2-Azetidinone derivatives: design, synthesis and evaluation of cholesterol absorption inhibitors.


:Fourteen new derivatives of the 2-azetidinone cholesterol absorption inhibitors have been synthesized, and three of them were enantiomerically pure. All the new compounds were evaluated for their activity to inhibit cholesterol absorption in rats, and most of them showed comparable effects in lowering the levels of total cholesterol in the serum.


Eur J Med Chem


Wang Y,Zhang H,Huang W,Kong J,Zhou J,Zhang B




Has Abstract


2009-04-01 00:00:00














  • Synthesis and in vitro anticancer activity evaluation of novel bioreversible phosphate inositol derivatives.

    abstract::The chemistry and biology of phosphorylated inositols have become intense areas of research during the last two decades due to their involvement in various cellular signaling processes. However, the metabolic instability by phosphatases or kinases and poor penetration make it difficult to become a drug used in the cli...

    journal_title:European journal of medicinal chemistry

    pub_type: 杂志文章


    authors: Chen W,Deng Z,Chen K,Dou D,Song F,Li L,Xi Z

    更新日期:2015-03-26 00:00:00

  • Synthesis, analgesic and anti-inflammatory activities evaluation of some bi-, tri- and tetracyclic condensed pyrimidines.

    abstract::Novel series of bicyclic pyrrolo[1,2-c]pyrimidines 3a-g, 5, 6a, b, and 7a, b, tricyclic pyrimido[5,4-e]pyrrolo[1,2-c]pyrimidines 8a-c, 9a-g, 13a-c, 17, 18a, b, 19, 20a,b and 21 and tetracyclic condensed pyrimidines 14, 22 and 23 were synthesized through different chemical reactions. Structures of all synthesized pyrim...

    journal_title:European journal of medicinal chemistry

    pub_type: 杂志文章


    authors: Amin KM,Hanna MM,Abo-Youssef HE,George RF

    更新日期:2009-11-01 00:00:00

  • X-ray crystal structures of Enterococcus faecalis thymidylate synthase with folate binding site inhibitors.

    abstract::Infections caused by Enterococcus faecalis (Ef) represent nowadays a relevant health problem. We selected Thymidylate synthase (TS) from this organism as a potential specific target for antibacterial therapy. We have previously demonstrated that species-specific inhibition of the protein can be achieved despite the re...

    journal_title:European journal of medicinal chemistry

    pub_type: 杂志文章


    authors: Catalano A,Luciani R,Carocci A,Cortesi D,Pozzi C,Borsari C,Ferrari S,Mangani S

    更新日期:2016-11-10 00:00:00

  • Diverse chemical space of indoleamine-2,3-dioxygenase 1 (Ido1) inhibitors.

    abstract::Indoleamine-2,3-dioxygenase 1 (IDO1) catalyses the first and rate limiting step of kynurenine pathway accounting for the major contributor of L-Tryptophan degradation. The Kynurenine metabolites are identified as essential cofactors, antagonists, neurotoxins, immunomodulators, antioxidants as well as carcinogens. The ...

    journal_title:European journal of medicinal chemistry

    pub_type: 杂志文章,评审


    authors: Singh R,Salunke DB

    更新日期:2021-02-05 00:00:00

  • Natural oxyprenylated coumarins are modulators of melanogenesis.

    abstract::Naturally occurring coumarins 7-isopentenyloxycoumarin, auraptene, and umbelliprenin are able to modulate the biosynthesis of melanin in murine Melan-a cells probably through the interaction with selected biological targets like estrogen receptor β and aryl hydrocarbon receptor. Such a modulation strictly depends on t...

    journal_title:European journal of medicinal chemistry

    pub_type: 杂志文章


    authors: Fiorito S,Epifano F,Preziuso F,Cacciatore I,di Stefano A,Taddeo VA,de Medina P,Genovese S

    更新日期:2018-05-25 00:00:00

  • Synthesis and pharmacological evaluation of novel 5-substituted-1-(phenylsulfonyl)-2-methylbenzimidazole derivatives as anti-inflammatory and analgesic agents.

    abstract::A series of novel 5-substituted-1-(phenylsulfonyl)-2-methylbenzimidazole derivatives have been synthesized. The structures of these compounds were established by IR, 1H NMR, 13C NMR, Mass spectral data and elemental analyses. Compounds were evaluated for their anti-inflammatory and analgesic activity as well as gastri...

