Dimeric beta-turn peptidomimetics as ligands for the neurotrophin receptor TrkC.

abstract：:A series of oligo-peptide based catalysts were prepared using Fmoc solid-phase peptide synthesis. It was found that peptides with N-terminal proline residues catalyzed an aldol reaction yielding enantiomeric enriched product. Peptide H-Pro-Glu-Leu-Phe-OH catalyzed the reaction with good activity and moderate enantiose...

journal_title：Bioorganic & medicinal chemistry letters

authors： Kofoed J,Nielsen J,Reymond JL

更新日期：2003-08-04 00:00:00

abstract：:Thirty-two new derivatives of cerpegin (1,1,5-trimethylfuro[3,4-c]pyridine-3,4-dione) were designed and synthesized in high yield by a new method, combining several C(1) and N(5) substituents. All compounds were tested for their inhibitory effect on the CT-L, T-L and PA proteolytic activities of a purified mammalian 2...

journal_title：Bioorganic & medicinal chemistry letters

authors： Hovhannisyan A,Pham TH,Bouvier D,Qin L,Melikyan G,Reboud-Ravaux M,Bouvier-Durand M

更新日期：2013-05-01 00:00:00

abstract：:A series of 1-isoquinolinylguanidines are shown to be potent inhibitors of uPA with selectivity over tPA and plasmin. Potency is enhanced by the presence of a 4-halo and a 7-aryl substituent, particularly when substituted by a 3-carboxylic acid group. Compound 13j (UK-356,202) combines excellent potency and selectivit...

journal_title：Bioorganic & medicinal chemistry letters

authors： Barber CG,Dickinson RP,Fish PV

更新日期：2004-06-21 00:00:00

abstract：:Through synthesis and assays of peptidyl substrates, we could select substrates having peptidyl complementary against lipases. The best substrate showed 20-fold improved K(m) relative to non-peptidyl substrate. Using this information, we generated selective inhibitors. Lipase activities with peptidyl substrates were r...

journal_title：Bioorganic & medicinal chemistry letters

authors： Park S,Yu J

更新日期：2012-05-01 00:00:00

abstract：:A series of novel pyrazole peptidomimetics was synthesized from 3-aryl-1-arylmethyl-1H-pyrazole-5-carboxylic acid and amino acid ester. Structures of the compounds were characterized by means of IR, (1)H NMR and mass spectroscopy. Compounds 5e and 5k suppress effectively the growth of A549 lung cancer cells. Prelimina...

journal_title：Bioorganic & medicinal chemistry letters

authors： Liu YR,Luo JZ,Duan PP,Shao J,Zhao BX,Miao JY

更新日期：2012-11-15 00:00:00

abstract：:SAR studies for the exploration a novel class of anti-human immunodeficiency virus type 1 (HIV-1) agents based on the hematoxylin structure (1) are described. The systematic deoxygenations of 1 including asymmetric synthesis were conducted to obtain a compound showing high potencies for inhibiting the nuclear import a...

journal_title：Bioorganic & medicinal chemistry letters

authors： Ishii H,Koyama H,Hagiwara K,Miura T,Xue G,Hashimoto Y,Kitahara G,Aida Y,Suzuki M

更新日期：2012-02-01 00:00:00

abstract：:We synthesized novel vitamin K derivatives by converting the naphthoquinone group to benzene derivatives and benzoquinone. We evaluated their neuronal differentiation activities to investigate the effect of the quinone moiety on this process. We observed that the 1,4-quinone as well as the side chain part play importa...

journal_title：Bioorganic & medicinal chemistry letters

authors： Yoshimura H,Hirota Y,Soda S,Okazeri M,Takagi Y,Takeuchi A,Tode C,Kamao M,Osakabe N,Suhara Y

更新日期：2020-04-15 00:00:00

abstract：:A selection of 76 nitroheterocycles and related compounds from our in-house compound library was screened in vitro against the parasite Trypanosoma brucei rhodesiense, causative agent of human African trypanosomiasis (HAT). The unspecific cytotoxicity of the compounds was also evaluated against rat myoblast L6-cells t...

