Pholasin luminescence is enhanced by addition of dehydrocoelenterazine.

abstract：:We report herein a one-pot four-enzyme approach for the synthesis of the rare sugars d-psicose, d-sorbose, l-tagatose, and l-fructose with aldolase FucA from a thermophilic source (Thermus thermophilus HB8). Importantly, the cheap starting material DL-GP (DL-glycerol 3-phosphate), was used to significantly reduce the ...

journal_title：Bioorganic & medicinal chemistry letters

authors： Li Z,Cai L,Qi Q,Styslinger TJ,Zhao G,Wang PG

更新日期：2011-09-01 00:00:00

abstract：:The mu-opioid agonists endomorphin-1 (Tyr-Pro-Trp-Phe-NH(2)) and endomorphin-2 (Tyr-Pro-Phe-Phe-NH(2)) exhibit an extremely high selectivity for the mu-opioid receptor and thus represent a potential framework for modification into mu-antagonists. Here we report on the synthesis and biological evaluation of novel [d-2-...

journal_title：Bioorganic & medicinal chemistry letters

authors： Fichna J,do-Rego JC,Janecki T,Staniszewska R,Poels J,Broeck JV,Costentin J,Schiller PW,Janecka A

更新日期：2008-02-15 00:00:00

abstract：:Several novel series of nitrile-containing fluoroquinolones with weakly basic amines are reported which have reduced potential for hERG (human ether-a-go-go gene) channel inhibition as measured by the dofetilide assay. The new fluoroquinolones are potent against both Gram-positive and fastidious Gram-negative strains,...

journal_title：Bioorganic & medicinal chemistry letters

authors： Murphy ST,Case HL,Ellsworth E,Hagen S,Huband M,Joannides T,Limberakis C,Marotti KR,Ottolini AM,Rauckhorst M,Starr J,Stier M,Taylor C,Zhu T,Blaser A,Denny WA,Lu GL,Smaill JB,Rivault F

更新日期：2007-04-15 00:00:00

abstract：:Amidino-phenoxy quinoline derivatives represent a new class of potent thrombin inhibitors with good selectivity and remarkably low molecular weight (M(W): 335-391). X-ray analyses of thrombin-bound inhibitors revealed that enzyme inhibition is mainly based on hydrophobic interactions. ...

journal_title：Bioorganic & medicinal chemistry letters

authors： Ries UJ,Priepke HW,Hauel NH,Haaksma EE,Stassen JM,Wienen W,Nar H

更新日期：2003-07-21 00:00:00

abstract：:Twelve dimeric peptidomimetics 1 were prepared via a divergent-convergent strategy. These peptidomimetics incorporated the same amino acids as i +1 and i + 2 residues in key beta-turns of the neurotrophin NT-3. Cytosensor microphysiometry was used to gauge the effects of the dimers 1 on cells that overexpress the NT-3...

journal_title：Bioorganic & medicinal chemistry letters

authors： Zhang AJ,Khare S,Gokulan K,Linthicum DS,Burgess K

更新日期：2001-01-22 00:00:00

abstract：:A series of N,1,3-triphenyl-1H-pyrazole-4-carboxamide derivatives have been designed, synthesized and evaluated for their potential antiproliferation activity and Aurora-A kinase inhibitory activity. Among all the compounds, compound 10e possessed the most potent biological activity against HCT116 and MCF-7 cell lines...

journal_title：Bioorganic & medicinal chemistry letters

authors： Li X,Lu X,Xing M,Yang XH,Zhao TT,Gong HB,Zhu HL

更新日期：2012-06-01 00:00:00

abstract：:Homology modeling of candida lanosterol C-14 demethylase, synthesis and in vitro antifungal activities of cyclohexyl analogs of restricticin are described. ...

journal_title：Bioorganic & medicinal chemistry letters

authors： Tsukuda T,Shiratori Y,Watanabe M,Ontsuka H,Hattori K,Shirai M,Shimma N

更新日期：1998-07-21 00:00:00

abstract：:The title compound (4A) was synthesized and tested as a mechanism-based inactivator of the sterol methyl transferase (SMT) enzyme from Prototheca wickerhamii. Using cycloartenol as substrate, 4A was found to exhibit time-dependent inactivation kinetics, generating a Ki value of 30 microM and Kinact value of 0.30 min-1...

