Carbonic anhydrase inhibitors: binding of indanesulfonamides to the human isoform II.

abstract：:The renin angiotensin aldosterone system (RAAS) is a hormonal cascade involved in the regulation of blood pressure and electrolyte balance, and represents a common target for the treatment of various diseases including hypertension, heart failure, and diabetes. Herein we present a novel 18 F-labeled derivative of the ...

journal_title：ChemMedChem

authors： Hoffmann M,Chen X,Hirano M,Arimitsu K,Kimura H,Higuchi T,Decker M

更新日期：2018-12-06 00:00:00

abstract：:Dual inhibition of microsomal prostaglandin E2 synthase-1 (mPGES-1) and 5-lipoxygenase (5-LO), two key enzymes involved in pro-inflammatory eicosanoid biosynthesis, represents a new strategy for treating inflammatory disorders. Herein we report the discovery of 2,4-thiazolidinedione-based mPGES-1/5-LO dual inhibitors ...

journal_title：ChemMedChem

authors： Lauro G,Terracciano S,Cantone V,Ruggiero D,Fischer K,Pace S,Werz O,Bruno I,Bifulco G

更新日期：2020-03-18 00:00:00

abstract：:A small library of 17 organoruthenium compounds with the general formula [RuII (fcl)(chel)(L)]n+ (in which fcl=face capping ligand, chel=chelating bidentate ligand, and L=monodentate ligand) were screened for inhibitory activity against cholinesterases and glutathione-S-transferases of human and animal origins. Compou...

journal_title：ChemMedChem

authors： Ristovski S,Uzelac M,Kljun J,Lipec T,Uršič M,Zemljič Jokhadar Š,Žužek MC,Trobec T,Frangež R,Sepčić K,Turel I

更新日期：2018-10-22 00:00:00

abstract：:A novel class of isochroman dopamine analogues, originally reported by Abbott Laboratories, have >100-fold selectivity for D₁-like over D₂-like receptors. We synthesized a parallel series of chroman compounds and showed that repositioning the oxygen atom in the heterocyclic ring decreases potency and confers D₂-like r...

journal_title：ChemMedChem

authors： Bonner LA,Laban U,Chemel BR,Juncosa JI,Lill MA,Watts VJ,Nichols DE

更新日期：2011-06-06 00:00:00

abstract：:Antimicrobial peptides (AMPs) are promising candidates to help circumvent antibiotic resistance, which is an increasing clinical problem. Amino-terminal copper and nickel (ATCUN) binding motifs are known to actively form reactive oxygen species (ROS) upon metal binding. The combination of these two peptidic constructs...

journal_title：ChemMedChem

authors： Libardo MD,Cervantes JL,Salazar JC,Angeles-Boza AM

更新日期：2014-08-01 00:00:00

abstract：:The clinical use of N,N'-bis(2-hydroxybenzyl)ethylenediamine-N,N'-diacetic acid (HBED) has been hindered by its lack of bioavailability. N,N'-bis(2-boronic pinacol ester benzyl)ethylenediamine-N,N'-diacetic acid methyl, ethyl, and isopropyl esters 7 a-c, respectively, and their dimesylate salts 8 a-c, are double prodr...

journal_title：ChemMedChem

authors： Thiele NA,Sloan KB

更新日期：2016-08-05 00:00:00

abstract：:Members of the Eph receptor tyrosine kinase family play essential roles in the pathogenesis of cancer and are therefore promising candidates for molecular imaging by positron emission tomography (PET), for example. In this regard, radiochemical access to novel PET radiotracers derived from potent inhibitors that targe...

journal_title：ChemMedChem

authors： Mamat C,Mosch B,Neuber C,Köckerling M,Bergmann R,Pietzsch J

更新日期：2012-11-01 00:00:00

abstract：:Opening up ion channels: We synthesised a series of anthraquinone analogues, called the GoSlo-SR family. Their effects on bladder smooth muscle BK channels were examined and, as shown, shifted voltage dependent activation >-100 mV (at 10 μM). They were more efficacious than NS11021 and could provide a new scaffold for...