journal_title：Bioorganic & medicinal chemistry letters

authors： Arán VJ,Kaiser M,Dardonville C

更新日期：2012-07-15 00:00:00

abstract：:New cis-fused tetrahydrochromeno[4,3-b]quinolines have been synthesized by intramolecular [4+2] imino-Diels-Alder reactions of 2-azadienes derived in situ from aromatic amines and 7-O-prenyl derivatives of 8-formyl-2,3-disubstituted chromenones in the presence of 20mol% Yb(OTf)(3) in acetonitrile under reflux conditio...

journal_title：Bioorganic & medicinal chemistry letters

authors： Nagaiah K,Venkatesham A,Srinivasa Rao R,Saddanapu V,Yadav JS,Basha SJ,Sarma AV,Sridhar B,Addlagatta A

更新日期：2010-06-01 00:00:00

abstract：:Cyclic azobenzene carboxylic acid was synthesized using a shortened route. After reaction with D-threolinol, the resulting cyclic azobenzene-D-threolinol (cAB-Thr) building block was transformed into the corresponding DMTr-protected phosphoramidite, and incorporated into oligodeoxynucleotides at various positions and ...

journal_title：Bioorganic & medicinal chemistry letters

authors： Eljabu F,Dhruval J,Yan H

更新日期：2015-12-01 00:00:00

abstract：:Prothrombin is a vitamin K-dependent serine protease and plays pivotal roles in both procoagulant and anticoagulant pathway of hemostasis. In this study, prothrombin purified from porcine plasma was modified through PEGylation at N-terminal residue using 40 kDa PEG-phenyl-isothiocyanate (PIT-PEG40K). The monoPEGylated...

journal_title：Bioorganic & medicinal chemistry letters

authors： Zhou JG,Chen YM

更新日期：2011-06-01 00:00:00

abstract：:Radioligands are powerful tools for examining the pharmacological profiles of chemical leads and thus facilitate drug discovery. In this study, we identified and characterized 3-([1,1,1-(3)H]methyl)-2-(4-{[3-(1-pyrrolidinyl)propyl]oxy} phenyl)-4(3H)-quinazolinone ([(3)H]1) as a potent and selective radioligand for his...

journal_title：Bioorganic & medicinal chemistry letters

authors： Mitobe Y,Ito S,Mizutani T,Nagase T,Sato N,Tokita S

更新日期：2009-08-01 00:00:00

abstract：:A protocol applicable for the synthesis of an oseltamivir positron emission tomography (PET) tracer was developed. Acetylation of amine 3 with CH(3)COCl, followed by deprotection and aqueous workup, produced oseltamivir 4 from 3 within 10 min. The obtained 4 was sufficiently pure for PET studies. This method can be ex...

journal_title：Bioorganic & medicinal chemistry letters

authors： Morita M,Sone T,Yamatsugu K,Sohtome Y,Matsunaga S,Kanai M,Watanabe Y,Shibasaki M

更新日期：2008-01-15 00:00:00

abstract：:Triterpene derivatives were analyzed for anti-HIV-1 activity and for cellular toxicity. Betulinic aldehyde, betulinic nitrile, and morolic acid derivatives were identified to have anti-HIV-1 activity. These derivatives inhibit a late step in virus replication, likely virus maturation. ...

journal_title：Bioorganic & medicinal chemistry letters

authors： Dorr CR,Yemets S,Kolomitsyna O,Krasutsky P,Mansky LM

更新日期：2011-01-01 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：:The fungal pathogen Candida glabrata encodes for a β-carbonic anhydrase (CA, EC 4.2.1.1), CgNce103, recently discovered. Only anions have been investigated as CgNce103 inhibitors up until now. Here we report the first sulfonamides inhibition study of this enzyme. Simple sulfonamides showed weak or moderate CgNce103 in...

journal_title：Bioorganic & medicinal chemistry letters

authors： Vullo D,Leewattanapasuk W,Mühlschlegel FA,Mastrolorenzo A,Capasso C,Supuran CT

更新日期：2013-05-01 00:00:00

abstract：:A series of canthin-6-one analogues were designed and synthesized in order to study their antibacterial activity and structure-activity relationships. Compound 22 showed a broad spectrum of antibacterial activity and exhibited better bactericidal effect (8-fold superiority against Staphylococcus aureus and 2-fold supe...

