当前位置： SCI文献检索 > EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY期刊下所有文献 > Towards the development of 5-HT₇ ligands combining serotonin-like and arylpiperazine moieties.

Towards the development of 5-HT₇ ligands combining serotonin-like and arylpiperazine moieties.

Abstract：

:Many known 5-HT7 ligands contain either a serotonin-like or an arylpiperazine structure that, in published SAR studies, are generally supposed to bind the same receptor pocket. Conversely, we explored the hypothesis that two such moieties can co-exist in the same ligand, binding to different pockets. We thus designed and synthesized a set of compounds including both a 5-hydroxyindol-3-ylethyl and a 1-arylpiperazine moieties connected by a short linker. The compounds were tested for their affinity for human 5-HT7 serotonin receptor. We further prepared a novel series of 5-HT7 ligands, where the 5-hydroxyindol-3-ylethyl moiety was bioisosterically replaced by a 3-hydroxyanilinoalkyl one. Among the newly synthesized compounds, potent ligands at the 5-HT7 receptor, behaving as antagonists in functional tests, were identified, even if they showed limited subtype selectivity. Docking studies within a model of the 5-HT7 receptor showed that the binding site can actually accommodate both moieties, with the serotonin-like one in the putative orthosteric site and the arylpiperazine one occupying an accessory pocket. The present results demonstrate that it is possible to devise and develop new 5-HT7 ligands merging two privileged structures in the same molecule.

journal_name

Eur J Med Chem

journal_title

European journal of medicinal chemistry

authors

Spadoni G,Bedini A,Bartolucci S,Pala D,Mor M,Riccioni T,Borsini F,Cabri W,Celona D,Marzi M,Tarzia G,Rivara S,Minetti P

doi

10.1016/j.ejmech.2014.04.034

subject

Has Abstract

pub_date

2014-06-10 00:00:00

pages

8-35

eissn

0223-5234

issn

1768-3254

pii

S0223-5234(14)00355-9

journal_volume

80

pub_type

杂志文章

相关文献

EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY文献大全
  • One-pot microwave assisted synthesis of new 2-alkoxycarbonylmethylene-4-oxo-1,5-benzo-, naphtho-, and pyridodiazepines and assessment of their cytogenetic activity.

    abstract：:1,5-Benzo-, naphtho-, and pyridodiazepines 3 have been synthesized in excellent yields in one-step from the reaction of o-phenylenediamines with acetonedicarboxylates through microwave assisted acid catalysis. In order to ascertain their cytogenetic activity in vitro at doses equivalent to the per os doses of common 1...

    journal_title：European journal of medicinal chemistry

    pub_type： 杂志文章

    doi：10.1016/j.ejmech.2013.06.028

    authors： Eleftheriadis N,Neochoritis CG,Tsoleridis CA,Stephanidou-Stephanatou J,Iakovidou-Kritsi Z

    更新日期：2013-09-01 00:00:00

  • Synthesis and biological activity of novel N6-substituted and 2,N6-disubstituted adenine ribo- and 3'-C-methyl-ribonucleosides as antitumor agents.

    abstract：:A series of N6-aminopurine-9-β-D-ribonucleosides and ribose-modified 3'-C-methyl analogues substituted at N6-position with a small group like hydroxy, methoxy or amino group or at C2(N6) position have been synthesized and tested against a panel of human leukemia and carcinoma cell lines. N6-Hydrazino-9-β-D-ribofuranos...

    journal_title：European journal of medicinal chemistry

    pub_type： 杂志文章

    doi：10.1016/j.ejmech.2011.01.055

    authors： Cappellacci L,Petrelli R,Franchetti P,Vita P,Kusumanchi P,Kumar M,Jayaram HN,Zhou B,Yen Y,Grifantini M

    更新日期：2011-05-01 00:00:00

  • Thioether-based 2-aminobenzamide derivatives: Novel HDAC inhibitors with potent in vitro and in vivo antitumor activity.

