Quantitative screening of EGF receptor-binding peptides by using a peptide library with multiple fluorescent amino acids as fluorescent tags.

abstract：:The designed cytosine-carbohydrate hybrid molecule selectively recognized and stabilized the bulged duplex DNA possessing the complementary bulged DNA base, guanine, while the nucleotide base itself did not exhibit any such ability. It was also found that the assistance of the carbohydrate to stabilize the interaction...

journal_title：Bioorganic & medicinal chemistry letters

authors： Idutsu Y,Sasaki A,Matsumura S,Toshima K

更新日期：2005-10-01 00:00:00

abstract：:Apoptotic cell death is the cause of the loss of insulin-producing β-cells in all forms of diabetes mellitus. The identification of small molecules capable of protecting cytokine-induced apoptosis could form the basis of useful therapeutic interventions. Here in, we present the discovery and synthesis of new benzimida...

journal_title：Bioorganic & medicinal chemistry letters

authors： Zawawi NK,Rajput SA,Taha M,Ahmat N,Ismail NH,Abdullah N,Khan KM,Choudhary MI

更新日期：2015-10-15 00:00:00

abstract：:Poly(ADP-ribose) (PAR) is an important biopolymer, which is involved in various life processes such as DNA repair and replication, modulation of chromatin structure, transcription, cell differentiation, and in pathogenesis of various diseases such as cancer, diabetes, ischemia and inflammations. PAR is the most electr...

journal_title：Bioorganic & medicinal chemistry letters

authors： Drenichev MS,Mikhailov SN

更新日期：2016-08-01 00:00:00

abstract：:The structure of the S1P2 antagonist 1 has been modified with the aim of improving its oral bioavailability. The chemical modification of the alkyl chain and carboxylic acid moieties of 1 led to significant improvements in the oral exposure of compounds belonging to this series. The optimization of the ring size of th...

journal_title：Bioorganic & medicinal chemistry letters

authors： Kusumi K,Shinozaki K,Yamaura Y,Hashimoto A,Kurata H,Naganawa A,Otsuki K,Matsushita T,Sekiguchi T,Kakuuchi A,Yamamoto H,Seko T

更新日期：2016-02-15 00:00:00

abstract：:Starting from a non-selective pyrazolo-pyrimidone lead, the sequential use of parallel medicinal chemistry and directed synthesis led to the discovery of potent, highly selective, and orally bioavailable PDE9 inhibitors. The availability of these tools allowed for a thorough evaluation of the therapeutic potential of ...

journal_title：Bioorganic & medicinal chemistry letters

authors： Deninno MP,Andrews M,Bell AS,Chen Y,Eller-Zarbo C,Eshelby N,Etienne JB,Moore DE,Palmer MJ,Visser MS,Yu LJ,Zavadoski WJ,Michael Gibbs E

更新日期：2009-05-01 00:00:00

abstract：:DNA binding ligands with potent antimicrobial activity against Gram-positive bacteria were further optimized by variation of the internal aromatic amino acids. This modification led to compounds with improved in vivo efficacy in lethal murine models of peritonitis (methicillin-resistant S. aureus, MRSA) and lung infec...

journal_title：Bioorganic & medicinal chemistry letters

authors： Bürli RW,Kaizerman JA,Duan JX,Jones P,Johnson KW,Iwamoto M,Truong K,Hu W,Stanton T,Chen A,Touami S,Gross M,Jiang V,Ge Y,Moser HE

更新日期：2004-05-03 00:00:00

abstract：:PNU-159682 is a highly potent secondary metabolite of nemorubicin belonging to the anthracycline class of natural products. Due to its extremely high potency and only partially understood mechanism of action, it was deemed an interesting starting point for the development of a new suite of linker drugs for antibody dr...

journal_title：Bioorganic & medicinal chemistry letters

authors： Holte D,Lyssikatos JP,Valdiosera AM,Swinney Z,Sisodiya V,Sandoval J,Lee C,Aujay MA,Tchelepi RB,Hamdy OM,Gu C,Lin B,Sarvaiya H,Pysz MA,Laysang A,Williams S,Jun Lee D,Holda MK,Purcell JW,Gavrilyuk J

更新日期：2020-12-15 00:00:00

abstract：:The vertebrate Cys-loop family of ligand-gated ion channels (LGICs) are comprised of nicotinic acetylcholine (nAChR), serotonin type 3 (5-HT3R), γ-aminobutyric acid (GABAAR), and glycine (GlyR) receptors. Here, we review efforts to discover selective small molecules targeting one or more Cys-loop receptors, with a foc...

