Asymmetric reduction of 3-aryl-3-keto esters using Rhizopus species.

abstract：:Polyamides consisting of N-methylpyrrole (Py), N-methylimidazole (Im), and N-methyl-3-hydroxypyrrole (Hp) are synthetic ligands that recognize predetermined DNA sequences with affinities and specificities comparable to many DNA-binding proteins. As derivatives of the natural products distamycin and netropsin, Py/Im/Hp...

journal_title：Bioorganic & medicinal chemistry

authors： Bremer RE,Szewczyk JW,Baird EE,Dervan PB

更新日期：2000-08-01 00:00:00

abstract：:Serine peptidases are a large, well-studied, and medically important class of peptidases. Despite the attention these enzymes have received, details concerning the substrate specificity of even some of the best known enzymes in this class are lacking. One approach to rapidly characterizing substrate specificity for pe...

journal_title：Bioorganic & medicinal chemistry

authors： Furlong ST,Mauger RC,Strimpler AM,Liu YP,Morris FX,Edwards PD

更新日期：2002-11-01 00:00:00

abstract：:With the goal of developing multitargeted receptor tyrosine kinase inhibitors that display potent inhibition against PDGFRβ and VEGFR-2 we designed and synthesized eleven N(4)-(3-bromophenyl)-7-(substitutedbenzyl) pyrrolo[2,3-d]pyrimidines 9a-19a. These compounds were obtained from the key intermediate N(4)-(3-bromoph...

journal_title：Bioorganic & medicinal chemistry

authors： Gangjee A,Zaware N,Raghavan S,Yang J,Thorpe JE,Ihnat MA

更新日期：2012-04-01 00:00:00

abstract：:Hormone sensitive lipase (HSL) has emerged as an attractive target for the treatment of dyslipidemia. We previously reported compound 1 as a potent and orally active HSL inhibitor. Although an attractive profile was demonstrated, subsequent studies revealed that compound 1 has a bioactivation liability. The oxygen-car...

journal_title：Bioorganic & medicinal chemistry

authors： Ogiyama T,Yamaguchi M,Kurikawa N,Honzumi S,Yamamoto Y,Sugiyama D,Takakusa H,Inoue SI

更新日期：2017-04-01 00:00:00

abstract：:P2X4 receptor has become an interesting molecular target for treatment and PET imaging of neuroinflammation and associated brain diseases such as Alzheimer's disease. This study reports the first design, synthesis, radiolabeling and biological evaluation of new candidate PET P2X4 receptor radioligands using 5-BDBD, a ...

journal_title：Bioorganic & medicinal chemistry

authors： Wang M,Gao M,Meyer JA,Peters JS,Zarrinmayeh H,Territo PR,Hutchins GD,Zheng QH

更新日期：2017-07-15 00:00:00

abstract：:Two novel C(27)N(3)-type Lycopodium alkaloids, cryptadines A (1) and B (2) consisting of two octahydroquinoline rings (C(11)N) and a piperidine ring (C(5)N), have been isolated from the club moss Lycopodium cryptomerinum, and their structures and relative stereochemistry were elucidated on the basis of spectroscopic d...

journal_title：Bioorganic & medicinal chemistry

authors： Koyama K,Hirasawa Y,Kobayashi J,Morita H

更新日期：2007-12-15 00:00:00

abstract：:This study discovered that glycyrrhetinic acid inhibited the human 20S proteasome at 22.3microM. Esterification of the C-3 hydroxyl group on glycyrrhetinic acid with various carboxylic acid reagents yielded a series of analogs with marked improved potency. Among the derivatives, glycyrrhetinic acid 3-O-isophthalate (1...

journal_title：Bioorganic & medicinal chemistry

authors： Huang L,Yu D,Ho P,Qian K,Lee KH,Chen CH

更新日期：2008-07-15 00:00:00

abstract：:The biochemically unique structures of sugar residues in the outer cell wall of Mycobacterium tuberculosis (MTB) make the pathways for their biosynthesis and utilization attractive targets for the development of new and selective anti-tubercular agents. A cell-free assay system for galactosyltransferase activity using...

