当前位置： SCI文献检索 > BIOORGANIC & MEDICINAL CHEMISTRY LETTERS期刊下所有文献 > Synthesis and antiplatelet effects of an isoxazole series of glycoprotein IIb/IIIa antagonists.

Synthesis and antiplatelet effects of an isoxazole series of glycoprotein IIb/IIIa antagonists.

Abstract：

:Despite the excellent in vitro potency of a series of benzamide glycoprotein IIb/IIIa antagonists, which have been reported previously, poor in vivo potency in the inhibition of platelet aggregation was observed when the most potent inhibitor XU057 was dosed intravenously to dogs. In this communication, we report that replacement of the benzamide in XU057 with an isoxazolecarboxamide resulted in significant improvement in in vivo potency. More importantly, the analogue XU065 showed an excellent oral antiplatelet effect in dogs.

journal_name

Bioorg Med Chem Lett

journal_title

Bioorganic & medicinal chemistry letters

authors

Xue CB,Roderick J,Mousa S,Olson RE,DeGrado WF

doi

10.1016/s0960-894x(98)00637-4

subject

Has Abstract

pub_date

1998-12-15 00:00:00

pages

3499-504

issue

24

eissn

0960-894X

issn

1464-3405

pii

S0960894X98006374

journal_volume

8

pub_type

杂志文章

相关文献

BIOORGANIC & MEDICINAL CHEMISTRY LETTERS文献大全
  • Array synthesis of novel lipodepsipeptide.

    abstract：:Synthetic array technology was utilized to rapidly synthesize and analyze a diverse set of reductive alkylation analogues of daptomycin. Analysis of the array suggested the use of polar functionality such as sulfonamides or amide or polar spaces such as piperazine would beneficially affect activity. ...

    journal_title：Bioorganic & medicinal chemistry letters

    pub_type： 杂志文章

    doi：10.1016/j.bmcl.2003.07.025

    authors： Siedlecki J,Hill J,Parr I,Yu X,Morytko M,Zhang Y,Silverman J,Controneo N,Laganas V,Li T,Li J,Keith D,Shimer G,Finn J

    更新日期：2003-12-01 00:00:00

  • Antimitotic activity of structurally simplified biaryl analogs of the anticancer agents colchicine and combretastatin A4.

    abstract：:Two substituted biaryl analogues of colchicine and combretastatin A4, readily available through a one-step, protecting group free Suzuki-Miyaura reaction were discovered to exhibit anticancer activity while simultaneously being of low cytotoxicity to noncancerous cell lines. The compounds were shown to initiate apopto...

    journal_title：Bioorganic & medicinal chemistry letters

    pub_type： 杂志文章

    doi：10.1016/j.bmcl.2014.10.090

    authors： McNulty J,van den Berg S,Ma D,Tarade D,Joshi S,Church J

    更新日期：2015-01-01 00:00:00

  • Chemical constituents from the fruit of Gardenia jasminoides and their inhibitory effects on nitric oxide production.

    abstract：:Three new iridoid glycosides, 6"-O-trans-caffeoylgenipin gentiobioside (1), genipin 1-O-β-D-apiofuranosyl (1→6)-β-D-glucopyranoside (2), genipin 1-O-α-D-xylopyranosyl (1→6)-β-D-glucopyranoside (3), three new monocyclic monoterpenoids, jasminoside R (4), jasminoside S (5), jasminoside T (6), together with nine known ir...

    journal_title：Bioorganic & medicinal chemistry letters

    pub_type： 杂志文章

    doi：10.1016/j.bmcl.2012.11.099

    authors： Peng K,Yang L,Zhao S,Chen L,Zhao F,Qiu F

    更新日期：2013-02-15 00:00:00

  • Synthesis and biological evaluation of deoxy-hematoxylin derivatives as a novel class of anti-HIV-1 agents.

    abstract：:SAR studies for the exploration a novel class of anti-human immunodeficiency virus type 1 (HIV-1) agents based on the hematoxylin structure (1) are described. The systematic deoxygenations of 1 including asymmetric synthesis were conducted to obtain a compound showing high potencies for inhibiting the nuclear import a...

    journal_title：Bioorganic & medicinal chemistry letters

    pub_type： 杂志文章

    doi：10.1016/j.bmcl.2011.06.066

    authors： Ishii H,Koyama H,Hagiwara K,Miura T,Xue G,Hashimoto Y,Kitahara G,Aida Y,Suzuki M