journal_title：Bioorganic & medicinal chemistry letters

authors： Sparling BA,DiMauro EF

更新日期：2017-08-01 00:00:00

abstract：:Cannabinoid CB(1) receptor antagonists reduce body weight in rodents and humans, but their clinical utility as anti-obesity agents is limited by centrally mediated side effects. Here, we describe the first mixed CB(1) antagonist/CB(2) agonist, URB447 ([4-amino-1-(4-chlorobenzyl)-2-methyl-5-phenyl-1H-pyrrol-3-yl](pheny...

journal_title：Bioorganic & medicinal chemistry letters

authors： LoVerme J,Duranti A,Tontini A,Spadoni G,Mor M,Rivara S,Stella N,Xu C,Tarzia G,Piomelli D

更新日期：2009-02-01 00:00:00

abstract：:We have developed a new methodology for producing new molecules that bind to dsDNA using DNA-templated click chemistry. The click reactions between the minor groove binding peptide and acridine intercalators were accelerated by the addition of dsDNA. Furthermore, the resulting peptide-acridine conjugate showed a sligh...

journal_title：Bioorganic & medicinal chemistry letters

authors： Imoto S,Hirohama T,Nagatsugi F

更新日期：2008-10-15 00:00:00

abstract：:In order to define the structural requirements of phenylthiourea (PTU), a series of thiourea and thiosemicarbazone analogs were prepared and evaluated as inhibitors of melanogenesis in melanoma B16 cells. The most potent analog was 2-(4-tert-butylbenzylidene)hydrazinecarbothioamide (1u) with an IC(50) value of 2.7 mic...

journal_title：Bioorganic & medicinal chemistry letters

authors： Thanigaimalai P,Hoang TA,Lee KC,Bang SC,Sharma VK,Yun CY,Roh E,Hwang BY,Kim Y,Jung SH

更新日期：2010-05-01 00:00:00

abstract：:A series of competitive, reversible cathepsin S (CatS) inhibitors was investigated. An earlier disclosure detailed the discovery of the 4-(2-keto-1-benzimidazolinyl)-piperidin-1-yl moiety as an effective replacement for the 4-arylpiperazin-1-yl group found in our screening hit. Continued investigation into replacement...

journal_title：Bioorganic & medicinal chemistry letters

authors： Grice CA,Tays K,Khatuya H,Gustin DJ,Butler CR,Wei J,Sehon CA,Sun S,Gu Y,Jiang W,Thurmond RL,Karlsson L,Edwards JP

更新日期：2006-04-15 00:00:00

abstract：:Analogues related to dirlotapide (1), a gut-selective inhibitor of microsomal triglyceride transfer protein (MTP) were prepared with the goal of further reducing the potential for unwanted liver MTP inhibition and associated side-effects. Compounds were designed to decrease active metabolite load: reducing MTP activit...

journal_title：Bioorganic & medicinal chemistry letters

authors： Robinson RP,Bartlett JA,Bertinato P,Bessire AJ,Cosgrove J,Foley PM,Manion TB,Minich ML,Ramos B,Reese MR,Schmahai TJ,Swick AG,Tess DA,Vaz A,Wolford A

更新日期：2011-07-15 00:00:00

abstract：:Treatment of diseases such as African sleeping sickness and leishmaniasis often depends on relatively expensive or toxic drugs, and resistance to current chemotherapeutics is an issue in treating these diseases and malaria. In this study, a new semi-synthetic berberine analogue, 5,6-didehydro-8,8-diethyl-13-oxodihydro...

journal_title：Bioorganic & medicinal chemistry letters

authors： Bahar M,Deng Y,Zhu X,He S,Pandharkar T,Drew ME,Navarro-Vázquez A,Anklin C,Gil RR,Doskotch RW,Werbovetz KA,Kinghorn AD

更新日期：2011-05-01 00:00:00

abstract：:Low brain levels of the inhibitory neurotransmitter gamma-aminobutyric acid (GABA) lead to convulsions. Inhibition of GABA aminotransferase increases the concentration of GABA and can terminate the convulsions. Earlier we reported the synthesis of (1S,3S)-3-amino-4-difluoromethylenecyclopentanecarboxylic acid (2), whi...