journal_title：Bioorganic & medicinal chemistry

authors： Pathak AK,Besra GS,Crick D,Maddry JA,Morehouse CB,Suling WJ,Reynolds RC

更新日期：1999-11-01 00:00:00

abstract：:A series of novel 1-methyl-3-substituted quinazoline-2,4-dione derivatives were designed, synthesized, and characterized by (1)H NMR, (13)C NMR and MS spectral data. Their inhibition against chitin synthase (CHS) and antifungal activities were evaluated in vitro. Results showed compounds 5b, 5c, 5e, 5f, 5j, 5k, 5l, an...

journal_title：Bioorganic & medicinal chemistry

authors： Ji Q,Yang D,Wang X,Chen C,Deng Q,Ge Z,Yuan L,Yang X,Liao F

更新日期：2014-07-01 00:00:00

abstract：:12-O-β-D-glucopyranosyl jasmonic acid (JAG) shows unique biological activities, including leaf-closing of Samanea saman. It is expected that the mode of action for such regulation is distinct from that of other jasmonates. We developed high-performance compact molecular probes (CMPs) based on JAG that can be used for ...

journal_title：Bioorganic & medicinal chemistry

authors： Ueda M,Yang G,Ishimaru Y,Itabashi T,Tamura S,Kiyota H,Kuwahara S,Inomata S,Shoji M,Sugai T

更新日期：2012-10-01 00:00:00

abstract：:Serotonin (5-hydroxytryptamine, 5-HT) is an important signaling molecule in the central nervous system (CNS) and in non-neuronal tissues and organs. Serotonin mediates a positive chronotropic and inotropic response through 5-HT4 receptors in the atrium and ventricle of the heart. Recent investigations have revealed in...

journal_title：Bioorganic & medicinal chemistry

authors： Brudeli B,Andressen KW,Moltzau LR,Nilsen NO,Levy FO,Klaveness J

更新日期：2013-11-15 00:00:00

abstract：:Soluble epoxide hydrolase (sEH) is a potential target for the treatment of inflammation and hypertension. X-ray crystallographic fragment screening was used to identify fragment hits and their binding modes. Eight fragment hits were identified via soaking of sEH crystals with fragment cocktails, and the co-crystal str...

journal_title：Bioorganic & medicinal chemistry

authors： Amano Y,Tanabe E,Yamaguchi T

更新日期：2015-05-15 00:00:00

abstract：:A nuclear factor-κB (NF-κB) luciferase assay has been employed to identify the bengamides, previously known for their anti-tumor activity, as a new class of immune modulators. A unique element of this study was that the bengamide analogs were isolated from two disparate sources, Myxococcus virescens (bacterium) and Ja...

journal_title：Bioorganic & medicinal chemistry

authors： Johnson TA,Sohn J,Vaske YM,White KN,Cohen TL,Vervoort HC,Tenney K,Valeriote FA,Bjeldanes LF,Crews P

更新日期：2012-07-15 00:00:00

abstract：:γ-Amino butyric acid (GABA) is the major inhibitory neurotransmitter in the mammalian central nervous system (CNS). A malfunction of the GABAergic neurotransmission is connected to several neuronal disorders like epilepsy, Alzheimer's disease, neuropathic pain, and depression. One possibility to enhance GABA levels in...

journal_title：Bioorganic & medicinal chemistry

authors： Quandt G,Höfner G,Wanner KT

更新日期：2013-06-01 00:00:00

abstract：:Hepatocyte growth factor activator (HGFA), matriptase and hepsin are all S1 trypsin-like serine endopeptidases. HGFA is a plasma protease while hepsin and matriptase are type II transmembrane proteases (TTSPs). Upregulated expression and activity of all three proteases is associated with aberrant cancer cell signaling...

journal_title：Bioorganic & medicinal chemistry

authors： Franco FM,Jones DE,Harris PK,Han Z,Wildman SA,Jarvis CM,Janetka JW

更新日期：2015-05-15 00:00:00

abstract：:Three peptide amides, HPRK(Py)(4)HPRK-NH(2) (PyH-12), HPRK(Py)(3)HPRK-NH(2) (PyH-11) and HPRK(Py)(2)HPRK-NH(2) (PyH-10), incorporating two HPRK motifs and various 4-amino-1-methylpyrrole-2-carboxylic acid residues (Py) were synthesized by solid-phase peptide methodology. The binding of these three peptides to a 5'-32P...