    更新日期：2012-02-01 00:00:00

  • Penicinoline, a new pyrrolyl 4-quinolinone alkaloid with an unprecedented ring system from an endophytic fungus Penicillium sp.

    abstract：:A new pyrrolyl 4-quinolinone alkaloid with an unprecedented ring system, named penicinoline (1) was isolated from a mangrove endophytic fungus. The structure of 1 was elucidated by spectroscopic methods and comparison with its derivative, penicinotam (1a), an unexpected lactam that was obtained from 1 by intramolecula...

    journal_title：Bioorganic & medicinal chemistry letters

    pub_type： 杂志文章

    doi：10.1016/j.bmcl.2010.04.043

    authors： Shao CL,Wang CY,Gu YC,Wei MY,Pan JH,Deng DS,She ZG,Lin YC

    更新日期：2010-06-01 00:00:00

  • Anti-HIV activity of stilbene-related heterocyclic compounds.

    abstract：:Viral transcription has not been routinely targeted in the development of new antiviral drugs. This crucial step of the viral cycle depends on the concerted action of cellular and viral proteins such as NF-kappaB and Tat. In the present study, stilbene-related heterocyclic compounds including benzalphthalide, phthalaz...

    journal_title：Bioorganic & medicinal chemistry letters

    pub_type： 杂志文章

    doi：10.1016/j.bmcl.2006.04.087

    authors： Bedoya LM,del Olmo E,Sancho R,Barboza B,Beltrán M,García-Cadenas AE,Sánchez-Palomino S,López-Pérez JL,Muñoz E,San Feliciano A,Alcamí J

    更新日期：2006-08-01 00:00:00

  • Polymer-supported catalysts: enantioselective hydrogenation and hydrogen transfer reduction.

    abstract：:Different types of heterogenized catalysts were involved in asymmetric reactions. Hydrogen transfer reduction was performed with amino alcohols derived from poly((S)-(GMA-co-EGDMA or DVB)) and hydrogenation with BINAP grafted onto PEG or copolymerized with isocyanates as ligands. Attempts of catalysts recycling are re...

    journal_title：Bioorganic & medicinal chemistry letters

    pub_type： 杂志文章

    doi：10.1016/s0960-894x(02)00258-5

    authors： Saluzzo C,Lamouille T,Hérault D,Lemaire M

    更新日期：2002-07-22 00:00:00

  • A stepwise dechlorination/cross-coupling strategy to diversify the vancomycin 'in-chloride'.

    abstract：:In an effort to rapidly access vancomycin analogues bearing diverse functionality at the 6c-Cl (the 'in-chloride') position, a two-step dechlorination/cross-coupling protocol was developed. Conditions for efficient cross-coupling of the relatively unreactive 6c-Cl group were found that ensure high conversion with mini...

    journal_title：Bioorganic & medicinal chemistry letters

    pub_type： 杂志文章

    doi：10.1016/j.bmcl.2015.12.027

    authors： Wadzinski TJ,Gea KD,Miller SJ

    更新日期：2016-02-01 00:00:00

  • Synthesis and preliminary cytotoxicity of nitrogen mustard derivatives of distamycin A.

    abstract：:Distamycin and nitrogen mustard conjugates, in which the nitrogen mustard unit was coupled to the C-terminus of the pyrrole, were synthesized. The switching of the nitrogen mustard unit from the N-terminus to the C-terminus did not compromise the compound's cytotoxicity. Compound 3, bearing three pyrrole units, was hi...

    journal_title：Bioorganic & medicinal chemistry letters

    pub_type： 杂志文章

    doi：10.1016/s0960-894x(02)00986-1

    authors： Wang Y,Wright SC,Larrick JW

    更新日期：2003-02-10 00:00:00

  • Novel dammarane-type triterpenes isolated from hydrolyzate of total Gynostemma pentaphyllum saponins.

    abstract：:In this study, five novel triterpenes were isolated from hydrolyzate of total saponins from Gynostemma pentaphyllum and identified as gypensapogenin H (1), gypensapogenin I (2), gypensapogenin L (3), gypensapogenin J (4) and gypensapogenin K (5), three of which (1-3) possess unprecedented ring A. All the isolated comp...