    abstract：:Previously, we focused on a series of 2-aminobenzamide-based histone deacetylase (HDAC) inhibitors, compound 9 of which displayed potent HDAC inhibitory activity against HDAC1 and HDAC2, and moderate anti-proliferative activity against several cancer cell lines. In the current study, we have designed and synthesized a...

    journal_title：European journal of medicinal chemistry

    pub_type： 杂志文章

    doi：10.1016/j.ejmech.2019.05.007

    authors： Yun F,Cheng C,Ullah S,He J,Zahi MR,Yuan Q

    更新日期：2019-08-15 00:00:00

  • In vitro PAI-1 inhibitory activity of oxalamide derivatives.

    abstract：:A number of oxalamide derivatives have been synthesized and evaluated for PAI-1 inhibitory activity. In vitro PAI-1 inhibitory activities of oxalamide derivatives are evaluated by chromogenic assay. Few compounds have shown significant PAI-1 inhibitory activity. ...

    journal_title：European journal of medicinal chemistry

    pub_type： 杂志文章

    doi：10.1016/j.ejmech.2007.05.011

    authors： Jain MR,Shetty S,Chakrabarti G,Pandya V,Sharma A,Parmar B,Srivastava S,Raviya M,Soni H,Patel PR

    更新日期：2008-04-01 00:00:00

  • (5aR)-5a-C-Pentyl-4-epi-isofagomine: A powerful inhibitor of lysosomal β-galactosidase and a remarkable chaperone for mutations associated with GM1-gangliosidosis and Morquio disease type B.

    abstract：:This report is about the identification, synthesis and initial biological characterization of derivatives of 4-epi-isofagomine as pharmacological chaperones (PC) for human lysosomal β-galactosidase. The two epimers of 4-epi-isofagomine carrying a pentyl group at C-5a, namely (5aR)- and (5aS)-5a-C-pentyl-4-epi-isofagom...

    journal_title：European journal of medicinal chemistry

    pub_type： 杂志文章

    doi：10.1016/j.ejmech.2016.09.095

    authors： Front S,Biela-Banaś A,Burda P,Ballhausen D,Higaki K,Caciotti A,Morrone A,Charollais-Thoenig J,Gallienne E,Demotz S,Martin OR

    更新日期：2017-01-27 00:00:00

  • Discovery of anxiolytic 2-ferrocenyl-1,3-thiazolidin-4-ones exerting GABAA receptor interaction via the benzodiazepine-binding site.

    abstract：:Herein, we report on the synthesis, spectral, crystallographic and electrochemical properties of a small library of N-substituted 2-ferrocenyl-1,3-thiazolidin-4-ones, designed as novel GABAA benzodiazepine-binding site ligands. The anxiolytic properties of the title compounds were evaluated in several different in viv...

    journal_title：European journal of medicinal chemistry

    pub_type： 杂志文章

    doi：10.1016/j.ejmech.2014.05.062

    authors： Pejović A,Denić MS,Stevanović D,Damljanović I,Vukićević M,Kostova K,Tavlinova-Kirilova M,Randjelović P,Stojanović NM,Bogdanović GA,Blagojević P,D'hooghe M,Radulović NS,Vukićević RD

    更新日期：2014-08-18 00:00:00

  • Synthesis and structure-activity relationships of guaiane-type sesquiterpene lactone derivatives with respect to inhibiting NO production in lipopolysaccharide-induced RAW 264.7 macrophages.

    abstract：:A guaiane framework was scaffolded by photochemical rearrangement reactions using α-santonin 1 as a starting material. Then, using a series of reactions, we synthesized the guaiane-type sesquiterpene lactone 5 in high yield. The inhibitory activities of compound 5 and of a series of derivatives on nitric oxide (NO) re...