journal_title：Bioorganic & medicinal chemistry letters

authors： Nes WD,He L,Mangla AT

更新日期：1998-12-15 00:00:00

abstract：:A series of N6,2-disubstituted adenosine analogues have been synthesized and their functional activity measured against A2a and A1 receptors. Examples of compounds with both a lipophilic N6-substituent and amino-functionalized 2-position were highly active at the A2a receptor on the human neutrophil. ...

journal_title：Bioorganic & medicinal chemistry letters

authors： Keeling SE,Albinson FD,Ayres BE,Butchers PR,Chambers CL,Cherry PC,Ellis F,Ewan GB,Gregson M,Knight J,Mills K,Ravenscroft P,Reynolds LH,Sanjar S,Sheehan MJ

更新日期：2000-02-21 00:00:00

abstract：:Guided by co-crystal structural information obtained from a different series we were exploring, a scaffold morphing and SBDD approach led to the discovery of the 1,4-disubstituted indazole series as a novel class of GKAs that potently activate GK in enzyme and cell assays. anti-diabetic OGTT efficacy was demonstrated ...

journal_title：Bioorganic & medicinal chemistry letters

authors： Cheruvallath ZS,Gwaltney SL 2nd,Sabat M,Tang M,Wang H,Jennings A,Hosfield D,Lee B,Wu Y,Halkowycz P,Grimshaw CE

更新日期：2017-06-15 00:00:00

abstract：:From our modulator library an interesting inhibitor of breast cancer resistance protein (BCRP) was identified. Due to its high inhibitory potency, this compound may serve as a promising novel lead for the design of new and potent modulators. This adds a new structural class to the few known highly active BCRP inhibito...

journal_title：Bioorganic & medicinal chemistry letters

authors： Pick A,Müller H,Wiese M

更新日期：2010-01-01 00:00:00

abstract：:A small library of 1-aminoalkyl 2-naphthols has been synthesized through the direct Mannich reaction of 2-naphthols with (hetero)aromatic aldehydes and secondary amines. All of the Mannich bases having a thiophen-2-yl ring in their structure had good activity against Gram-positive bacteria, irrespective of the nature ...

journal_title：Bioorganic & medicinal chemistry letters

authors： Roman G,Năstasă V,Bostănaru AC,Mareş M

更新日期：2016-05-15 00:00:00

abstract：:Reaction of TBDMS-protected bile acids (cholic, chenodeoxycholic, deoxycholic, lithocholic, ursodeoxycholic acids) or dehydrocholic acid with aromatic/heterocyclic sulfonamides possessing free amino/hydroxy moieties, in the presence of carbodiimides, afforded after deprotection of the OTBDMS ethers, a series of sulfon...

journal_title：Bioorganic & medicinal chemistry letters

authors： Scozzafava A,Supuran CT

更新日期：2002-06-17 00:00:00

abstract：:A series of 1H-1,2,3-triazole/acylhydrazide-tethered tetrahydro-β-carboline-4-aminoquinoline conjugates was synthesized with an aim to study their anti-plasmodial structure-activity relationship. The presence of 1H-1,2,3-triazole-core along with a flexible alkyl chain length on aminoquinoline core has favourable influ...

journal_title：Bioorganic & medicinal chemistry letters

authors： Sharma B,Kaur S,Legac J,Rosenthal PJ,Kumar V

更新日期：2020-01-15 00:00:00

abstract：:A 2-pyrrolidinone ring containing a single hydroxymethyl side chain effectively replaces the N-acetylamino group of 4-(N-acetylamino)-3-guanidinobenzoic acid, a low micromolar inhibitor of influenza neuraminidase. This novel structural template affords new opportunities to evolve more potent benzoic acid inhibitors. ...

journal_title：Bioorganic & medicinal chemistry letters

authors： Brouillette WJ,Atigadda VR,Luo M,Air GM,Babu YS,Bantia S

更新日期：1999-07-19 00:00:00

abstract：:Coexpression of EGFR and HER2 has been found in many tumors such as breast, ovarian, colon and prostate cancers, with poor prognosis of the patients. Herein, our team has designed and synthesized new eighteen compounds with 6-substituted 4-anilinoquinazoline core to selectively inhibit EGFR/HER2 tyrosine kinases. Twel...