    journal_title：Bioorganic & medicinal chemistry letters

    pub_type： 杂志文章

    doi：10.1016/j.bmcl.2015.06.022

    authors： Zhang XS,Cao JQ,Zhao C,Wang XD,Wu XJ,Zhao YQ

    更新日期：2015-08-15 00:00:00

  • Development of indole/indazole-aminopyrimidines as inhibitors of c-Jun N-terminal kinase (JNK): optimization for JNK potency and physicochemical properties.

    abstract：:A novel series of indole/indazole-aminopyrimidines was designed and synthesized with an aim to achieve optimal potency and selectivity for the c-Jun kinase family or JNKs. Structure guided design was used to optimize the series resulting in a significant potency improvement. The best compound (17) has IC50 of 3 nM for...

    journal_title：Bioorganic & medicinal chemistry letters

    pub_type： 信件

    doi：10.1016/j.bmcl.2013.04.029

    authors： Gong L,Han X,Silva T,Tan YC,Goyal B,Tivitmahaisoon P,Trejo A,Palmer W,Hogg H,Jahagir A,Alam M,Wagner P,Stein K,Filonova L,Loe B,Makra F,Rotstein D,Rapatova L,Dunn J,Zuo F,Dal Porto J,Wong B,Jin S,Chang A,T

    更新日期：2013-06-15 00:00:00

  • Hydroxyl substituted benzoic acid/cinnamic acid derivatives: Tyrosinase inhibitory kinetics, anti-melanogenic activity and molecular docking studies.

    abstract：:The inhibition of tyrosinase is an established strategy for treating hyperpigmentation. Our previous findings demonstrated that cinnamic acid and benzoic acid scaffolds can be effective tyrosinase inhibitors with low toxicity. The hydroxyl substituted benzoic and cinnamic acid moieties of these precursors were incorpo...

    journal_title：Bioorganic & medicinal chemistry letters

    pub_type： 杂志文章

    doi：10.1016/j.bmcl.2019.126722

    authors： Nazir Y,Saeed A,Rafiq M,Afzal S,Ali A,Latif M,Zuegg J,Hussein WM,Fercher C,Barnard RT,Cooper MA,Blaskovich MAT,Ashraf Z,Ziora ZM

    更新日期：2020-01-01 00:00:00

  • Design, synthesis, biological evaluation and molecular modeling of dihydropyrazole sulfonamide derivatives as potential COX-1/COX-2 inhibitors.

    abstract：:Novel dihydropyrazole sulfonamide derivatives (30-56) were designed, synthesized, and evaluated for their biological activities as COX-1 and COX-2 inhibitors. In vitro biological evaluation against three human tumor cell lines revealed that most target compounds showed antiproliferative activities. Among the compounds...

    journal_title：Bioorganic & medicinal chemistry letters

    pub_type： 杂志文章

    doi：10.1016/j.bmcl.2015.03.022

    authors： Chen Z,Wang ZC,Yan XQ,Wang PF,Lu XY,Chen LW,Zhu HL,Zhang HW

    更新日期：2015-05-01 00:00:00

  • Discovery of fused 5,6-bicyclic heterocycles as γ-secretase modulators.

    abstract：:We herein report the discovery of four series of fused 5,6-bicyclic heterocycles as γ-secretase modulators. Synthesis and SAR of these series are discussed. These compounds represent a new class of γ-secretase modulators that demonstrate moderate to good in vitro potency in inhibiting Aβ(42) production. ...

    journal_title：Bioorganic & medicinal chemistry letters

    pub_type： 杂志文章

    doi：10.1016/j.bmcl.2010.12.012

    authors： Qin J,Dhondi P,Huang X,Mandal M,Zhao Z,Pissarnitski D,Zhou W,Aslanian R,Zhu Z,Greenlee W,Clader J,Zhang L,Cohen-Williams M,Jones N,Hyde L,Palani A

    更新日期：2011-01-15 00:00:00

  • Synthesis, 3D-structure and stability analyses of NRPa-308, a new promising anti-cancer agent.

    abstract：:We report herein the synthesis of a newly described anti-cancer agent, NRPa-308. This compound antagonizes Neuropilin-1, a multi-partners transmembrane receptor overexpressed in numerous tumors, and thereby validated as promising target in oncology. The preparation of NRPa-308 proved challenging because of the orthogo...