    journal_title：European journal of medicinal chemistry

    pub_type： 杂志文章

    doi：10.1016/j.ejmech.2014.06.043

    authors： Chen H,Chen BY,Liu CT,Zhao Z,Shao WH,Yuan H,Bi KJ,Liu JY,Sun QY,Zhang WD

    更新日期：2014-08-18 00:00:00

  • Antifungal activities of novel non-azole molecules against S. cerevisiae and C. albicans.

    abstract：:Because of the increasing number of immunocompromised patients and due to problems with antifungal treatment, especially with the most widely used antifungals, azoles, there is an urgent need for new, potent and safe antifungals with fewer cytochrome P450 (CYP)-mediated interactions with other drugs. In the present st...

    journal_title：European journal of medicinal chemistry

    pub_type： 杂志文章

    doi：10.1016/j.ejmech.2011.10.053

    authors： Tani N,Rahnasto-Rilla M,Wittekindt C,Salminen KA,Ritvanen A,Ollakka R,Koskiranta J,Raunio H,Juvonen RO

    更新日期：2012-01-01 00:00:00

  • Benzo[d]thiazol-2(3H)-ones as new potent selective CB2 agonists with anti-inflammatory properties.

    abstract：:The high distribution of CB2 receptors in immune cells suggests their important role in the control of inflammation. Growing evidence offers this receptor as an attractive therapeutic target: selective CB2 agonists are able to modulate inflammation without triggering psychotropic effects. In this work, we report a new...

    journal_title：European journal of medicinal chemistry

    pub_type： 杂志文章

    doi：10.1016/j.ejmech.2018.12.008

    authors： Leleu-Chavain N,Baudelet D,Heloire VM,Rocha DE,Renault N,Barczyk A,Djouina M,Body-Malapel M,Carato P,Millet R

    更新日期：2019-03-01 00:00:00

  • Asymmetric 1,5-diarylpenta-1,4-dien-3-ones: Antiproliferative activity in prostate epithelial cell models and pharmacokinetic studies.

    abstract：:To further engineer dienones with optimal combinations of potency and bioavailability, thirty-four asymmetric 1,5-diarylpenta-1,4-dien-3-ones (25-58) have been designed and synthesized for the evaluation of their in vitro anti-proliferative activity in three human prostate cancer cell lines and one non-neoplastic pros...

    journal_title：European journal of medicinal chemistry

    pub_type： 杂志文章

    doi：10.1016/j.ejmech.2017.05.062

    authors： Zhang X,Guo S,Chen C,Perez GR,Zhang C,Patanapongpibul M,Subrahmanyam N,Wang R,Keith J,Chen G,Dong Y,Zhang Q,Zhong Q,Zheng S,Wang G,Chen QH

    更新日期：2017-09-08 00:00:00

  • Synthesis and SAR studies of mono O-prenylated coumarins as potent 15-lipoxygenase inhibitors.

    abstract：:All of the mono isopentenyloxy, -geranyloxy and -farnesyloxy derivatives of coumarin were synthesized and their inhibitory potency against soybean 15-lipoxygenase (SLO) and human 15-lipoxygenase-1 (HLO-1) were determined. Amongst the synthetic analogs, 5-farnesyloxycoumarin showed the most potent inhibitory activity a...

    journal_title：European journal of medicinal chemistry

    pub_type： 杂志文章

    doi：10.1016/j.ejmech.2012.09.006

    authors： Iranshahi M,Jabbari A,Orafaie A,Mehri R,Zeraatkar S,Ahmadi T,Alimardani M,Sadeghian H

    更新日期：2012-11-01 00:00:00

  • Design and synthesis of some new pyrazolyl-pyrazolines as potential anti-inflammatory, analgesic and antibacterial agents.

    abstract：:In the present study, an efficient synthesis of some new substituted pyrazoline derivatives linked to a substituted pyrazole scaffold was performed by a multistep reaction sequences and compounds were screened for their anti-inflammatory, analgesic and antibacterial activities. The preliminary results revealed that th...