journal_title：Bioorganic & medicinal chemistry letters

authors： Dai J,Dan W,Zhang Y,He M,Wang J

更新日期：2018-10-01 00:00:00

abstract：:Herein we describe design strategies that led to the discovery of novel pyridopyrazine-1,6-dione γ-secretase modulators (GSMs) incorporating an indole motif as a heterocyclic replacement for a naphthyl moiety that was present in the original lead 9. Tactics involving parallel medicinal chemistry and in situ monomer sy...

journal_title：Bioorganic & medicinal chemistry letters

authors： Pettersson M,Johnson DS,Humphrey JM,Am Ende CW,Evrard E,Efremov I,Kauffman GW,Stepan AF,Stiff CM,Xie L,Bales KR,Hajos-Korcsok E,Murrey HE,Pustilnik LR,Steyn SJ,Wood KM,Verhoest PR

更新日期：2015-02-15 00:00:00

abstract：:Medicinal chemistry optimization of an impurity isolated during the scale-up synthesis of a pyridylsulfonamide type dopamine D(3)/D(2) compound (1) led to a series of new piperazine derivatives having affinity to both dopamine D(3) and D(2) receptors. Several members of this group showed excellent pharmacokinetic and ...

journal_title：Bioorganic & medicinal chemistry letters

authors： Agai-Csongor E,Domány G,Nógrádi K,Galambos J,Vágó I,Keserű GM,Greiner I,Laszlovszky I,Gere A,Schmidt E,Kiss B,Vastag M,Tihanyi K,Sághy K,Laszy J,Gyertyán I,Zájer-Balázs M,Gémesi L,Kapás M,Szombathelyi Z

更新日期：2012-05-15 00:00:00

abstract：:In this communication, human 11β-hydroxysteroid dehydrogenase type 1 (11β-HSD1) inhibitory activities of a novel series of diarylsulfones are described. Optimization of this series resulted in several highly potent 11β-HSD1 inhibitors with excellent pharmacokinetic (PK) properties. Compound (S)-25 showed excellent eff...

journal_title：Bioorganic & medicinal chemistry letters

authors： Yan X,Wang Z,Sudom A,Cardozo M,DeGraffenreid M,Di Y,Fan P,He X,Jaen JC,Labelle M,Liu J,Ma J,McMinn D,Miao S,Sun D,Tang L,Tu H,Ursu S,Walker N,Ye Q,Powers JP

更新日期：2010-12-01 00:00:00

abstract：:In order to obtain rigidity within the sugar moiety of nucleosides, the bicyclic pyrimidine derivatives of N,O-isoxazolidines were designed and synthesized by using 1,3-dipolar cycloaddition of Delta(1)-pyrrolidine-1-oxide and the appropriate vinyl-nucleobases. ...

journal_title：Bioorganic & medicinal chemistry letters

authors： Procopio A,Alcaro S,De Nino A,Maiuolo L,Ortuso F,Sindona G

更新日期：2005-02-01 00:00:00

abstract：:Potent and selective antagonists of the adenosine A2A receptor often contain a nitrogen-rich fused-ring heterocyclic core. Replacement of the core with an isomeric ring system has previously been shown to improve target affinity, selectivity, and in vivo activity. This paper describes the preparation, by a novel route...

journal_title：Bioorganic & medicinal chemistry letters

authors： Dowling JE,Vessels JT,Haque S,Chang HX,van Vloten K,Kumaravel G,Engber T,Jin X,Phadke D,Wang J,Ayyub E,Petter RC

更新日期：2005-11-01 00:00:00

abstract：:Bruton's Tyrosine Kinase (BTK) is one of the crucial kinases for the B cell maturation and mast cell activation, and specific inhibitors of BTK are considered to be attractive targets in drug discovery research. In this Letter, we have designed and synthesized a new fluorescent probe for TR-FRET-based high-throughput ...

journal_title：Bioorganic & medicinal chemistry letters

authors： Asami T,Kawahata W,Sawa M

更新日期：2015-01-01 00:00:00

abstract：:In an effort to develop antagonists for kappa-mu opioid receptor heterodimers, a series of bivalent ligands 3-6 containing kappa- and mu-antagonist pharmacophores were designed and synthesized. Evaluation of the series in HEK-293 cells revealed 4 (KMN-21) to selectively antagonize the activation of kappa-mu heterodime...