    journal_title：Bioorganic & medicinal chemistry letters

    pub_type： 杂志文章

    doi：10.1016/j.bmcl.2019.126710

    authors： Brachet E,Dumond A,Liu WQ,Fabre M,Selkti M,Raynaud F,Hermine O,Benhida R,Belmont P,Garbay C,Lepelletier Y,Ronco C,Pagès G,Demange L

    更新日期：2019-12-15 00:00:00

  • Structure-based design of ketone-containing, tripeptidyl human rhinovirus 3C protease inhibitors.

    abstract：:Tripeptide-derived molecules incorporating C-terminal ketone electrophiles were evaluated as reversible inhibitors of the cysteine-containing human rhinovirus 3C protease (3CP). An optimized example of such compounds displayed potent 3CP inhibition activity (K = 0.0045 microM) and in vitro antiviral properties (EC50=0...

    journal_title：Bioorganic & medicinal chemistry letters

    pub_type： 杂志文章

    doi：10.1016/s0960-894x(99)00587-9

    authors： Dragovich PS,Zhou R,Webber SE,Prins TJ,Kwok AK,Okano K,Fuhrman SA,Zalman LS,Maldonado FC,Brown EL,Meador JW 3rd,Patick AK,Ford CE,Brothers MA,Binford SL,Matthews DA,Ferre RA,Worland ST

    更新日期：2000-01-03 00:00:00

  • Aminoalkoxybenzyl pyrrolidines as novel human urotensin-II receptor antagonists.

    abstract：:High throughput screening of the corporate compound collection led to the discovery of a novel series of substituted aminoalkoxybenzyl pyrrolidines as human urotensin-II receptor antagonists. The synthesis, initial structure-activity relationships, and optimization of the initial hit that led to the identification of ...

    journal_title：Bioorganic & medicinal chemistry letters

    pub_type： 杂志文章

    doi：10.1016/j.bmcl.2005.04.074

    authors： Jin J,Dhanak D,Knight SD,Widdowson K,Aiyar N,Naselsky D,Sarau HM,Foley JJ,Schmidt DB,Bennett CD,Wang B,Warren GL,Moore ML,Keenan RM,Rivero RA,Douglas SA

    更新日期：2005-07-01 00:00:00

  • A new selective fluorescent probe based on tamoxifen.

    abstract：:Developing targeted validation probes that can interrogate biology is of interest for both chemists and biologists. The synthesis of suitable compounds provides a means for avoiding the costly labeling of cells with specific antibodies and the bias associated with the interpretation of biological validation experiment...

    journal_title：Bioorganic & medicinal chemistry letters

    pub_type： 杂志文章

    doi：10.1016/j.bmcl.2016.09.028

    authors： Ho LA,Thomas E,McLaughlin RA,Flematti GR,Fuller RO

    更新日期：2016-10-15 00:00:00

  • Poly-guanidinoethylphenylethers organised around a benzene ring: synthesis and evaluation of their antibacterial and cytotoxic properties.

    abstract：:A new family of poly-guanidinium species with a benzene core as the organising agent has been developed. Their antibacterial properties have been evaluated against reference Gram positive and Gram negative bacteria, and their cytotoxicity against eukaryotic cells. Most of these compounds exhibited Minimum Inhibitory C...

    journal_title：Bioorganic & medicinal chemistry letters

    pub_type： 杂志文章

    doi：10.1016/j.bmcl.2014.09.013

    authors： Massimba Dibama H,Mourer M,Duval RE,Regnouf-de-Vains JB

    更新日期：2014-10-15 00:00:00

  • 2-Amino-aryl-7-aryl-benzoxazoles as potent, selective and orally available JAK2 inhibitors.

    abstract：:A series of novel benzoxazole derivatives has been designed and shown to exhibit attractive JAK2 inhibitory profiles in biochemical and cellular assays, capable of delivering compounds with favorable PK properties in rats. Synthesis and structure-activity relationship data are also provided. ...

    journal_title：Bioorganic & medicinal chemistry letters

    pub_type： 杂志文章

    doi：10.1016/j.bmcl.2010.01.069

    authors： Gerspacher M,Furet P,Pissot-Soldermann C,Gaul C,Holzer P,Vangrevelinghe E,Lang M,Erdmann D,Radimerski T,Regnier CH,Chene P,De Pover A,Hofmann F,Baffert F,Buhl T,Aichholz R,Blasco F,Endres R,Trappe J,Drueckes P