journal_title：Bioorganic & medicinal chemistry letters

authors： Yuan H,Silverman RB

更新日期：2007-03-15 00:00:00

abstract：:A collection of aryl sulfonamido indanes based on the lead compound 1 was synthesized and evaluated for Kv1.5 inhibitory activity. Kv1.5 inhibitors have the potential to be atrium-selective agents for treatment of atrial fibrillation. (1R,2R)-1 has an IC(50) of 0.033microM against Kv1.5 and is selective against other ...

journal_title：Bioorganic & medicinal chemistry letters

authors： Gross MF,Beaudoin S,McNaughton-Smith G,Amato GS,Castle NA,Huang C,Zou A,Yu W

更新日期：2007-05-15 00:00:00

abstract：:We describe the synthesis and binding affinities on D(2), 5-HT(2A) and 5-HT(2C) receptors of 6-aminomethyl-6,7-dihydro-1H-indazol-4(5H)-ones and 6-aminomethyl-6,7-dihydro-3-methyl-benzo[d]isoxazol-4(5H)-ones, as conformationally constrained butyrophenone analogues. One of the new compounds showed good in vitro binding...

journal_title：Bioorganic & medicinal chemistry letters

authors： Barceló M,Raviña E,Masaguer CF,Domínguez E,Areias FM,Brea J,Loza MI

更新日期：2007-09-01 00:00:00

abstract：:Bisubstrate analog inhibitors in which a nicotinamide mimic is attached to a series of structurally diversified guanidines (arginine mimics) were synthesized and evaluated for inhibition of cholera toxin. The mechanism-based bisubstrate inhibitors were up to 1400-fold more potent than the natural substrate NAD+ and 40...

journal_title：Bioorganic & medicinal chemistry letters

authors： Zhang G

更新日期：2008-07-01 00:00:00

abstract：:2-O-carboxymethylpyrogallol derivatives (4-17) were synthesized, with their in vitro inhibitory activities against PTP1B and in vivo antihyperglycemic effects examined. Compound 14, the most potent among the series, showed a K(i) value of 1.1 microM against PTP1B, 7-fold lower than that against TC-PTP. When compound 1...

journal_title：Bioorganic & medicinal chemistry letters

authors： Bhattarai BR,Shrestha S,Ham SW,Kim KR,Cheon HG,Lee KH,Cho H

更新日期：2007-10-01 00:00:00

abstract：:Bioactivity-guided fractionation of the CHCl3 extract from hooks of Uncaria rhynchophylla led to the isolation of two triterpene esters, namely uncarinic acids A (1) and B (2). Their structures were established by spectroscopic and chemical methods. These compounds inhibited phospholipase Cgamma1 with IC50 values of 3...

journal_title：Bioorganic & medicinal chemistry letters

authors： Lee JS,Yang MY,Yeo H,Kim J,Lee HS,Ahn JS

更新日期：1999-05-17 00:00:00

abstract：:A series of analogs of GLP-1(7-36) amide containing a Nepsilon-(2-[2-[2-(3-maleimidopropylamido)ethoxy]ethoxy]acetyl)lysine has been synthesized and the resulting derivatives were bioconjugated to Cys34 of human serum albumin (HSA). The GLP-1-HSA bioconjugates were analyzed in vitro to assess the stabilizing effect of...

journal_title：Bioorganic & medicinal chemistry letters

authors： Léger R,Thibaudeau K,Robitaille M,Quraishi O,van Wyk P,Bousquet-Gagnon N,Carette J,Castaigne JP,Bridon DP

更新日期：2004-09-06 00:00:00

abstract：:To make full use both of optical properties of quantum dots (QDs) and of specific interactions between aptamers and their ligands of interest, we employed QD-conjugated RNA aptamer interactions with histidine tag. QDs offer revolutionary fluorescence performance due to their long-term photostability, brilliant colors,...

journal_title：Bioorganic & medicinal chemistry letters

authors： Shin S,Kim IH,Kang W,Yang JK,Hah SS

更新日期：2010-06-01 00:00:00

abstract：:A group of novel synthetic indoloisoquinolines was prepared and its potential as a novel series of small-molecule anti-malarial leads was assessed. The structure-activity relationship on variation of three distinct regions of chemical space was investigated. A lead compound was generated with an activity close to that...