    journal_title：European journal of medicinal chemistry

    pub_type： 杂志文章

    doi：10.1016/j.ejmech.2015.07.002

    authors： Viveka S,Dinesha,Shama P,Nagaraja GK,Ballav S,Kerkar S

    更新日期：2015-08-28 00:00:00

  • Discovery of 4-phenyl-2H-benzo[b][1,4]oxazin-3(4H)-one derivatives as potent and orally active PI3K/mTOR dual inhibitors.

    abstract：:PI3K/Akt/mTOR signaling pathway plays an important role in cancer cell growth and survival. In this study, a new class of molecules with skeleton of 4-phenyl-2H-benzo[b] [1,4]oxazin-3(4H)-one were designed and synthesized targeting this pathway. Bioassays showed that, among all the molecules, 8d-1 was a pan-class I PI...

    journal_title：European journal of medicinal chemistry

    pub_type： 杂志文章

    doi：10.1016/j.ejmech.2019.06.021

    authors： Yan G,Pu C,Lan S,Zhong X,Zhou M,Hou X,Yang J,Shan H,Zhao L,Li R

    更新日期：2019-09-15 00:00:00

  • Potent naphthoquinones against antimony-sensitive and -resistant Leishmania parasites: synthesis of novel α- and nor-α-lapachone-based 1,2,3-triazoles by copper-catalyzed azide-alkyne cycloaddition.

    abstract：:Continuing our screening program for novel anti-parasite compounds, we synthesized seven 1,4-naphthoquinones coupled to 1,2,3-triazoles, five nor-β-lapachone-based 1,2,3-triazoles and ten α-lapachone-based 1,2,3-triazoles. These and other naphthoquinonoid compounds were evaluated for their activity against promastigot...

    journal_title：European journal of medicinal chemistry

    pub_type： 杂志文章

    doi：10.1016/j.ejmech.2013.02.038

    authors： Guimarães TT,Pinto Mdo C,Lanza JS,Melo MN,do Monte-Neto RL,de Melo IM,Diogo EB,Ferreira VF,Camara CA,Valença WO,de Oliveira RN,Frézard F,da Silva EN Jr

    更新日期：2013-05-01 00:00:00

  • Clubbed triazoles: a novel approach to antitubercular drugs.

    abstract：:In last few decades, though significant progress has been made in the treatment and control strategies of tubercular infections by introducing new diagnostic and monitoring tools and combination therapy, it still continues to be a severe problem. Thus with the aim of developing novel molecules with improved potency fo...

    journal_title：European journal of medicinal chemistry

    pub_type： 杂志文章

    doi：10.1016/j.ejmech.2006.12.001

    authors： Shiradkar M,Suresh Kumar GV,Dasari V,Tatikonda S,Akula KC,Shah R

    更新日期：2007-06-01 00:00:00

  • New glycosidic derivatives of histidine-containing dipeptides with antioxidant properties and resistant to carnosinase activity.

    abstract：:Synthesis, antioxidant properties and resistance to carnosinase hydrolysis of histidine-containing dipeptides are reported in this study. Carnosine (beta-alanyl-l-histidine), homocarnosine (gamma-aminobutyryl-l-histidine) and anserine (beta-alanyl-3-methyl-l-histidine) were covalently derivatized with beta-cyclodextri...

    journal_title：European journal of medicinal chemistry

    pub_type： 杂志文章

    doi：10.1016/j.ejmech.2007.03.038

    authors： Bellia F,Amorini AM,La Mendola D,Vecchio G,Tavazzi B,Giardina B,Di Pietro V,Lazzarino G,Rizzarelli E

    更新日期：2008-02-01 00:00:00

  • Synthesis and biological evaluation of (1,2,4)triazole[4,3-a]pyridine derivatives as potential therapeutic agents for concanavalin A-induced hepatitis.

