Synthesis and characterisation of a new amphotericin B-methoxypoly(ethylene glycol) conjugate.

abstract：:In an effort to develop inhibitors of VanX, the phosphonamidate analogs of D-Ala-D-Ala dipeptides, N-[(1-aminoethyl) hydroxyphosphinyl]-glycine (1a), -alanine (1b), -valine (1c), -leucine (1d) and -phenylalanine (1e) were synthesized, characterized and evaluated using recombinant VanX. The crystal structure of the int...

journal_title：Bioorganic & medicinal chemistry letters

authors： Yang KW,Cheng X,Zhao C,Liu CC,Jia C,Feng L,Xiao JM,Zhou LS,Gao HZ,Yang X,Zhai L

更新日期：2011-12-01 00:00:00

abstract：:(Me)FGC(Bz)DEVD was radiolabeled with technetium-99m in high yield. This tracer was preferentially accumulated in apoptotic cells in the in vitro studies. Tumor uptake occurred in vivo after cisplatin injection due to the apoptosis induction, which not observed in the untreated tumors. Therefore, (99m)Tc-(Me)FGCDEVD i...

journal_title：Bioorganic & medicinal chemistry letters

authors： Bohn P,Mouchard F,Rouvet J,de Boisgrollier AC,Vera P

更新日期：2013-03-01 00:00:00

abstract：:A series of 7-acyloxymethylcamptothecin and 20-O-acyl-7-acyloxymethylcamptothecin derivatives were regioselectively prepared on different solvents. 7-Acyloxymethylcamptothecins possess more efficacy than 20-O-acyl-7-acyloxymethylcamptothecins against six human cancer cell lines in vitro. ...

journal_title：Bioorganic & medicinal chemistry letters

authors： Pan XD,Han R,Sun PY

更新日期：2003-11-03 00:00:00

abstract：:A new series of 2-(benzyloxy)benzamides are presented that are potent functional antagonists of TRPM8 and possess improved LipE and LE compared to the original lead. They were discovered through a series of compound libraries and we present a powerful visualization method for the chemical space explored with each libr...

journal_title：Bioorganic & medicinal chemistry letters

authors： Brown A,Ellis D,Favor DA,Kirkup T,Klute W,MacKenny M,McMurray G,Stennett A

更新日期：2013-11-15 00:00:00

abstract：:GTP cyclohydrolase (GCYH-I) is an enzyme in the folate biosynthesis pathway that has not been previously exploited as an antibiotic target, although several pathogens including N. gonorrhoeae use a form of the enzyme GCYH-IB that is structurally distinct from the human homologue GCYH-IA. A comparison of the crystal st...

journal_title：Bioorganic & medicinal chemistry letters

authors： Samaan GN,Paranagama N,Haque A,Hecht DA,Swairjo MA,Purse BW

更新日期：2020-01-15 00:00:00

abstract：:The capabilities of 20 strains of fungi to transform acetyl-11-keto-β-boswellic (AKBA) were screened. And biotransformation of AKBA by Cunninghamella blakesleana AS 3.970 afforded five metabolites (1-5), while two metabolites (6, 7) were isolated from biotransformation of Cunninghamella elegans AS 3.1207. The chemical...

journal_title：Bioorganic & medicinal chemistry letters

authors： Sun Y,Liu D,Xi R,Wang X,Wang Y,Hou J,Zhang B,Wang C,Liu K,Ma X

更新日期：2013-03-01 00:00:00

abstract：:Several benzofuran derivatives linked to a 3-indoletetrahydropyridine through an alkyl chain were prepared and evaluated for serotonin transporter and 5-HT(1A) receptor affinities. Their design, synthesis and structure-activity relationships are described. ...

journal_title：Bioorganic & medicinal chemistry letters

authors： Venkatesan AM,Dos Santos O,Ellingboe J,Evrard DA,Harrison BL,Smith DL,Scerni R,Hornby GA,Schechter LE,Andree TH

更新日期：2010-02-01 00:00:00

abstract：:Coibamide A is a highly potent antiproliferative cyclic depsipeptide, which was originally isolated from a Panamanian marine cyanobacterium. In this study, the synthesis of coibamide A has been investigated using Fmoc-based solid-phase peptide synthesis followed by the cleavage of the resulting linear peptide from the...

