Synthesis and NK1/NK2 receptor activity of substituted-4(Z)-(methoxyimino)pentyl-1-piperazines.

abstract：:Novel quinolone-macrocycle conjugates displayed submicromolar antibacterial activity against Escherichia coli and Staphylococcus aureus bacterial strains. An analogous open-chain structure was not active at 100 microM against the same pathogenic strains. ...

journal_title：Bioorganic & medicinal chemistry letters

authors： Jefferson EA,Swayze EE,Osgood SA,Miyaji A,Risen LM,Blyn LB

更新日期：2003-05-19 00:00:00

abstract：:A novel curcumin mimic library (14a-14h and 15a-15h) possessing variously substituted benzimidazole groups was synthesized through the aldol reaction of (E)-4-(4-hydroxy-3-methoxyphenyl)but-3-en-2-one (7) or (E)-4-(3-hydroxy-4-methoxyphenyl)but-3-en-2-one (13) with diversely substituted benzimidazolyl-2-carbaldehyde (...

journal_title：Bioorganic & medicinal chemistry letters

authors： Woo HB,Eom YW,Park KS,Ham J,Ahn CM,Lee S

更新日期：2012-01-15 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：:Ubiquitin-dependent proteolysis of cellular proteins is one of the major pathways to regulate protein function posttranslationally. Here we demonstrate a potentially general method of degrading any targeted proteins by the ubiquitin-dependent proteolysis in living cells, using small-molecule proteolysis inducer (SMPI)...

journal_title：Bioorganic & medicinal chemistry letters

authors： Zhang D,Baek SH,Ho A,Kim K

更新日期：2004-02-09 00:00:00

abstract：:Regioselective synthesis of a number of highly functionalized 3-benzylpyrimidino chromen-2-ones (4) were accomplished in a one pot three component reaction in acetic acid and determined their anti-microbial and anti-biofilm activities. Compounds 4o and 4p showed an excellent anti-microbial activity against Micrococcus...

journal_title：Bioorganic & medicinal chemistry letters

authors： Emmadi NR,Atmakur K,Bingi C,Godumagadda NR,Chityal GK,Nanubolu JB

更新日期：2014-01-15 00:00:00

abstract：:Cathepsin K is highly expressed in human osteoclasts, and is implicated in bone resorption. This makes it an attractive target for the treatment of osteoporosis. Peptides containing 2-amino-1'-hydroxymethyl ketones and 2-amino-1'-alkoxymethyl ketones were discovered as potent inhibitors of cathepsin K. A novel synthet...

journal_title：Bioorganic & medicinal chemistry letters

authors： Mendonca RV,Venkatraman S,Palmer JT

更新日期：2002-10-21 00:00:00

abstract：:Selective phosphodiesterase 2 (PDE2) inhibitors are shown to have efficacy in a rat model of osteoarthritis (OA) pain. We identified potent, selective PDE2 inhibitors by optimizing residual PDE2 activity in a series of phosphodiesterase 4 (PDE4) inhibitors, while minimizing PDE4 inhibitory activity. These newly design...

journal_title：Bioorganic & medicinal chemistry letters

authors： Plummer MS,Cornicelli J,Roark H,Skalitzky DJ,Stankovic CJ,Bove S,Pandit J,Goodman A,Hicks J,Shahripour A,Beidler D,Lu XK,Sanchez B,Whitehead C,Sarver R,Braden T,Gowan R,Shen XQ,Welch K,Ogden A,Sadagopan N,Baum H

更新日期：2013-06-01 00:00:00

abstract：:A series of 9-aminoalkanamido-1-azabenzanthrones derviatives (3a-i Ar-NHCO(CH(2))(n)NR(1)R(2)) and their quaternary methiodide salts (4a-g Ar-NHCO(CH(2))(n)N(+)(CH(3))R(1)R(2)I(-)) were designed and synthesized as acetylcholinesterase (AChE) or butyrylcholinesterase (BuChE) inhibitors. The synthetic compounds exhibite...

journal_title：Bioorganic & medicinal chemistry letters

authors： Tang H,Ning FX,Wei YB,Huang SL,Huang ZS,Chan AS,Gu LQ

更新日期：2007-07-01 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：:A new family of photonuclease, thiadiazole-naphthalimide were synthesized and evaluated. Thiadiazole group was incorporated for the first time. These compounds intercalated into DNA efficiently and damaged DNA as low as 10 microM photochemically. Mechanism experiment showed that electron transfer and radicals were inv...

journal_title：Bioorganic & medicinal chemistry letters

authors： Li Y,Xu Y,Qian X,Qu B

更新日期：2003-10-20 00:00:00

abstract：:Structure-activity relationship (SAR) efforts around our initial lead compound 1 led to the identification of potent P2X(7) receptor antagonists with improved pharmacokinetic profiles. These compounds were potent and selective at the P2X(7) receptor in both human and rodent. Compound (entry 31) exhibited oral efficacy...

journal_title：Bioorganic & medicinal chemistry letters

authors： Matasi JJ,Brumfield S,Tulshian D,Czarnecki M,Greenlee W,Garlisi CG,Qiu H,Devito K,Chen SC,Sun Y,Bertorelli R,Geiss W,Le VD,Martin GS,Vellekoop SA,Haber J,Allard ML