    abstract：:A series of (1,2,4)triazole[4,3-a]pyridine (TZP) derivatives have been designed and synthesized. Compound 8d was identified as having the most potent inhibitory activity on NO release in response to lipopolysaccharide (LPS) stimulation and inhibition of the migration induced by MCP-1 protein on RAW264.7 macrophages. B...

    journal_title：European journal of medicinal chemistry

    pub_type： 杂志文章

    doi：10.1016/j.ejmech.2019.06.025

    authors： Shi Y,Wang Q,Rong J,Ren J,Song X,Fan X,Shen M,Xia Y,Wang N,Liu Z,Hu Q,Ye T,Yu L

    更新日期：2019-10-01 00:00:00

  • Discovery of carboxyl-containing biaryl ureas as potent RORγt inverse agonists.

    abstract：:GSK805 (1) is a potent RORγt inverse agonist, but a drawback of 1 is its low solubility, leading to a limited absorption in high doses. We have explored detailed structure-activity relationship on the amide linker, biaryl and arylsulfonyl moieties of 1 trying to improve solubility while maintaining RORγt activity. As ...

    journal_title：European journal of medicinal chemistry

    pub_type： 杂志文章

    doi：10.1016/j.ejmech.2020.112536

    authors： Sun N,Huang Y,Yu M,Zhao Y,Chen JA,Zhu C,Song M,Guo H,Xie Q,Wang Y

    更新日期：2020-09-15 00:00:00

  • Design, synthesis and biological evaluation of uncharged catechol derivatives as selective inhibitors of PTP1B.

    abstract：:Protein tyrosine phosphatases 1B (PTP1B) is a promising and validated therapeutic target to effectively treat T2DM and obesity. However, the development of charged PTP1B inhibitors was restricted due to their low cell permeability and poor bioavailability. Based on active natural products, two series of uncharged cate...

    journal_title：European journal of medicinal chemistry

    pub_type： 杂志文章

    doi：10.1016/j.ejmech.2017.05.007

    authors： Li XQ,Xu Q,Luo J,Wang LJ,Jiang B,Zhang RS,Shi DY

    更新日期：2017-08-18 00:00:00

  • Design, synthesis, and fungicidal evaluation of a series of novel 5-methyl-1H-1,2,3-trizole-4-carboxyl amide and ester analogues.

    abstract：:Succinate dehydrogenase inhibitors (SDHIs) are efficient fungicides that are widely used to control plant diseases caused by phytopathogenic fungi, although their effectiveness is undermined by the development of resistance across a range of different fungi. One of the most common structural features of SDHIs is their...

    journal_title：European journal of medicinal chemistry

    pub_type： 杂志文章

    doi：10.1016/j.ejmech.2014.08.029

    authors： Wang ZJ,Gao Y,Hou YL,Zhang C,Yu SJ,Bian Q,Li ZM,Zhao WG

    更新日期：2014-10-30 00:00:00

  • Continued exploration of 1,2,4-oxadiazole periphery for carbonic anhydrase-targeting primary arene sulfonamides: Discovery of subnanomolar inhibitors of membrane-bound hCA IX isoform that selectively kill cancer cells in hypoxic environment.

    abstract：:An expanded set of diversely substituted 1,2,4-oxadiazole-containing primary aromatic sulfonamides was synthesized and tested for inhibition of human carbonic anhydrase I, II, IX and XII isoforms. The initial biochemical profiling revealed a significantly more potent inhibition of cancer-related, membrane-bound isofor...

    journal_title：European journal of medicinal chemistry

    pub_type： 杂志文章

    doi：10.1016/j.ejmech.2018.12.049

    authors： Krasavin M,Shetnev A,Sharonova T,Baykov S,Kalinin S,Nocentini A,Sharoyko V,Poli G,Tuccinardi T,Presnukhina S,Tennikova TB,Supuran CT