journal_title：Bioorganic & medicinal chemistry letters

authors： Nabika R,Suyama TL,Hau AM,Misu R,Ohno H,Ishmael JE,McPhail KL,Oishi S,Fujii N

更新日期：2015-01-15 00:00:00

abstract：:A potent and novel class of product-like inhibitors of the HCV NS3 protease was discovered by employing a phosphinic acid as a carboxylate isostere. The replicon activity and pharmacokinetic profile of this series of compounds was optimized by exploring the substitution of the phosphinic acid, as well as conformationa...

journal_title：Bioorganic & medicinal chemistry letters

authors： Clarke MO,Chen X,Cho A,Delaney WE 4th,Doerffler E,Fardis M,Ji M,Mertzman M,Pakdaman R,Pyun HJ,Rowe T,Yang CY,Sheng XC,Kim CU

更新日期：2011-06-15 00:00:00

abstract：:A series of indole ring containing compounds were designed based on the structure of the gp41 complex in the region of the hydrophobic pocket. These compounds were synthesized using a Suzuki Coupling reaction, and evaluated using a fluorescence binding assay and cell-cell fusion assay. The observed inhibition constant...

journal_title：Bioorganic & medicinal chemistry letters

authors： Zhou G,Wu D,Hermel E,Balogh E,Gochin M

更新日期：2010-03-01 00:00:00

abstract：:The general strategy and rationale underlying the design of COPD therapeutics that possess protease inhibitory activity and are also capable of releasing a species that attenuates inflammation by inhibiting caspase-1, are described. The synthesis and in vitro biochemical evaluation of a dual function molecule that seq...

journal_title：Bioorganic & medicinal chemistry letters

authors： Dou D,He G,Alliston KR,Groutas WC

更新日期：2011-05-15 00:00:00

abstract：:A novel series of readily water soluble 8-methylureido-4,5-dihydro-4-oxo-10H-imidazo[1,2-a]indeno[1,2-e]++ +pyrazines were synthesized. The -10-yl acetic acid ((+)-3) and -10-carboxylidene (4) derivatives exhibit potent affinities (IC50=4 and 19 nM, respectively) and antagonist properties (IC50 = 2 and 3 nM, respectiv...

journal_title：Bioorganic & medicinal chemistry letters

authors： Mignani S,Bohme GA,Boireau A,Cheve M,Damour D,Debono MW,Genevois-Borella A,Imperato A,Jimonet P,Pratt J,Randle JC,Ribeill Y,Vuilhorgne M,Stutzmann JM

更新日期：2000-03-20 00:00:00

abstract：:2-Propargylthiobenzimidazole 1, 4-bromomethyl coumarins/1-aza-coumarins 2/3 and sodium azide have been reacted in one pot under Click chemistry conditions to give exclusively 1,4-disubstituted triazoles 5a-n. Anti-tubercular assays against M. tuberculosis (H37Rv) coupled with in silico molecular docking studies indica...

journal_title：Bioorganic & medicinal chemistry letters

authors： Anand A,Kulkarni MV,Joshi SD,Dixit SR

更新日期：2016-10-01 00:00:00

abstract：:Extensive SAR studies and optimization of ADME properties of benzimidazol-2-one derivatives led to the identification of BMS-433771 (3) as an orally active RSV fusion inhibitor. In order to extend the structure-activity relationships for this compound series, substitution of the benzimidazole ring was examined with a ...

journal_title：Bioorganic & medicinal chemistry letters

authors： Wang XA,Cianci CW,Yu KL,Combrink KD,Thuring JW,Zhang Y,Civiello RL,Kadow KF,Roach J,Li Z,Langley DR,Krystal M,Meanwell NA

更新日期：2007-08-15 00:00:00

abstract：:A series of N-7-methyl-imidazolopyrimidine inhibitors of the mTOR kinase have been designed and prepared, based on the hypothesis that the N-7-methyl substituent on imidazolopyrimidine would impart selectivity for mTOR over the related PI3Kα and δ kinases. The corresponding N-Me substituted pyrrolo[3,2-d]pyrimidines a...