journal_title：Bioorganic & medicinal chemistry letters

authors： Horrocks P,Fallon S,Denman L,Devine O,Duffy LJ,Harper A,Meredith EL,Hasenkamp S,Sidaway A,Monnery D,Phillips TR,Allin SM

更新日期：2012-02-15 00:00:00

abstract：:The present study describes the optimization of a series of novel benzoxazole-piperidine (piperazine) derivatives combining high dopamine D2 and serotonin 5-HT1A, 5-HT2A receptor affinities. Of these derivatives, the pharmacological features of compound 29 exhibited high affinities for the DA D2, 5-HT1A and 5-HT2A rec...

journal_title：Bioorganic & medicinal chemistry letters

authors： Huang L,Zhang W,Zhang X,Yin L,Chen B,Song J

更新日期：2015-11-15 00:00:00

abstract：:After the widespread use of the acyclic purine nucleoside analogues for therapy of herpes simplex virus (HSV) infection since the 1980s, new antiviral strategies are urgently needed to counter the emergence of drug-resistant clinical isolates. In this report, we define the anti-HSV efficacies of three optimized 2-amin...

journal_title：Bioorganic & medicinal chemistry letters

authors： Xiang YF,Qian CW,Xing GW,Hao J,Xia M,Wang YF

更新日期：2012-07-15 00:00:00

abstract：:In our efforts to develop CGRP receptor antagonists as backups to MK-3207, 2, we employed a scaffold hopping approach to identify a series of novel oxazolidinone-based compounds. The development of a structurally diverse, potent (20, cAMP+HS IC50=0.67 nM), and selective compound (hERG IC50=19 μM) with favorable rodent...

journal_title：Bioorganic & medicinal chemistry letters

authors： Crowley BM,Stump CA,Nguyen DN,Potteiger CM,McWherter MA,Paone DV,Quigley AG,Bruno JG,Cui D,Culberson JC,Danziger A,Fandozzi C,Gauvreau D,Kemmerer AL,Menzel K,Moore EL,Mosser SD,Reddy V,White RB,Salvatore CA,Kane S

更新日期：2015-11-01 00:00:00

abstract：:Bacterial resistance to β-lactam antibiotics caused by class B metallo-β-lactamases (MBL), especially for certain hospital-acquired, Gram-negative pathogens, poses a significant threat to public health. We report several 2-substituted 4,5-dihydrothiazole-4-carboxylic acids to be novel MBL inhibitors. Structure activit...

journal_title：Bioorganic & medicinal chemistry letters

authors： Chen P,Horton LB,Mikulski RL,Deng L,Sundriyal S,Palzkill T,Song Y

更新日期：2012-10-01 00:00:00

abstract：:Current Letter presents design, synthesis and biological evaluation of a novel series of pyrazolylthiazole carboxylates 1a-1p and corresponding acid derivatives 2a-2p. All 32 novel compounds were tested for their in vivo anti-inflammatory activity by carrageenan-induced rat paw edema method as well as for in vitro ant...

journal_title：Bioorganic & medicinal chemistry letters

authors： Khloya P,Kumar S,Kaushik P,Surain P,Kaushik D,Sharma PK

更新日期：2015-03-15 00:00:00

abstract：:A series of novel spiroketal-based NK(1) antagonists is described. The effect of modifications to the spiroether ring and aromatic substituents are discussed, leading to the identification of compounds with high affinity and excellent CNS penetration. ...

journal_title：Bioorganic & medicinal chemistry letters

authors： Seward EM,Carlson E,Harrison T,Haworth KR,Herbert R,Kelleher FJ,Kurtz MM,Moseley J,Owen SN,Owens AP,Sadowski SJ,Swain CJ,Williams BJ

更新日期：2002-09-16 00:00:00

abstract：:The 2',6'-dimethyl-l-tyrosine (Dmt) enhances receptor affinity, functional bioactivity and in vivo analgesia of opioid peptides. To further investigate its direct influence on these opioid parameters, we developed a series of compounds (H-Dmt-NH-X). Among them, H-Dmt-NH-CH(3) showed the highest affinity (K(i)mu=7.45 n...

journal_title：Bioorganic & medicinal chemistry letters

authors： Fujita Y,Tsuda Y,Motoyama T,Li T,Miyazaki A,Yokoi T,Sasaki Y,Ambo A,Niizuma H,Jinsmaa Y,Bryant SD,Lazarus LH,Okada Y

更新日期：2005-02-01 00:00:00