    更新日期：2019-02-15 00:00:00

  • 2-hydroxyisoquinoline-1,3(2H,4H)-diones as inhibitors of HIV-1 integrase and reverse transcriptase RNase H domain: influence of the alkylation of position 4.

    abstract：:We report herein the synthesis of a series of fifteen 2-hydroxyisoquinoline-1,3(2H,4H)-dione derivatives. Alkyl and arylalkyl groups were introduced on position 4 of the basis scaffold. All the compounds presented poor inhibitory properties against HIV-1 reverse transcriptase ribonuclease H (RNase H). Four compounds i...

    journal_title：European journal of medicinal chemistry

    pub_type： 杂志文章

    doi：10.1016/j.ejmech.2010.11.033

    authors： Billamboz M,Bailly F,Lion C,Calmels C,Andréola ML,Witvrouw M,Christ F,Debyser Z,De Luca L,Chimirri A,Cotelle P

    更新日期：2011-02-01 00:00:00

  • Design, synthesis and antiviral activity of novel quinazolinones.

    abstract：:HIV-1 integrase (IN) is a validated therapeutic target for antiviral drug design. However, the emergence of viral strains resistant to clinically studied IN inhibitors demands the discovery of novel inhibitors that are structurally as well as mechanistically different. Herein, a series of quinazolinones were designed ...

    journal_title：European journal of medicinal chemistry

    pub_type： 杂志文章

    doi：10.1016/j.ejmech.2012.04.010

    authors： Wang Z,Wang M,Yao X,Li Y,Tan J,Wang L,Qiao W,Geng Y,Liu Y,Wang Q

    更新日期：2012-07-01 00:00:00

  • Synthesis of a new series of heterocyclic scaffolds for medicinal purposes.

    abstract：:A new series of substituted 8-fluro-4H-pyrimido[2,1-b] [1,3]benzothiazole-4-ones () substituted 7-methyl-4H-isoxazolo[2,3-a]pyrimidin-4-ones, and substituted 2-methyl-5,6,7,8-tetrahydro-9H-isoxazolo[2,3-a]pyridopyrimidin-9-ones, compounds I-VII, have been prepared via condensation of beta-keto esters with 2-aminopyrid...

    journal_title：European journal of medicinal chemistry

    pub_type： 杂志文章

    doi：10.1016/j.ejmech.2006.03.025

    authors： Hilal HS,Ali-Shtayeh MS,Arafat R,Al-Tel T,Voelter W,Barakat A

    更新日期：2006-08-01 00:00:00

  • Synthesis, characterization and in vitro biological activity studies of Cu-M (M = Cu2+, Co2+, Ni2+, Mn2+, Zn2+) bimetallic complexes.

    abstract：:Six new bimetallic complexes of the type CuCu, CuCo, CuNi, CuZn and CuMn were prepared. The structures of these complexes and the ligand have been proposed on the basis of FAB mass, elemental analysis, UV-vis, IR, EPR and CV studies. All the complexes completely cleave pBS (SK-) DNA at a concentration of 10 microM; ho...

    journal_title：European journal of medicinal chemistry

    pub_type： 杂志文章

    doi：10.1016/j.ejmech.2005.11.016

    authors： Rupesh KR,Deepalatha S,Krishnaveni M,Venkatesan R,Jayachandran S

    更新日期：2006-12-01 00:00:00

  • New bis(hydroxymethyl) alkanoate curcuminoid derivatives exhibit activity against triple-negative breast cancer in vitro and in vivo.

    abstract：:Novel bis(hydroxymethyl) alkanoate curcuminoid derivatives were designed, synthesized and screened for in vitro antiproliferative and in vivo antitumor activity. Selected new compound 9a and curcumin were further evaluated for inhibitory activity against ER+/PR+ breast cancer (MCF-7, T47D), HER 2+ breast cancer (SKBR3...