    更新日期：2010-03-01 00:00:00

  • 7-Oxopyrrolopyridine-derived DPP4 inhibitors-mitigation of CYP and hERG liabilities via introduction of polar functionalities in the active site.

    abstract：:Design, synthesis, and SAR of 7-oxopyrrolopyridine-derived DPP4 inhibitors are described. The preferred stereochemistry of these atropisomeric biaryl analogs has been identified as Sa. Compound (+)-3t, with a K(i) against DPP4, DPP8, and DPP9 of 0.37 nM, 2.2, and 5.7 μM, respectively, showed a significant improvement ...

    journal_title：Bioorganic & medicinal chemistry letters

    pub_type： 杂志文章

    doi：10.1016/j.bmcl.2011.09.074

    authors： Wang W,Devasthale P,Wang A,Harrity T,Egan D,Morgan N,Cap M,Fura A,Klei HE,Kish K,Weigelt C,Sun L,Levesque P,Li YX,Zahler R,Kirby MS,Hamann LG

    更新日期：2011-11-15 00:00:00

  • Substituted indoles as selective protease activated receptor 4 (PAR-4) antagonists: Discovery and SAR of ML354.

    abstract：:Herein we report the discovery and SAR of an indole-based protease activated receptor-4 (PAR-4) antagonist scaffold derived from a similarity search of the Vanderbilt HTS collection, leading to MLPCN probe ML354 (VU0099704). Using a novel PAC-1 fluorescent αIIbβ3 activation assay this probe molecule antagonist was fou...

    journal_title：Bioorganic & medicinal chemistry letters

    pub_type： 杂志文章

    doi：10.1016/j.bmcl.2014.08.021

    authors： Wen W,Young SE,Duvernay MT,Schulte ML,Nance KD,Melancon BJ,Engers J,Locuson CW 2nd,Wood MR,Daniels JS,Wu W,Lindsley CW,Hamm HE,Stauffer SR

    更新日期：2014-10-01 00:00:00

  • Successful bridging from a peptide to a non peptide antagonist at the human tachykinin NK-2 receptor.

    abstract：:Non peptide products have been found to show nanomolar binding and functional affinities at the human tachykinin NK-2 receptor. The new antagonists do not possess stereogenic centers and their thermal behaviour in solution is featured by a peculiar set of conformational stereoisomers. A macroscopic viewpoint is prefer...

    journal_title：Bioorganic & medicinal chemistry letters

    pub_type： 杂志文章

    doi：10.1016/s0960-894x(02)00539-5

    authors： Altamura M,Canfarini F,Catalioto RM,Guidi A,Pasqui F,Renzetti AR,Triolo A,Maggi CA

    更新日期：2002-10-21 00:00:00

  • Synthesis, anti-plasmodial and cytotoxic evaluation of 1H-1,2,3-triazole/acyl hydrazide integrated tetrahydro-β-carboline-4-aminoquinoline conjugates.

    abstract：:A series of 1H-1,2,3-triazole/acylhydrazide-tethered tetrahydro-β-carboline-4-aminoquinoline conjugates was synthesized with an aim to study their anti-plasmodial structure-activity relationship. The presence of 1H-1,2,3-triazole-core along with a flexible alkyl chain length on aminoquinoline core has favourable influ...

    journal_title：Bioorganic & medicinal chemistry letters

    pub_type： 杂志文章

    doi：10.1016/j.bmcl.2019.126810

    authors： Sharma B,Kaur S,Legac J,Rosenthal PJ,Kumar V

    更新日期：2020-01-15 00:00:00

  • Synthesis and biological evaluation of new symmetric curcumin derivatives.

    abstract：:A series of novel curcumin bisacetamides aiming of enriching their biological activities have been synthesized. The synthesized compounds were screened for their in vitro antioxidant, anti-inflammatory and cytotoxic activities. All the compounds exhibited potent to good anti-inflammatory, antioxidant and noteworthy cy...