journal_title：ChemMedChem

authors： Roy S,Morayo Akande A,Large RJ,Webb TI,Camarasu C,Sergeant GP,McHale NG,Thornbury KD,Hollywood MA

更新日期：2012-10-01 00:00:00

abstract：:4H-1,2,4-Benzothiadiazine-1,1-dioxides with various substituents in positions 3, 5, and 7 were synthesized and tested as K(ATP) channel agonists in artificial cell systems (CHO cells transfected with SUR1/Kir6.2, and HEK 293 transfected with SUR2B/Kir6.1) as model systems for insulin-secreting pancreatic beta-cells an...

journal_title：ChemMedChem

authors： Lachenicht S,Fischer A,Schmidt C,Winkler M,Rood A,Lemoine H,Braun M

更新日期：2009-11-01 00:00:00

abstract：:The DATA chelators are a novel class of tri-anionic ligands based on 6-amino-1,4-diazepine-triacetic acid, which have been introduced recently for the chelation of (68)Ga. Compared with macrocyclic chelators based on the cyclen scaffold (i.e., DOTA, DO3A, and DO2A derivatives), DATA chelators undergo quantitative radi...

journal_title：ChemMedChem

authors： Seemann J,Waldron BP,Roesch F,Parker D

更新日期：2015-06-01 00:00:00

abstract：:Abnormally high corticosteroid levels are responsible for the onset of serious hormone-related diseases, and the inhibition of their biosynthesis by targeting cytochrome P450 (CYP) isoforms CYP11B1 and CYP11B2 has emerged as a promising strategy to restore healthy physiological levels of corticosteroids. With the aim ...

journal_title：ChemMedChem

authors： Gobbi S,Hu Q,Zimmer C,Belluti F,Rampa A,Hartmann RW,Bisi A

更新日期：2016-08-19 00:00:00

abstract：:A strategy that combines virtual screening and structure-guided selection of fragments was used to identify three unexplored classes of human DHODH inhibitor compounds: 4-hydroxycoumarins, fenamic acids, and N-(alkylcarbonyl)anthranilic acids. Structure-guided selection of fragments targeting the inner subsite of the ...

journal_title：ChemMedChem

authors： Fritzson I,Svensson B,Al-Karadaghi S,Walse B,Wellmar U,Nilsson UJ,da Graça Thrige D,Jönsson S

更新日期：2010-04-06 00:00:00

abstract：:The in silico design, synthesis, and biological evaluation of ten potent type II dehydroquinase inhibitors are described. These compounds contain an anhydroquinate core, incorporated as a mimic of the enolate reaction intermediate. This substructure is attached by a variety of linking units to a terminal phenyl group ...

journal_title：ChemMedChem

authors： Payne RJ,Peyrot F,Kerbarh O,Abell AD,Abell C

更新日期：2007-07-01 00:00:00

abstract：:Progesterone plays an important role in the female reproductive system. However, there is also evidence that gynecologic disorders/diseases such as uterine fibroids and endometriosis are progesterone-dependent. Steroidal and non-steroidal selective progesterone receptor modulators (SPRMs) have shown potential for the ...

journal_title：ChemMedChem

authors： Möller C,Bone W,Cleve A,Klar U,Rotgeri A,Rottmann A,Schultze-Mosgau MH,Wagenfeld A,Schwede W

更新日期：2018-11-06 00:00:00

abstract：:Given its role in the mediation of energy and glucose homeostasis, the G-protein-coupled bile acid receptor 1 (TGR5) is considered a potential target for the treatment of type 2 diabetes mellitus and other metabolic disorders. By thorough analysis of diverse structures of published TGR5 agonists, a hypothetical ligand...