journal_title：Bioorganic & medicinal chemistry

authors： Chang JC,Yang CH,Chou PY,Yang WH,Chou IC,Lu CT,Lin PH,Hou RC,Jeng KC,Cheng CC,Sheh L

更新日期：2004-01-02 00:00:00

abstract：:While hemoglobin is one of the most well characterized proteins due to its function in oxygen transport, few additional properties of hemoglobin have been described. While screening serum samples for novel antimicrobial factors, it was found that intact hemoglobin tetramers, including that from human, exhibited consid...

journal_title：Bioorganic & medicinal chemistry

authors： Parish CA,Jiang H,Tokiwa Y,Berova N,Nakanishi K,McCabe D,Zuckerman W,Xia MM,Gabay JE

更新日期：2001-02-01 00:00:00

abstract：:To investigate the effect of elongating base-pair (bp) recognition sequences, we synthesized N-methylpyrrole-N-methylimidazole (PI) polyamide conjugates with eight-bp recognition (3-5). The DNA alkylating activities of conjugates 3-5 were evaluated by high-resolution denaturing polyacrylamide gel electrophoresis with ...

journal_title：Bioorganic & medicinal chemistry

authors： Takagaki T,Bando T,Kitano M,Hashiya K,Kashiwazaki G,Sugiyama H

更新日期：2011-10-01 00:00:00

abstract：:Alpha7 agonists were identified via GOLD (CCDC) docking in the putative agonist binding site of an alpha7 homology model and a series of aminoalkyl benzoimidazoles was synthesised to obtain potentially brain penetrant drugs. The array was prepared starting from the reaction of ortho-fluoronitrobenzenes with a selectio...

journal_title：Bioorganic & medicinal chemistry

authors： Micco I,Nencini A,Quinn J,Bothmann H,Ghiron C,Padova A,Papini S

更新日期：2008-03-01 00:00:00

abstract：:This article has been withdrawn at the request of the author(s) and/or editor. The Publisher apologizes for any inconvenience this may cause. The full Elsevier Policy on Article Withdrawal can be found at http://www.elsevier.com/locate/withdrawalpolicy. ...

journal_title：Bioorganic & medicinal chemistry

authors： Tandon V,Chhikara BS,Chandra R,Mishra AK

更新日期：2006-02-21 00:00:00

abstract：:A series of zatebradine analogues, differing in the basic moiety and in the methylene spacer, have been synthesized; their negative chronotropic activity has been determined in guinea pig atria. The most active compounds have been studied for their blocking properties on the hyperpolarization-activated current If (whi...

journal_title：Bioorganic & medicinal chemistry

authors： Romanelli MN,Cerbai E,Dei S,Guandalini L,Martelli C,Martini E,Scapecchi S,Teodori E,Mugelli A

更新日期：2005-02-15 00:00:00

abstract：:Targeting tumor vasculature represents an intriguing therapeutic strategy in the treatment of cancer. In an effort to discover new vascular disrupting agents with improved water solubility and potentially greater bioavailability, various amino acid prodrug conjugates (AAPCs) of potent amino combretastatin, amino dihyd...

journal_title：Bioorganic & medicinal chemistry

authors： Devkota L,Lin CM,Strecker TE,Wang Y,Tidmore JK,Chen Z,Guddneppanavar R,Jelinek CJ,Lopez R,Liu L,Hamel E,Mason RP,Chaplin DJ,Trawick ML,Pinney KG

更新日期：2016-03-01 00:00:00

abstract：:A series of benzene sulfonamide carbonic anhydrase (CA, EC 4.2.1.1) inhibitors which incorporate lipophilic 4-alkoxy- and 4-aryloxy moieties, together with several derivatives of ethoxzolamide and sulfanilamide are reported. These derivatives were investigated as inhibitors of the metalloenzyme carbonic anhydrase (CA,...

journal_title：Bioorganic & medicinal chemistry

authors： Carta F,Di Cesare Mannelli L,Pinard M,Ghelardini C,Scozzafava A,McKenna R,Supuran CT