    journal_title：Bioorganic & medicinal chemistry letters

    pub_type： 杂志文章

    doi：10.1016/j.bmcl.2015.07.088

    authors： Sribalan R,Kirubavathi M,Banuppriya G,Padmini V

    更新日期：2015-10-01 00:00:00

  • Synthesis and antihormonal properties of novel 11β-benzoxazole-substituted steroids.

    abstract：:Early studies led to the identification of 11β-aryl-4',5'-dihydrospiro[estra-4,9-diene-17β,4'-oxazole] analogs with potent and more selective antiprogestational activity compared to antiglucocorticoid activity than mifepristone. In the present study, we replaced the 4'-dimethylaminophenyl group of mifepristone with th...

    journal_title：Bioorganic & medicinal chemistry letters

    pub_type： 杂志文章

    doi：10.1016/j.bmcl.2011.12.110

    authors： Jin C,Fix SE,Kepler JA,Cook CE

    更新日期：2012-02-15 00:00:00

  • Synthesis of 1,6,7,8-tetrahydro-naphtho[2,3-d]-azepino[4,5-b]indole-9,14-diones and their inhibitory effects on pro-inflammatory cytokines.

    abstract：:A rapid route to a series of naphthoquinone-fused indole derivatives via irradiation in a modified commercial domestic microwave is reported. The desired products were produced in high yields and short reaction times. The naphthoquinone-fused indole derivatives were evaluated for their pro-inflammatory cytokines respo...

    journal_title：Bioorganic & medicinal chemistry letters

    pub_type： 杂志文章

    doi：10.1016/j.bmcl.2009.07.154

    authors： Phutdhawong WS,Ruensamran W,Phutdhawong W,Taechowisan T

    更新日期：2009-10-01 00:00:00

  • Trithiocarbonates: exploration of a new head group for HDAC inhibitors.

    abstract：:Inhibition of histone deacetylases class I/II enzymes is a new, promising approach for cancer therapy. In the present study, we disclose a new structural class of HDAC inhibitors with the trithiocarbonate motif. A clear structure-activity-relationship was obtained for the cap-linker motif and the putative Zn(2+) compl...

    journal_title：Bioorganic & medicinal chemistry letters

    pub_type： 杂志文章

    doi：10.1016/j.bmcl.2007.06.063

    authors： Dehmel F,Ciossek T,Maier T,Weinbrenner S,Schmidt B,Zoche M,Beckers T

    更新日期：2007-09-01 00:00:00

  • 10-Hydroxy-7,8-dihydropyrazino[1',2':1,5]pyrrolo[2,3-d]pyridazine-1,9(2H,6H)-diones: potent, orally bioavailable HIV-1 integrase strand-transfer inhibitors with activity against integrase mutants.

    abstract：:A series of 10-hydroxy-7,8-dihydropyrazino[1',2':1,5]pyrrolo[2,3-d]pyridazine-1,9(2H,6H)-diones was synthesized and tested for their inhibition of HIV-1 replication in cell culture. Structure-activity studies indicated that high antiviral potency against wild-type virus as well as viruses containing integrase mutation...

    journal_title：Bioorganic & medicinal chemistry letters

    pub_type： 杂志文章

    doi：10.1016/j.bmcl.2008.07.037

    authors： Wiscount CM,Williams PD,Tran LO,Embrey MW,Fisher TE,Sherman V,Homnick CF,Donnette Staas D,Lyle TA,Wai JS,Vacca JP,Wang Z,Felock PJ,Stillmock KA,Witmer MV,Miller MD,Hazuda DJ,Day AM,Gabryelski LJ,Ecto LT,Schleif WA

    更新日期：2008-08-15 00:00:00

  • Structure-activity and in vivo evaluation of a novel lipoprotein lipase (LPL) activator.

    abstract：:Elevated triglycerides (TG) contribute towards increased risk for cardiovascular disease. Lipoprotein lipase (LPL) is an enzyme that is responsible for the metabolism of core triglycerides of very-low density lipoproteins (VLDL) and chylomicrons in the vasculature. In this study, we explored the structure-activity rel...

    journal_title：Bioorganic & medicinal chemistry letters

    pub_type： 杂志文章

    doi：10.1016/j.bmcl.2016.11.053

    authors： Geldenhuys WJ,Caporoso J,Leeper TC,Lee YK,Lin L,Darvesh AS,Sadana P

    更新日期：2017-01-15 00:00:00