    journal_title：European journal of medicinal chemistry

    pub_type： 杂志文章

    doi：10.1016/j.ejmech.2017.03.006

    authors： Hsieh MT,Chang LC,Hung HY,Lin HY,Shih MH,Tsai CH,Kuo SC,Lee KH

    更新日期：2017-05-05 00:00:00

  • Discovery of pyrazole as C-terminus of selective BACE1 inhibitors.

    abstract：:We recently discovered and reported dual inhibitor 5 of AChE and BACE1 with N-benzylpiperidine ethyl as C-terminus. Compound 5 showed potent inhibitory activities for BACE1, and could reduce endogenous Aβ1-40 production in APP transgenic mice. In present work, we rapidly identified substituted triazole as the C-termin...

    journal_title：European journal of medicinal chemistry

    pub_type： 杂志文章

    doi：10.1016/j.ejmech.2013.06.027

    authors： Zou Y,Xu L,Chen W,Zhu Y,Chen T,Fu Y,Li L,Ma L,Xiong B,Wang X,Li J,He J,Zhang H,Xu Y,Li J,Shen J

    更新日期：2013-10-01 00:00:00

  • PRODRUGS FOR NITROREDUCTASE BASED CANCER THERAPY- 2: Novel amide/Ntr combinations targeting PC3 cancer cells.

    abstract：:The use of nitroreductases (NTR) that catalyze the reduction of nitro compounds by using NAD(P)H in GDEPT (Gene-directed enzyme prodrug therapy) studies which minimize toxicity at healthy cells and increases concentration of drugs at cancer cells is remarkable. Discovery of new prodrug/NTR combinations is necessary to...

    journal_title：European journal of medicinal chemistry

    pub_type： 杂志文章

    doi：10.1016/j.ejmech.2019.03.035

    authors： Güngör T,Önder FC,Tokay E,Gülhan ÜG,Hacıoğlu N,Tok TT,Çelik A,Köçkar F,Ay M

    更新日期：2019-06-01 00:00:00

  • Design, synthesis, and biodistribution studies of new analogues of marine alkaloids: Potent in vitro and in vivo fungicidal agents against Candida spp.

    abstract：:Invasive candidiasis, such as intra-abdominal candidiasis (IAC), is a significant cause of morbidity and mortality worldwide. IAC is still poorly understood, and its treatment represents a challenge for public health. In this study, we showed the in vitro anti-Candida activity of four alkaloid synthetic derivatives an...

    journal_title：European journal of medicinal chemistry

    pub_type： 杂志文章

    doi：10.1016/j.ejmech.2020.113048

    authors： Andrade JT,Lima WG,Sousa JF,Saldanha AA,Nívea Pereira De Sá,Morais FB,Prates Silva MK,Ribeiro Viana GH,Johann S,Soares AC,Araújo LA,Antunes Fernandes SO,Cardoso VN,Siqueira Ferreira JM

    更新日期：2021-01-15 00:00:00

  • Stereoselective synthesis and biological evaluation of (R)-rugulactone, (6R)-((4R)-hydroxy-6-phenyl-hex-2-enyl)-5,6-dihydro-pyran-2-one and its 4S epimer.

    abstract：:A simple and highly efficient synthetic route has been developed for synthesis of (R)-rugulactone (1a), (6R)-((4R)-hydroxy-6-phenyl-hex-2-enyl)-5,6-dihydro-pyran-2-one (1b) and its 4S epimer 1c by employing proline-catalyzed alpha-aminooxylation, Sharpless epoxidation, Mitsunobu reaction as chirality introuducing step...

    journal_title：European journal of medicinal chemistry

    pub_type： 杂志文章

    doi：10.1016/j.ejmech.2010.07.036

    authors： Reddy DK,Shekhar V,Prabhakar P,Chinna Babu B,Siddhardha B,Murthy US,Venkateswarlu Y

    更新日期：2010-10-01 00:00:00