    journal_title:European journal of medicinal chemistry

    pub_type: 杂志文章


    authors: Gaba M,Singh D,Singh S,Sharma V,Gaba P

    更新日期:2010-06-01 00:00:00

  • Synthesis of antiplatelet ortho-carbonyl hydroquinones with differential action on platelet aggregation stimulated by collagen or TRAP-6.

    abstract::Cardiovascular diseases are the leading cause of death in the world. Platelets have a major role in cardiovascular events as they bind to the damaged endothelium activating and forming thrombi. Although some hydroquinone scaffold-containing compounds have known antiplatelet activities, currently there is a lack of evi...

    journal_title:European journal of medicinal chemistry

    pub_type: 杂志文章


    authors: Méndez D,Urra FA,Millas-Vargas JP,Alarcón M,Rodríguez-Lavado J,Palomo I,Trostchansky A,Araya-Maturana R,Fuentes E

    更新日期:2020-04-15 00:00:00

  • Synthesis and evaluation of in vitro anti-microbial and anti-tubercular activity of 2-styryl benzimidazoles.

    abstract::A new series of novel 5-(nitro/bromo)-styryl-2-benzimidazoles (1-12) has been synthesized by simple, mild and efficient synthetic protocol by attempted condensation of 5-(nitro/bromo)-o-phenylenediamine with trans-cinnamic acids in ethylene glycol. Screening for in vitro anti-tubercular activity against Mycobacterium ...

    journal_title:European journal of medicinal chemistry

    pub_type: 杂志文章


    authors: Shingalapur RV,Hosamani KM,Keri RS

    更新日期:2009-10-01 00:00:00

  • Synthesis, antimicrobial, antimycobacterial and structure-activity relationship of substituted pyrazolo-, isoxazolo-, pyrimido- and mercaptopyrimidocyclohepta[b]indoles.

    abstract::A new class of heterocycles, specifically substituted pyrazolo-, isoxazolo- and pyrimidocyclohepta[b]indoles, has been prepared by condensation of substituted 7-(hydroxymethylene)-7,8,9,10-tetrahydrocyclohepta[b]indol-6(5H)-ones with hydrazine hydrate, hydroxylamine hydrochloride, phenylhydrazine, urea and thiourea, r...

    journal_title:European journal of medicinal chemistry

    pub_type: 杂志文章


    authors: Yamuna E,Kumar RA,Zeller M,Rajendra Prasad KJ

    更新日期:2012-01-01 00:00:00

  • Synthesis and neuromuscular blocking activity of 16beta-piperidinosteroidal derivatives.

    abstract::The synthesis and pharmacological profiles of some new steroidal mono- and bisquaternary ammonium derivatives have been described. The compounds featured have been conceptually derived structurally from two lead structures: pancuronium bromide 1 and chandonium iodide 2. In vitro and in vivo neuromuscular blocking stud...

    journal_title:European journal of medicinal chemistry

    pub_type: 杂志文章


    authors: Jindal DP,Piplani P,Fajrak H,Prior C,Marshall IG

    更新日期:2001-02-01 00:00:00

  • Activity and molecular modeling of a new small molecule active against NNRTI-resistant HIV-1 mutants.

    abstract::In this preliminary study we report the antiviral screening of triazolo[4,5-g]quinoline derivatives (compounds 1-6). 4,9-Dihydrotriazolo[4,5-g]quinoline-1-oxide (1) stood out as a new, small molecule endowed with a selective, promising activity in cell-based assays against HIV-1wt and clinically relevant NNRTI resista...

    journal_title:European journal of medicinal chemistry

    pub_type: 杂志文章


    authors: Carta A,Pricl S,Piras S,Fermeglia M,La Colla P,Loddo R

    更新日期:2009-12-01 00:00:00

  • 5D-QSAR for spirocyclic sigma1 receptor ligands by Quasar receptor surface modeling.

    abstract::Based on a contiguous and structurally as well as biologically diverse set of 87 sigma(1) ligands, a 5D-QSAR study was conducted in which a quasi-atomistic receptor surface modeling approach (program package Quasar) was applied. The superposition of the ligands was performed with the tool Pharmacophore Elucidation (MO...