journal_title：ChemMedChem

authors： Zhu J,Ye Y,Ning M,Mándi A,Feng Y,Zou Q,Kurtán T,Leng Y,Shen J

更新日期：2013-07-01 00:00:00

abstract：:A structure-activity relationship around the amine group of the ambruticin VS series has been developed for antifungal activity. It was shown that the amine can be alkylated through reductive amination without loss of potency. However, if it is converted into either an amide, carbamate, or urea, a significant loss of ...

journal_title：ChemMedChem

authors： Tian ZQ,Wang Z,Xu Y,Tran CQ,Myles DC,Zhong Z,Simmons J,Vetcher L,Katz L,Li Y,Shaw SJ

更新日期：2008-06-01 00:00:00

abstract：:Small-molecule inhibitors of hypoxia-inducible factor prolyl hydroxylases (HIF-PHs) are currently under clinical development as novel treatment options for chronic kidney disease (CKD) associated anemia. Inhibition of HIF-PH mimics hypoxia and leads to increased erythropoietin (EPO) expression and subsequently increas...

journal_title：ChemMedChem

authors： Beck H,Jeske M,Thede K,Stoll F,Flamme I,Akbaba M,Ergüden JK,Karig G,Keldenich J,Oehme F,Militzer HC,Hartung IV,Thuss U

更新日期：2018-05-23 00:00:00

abstract：:Designed multitarget ligands are a popular approach to generating efficient and safe drugs, and fragment-based strategies have been postulated as a versatile avenue to discover multitarget ligand leads. To systematically probe the potential of fragment-based multiple ligand discovery, we have employed a large fragment...

journal_title：ChemMedChem

authors： Brunst S,Kramer JS,Kilu W,Heering J,Pollinger J,Hiesinger K,George S,Steinhilber D,Merk D,Proschak E

更新日期：2020-12-06 00:00:00

abstract：:We previously found that p97 ATPase inhibitors 2-(2-amino-1H-benzo[d]imidazol-1-yl)-N-benzyl-8-methoxyquinazolin-4-amine (ML240) and 2-(2H-benzo[b][1,4]oxazin-4(3H)-yl)-N-benzyl-5,6,7,8-tetrahydroquinazolin-4-amine (ML241) specifically target the D2 domain of wild-type p97. In addition, one of the major p97 cofactors,...

journal_title：ChemMedChem

authors： Fang CJ,Gui L,Zhang X,Moen DR,Li K,Frankowski KJ,Lin HJ,Schoenen FJ,Chou TF

更新日期：2015-01-01 00:00:00

abstract：:Vascular endothelial growth factor receptor 2 (VEGFR2) has been proven to play a major role in the regulation of tumor angiogenesis. A series of novel glycyrrhetic acid derivatives were synthesized and evaluated for their VEGFR2 inhibitory activity as well as their antiproliferative properties against four cancer cell...

journal_title：ChemMedChem

authors： Yan TL,Bai LF,Zhu HL,Zhang WM,Lv PC

更新日期：2017-07-06 00:00:00

abstract：:Nanoscale materials hold great promise in the therapeutic field. In particular, as carriers or vectors, they help bioactive molecules reach their primary targets. Furthermore, by themselves, certain nanomaterials-regarded as protective-can modulate particular metabolic pathways that are deregulated in pathological sit...

journal_title：ChemMedChem

authors： Bianco A,Muller S

更新日期：2016-01-19 00:00:00

abstract：:A novel and facile synthesis of quinoxalinone derivatives was developed in which a wide range of 3-chloroquinoxalin-2(1H)-ones as key intermediates can be generated chemo- and regioselectively in good yields from corresponding quinoxaline-2,3(1H,4H)-diones. This new protocol is arguably superior, as it allows the desi...

journal_title：ChemMedChem

authors： Yang Y,Zhang S,Wu B,Ma M,Chen X,Qin X,He M,Hussain S,Jing C,Ma B,Zhu C

更新日期：2012-05-01 00:00:00

abstract：:A series of new 5-alkyl-2-phenylaminocarbonylmethylthiopyrimidin-4(3H)-ones bearing variously substituted arylmethyl moieties at the C6 position of the pyrimidine ring were synthesized and evaluated for anti-HIV activity in MT-4 cells. Most of these new congeners exhibited moderate to good activities against the wild-...