journal_title：Bioorganic & medicinal chemistry letters

authors： Elkamhawy A,Farag AK,Viswanath AN,Bedair TM,Leem DG,Lee KT,Pae AN,Roh EJ

更新日期：2015-11-15 00:00:00

abstract：:2-Phenyl-4-piperidinyl-6,7-dihydrothieno[3,4-d]pyrimidine derivative (2) was found to be a new PDE4 inhibitor with moderate PDE4B activity (IC50=150 nM). A number of derivatives with a variety of 4-amino substituents and fused bicyclic pyrimidines were synthesized. Among these, 5,5-dioxo-7,8-dihydro-6H-thiopyrano[3,2-...

journal_title：Bioorganic & medicinal chemistry letters

authors： Goto T,Shiina A,Yoshino T,Mizukami K,Hirahara K,Suzuki O,Sogawa Y,Takahashi T,Mikkaichi T,Nakao N,Takahashi M,Hasegawa M,Sasaki S

更新日期：2013-06-01 00:00:00

abstract：:We describe herein a novel series of 3-amino-4-hydrazine-cyclobut-3-ene-1,2-diones as potent and selective inhibitors against the CXCR2 chemokine receptor and IL-8-mediated chemotaxis of a CXCR2-expressing cell line. Furthermore, these alkyl-hydrazine series inhibitors such as 5b demonstrated acceptable metabolic stab...

journal_title：Bioorganic & medicinal chemistry letters

authors： Liu S,Liu Y,Wang H,Ding Y,Wu H,Dong J,Wong A,Chen SH,Li G,Chan M,Sawyer N,Gervais FG,Henault M,Kargman S,Bedard LL,Han Y,Friesen R,Lobell RB,Stout DM

更新日期：2009-10-01 00:00:00

abstract：:We describe here the generation of a lead compound and its optimization studies that led to the identification of a novel GPR119 agonist. Based on a spirocyclic cyclohexane structure reported in our previous work, we identified compound 8 as a lead compound, being guided by ligand-lipophilicity efficiency (LLE), which...

journal_title：Bioorganic & medicinal chemistry letters

authors： Harada K,Mizukami J,Watanabe T,Mori G,Ubukata M,Suwa K,Fukuda S,Negoro T,Sato M,Inaba T

更新日期：2019-02-01 00:00:00

abstract：:2-Octyl gamma-bromoacetoacetate (O gamma Br), an endogenous compound originally isolated from human cerebrospinal fluid (CSF), has previously been demonstrated to increase REM sleep duration in cats. Based on the chemical structure of O gamma Br and its reported sleep-inducing effects, we synthesized O gamma Br along ...

journal_title：Bioorganic & medicinal chemistry letters

authors： Patricelli MP,Patterson JE,Boger DL,Cravatt BF

更新日期：1998-03-17 00:00:00

abstract：:A series of novel pyrimidone analogues have been designed and synthesized as HIV-1 integrase (IN) inhibitors. This study demonstrated that introducing a substituent in the N1-position of the pyrimidone scaffold does not significantly influence IN inhibitory activity. Molecular docking studies showed these compounds co...

journal_title：Bioorganic & medicinal chemistry letters

authors： Yu S,Sanchez TW,Liu Y,Yin Y,Neamati N,Zhao G

更新日期：2013-11-15 00:00:00

abstract：:Atropisomerism is stereochemistry arising from restricted bond rotation that creates a chiral axis. Atropisomers are subject to time-dependent inversion of chirality via bond rotation, a property which in drug molecules introduces complexity and challenges for drug discovery and development processes. Greater recognit...

journal_title：Bioorganic & medicinal chemistry letters

authors： Glunz PW

更新日期：2018-01-15 00:00:00

abstract：:Carbohydrate chip technology has a great potential for the high-throughput evaluation of carbohydrate-protein interactions. Herein, we report syntheses of novel sulfated oligosaccharides possessing heparin and heparan sulfate partial disaccharide structures, their immobilization on gold-coated chips to prepare array-t...