journal_title：Bioorganic & medicinal chemistry letters

authors： Lee W,Ortwine DF,Bergeron P,Lau K,Lin L,Malek S,Nonomiya J,Pei Z,Robarge KD,Schmidt S,Sideris S,Lyssikatos JP

更新日期：2013-09-15 00:00:00

abstract：:Herein we report the synthesis of a series of bicyclo[3.2.1]octanes and their binding characteristics at the dopamine and serotonin transporters. The data confirm that a heteroatom at position 8 of the tropane nucleus is not a prerequisite for binding since the bicyclo[3.2.1]octanes prove potent inhibitors of both tra...

journal_title：Bioorganic & medicinal chemistry letters

authors： Meltzer PC,Blundell P,Chen Z,Yong YF,Madras BK

更新日期：1999-03-22 00:00:00

abstract：:The design and synthesis of a novel series of non-nucleoside HIV reverse transcriptase inhibitors (NNRTIs) based on a pyrazole template is described. These compounds are active against wild type reverse transcriptase (RT) and retain activity against clinically important mutants. ...

journal_title：Bioorganic & medicinal chemistry letters

authors： Mowbray CE,Burt C,Corbau R,Perros M,Tran I,Stupple PA,Webster R,Wood A

更新日期：2009-10-01 00:00:00

abstract：:We have synthesized and evaluated a series of 1,4-disubstituted-triazole derivatives for inhibition of the rat Na(V)1.6 sodium channel isoform, an isoform thought to play an important role in controlling neuronal firing. Starting from a series of 2,4(1H)-diarylimidazoles previously published, we decided to extend the ...

journal_title：Bioorganic & medicinal chemistry letters

authors： Rivara M,Patel MK,Amori L,Zuliani V

更新日期：2012-10-15 00:00:00

abstract：:Two natural piperamides (piperlonguminine and refrofractamide A) and their derivatives were synthesized and evaluated for inhibitory activity against histone deacetylases, as well as the HCT-116 human colon cancer cell line. The preliminary structure activity relationship was discussed. Compounds featuring a hydroxami...

journal_title：Bioorganic & medicinal chemistry letters

authors： Luo Y,Liu HM,Su MB,Sheng L,Zhou YB,Li J,Lu W

更新日期：2011-08-15 00:00:00

abstract：:The present work reports on the preparation of glass surfaces coated with NPPOC-protected aminooxy groups and their use for the patterning of oligonucleotides on glass slides and in capillary tubes. The method involves the use of surfaces coated with amino groups using (gamma-aminopropyl)triethoxy silane and subsequen...

journal_title：Bioorganic & medicinal chemistry letters

authors： Dendane N,Hoang A,Defrancq E,Vinet F,Dumy P

更新日期：2008-04-15 00:00:00

abstract：:The synthesis and biological activity of novel glycoprotein IIb-IlIa anatagonists containing 3-azaspiro[5.5]undec-9-yl nucleus are described. The potent activity of these compounds as platelet aggregation inhibitors demonstrates the utility of the monoazaspirocyclic structure as central template for nonpeptide RGD mim...

journal_title：Bioorganic & medicinal chemistry letters

authors： Pandey A,Seroogy J,Volkots D,Smyth MS,Rose J,Mehrotra MM,Heath J,Ruhter G,Schotten T,Scarborough RM

更新日期：2001-05-21 00:00:00

abstract：:Three new pseudo-symmetrical tamoxifen derivatives, RID-B (15), C (16), and D (17), were synthesized via the novel three-component coupling reaction, and the structure-activity relationships of the pseudo-symmetrical tamoxifen derivatives were examined. It was discovered that 15 strongly inhibits the viability of HL-6...

journal_title：Bioorganic & medicinal chemistry letters

authors： Shiina I,Sano Y,Nakata K,Kikuchi T,Sasaki A,Ikekita M,Hasome Y

更新日期：2007-05-01 00:00:00

abstract：:New carbon-11 labeled D-luciferin analogs D-luciferin [(11)C]methyl ester ([(11)C]LMEster, [(11)C]1) and D-luciferin [(11)C]methyl ether ([(11)C]LMEther, [(11)C]2) were synthesized in 25-55% radiochemical yield. PET studies with [(11)C]LMEster and [(11)C]LMEther demonstrate a lower retention of the C-11 label at 45 mi...

