Analogues of dealanylalahopcin are inhibitors of human HIF prolyl hydroxylases.

abstract：:Numerous potent P2X3 antagonists have been discovered and the therapeutic potential of P2X3 antagonism already comprises proof-of-concept data obtained in clinical trials with the most advanced compound. We have lately reported the discovery and optimization of thia-triaza-tricycle compounds with potent P2X3 antagonis...

journal_title：Bioorganic & medicinal chemistry letters

authors： Szántó G,Makó A,Vágó I,Hergert T,Bata I,Farkas B,Kolok S,Vastag M

更新日期：2016-08-15 00:00:00

abstract：:A series of novel 1,3,4-oxadiazole/thiadiazole-chalcone conjugates were synthesized and their in vitro and in vivo antiviral activities were evaluated via microscale thermophoresis method and half-leaf method, respectively. The in vitro results indicated that compounds 7g, 7l, 8h, and 8l displayed good antiviral activ...

journal_title：Bioorganic & medicinal chemistry letters

authors： Gan X,Hu D,Chen Z,Wang Y,Song B

更新日期：2017-09-15 00:00:00

abstract：:A novel series of triazole tethered coumarin-benzotriazole hybrids based on donepezil skeleton has been designed and synthesized as multifunctional agents for the treatment of Alzheimer's disease (AD). Among the synthesized compounds 13b showed most potent acetylcholinesterase (AChE) inhibition (IC50 = 0.059 μΜ) with ...

journal_title：Bioorganic & medicinal chemistry letters

authors： Singh A,Sharma S,Arora S,Attri S,Kaur P,Kaur Gulati H,Bhagat K,Kumar N,Singh H,Vir Singh J,Mohinder Singh Bedi P

更新日期：2020-10-15 00:00:00

abstract：:The protein-tyrosine phosphatase (PTP) 'YopH' is a virulence factor of Yersinia pestis, the causative agent of plague. Potential use of Yersinia as a bioterrorism agent renders YopH inhibitors of therapeutic importance. Previously, we had examined the inhibitory potencies of a variety of phosphotyrosyl (pTyr) mimetics...

journal_title：Bioorganic & medicinal chemistry letters

authors： Lee K,Gao Y,Yao ZJ,Phan J,Wu L,Liang J,Waugh DS,Zhang ZY,Burke TR Jr

更新日期：2003-08-04 00:00:00

abstract：:A series of new coumarin-based 1,2,4-triazole derivatives were designed, synthesized and evaluated for their antimicrobial activities in vitro against four Gram-positive bacteria (Staphylococcus aureus, MRSA, Bacillus subtilis and Micrococcus luteus), four Gram-negative bacteria (Escherichia coli, Proteus vulgaris, Sa...

journal_title：Bioorganic & medicinal chemistry letters

authors： Shi Y,Zhou CH

更新日期：2011-02-01 00:00:00

abstract：:Hitherto unknown protective effect of N,α-L-rhamnopyranosyl vincosamide (VR), isolated from Moringa oleifera leaves in isoproterenol (ISO)-induced cardiac toxicity was evaluated in rats. Oral administration of VR at 40 mg/kg for 7 days markedly reduced the ISO-induced increase in the levels of serum cardiac markers su...

journal_title：Bioorganic & medicinal chemistry letters

authors： Panda S,Kar A,Sharma P,Sharma A

更新日期：2013-02-15 00:00:00

abstract：:Benzalacetone synthase (BAS) and chalcone synthase (CHS) are plant-specific type III polyketide synthases (PKSs), sharing 70% amino acid sequence identity and highly homologous overall protein structures. BAS catalyzes the decarboxylative coupling of 4-coumaroyl-CoA with malonyl-CoA to produce the diketide benzalaceto...

journal_title：Bioorganic & medicinal chemistry letters

authors： Shimokawa Y,Morita H,Abe I

更新日期：2010-09-01 00:00:00

abstract：:Two well-defined oxidative chlorination-cyclization processes have been developed for the stereoselective synthesis of a variety of 4-amido-isothiazolidinone oxide derivatives. The stereochemistry of the cyclization products was confirmed by X-ray crystallography. These new compounds were designed as bacterial serine ...

journal_title：Bioorganic & medicinal chemistry letters

authors： Chen Z,Demuth TP Jr,Wireko FC

更新日期：2001-08-20 00:00:00

abstract：:The reductive amination of an amino acid derived glyoxal, with the free amino group of a protected amino acid or oligopeptide fragment, has been developed as a simple and efficient method for the preparation of ketomethylene amino pseudo-oligopeptide isosteres Aa psi(COCH2NH)Aa. Trichlorosilane-DMF is the reagent of c...

journal_title：Bioorganic & medicinal chemistry letters

authors： Groarke M,Hartzoulakis B,McKervey MA,Walker B,Williams CH

更新日期：2000-01-17 00:00:00

abstract：:Based on the favorable antiviral profiles of 4'-substituted nucleosides, novel 1-(2'-deoxy-2'-fluoro-4'-C-ethynyl-beta-D-arabinofuranosyl)-uracil (1a), -thymine (1b), and -cytosine (2) analogs were synthesized. Compounds 1b and 2 exhibited potent anti-HIV-1 activity with IC(50) values of 86 and 1.34 nM, respectively, ...