更新日期：2011-06-15 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：:Sphingosine-1-phosphate (S1P) is an important regulator of a wide variety of biological processes acting as an endogenous ligand to EDG/S1P receptors. In an effort to establish structure-activity relationship between EDG/S1P and ligands, we report herein homology modeling study of EDG-1/S1P(1), syntheses of S1P analog...

journal_title：Bioorganic & medicinal chemistry letters

authors： Lim HS,Park JJ,Ko K,Lee MH,Chung SK

更新日期：2004-05-17 00:00:00

abstract：:DNA G-quadruplex is an attractive drug target for anticancer therapy. Most G-quadruplex ligands have little selectivity, due to π-stacking interaction with common G-tetrads surface. Thanks to the varieties of G-quadruplex grooves, the groove-binding ligand is expected to create high selectivity. Therefore, developing ...

journal_title：Bioorganic & medicinal chemistry letters

authors： Li J,Jin X,Hu L,Wang J,Su Z

更新日期：2011-12-01 00:00:00

abstract：:In silico modelling was used to guide the positioning of the fluorescent dye NBD-F on the cannabinoid CB2 receptor agonist JWH-015. While the ultimate fluorescent conjugate lost extensive binding affinity to the cannabinoid CB2 receptor, affinity and efficacy studies on the naphthoyl 3-position modified precursor mole...

journal_title：Bioorganic & medicinal chemistry letters

authors： Yates AS,Doughty SW,Kendall DA,Kellam B

更新日期：2005-08-15 00:00:00

abstract：:A series of 1-aminotetralin scaffolds was synthesized via metal-catalyzed ring-opening reactions of heterobicyclic alkenes. Small libraries of amides and amines were made using the amino group of each scaffold as a handle. Screening of these libraries against human opioid receptors led to the identification of (S)-(S)...

journal_title：Bioorganic & medicinal chemistry letters

authors： Dockendorff C,Jin S,Olsen M,Lautens M,Coupal M,Hodzic L,Spear N,Payza K,Walpole C,Tomaszewski MJ

更新日期：2009-02-15 00:00:00

abstract：: ...

journal_title：Bioorganic & medicinal chemistry letters

authors： Feng JH,Hu XL,Lv XY,Wang BL,Lin J,Zhang XQ,Ye WC,Xiong F,Wang H

更新日期：2019-01-15 00:00:00

abstract：:Paclitaxel (PTX) was complexed with beta-cyclodextrin (1), 2,6-dimethyl-beta-cyclodextrin (2) and 2,3,6-trimethyl-beta-cyclodextrin (3). PTX-CYD complexes were characterized both at the solid and liquid states. Experimental findings are in agreement with molecular modeling analysis, which showed different PTX-CYD inte...

journal_title：Bioorganic & medicinal chemistry letters

authors： Alcaro S,Ventura CA,Paolino D,Battaglia D,Ortuso F,Cattel L,Puglisi G,Fresta M

更新日期：2002-06-17 00:00:00

abstract：:A series of novel benzoxazole derivatives has been designed and shown to exhibit attractive JAK2 inhibitory profiles in biochemical and cellular assays, capable of delivering compounds with favorable PK properties in rats. Synthesis and structure-activity relationship data are also provided. ...

journal_title：Bioorganic & medicinal chemistry letters

authors： Gerspacher M,Furet P,Pissot-Soldermann C,Gaul C,Holzer P,Vangrevelinghe E,Lang M,Erdmann D,Radimerski T,Regnier CH,Chene P,De Pover A,Hofmann F,Baffert F,Buhl T,Aichholz R,Blasco F,Endres R,Trappe J,Drueckes P

更新日期：2010-03-01 00:00:00

abstract：:A new class of chymase inhibitor featuring a benzimidazolone core with an acid side chain and a P(1) hydrophobic moiety is described. Incubation of the lead compound with GSH resulted in the formation of a GSH conjugate on the benzothiophene P(1) moiety. Replacement of the benzothiophene with different heterocyclic sy...

journal_title：Bioorganic & medicinal chemistry letters

authors： Lo HY,Nemoto PA,Kim JM,Hao MH,Qian KC,Farrow NA,Albaugh DR,Fowler DM,Schneiderman RD,Michael August E,Martin L,Hill-Drzewi M,Pullen SS,Takahashi H,De Lombaert S

更新日期：2011-08-01 00:00:00

abstract：:The structure-activity relationship and the synthesis of novel N-[(3S)-pyrrolidin-3-yl]benzamides as dual serotonin and noradrenaline monoamine reuptake inhibitors (SNRI) is described. Preferred compound 9 aka PF-184,298 is a potent SNRI with good selectivity over dopamine reuptake inhibition (DRI), good in vitro meta...

journal_title：Bioorganic & medicinal chemistry letters

authors： Wakenhut F,Allan GA,Fish PV,Fray MJ,Harrison AC,McCoy R,Phillips SC,Ryckmans T,Stobie A,Westbrook D,Westbrook SL,Whitlock GA