journal_title：Bioorganic & medicinal chemistry letters

authors： Zhang S,Yekkirala A,Tang Y,Portoghese PS

更新日期：2009-12-15 00:00:00

abstract：:We have synthesized and evaluated a new series of acyclic P4-benzoxaborole-based HCV NS3 protease inhibitors. Structure-activity relationships were investigated, leading to the identification of compounds 5g and 17 with low nanomolar potency in the enzymatic and cell-based replicon assay. The linker-truncated compound...

journal_title：Bioorganic & medicinal chemistry letters

authors： Li X,Zhang S,Zhang YK,Liu Y,Ding CZ,Zhou Y,Plattner JJ,Baker SJ,Bu W,Liu L,Kazmierski WM,Duan M,Grimes RM,Wright LL,Smith GK,Jarvest RL,Ji JJ,Cooper JP,Tallant MD,Crosby RM,Creech K,Ni ZJ,Zou W,Wright J

更新日期：2011-04-01 00:00:00

abstract：:Two new cyclic octapeptides, mariannamides A (1) and B (2), have been isolated from Mariannaea elegans NBRC102301, a Pinus densiflora-derived filamentous fungus. Their structures were elucidated to be cyclo-(l-Leu1-l-Pro1-l-Pro2-l-Leu2-l-Ile1-l-Pro3-l-Val1-l-Ile2) and cyclo-(l-Leu1-l-Pro1-l-Pro2-l-Leu2-l-Ile1-l-Pro3-l...

journal_title：Bioorganic & medicinal chemistry letters

authors： Ishiuchi K,Hirose D,Kondo T,Watanabe K,Terasaka K,Makino T

更新日期：2020-02-15 00:00:00

abstract：:Pyrrole-imidazole polyamides can be synthesized to target predetermined sequences of DNA with nanomolar affinity and high specificity, and have been shown to modulate gene transcription both in vitro and in vivo. To make polyamides more readily available to biological laboratories, we have developed a rapid solid-phas...

journal_title：Bioorganic & medicinal chemistry letters

authors： Krutzik PO,Chamberlin AR

更新日期：2002-08-19 00:00:00

abstract：:Menin functions as an oncogenic cofactor of mixed lineage leukaemia (MLL) fusion proteins in leukaemogenesis. The menin-MLL interface is a potential therapeutic target in acute leukaemia cases. In this study, approximately 900 clinical compounds were evaluated and ranked using pharmacophore-based virtual screening, th...

journal_title：Bioorganic & medicinal chemistry letters

authors： Li L,Zhou R,Geng H,Yue L,Ye F,Xie Y,Liu J,Kong X,Jiang H,Huang J,Luo C

更新日期：2014-05-01 00:00:00

abstract：:A series of phenoxy benzoxaboroles were synthesized and screened for their inhibitory activity against PDE4 and cytokine release. 5-(4-Cyanophenoxy)-2,3-dihydro-1-hydroxy-2,1-benzoxaborole (AN2728) showed potent activity both in vitro and in vivo. This compound is now in clinical development for the topical treatment ...

journal_title：Bioorganic & medicinal chemistry letters

authors： Akama T,Baker SJ,Zhang YK,Hernandez V,Zhou H,Sanders V,Freund Y,Kimura R,Maples KR,Plattner JJ

更新日期：2009-04-15 00:00:00

abstract：:Aminoisoquinoline and isoquinoline groups have successfully replaced the more basic P1 benzamidine group of an acylsulfonamide factor VIIa inhibitor. Inhibitory activity was optimized by the identification of additional hydrophobic and hydrophilic P' binding interactions. The molecular details of these interactions we...

journal_title：Bioorganic & medicinal chemistry letters

authors： Glunz PW,Zhang X,Zou Y,Delucca I,Nirschl AH,Cheng X,Weigelt CA,Cheney DL,Wei A,Anumula R,Luettgen JM,Rendina AR,Harpel M,Luo G,Knabb R,Wong PC,Wexler RR,Priestley ES

更新日期：2013-09-15 00:00:00