更新日期：2015-04-15 00:00:00

abstract：:3-Metoxycarbonyl isoquinolone derivative 1 has been identified as a potent JNK inhibitor and significantly inhibited cardiac hypertrophy in a rat pressure-overload model. Herein, a series of isoquinolones with an imidazolylmethyl or a pyrazolylmethyl group at the 2-position were designed based on X-ray crystallographi...

journal_title：Bioorganic & medicinal chemistry

authors： Asano Y,Kitamura S,Ohra T,Itoh F,Kajino M,Tamura T,Kaneko M,Ikeda S,Igata H,Kawamoto T,Sogabe S,Matsumoto S,Tanaka T,Yamaguchi M,Kimura H,Fukumoto S

更新日期：2008-04-15 00:00:00

abstract：:All eight stereoisomers of saxagliptin have been synthesized and evaluated for their inhibitory activity against DPP-IV. It was unambiguously confirmed that the configuration of saxagliptin was critical to potent inhibition of DPP-IV. Docking study was performed to elucidate the configuration-activity relationship of ...

journal_title：Bioorganic & medicinal chemistry

authors： Dong J,Gong Y,Liu J,Chen X,Wen X,Sun H

更新日期：2014-02-15 00:00:00

abstract：:Several rationally designed analogs of 3-fluoro-2-oxo-3-phenylpropionic acid were chemically synthesized, and the reactions of the hydrate form of these compounds with 4-hydroxyphenylpyruvate dioxygenase from pig liver as inhibitors were examined. Compounds 14a and 14b were found to be potent competitive inhibitors of...

journal_title：Bioorganic & medicinal chemistry

authors： Ling TS,Shiu S,Yang DY

更新日期：1999-07-01 00:00:00

abstract：:As one of our ongoing research project concerning development of a novel anti-influenza virus agent, dihydrofuran-fused perhydrophenanthrenes were derivatized by means of Williamson ether synthesis and Suzuki-Miyaura cross coupling reactions. Newly synthesized compounds were subjected to evaluation of anti-influenza v...

journal_title：Bioorganic & medicinal chemistry

authors： Matsuya Y,Suzuki N,Kobayashi SY,Miyahara T,Ochiai H,Nemoto H

更新日期：2010-02-15 00:00:00

abstract：:Previously, bioassay-guided separation led us to isolate eleven novel steroidal alkaloids named cortistatins from the marine sponge Corticium simplex. These cortistatins were classified into three types based on the chemical structure of the side chain part, that is, isoquinoline, N-methyl piperidine or 3-methylpyridi...

journal_title：Bioorganic & medicinal chemistry

authors： Aoki S,Watanabe Y,Tanabe D,Arai M,Suna H,Miyamoto K,Tsujibo H,Tsujikawa K,Yamamoto H,Kobayashi M

更新日期：2007-11-01 00:00:00

abstract：:On the grounds of previous encouraging results on the antitumor activity of (1E,3E)-1,4-bis(1-naphthyl)-2,3-dinitro-1,3-butadiene (1), we have designed and synthesized two new molecules [(1E,3E)-1,4-bis(4-carboxy-1-naphthyl)-2,3-dinitro-1,3-butadiene (2) and methyl (2Z,4E)-2-methylsulfanyl-5-(1-naphthyl)-4-nitro-2,4-p...

journal_title：Bioorganic & medicinal chemistry

authors： Petrillo G,Mariggiò MA,Aiello C,Cordazzo C,Fenoglio C,Morganti S,Croce M,Rizzato E,Spinelli D,Maccagno M,Bianchi L,Prevosto C,Tavani C,Viale M

更新日期：2008-01-01 00:00:00

abstract：:A facile synthesis of dl-6,10,14-trimethylpentadecan-2-ol (1) a pheromone component of rice moth, Corcyra cephalonica Stainton and 5,9,13-trimethyltetradecanoic acid (2) a component of marine sponge, Cinachyrella alloclada Uliczka, using a common, intermediate, hexahydrofarnesol is accomplished. The salient features f...

journal_title：Bioorganic & medicinal chemistry

authors： Rane SS,Chadha MS,Mamdapur VR

更新日期：1993-12-01 00:00:00