    journal_title:European journal of medicinal chemistry

    pub_type: 杂志文章


    authors: Oberdorf C,Schmidt TJ,Wünsch B

    更新日期:2010-07-01 00:00:00

  • Synthesis and biological screening of 2'-aryl/benzyl-2-aryl-4-methyl-4',5-bithiazolyls as possible anti-tubercular and antimicrobial agents.

    abstract::A series of 2'-aryl/benzyl-2-aryl-4-methyl-4',5-bithiazolyl derivatives, 25-64 were synthesized and evaluated for inhibitory activity against Mycobacterium smegmatis MC(2) 155 strain and antimicrobial activities against four pathogenic bacteria Bacillus subtilis, Staphylococcus aureus, Escherichia coli and Proteus vul...

    journal_title:European journal of medicinal chemistry

    pub_type: 杂志文章


    authors: Abhale YK,Sasane AV,Chavan AP,Deshmukh KK,Kotapalli SS,Ummanni R,Sayyad SF,Mhaske PC

    更新日期:2015-04-13 00:00:00

  • The evaluation of 1,4-benzoquinones as inhibitors of human monoamine oxidase.

    abstract::The monoamine oxidase (MAO) enzymes are of considerable pharmacological interest and inhibitors are used in the clinic for the treatment of major depressive disorder and Parkinson's disease. A limited number of studies have shown that the quinone class of compounds possesses MAO inhibition properties. Most notable amo...

    journal_title:European journal of medicinal chemistry

    pub_type: 杂志文章


    authors: Mostert S,Petzer A,Petzer JP

    更新日期:2017-07-28 00:00:00

  • Studies on quinones. Part 46. Synthesis and in vitro antitumor evaluation of aminopyrimidoisoquinolinequinones.

    abstract::In the search of structure-activity relationship studies and to explore the antitumor effect associated with the pyrimidoisoquinolinequinone scaffold, several diversily substituted 8-aminopyrimido[4,5-c]isoquinolinequinones were regioselectively synthesized. Variation in the structure of the nitrogen substituent bonde...

    journal_title:European journal of medicinal chemistry

    pub_type: 杂志文章


    authors: Vásquez D,Rodríguez JA,Theoduloz C,Calderon PB,Valderrama JA

    更新日期:2010-11-01 00:00:00

  • Synthesis and anti-cancer activity evaluation of 5-(2-carboxyethenyl)-isatin derivatives.

    abstract::A series of novel di- or trisubstituted isatin derivatives were designed and synthesized in 5-6 steps in 25-45% overall yields. Their structures were confirmed by 1H NMR and 13C NMR as well as LC-MS. The anticancer activity of the fourty-three new isatin derivatives against human T lymphocyte cells Jurkat was evaluate...

    journal_title:European journal of medicinal chemistry

    pub_type: 杂志文章


    authors: Teng YO,Zhao HY,Wang J,Liu H,Gao ML,Zhou Y,Han KL,Fan ZC,Zhang YM,Sun H,Yu P

    更新日期:2016-04-13 00:00:00

  • Mediterranean products as promising source of multi-target agents in the treatment of metabolic syndrome.

    abstract::Alteration of nutritional habits play an essential role on the risk of developing Metabolic Syndrome (MetS). Several epidemiological studies have shown that assuming diets rich of foods included in the Mediterranean diet (MetDiet) pattern like, such as olive oil, nuts, fruit, fiber, vegetables, wine and grain cereals ...

    journal_title:European journal of medicinal chemistry

    pub_type: 杂志文章,评审


    authors: Bagetta D,Maruca A,Lupia A,Mesiti F,Catalano R,Romeo I,Moraca F,Ambrosio FA,Costa G,Artese A,Ortuso F,Alcaro S,Rocca R

    更新日期:2020-01-15 00:00:00

  • Synthesis and biological evaluation of novel 2-aralkyl-5-substituted-6-(4'-fluorophenyl)-imidazo[2,1-b][1,3,4]thiadiazole derivatives as potent anticancer agents.

    abstract::Levamisole, the imidazo[2,1-b]thiazole derivative has been reported as a potential antitumor agent. In the present study, we synthesized, characterized and evaluated biological activity of its novel analogues with substitution in the aralkyl group and on imidazothiadiazole molecules with same chemical backbone but dif...