journal_title：Bioorganic & medicinal chemistry letters

authors： Wakao M,Saito A,Ohishi K,Kishimoto Y,Nishimura T,Sobel M,Suda Y

更新日期：2008-04-01 00:00:00

abstract：:With the aim of finding more potential inhibitors against NADH-fumarate reductase (specific target for treating helminthiasis and cancer) from natural resources, Talaromyces wortmannii was treated with the epigenome regulatory agent suberoylanilide hydroxamic acid, which resulted in the isolation of four new wortmanni...

journal_title：Bioorganic & medicinal chemistry letters

authors： Liu WC,Wang YY,Liu JH,Ke AB,Zheng ZH,Lu XH,Luan YS,Xiu ZL,Dong YS

更新日期：2016-11-01 00:00:00

abstract：:Analogues of the benzazepine dopamine D1 receptor antagonist SCH-23390 incorporating the cyclo-pentadienyltricarbonyl-rhenium (CPTR) moiety were synthesized and evaluated pharmacologically. The CPTR derivatives retained affinity (0.3-2.9 nM) and D1 selectivity of the parent compound, supporting their use as neuropharm...

journal_title：Bioorganic & medicinal chemistry letters

authors： Tamagnan G,Baldwin RM,Kula NS,Baldessarini RJ,Innis RB

更新日期：2000-05-15 00:00:00

abstract：:In vitro metabolic identification studies with a PI3K-α inhibitor lead molecule 1 identified a single predominant site of oxidative metabolism to be occurring within a tert.butyl moiety. Modification of the tert.butyl group within the lead molecule 1, to the corresponding d9-tert.butyl analogue 2, led to an increase i...

journal_title：Bioorganic & medicinal chemistry letters

authors： Fairhurst RA,Caravatti G,Guagnano V,Aichholz R,Blanz J,Blasco F,Wipfli P,Fritsch C,Maira SM,Schnell C,Seiler FH

更新日期：2016-10-01 00:00:00

abstract：:The transcription factor ΔFosB accumulates in response to chronic insults such as drugs of abuse, L-3,4-dihydroxyphenylalanine (l-DOPA) or stress in specific regions of the brain, triggering long lasting neural and behavioral changes that underlie aspects of drug addiction, dyskinesia, and depression. Thus, small mole...

journal_title：Bioorganic & medicinal chemistry letters

authors： Li Y,Liu Z,Aglyamova G,Chen J,Chen H,Bhandari M,White MA,Rudenko G,Zhou J

更新日期：2020-08-15 00:00:00

abstract：:Owning to the promising neuroprotective profile and the ability to cross the blood-brain barrier, triptolide has attracted extensive attention. Although its limited solubility and toxicity have greatly hindered clinical translation, triptolide has nonetheless emerged as a promising candidate for structure-activity rel...

journal_title：Bioorganic & medicinal chemistry letters

authors： Ning C,Mo L,Chen X,Tu W,Wu J,Hou S,Xu J

更新日期：2018-02-15 00:00:00

abstract：:A series of N1-activated C4-carboxy azetidinones was prepared and tested as inhibitors of human tryptase. The key stereochemical and functional features required for potency, serine protease specificity and aqueous stability were determined. From these studies compound 2, BMS-262084, was identified as a potent and sel...

journal_title：Bioorganic & medicinal chemistry letters

authors： Sutton JC,Bolton SA,Hartl KS,Huang MH,Jacobs G,Meng W,Ogletree ML,Pi Z,Schumacher WA,Seiler SM,Slusarchyk WA,Treuner U,Zahler R,Zhao G,Bisacchi GS

更新日期：2002-11-04 00:00:00

abstract：:Group A streptococcus is a Gram-positive bacteria that causes a range of infectious diseases. Targeting the bacteria, a new self-adjuvanting vaccine candidate, incorporating a carbohydrate carrier and an amino acid-based adjuvant, was synthesised utilising carbohydrate chemistry and solid-phase peptide synthesis proce...

journal_title：Bioorganic & medicinal chemistry letters

authors： Simerska P,Lu H,Toth I

更新日期：2009-02-01 00:00:00