journal_title：Bioorganic & medicinal chemistry letters

authors： Wang JQ,Pollok KE,Cai S,Stantz KM,Hutchins GD,Zheng QH

更新日期：2006-01-15 00:00:00

abstract：:A series of 4-aryl-3-aminoquinoline-2-one derivatives was synthesized and evaluated as activators of the cloned maxi-K channel mSlo (hSlo) expressed in Xenopus laevis oocytes using electrophysiological methods. A brain penetrable activator of maxi-K channels was identified and shown to be significantly active in the M...

journal_title：Bioorganic & medicinal chemistry letters

authors： Hewawasam P,Fan W,Knipe J,Moon SL,Boissard CG,Gribkoff VK,Starrett JE

更新日期：2002-07-08 00:00:00

abstract：:We report the synthesis and properties of two new seminaphthorhodafluor (SNARF) derivatives, SNARF-F and SNARF-Cl. Both these derivatives exhibit typical red shifts of absorption and fluorescence, and higher cell permeability as compared to traditional SNARF, while the pH-dependent dual-emission characteristics are we...

journal_title：Bioorganic & medicinal chemistry letters

authors： Nakata E,Nazumi Y,Yukimachi Y,Uto Y,Maezawa H,Hashimoto T,Okamoto Y,Hori H

更新日期：2011-03-15 00:00:00

abstract：:Peroxisome proliferator-activated receptors (PPARs) are attractive targets for the treatment of the metabolic syndrome. Especially a combination of PPARα and PPARγ agonistic activity seems worthwhile to be pursued. Herein we present the design and synthesis of a series of pirinixic acid derivatives as potent PPARα par...

journal_title：Bioorganic & medicinal chemistry letters

authors： Lamers C,Dittrich M,Steri R,Proschak E,Schubert-Zsilavecz M

更新日期：2014-08-15 00:00:00

abstract：:Dipeptidyl peptidase IV (DPP4) is a multifunctional type II transmembrane serine peptidase which regulates various physiological processes, most notably plasma glucose homeostasis by cleaving peptide hormones glucagon-like peptide-1 and glucose-dependent insulinotropic polypeptide. Inhibition of DPP4 is a potentially ...

journal_title：Bioorganic & medicinal chemistry letters

authors： Zhao G,Taunk PC,Magnin DR,Simpkins LM,Robl JA,Wang A,Robertson JG,Marcinkeviciene J,Sitkoff DF,Parker RA,Kirby MS,Hamann LG

更新日期：2005-09-15 00:00:00

abstract：:A new family of bioactive bromotyrosine derivatives, termed mololipids, was recently isolated from a Hawaiian sponge, but could not be resolved into individual components by chromatography. To complete their structural characterization and better understand structure-activity relationships, the first pure samples of d...

journal_title：Bioorganic & medicinal chemistry letters

authors： Schoenfeld RC,Lumb JP,Fantini J,Ganem B

更新日期：2000-12-04 00:00:00

abstract：:A series of (S)-N-(1,4-naphthoquinon-2-yl)-alpha-amino acid methyl esters 3-9, 2-N,N-dialkylamino-1,4-naphthoquinones 10-11 and 2-hydroxy-3-(2'-mercaptoimidazolyl)-1,4-naphthoquinones and their cyclic analogs 12-15 were synthesized and evaluated for antifungal and antibacterial activities. The structure-activity relat...

journal_title：Bioorganic & medicinal chemistry letters

authors： Tandon VK,Yadav DB,Singh RV,Chaturvedi AK,Shukla PK

更新日期：2005-12-01 00:00:00

abstract：:A regiochemical and stereochemical mixture of flexible linkers bearing terminal azide functionality was synthesized in two steps from squalene and was used to connect two high affinity NDP-alpha-MSH ligands or two low affinity MSH(4) ligands. The ligands were N-terminally acylated using N-hydroxysuccinimidoyl 5-hexyno...

journal_title：Bioorganic & medicinal chemistry letters

authors： Jagadish B,Sankaranarayanan R,Xu L,Richards R,Vagner J,Hruby VJ,Gillies RJ,Mash EA

更新日期：2007-06-15 00:00:00