    journal_title:European journal of medicinal chemistry

    pub_type: 杂志文章


    authors: Karki SS,Panjamurthy K,Kumar S,Nambiar M,Ramareddy SA,Chiruvella KK,Raghavan SC

    更新日期:2011-06-01 00:00:00

  • Synthetic phenylethanoid glycoside derivatives as potent neuroprotective agents.

    abstract::Several phenylethanoid glycoside derivatives were designed and synthesized. Most of the synthetic compounds showed significant neuroprotective effects, including antioxidative and anti-apoptotic properties. Specifically, target compounds displayed potent effects against various toxicities such as H2O2 and 6-hydroxydop...

    journal_title:European journal of medicinal chemistry

    pub_type: 杂志文章


    authors: Liu YG,Li X,Xiong DC,Yu B,Pu X,Ye XS

    更新日期:2015-05-05 00:00:00

  • Synthesis, properties, and perspectives of gem-diphosphono substituted-thiazoles.

    abstract::A series of substituted arylidene thiazoles were allowed to react with Wittig-Horner (WH) reagent, tetraethyl methyl-1,1-bisphosphonate, to produce via Michael addition reaction the corresponding heteroarylmethylenebisphosphonates (BPs) in different yields according to the experimental conditions. Acid hydrolysis of t...

    journal_title:European journal of medicinal chemistry

    pub_type: 杂志文章


    authors: Abdou WM,Ganoub NA,Geronikaki A,Sabry E

    更新日期:2008-05-01 00:00:00

  • Identification of crizotinib derivatives as potent SHIP2 inhibitors for the treatment of Alzheimer's disease.

    abstract::SH2 domain-containing inositol 5'-phosphatase 2 (SHIP2) is a lipid phosphatase that produce phosphatidylinositol 3,4-bisphosphate (PI(3,4)P2) from phosphatidylinositol 3,4,5-triphosphate (PI(3,4,5)P3), and is involved in many diseases such as neurodegenerative diseases. A recent report demonstrating that SHIP2 inhibit...

    journal_title:European journal of medicinal chemistry

    pub_type: 杂志文章


    authors: Lim JW,Kim SK,Choi SY,Kim DH,Gadhe CG,Lee HN,Kim HJ,Kim J,Cho SJ,Hwang H,Seong J,Jeong KS,Lee JY,Lim SM,Lee JW,Pae AN

    更新日期:2018-09-05 00:00:00

  • Dual-functional conjugates improving cancer immunochemotherapy by inhibiting tubulin polymerization and indoleamine-2,3-dioxygenase.

    abstract::A series of novel conjugates comprising tublin and IDO inhibitors were designed, synthesized and evaluated for their antiproliferative activity. Among them, HI5, composed of combretastatin A-4 (CA-4) and (D)-1-methyltryptophan (D-MT) by a linker, exhibited the most potent antitumor activity, in particular with higher ...

    journal_title:European journal of medicinal chemistry

    pub_type: 杂志文章


    authors: Hua S,Chen F,Wang X,Gou S

    更新日期:2020-03-01 00:00:00

  • Covalent allosteric modulation: An emerging strategy for GPCRs drug discovery.

    abstract::Designing covalent allosteric modulators brings new opportunities to the field of drug discovery towards G-protein-coupled receptors (GPCRs). Targeting an allosteric binding pocket can allow a modulator to have protein subtype selectivity and low drug resistance. Utilizing covalent warheads further enables the modulat...

    journal_title:European journal of medicinal chemistry

    pub_type: 杂志文章,评审


    authors: Bian Y,Jun JJ,Cuyler J,Xie XQ

    更新日期:2020-11-15 00:00:00

  • Pyrrolo[1,2-f]phenanthridines and related non-rigid analogues as antiviral agents.

    abstract::The pyrrolo[1,2-f]phenanthridines 8-22 and the corresponding non-rigid analogues 23-41 were synthesised and their ability to inhibit the replication of HIV-1 was tested. Only the polycyclic derivatives 10, 11, and 13 showed a weak anti-HIV activity, whereas several pyrrolo-phenanthridines (8, 10, 16-18) were found to ...

    journal_title:European journal of medicinal chemistry

    pub_type: 杂志文章


    authors: Almerico AM,Mingoia F,Diana P,Barraja P,Montalbano A,Lauria A,Loddo R,Sanna L,Delpiano D,Setzu MG,Musiu C