journal_title：ChemMedChem

authors： Yu M,Li Z,Liu S,Fan E,Pannecouque C,De Clercq E,Liu X

更新日期：2011-05-02 00:00:00

abstract：:AFMC-AIMECS meetings are internationally organized biannually by the Asian Federation for Medicinal Chemistry (AFMC) and are focused on recent studies in drug discovery and development both in academia and industry. Member organizations of the AFMC are the Pharmaceutical Society of Japan, the Chinese Pharmaceutical As...

journal_title：ChemMedChem

authors： Olgac A,Yalcin I,Aki-Yalcin E

更新日期：2020-01-07 00:00:00

abstract：:Chemical biology approaches have a long history in the exploration of the G-protein-coupled receptor (GPCR) family, which represents the largest and most important group of targets for therapeutics. The analysis of the human genome revealed a significant number of new members with unknown physiological function which ...

journal_title：ChemMedChem

authors： Jacoby E,Bouhelal R,Gerspacher M,Seuwen K

更新日期：2006-08-01 00:00:00

abstract：:Despite various inhibitors targeting the zinc center(s) of enzymes, drugs that target zinc fingers have not been examined in detail. We previously developed a dithiol compound named SN-1 that has an inhibitory effect on the function of zinc finger transcription factors, but its mechanism of action has not yet been elu...

journal_title：ChemMedChem

authors： Koga R,Radwan MO,Ejima T,Kanemaru Y,Tateishi H,Ali TFS,Ciftci HI,Shibata Y,Taguchi Y,Inoue JI,Otsuka M,Fujita M

更新日期：2017-12-07 00:00:00

abstract：:A group of acidic nucleosides were synthesized to develop a new class of ribonuclease A (RNase A) inhibitors. Our recent study on carboxymethylsulfonyl-modified nucleosides revealed some interesting results in RNase A inhibition. This positive outcome triggered an investigation of the role played by secondary sugar hy...

journal_title：ChemMedChem

authors： Datta D,Dasgupta S,Pathak T

更新日期：2014-09-01 00:00:00

abstract：:Human equilibrative nucleoside transporter 1 (hENT1) is a prototypical nucleoside transporter protein ubiquitously expressed on the cell surface of almost all human tissue. Given the role of hENT1 in the transport of nucleoside drugs, an important class of therapeutics in the treatment of various cancers and viral inf...

journal_title：ChemMedChem

authors： Rayala R,Theard P,Ortiz H,Yao S,Young JD,Balzarini J,Robins MJ,Wnuk SF

更新日期：2014-09-01 00:00:00

abstract：:Modern organizations conducting drug-discovery programs frequently apply high-throughput screening to generate novel hit structures for the indications of interest. Systematic hit-to-lead processes have been established at most pharmaceutical companies to ensure a smooth conversion of hits into high-quality lead struc...

journal_title：ChemMedChem

authors： Steinmeyer A

更新日期：2006-01-01 00:00:00

abstract：:Greater than the sum of its parts: Artemisinins are currently in phase I-II clinical trials against breast, colorectal and non-small-cell lung cancers. In an attempt to offer increased specificity, a series of hybrid artemisinin-polypyrrole minor groove binder conjugates are described. DNA binding/modelling studies an...

journal_title：ChemMedChem

authors： La Pensée L,Sabbani S,Sharma R,Bhamra I,Shore E,Chadwick AE,Berry NG,Firman J,Araujo NC,Cabral L,Cristiano ML,Bateman C,Janneh O,Gavrila A,Wu YH,Hussain A,Ward SA,Stocks PA,Cosstick R,O'Neill PM

更新日期：2013-05-01 00:00:00