

    pub_type： 杂志文章

    doi：10.1016/j.bmcl.2006.01.028

    authors： Li G,Hasvold LA,Tao ZF,Wang GT,Gwaltney SL 2nd,Patel J,Kovar P,Credo RB,Chen Z,Zhang H,Park C,Sham HL,Sowin T,Rosenberg SH,Lin NH

    更新日期：2006-04-15 00:00:00

  • Selective heterocyclic amidine inhibitors of human inducible nitric oxide synthase.

    abstract：:The potency and selectivity of a series of 5-hetero-2-iminohexahydroazepines were examined as inhibitors of the three human NOS isoforms. The effect of ring substitution of the 5-carbon for a heteroatom is presented. Potencies (IC(50)'s) for these inhibitors are in the low micromolar range for hi-NOS with some example...

    journal_title：Bioorganic & medicinal chemistry letters

    pub_type： 杂志文章

    doi：10.1016/s0960-894x(01)00523-6

    authors： Moormann AE,Metz S,Toth MV,Moore WM,Jerome G,Kornmeier C,Manning P,Hansen DW Jr,Pitzele BS,Webber RK

    更新日期：2001-10-08 00:00:00

  • Surface plasmon resonance-based detection of ladder-shaped polyethers by inhibition detection method.

    abstract：:Ladder-shaped polyether (LSP) compounds represented by brevetoxins and ciguatoxins were largely discovered in association with seafood poisoning. Thus, a quick quantification method for LSPs is potentially important. We examined a surface plasmon resonance method using desulfated-yessotoxin (dsYTX) immobilized on a se...

    journal_title：Bioorganic & medicinal chemistry letters

    pub_type： 杂志文章

    doi：10.1016/j.bmcl.2009.03.103

    authors： Mouri R,Oishi T,Torikai K,Ujihara S,Matsumori N,Murata M,Oshima Y

    更新日期：2009-05-15 00:00:00

  • Interaction of heterocyclic thiols/thiones eliminated from cephalosporins with iodine and its biological implications.

    abstract：:Hydrolysis of beta-lactam antibiotics by beta-lactamases (e.g., metallo-beta-lactamase, mbetal) is one of the major bacterial defense systems. These enzymes can catalyze the hydrolysis of a variety of antibiotics including the latest generation of cephalosporins, cephamycins and imipenem. It is shown in this paper tha...

    journal_title：Bioorganic & medicinal chemistry letters

    pub_type： 杂志文章

    doi：10.1016/j.bmcl.2010.04.087

    authors： Tamilselvi A,Mugesh G

    更新日期：2010-06-15 00:00:00

  • Quantitating the concentration of Py-Im polyamide-fluorescein conjugates in live cells.

    abstract：:Quantitative fluorescence-based methods have been developed to determine the nuclear concentration of polyamide-fluorescein conjugates in cell culture. Confocal laser scanning microscopy and flow cytometry techniques are utilized to plot calibration curves, from which the nuclear concentration can be interpolated. Upo...

    journal_title：Bioorganic & medicinal chemistry letters

    pub_type： 杂志文章

    doi：10.1016/j.bmcl.2008.05.063

    authors： Hsu CF,Dervan PB

    更新日期：2008-11-15 00:00:00

  • Discovery of dimeric inhibitors by extension into the entrance channel of HIV-1 reverse transcriptase.

    abstract：:Design of non-nucleoside inhibitors of HIV-1 reverse transcriptase is being pursued with computational guidance. Extension of azine-containing inhibitors into the entrance channel between Lys103 and Glu138 has led to the discovery of potent and structurally novel derivatives including dimeric inhibitors in an NNRTI-li...

    journal_title：Bioorganic & medicinal chemistry letters

    pub_type： 杂志文章

    doi：10.1016/j.bmcl.2011.12.132

    authors： Ekkati AR,Bollini M,Domaoal RA,Spasov KA,Anderson KS,Jorgensen WL

    更新日期：2012-02-15 00:00:00

  • Structure-based optimization of aminopyridines as PKCθ inhibitors.

    abstract：:The identification of a novel series of PKCθ inhibitors and subsequent optimization using docking based on a crystal structure of PKCθ is described. SAR was rapidly generated around an amino pyridine-ketone hit; (6-aminopyridin-2-yl)(2-aminopyridin-3-yl)methanone 2 leading to compound 21 which significantly inhibits p...

    journal_title：Bioorganic & medicinal chemistry letters

    pub_type： 杂志文章

    doi：10.1016/j.bmcl.2012.05.114

    authors： Jimenez JM,Davis C,Boyall D,Fraysse D,Knegtel R,Settimo L,Young S,Bolton C,Chiu P,Curnock A,Rasmussen R,Tanner A,Ager I

    更新日期：2012-07-15 00:00:00

  • Synthesis of new bergenin derivatives as potent inhibitors of inflammatory mediators NO and TNF-α.

    abstract：:Bergenin is an isocoumarin natural product which aides in fat loss, healthy weight maintenance, enhancing the lipolytic effects of norepinephrine, inhibiting the formation of interleukin 1α and cyclooxygenases-2. Here we describe the anti-inflammatory activity of new bergenin derivatives 1-15 in the respiratory burst ...

    journal_title：Bioorganic & medicinal chemistry letters

    pub_type： 杂志文章

    doi：10.1016/j.bmcl.2012.02.096

    authors： Shah MR,Arfan M,Amin H,Hussain Z,Qadir MI,Choudhary MI,VanDerveer D,Mesaik MA,Soomro S,Jabeen A,Khan IU

    更新日期：2012-04-15 00:00:00

  • Synthesis and antiviral activity of novel D- and L-2'-azido-2',3'-dideoxyribofuranosyl-4'-thiopyrimidines and purines.

    abstract：:Novel D- and L-2'-azido-2',3'-dideoxyribofuranosyl-4'-thiopyrimidines and purines have been synthesized starting from L-xylose and D-xylose, respectively. Among synthesized compounds tested against several viruses such as HIV-1, HSV-1, HSV-2, and HCMV, D-beta-N6-methyladenine (ent-22a) and D-alpha-N6-methyladenine (en...

    journal_title：Bioorganic & medicinal chemistry letters

    pub_type： 杂志文章

    doi：10.1016/s0960-894x(01)00006-3

    authors： Kim HO,Kim YH,Suh H,Jeong LS

    更新日期：2001-02-26 00:00:00