更新日期：2009-09-01 00:00:00

abstract：:The chemoenzymatic deacylation of ramoplanin A2 is described for the first time: ramoplanin A2 was Boc-protected and hydrogenated to Boc-protected tetrahydroramoplanin, which was subsequently deacylated using an acylase from Actinoplanes utahensis NRRL 12052. The chemoenzymatic process proceeded with 80% overall yield...

journal_title：Bioorganic & medicinal chemistry letters

authors： Gandolfi R,Marinelli F,Ragg E,Romano D,Molinari F

更新日期：2012-08-15 00:00:00

abstract：:The iridium(III)-catalyzed ortho-C-H amidation of benzoic acids with sulfonyl azides is described. These transformations allow the facile generation of N-sulfonyl anthranilic acids, which are known as crucial scaffolds found in biologically active molecules. In addition, all synthetic products were evaluated for in vi...

journal_title：Bioorganic & medicinal chemistry letters

authors： Han SH,Suh HS,Jo H,Oh Y,Mishra NK,Han S,Kim HS,Jung YH,Lee BM,Kim IS

更新日期：2017-05-15 00:00:00

abstract：:A new class of 1,2,3-triazol derivatives derived from nimesulide was designed as potential inhibitors of PDE4B. Synthesis of these compounds was carried out via a multi-step sequence consisting of copper-catalyzed azide-alkyne cycloaddition (CuAAC) as a key step in aqueous media. The required azide was prepared via th...

journal_title：Bioorganic & medicinal chemistry letters

authors： Mareddy J,Nallapati SB,Anireddy J,Devi YP,Mangamoori LN,Kapavarapu R,Pal S

更新日期：2013-12-15 00:00:00

abstract：:Prostate cancer is one of the leading causes of death among males in the world. Prostate cancer cells have been shown to express upregulated chemokine receptor CCR5, a G protein-coupled receptor (GPCR) that relates to the inflammation process. Anibamine, a natural product containing a pyridine ring and two aliphatic s...

journal_title：Bioorganic & medicinal chemistry letters

authors： Xu GG,Zaidi SA,Zhang F,Singh S,Raborg TJ,Yuan Y,Zhang Y

更新日期：2015-09-01 00:00:00

abstract：:Based on a series of diaryl amides the corresponding inverse amides have been found to be potent TRPV1 receptor antagonists. Benzimidazole and indazolone derivatives prepared retained good potency in vitro and indazolone 4a was identified as a novel TRPV1 receptor antagonist suitable for evaluating orally in animal mo...

journal_title：Bioorganic & medicinal chemistry letters

authors： Fletcher SR,McIver E,Lewis S,Burkamp F,Leech C,Mason G,Boyce S,Morrison D,Richards G,Sutton K,Jones AB

更新日期：2006-06-01 00:00:00

abstract：:We have designed and synthesized a novel series of 3-biphenylamino acid amides as cathepsin K inhibitors based on compound I. In these inhibitors, we have discovered 4-aminophenoxyacetic acids 43 and 47 with good IC(50) values, although lipophilic groups are favorable for the hydrophobic S1' pocket. ...

journal_title：Bioorganic & medicinal chemistry letters

authors： Shinozuka T,Shimada K,Matsui S,Yamane T,Ama M,Fukuda T,Taki M,Naito S

更新日期：2006-03-15 00:00:00

abstract：:The reaction of methoxypoly(ethylene glycol)-4-nitrophenyl carbonate with amphotericin B has been used to prepare a new conjugate of amphotericin B (mPEG-AmB). A preliminary screening of in vitro antifungal activity has suggested that mPEG-AmB possesses a similar effect and a similar spectrum of activity as the conven...

journal_title：Bioorganic & medicinal chemistry letters

authors： Sedlák M,Buchta V,Kubicová L,Simůnek P,Holcapek M,Kasparová P

更新日期：2001-11-05 00:00:00

abstract：:A scaffold hopping strategy was successfully applied in discovering 2-aminooxazole amides as potent DGAT1 inhibitors for the treatment of dyslipidemia. Further optimization in potency and PK properties resulted in a lead series with oral in vivo efficacy in a mouse postprandial triglyceridemia (PPTG) assay. ...

journal_title：Bioorganic & medicinal chemistry letters

authors： Kim HM,Smith MD,Kim JH,Caplen MA,Chan TY,McKittrick BA,Cook JA,van Heek M,Lachowicz J

更新日期：2013-12-01 00:00:00

abstract：:A serendipitous discovery that the metalloprotease binding profile of a novel class of 2-carboxamide-3-hydroxamic acid piperidines could be significantly attenuated by the modification of the unexplored P1 substituent enabled the design and synthesis of a novel 2-carboxamide-1-hydroxamic acid cyclohexyl scaffold core ...

journal_title：Bioorganic & medicinal chemistry letters

authors： Burns DM,Li YL,Shi E,He C,Xu M,Zhuo J,Zhang C,Qian DQ,Li Y,Wynn R,Covington MB,Katiyar K,Marando CA,Fridman JS,Scherle P,Friedman S,Metcalf B,Yao W

更新日期：2009-07-01 00:00:00