    更新日期:2002-01-01 00:00:00

  • Understanding the chemistry behind the antioxidant activities of butylated hydroxytoluene (BHT): a review.

    abstract::Hindered phenols find a wide variety of applications across many different industry sectors. Butylated hydroxytoluene (BHT) is a most commonly used antioxidant recognized as safe for use in foods containing fats, pharmaceuticals, petroleum products, rubber and oil industries. In the past two decades, there has been gr...

    journal_title:European journal of medicinal chemistry

    pub_type: 杂志文章,评审


    authors: Yehye WA,Rahman NA,Ariffin A,Abd Hamid SB,Alhadi AA,Kadir FA,Yaeghoobi M

    更新日期:2015-08-28 00:00:00

  • Synthesis and anticancer evaluation of some new hydrazone derivatives of 2,6-dimethylimidazo[2,1-b][1,3,4]thiadiazole-5-carbohydrazide.

    abstract::In this study, some novel 2,6-dimethyl-N'-substituted phenylmethylene-imidazo[2,1-b][1,3,4]thiadiazole-5-carbohydrazides (3a-3h) were synthesized from 2,6-dimethylimidazo-[2,1-b][1,3,4]thiadiazole-5-carbohydrazide (2). The newly synthesized compounds (3a-3h) were evaluated in the National Cancer Institute's 3-cell lin...

    journal_title:European journal of medicinal chemistry

    pub_type: 杂志文章


    authors: Terzioglu N,Gürsoy A

    更新日期:2003-07-01 00:00:00

  • Domino approach to 2-aroyltrimethoxyindoles as novel heterocyclic combretastatin A4 analogues.

    abstract::Two series of 2-aroyltrimethoxyindoles were designed to investigate the effects of the replacement of the trimethoxyphenyl ring of phenstatin with a trimethoxyindole moiety. These compounds were efficiently prepared through a domino palladium-catalyzed sequence from 2-gem-dibromovinylanilines substituted by three meth...

    journal_title:European journal of medicinal chemistry

    pub_type: 杂志文章


    authors: Arthuis M,Pontikis R,Chabot GG,Quentin L,Scherman D,Florent JC

    更新日期:2011-01-01 00:00:00

  • New naphthopyran analogues of LY290181 as potential tumor vascular-disrupting agents.

    abstract::A series of 19 analogues of the antiproliferative naphthopyran LY290181 were prepared for structure-activity relationship studies. We found the best activities for test compounds bearing small substituents at the meta position of the phenyl ring. The mode of action of LY290181 and eight new analogues was studied in de...

    journal_title:European journal of medicinal chemistry

    pub_type: 杂志文章


    authors: Schmitt F,Gold M,Rothemund M,Andronache I,Biersack B,Schobert R,Mueller T

    更新日期:2019-02-01 00:00:00

  • Quinolone antibiotic derivatives as new selective Axl kinase inhibitors.

    abstract::Axl is a new promising molecular target for antineoplastic therapies. A series of quinolone antibiotic derivatives were designed and synthesized as new selective Axl inhibitors. One of the most promising compound 8i bound tightly to Axl with a Kd value of 1.1 nM, and inhibited its kinase activity with an IC50 value of...

    journal_title:European journal of medicinal chemistry

    pub_type: 杂志文章


    authors: Tan L,Zhang Z,Gao D,Chan S,Luo J,Tu ZC,Zhang ZM,Ding K,Ren X,Lu X

    更新日期:2019-03-15 00:00:00

  • Design, synthesis and antiproliferative activity of novel 5-nitropyrimidine-2,4-diamine derivatives bearing alkyl acetate moiety.

    abstract::In order to discover new anticancer drug leads, a series of novel alkylamino pyrimidine derivatives were designed and synthesized based on our previous work via a ring-opening strategy. Biological evaluation with four human cancer cell lines (MDA-MB-231, A549, HepG2, and MCF-7) showed that most of these compounds poss...

    journal_title:European journal of medicinal chemistry

    pub_type: 杂志文章


    authors: Zhao PL,Li YH,Yang HK,Chen P,Zhang B,Sun Q,Li Q,You WW

    更新日期:2016-08-08 00:00:00