journal_title：Bioorganic & medicinal chemistry letters

authors： Wang Q,Li Y,Song C,Qian K,Chen CH,Lee KH,Chang J

更新日期：2010-07-15 00:00:00

abstract：:The discovery, synthesis, potential binding mode, and in vitro kinase profile of 3-(3-bromo-4-hydroxy-5-(2'-methoxyphenyl)-benzylidene)-5-bromo-1,3-dihydro-pyrrolo[2,3-b]pyridin-2-one, 3-[(1-methyl-1H-indol-3-yl)methylene]-1,3-dihydro-2H-pyrrolo[3,2-b]-pyridin-2-one as potent TrkA inhibitors are discussed. ...

journal_title：Bioorganic & medicinal chemistry letters

authors： Wood ER,Kuyper L,Petrov KG,Hunter RN 3rd,Harris PA,Lackey K

更新日期：2004-02-23 00:00:00

abstract：:A modified vancomycin binding pocket (D-O-E ring) incorporating an alpha-hydroxy-beta-amino acid at the AA4 position is designed and synthesized. Some of these compounds display potent bioactivities against both sensitive- and resistant-strains (8 microg/ml against VREF). Both the lipidated aminoglucose and the struct...

journal_title：Bioorganic & medicinal chemistry letters

authors： Jia Y,Gonzalez-Zamora E,Ma N,Liu Z,Bois-Choussy M,Malabarba A,Brunati C,Zhu J

更新日期：2005-10-15 00:00:00

abstract：:Sulfonate analogues of combretastatin A-4 have been prepared. These compounds compete with colchicine and combretastatin A-4 for the colchicine binding site on tubulin and are potent inhibitors of tubulin polymerization and cell proliferation. Importantly, these compounds also inhibit the proliferation of P-glycoprote...

journal_title：Bioorganic & medicinal chemistry letters

authors： Gwaltney SL 2nd,Imade HM,Barr KJ,Li Q,Gehrke L,Credo RB,Warner RB,Lee JY,Kovar P,Wang J,Nukkala MA,Zielinski NA,Frost D,Ng SC,Sham HL

更新日期：2001-04-09 00:00:00

abstract：:In this report we detail the evolution of our previously reported thiophene isoxazole BET inhibitor chemotype exemplified by CPI-3 to a novel bromodomain selective chemotype (the methyl isoxazoleazepine chemotype) exemplified by carboxamide 23. The methyl isoxazoleazepine chemotype provides potent inhibition of the br...

journal_title：Bioorganic & medicinal chemistry letters

authors： Hewitt MC,Leblanc Y,Gehling VS,Vaswani RG,Côté A,Nasveschuk CG,Taylor AM,Harmange JC,Audia JE,Pardo E,Cummings R,Joshi S,Sandy P,Mertz JA,Sims RJ 3rd,Bergeron L,Bryant BM,Bellon S,Poy F,Jayaram H,Tang Y,Albrecht

更新日期：2015-05-01 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：:Pholasin is a bioluminescent photoprotein of Pholas dactylus. Pholasin is a commercially available photoprotein used to measure intracellular reactive oxygen species. Although extensive efforts have been carried out to determine the chemical structure of the prosthetic (chromophore) group, it still remains unclear to ...

journal_title：Bioorganic & medicinal chemistry letters

authors： Kuse M,Tanaka E,Nishikawa T

更新日期：2008-10-15 00:00:00

abstract：:A one step synthesis of fluorescent 8-aryl-(7-deazaguanines) has been accomplished. Probes exhibit blue to green high quantum yield fluorescence in a variety of organic and aqueous solutions, high extinction coefficients, and large Stokes shifts often above 100 nm. The probes are highly cell permeable, and exhibit sta...

journal_title：Bioorganic & medicinal chemistry letters

authors： Dhimitruka I,Eubank TD,Gross AC,Khramtsov VV

更新日期：2015-10-15 00:00:00

abstract：:We report a dimerization strategy to enhance the antibacterial potency of an otherwise weak cationic amphiphilic polyproline helical (CAPH) peptide. Overall, the dimeric CAPHs were more active against Escherichia coli and Staphylococcus aureus than the monomeric counterpart, reaching up to a 60-fold increase in potenc...

journal_title：Bioorganic & medicinal chemistry letters

authors： Hernandez-Gordillo V,Geisler I,Chmielewski J

更新日期：2014-01-15 00:00:00

abstract：:2-(Anilino)imidazolines were identified as novel human 5-HT(1D) receptor ligands, but offered no particular advantage over previously reported 2-(benzyl)imidazolines. Pharmacokinetic and functional data were obtained for selected 2-(benzyl)imidazoline derivatives. ...

journal_title：Bioorganic & medicinal chemistry letters

authors： Prisinzano T,Dukat M,Law H,Slassi A,MacLean N,DeLannoy I,Glennon RA

更新日期：2004-09-20 00:00:00

abstract：:We report the discovery of potent agonists for the human formyl-peptide-like 1 receptor (hFPRL1). These compounds did not act at a closely related receptor denoted human formyl peptide receptor (hFPR) up to 10 microM concentration. Recent studies have indicated that agonizing this receptor may promote resolution of in...

journal_title：Bioorganic & medicinal chemistry letters

authors： Bürli RW,Xu H,Zou X,Muller K,Golden J,Frohn M,Adlam M,Plant MH,Wong M,McElvain M,Regal K,Viswanadhan VN,Tagari P,Hungate R

更新日期：2006-07-15 00:00:00

abstract：:The authentic standard PBB3 and its precursor N-desmethyl-PBB3 as well as TBS-protected N-desmethyl-PBB3 precursor for radiolabeling were synthesized from 5-bromo-2-nitropyridine, acrolein diethyl acetal, 6-methoxy-2-methylbenzothiazole, and diethylchlorophosphate with overall chemical yield 1% in six steps, 2% in fiv...

journal_title：Bioorganic & medicinal chemistry letters

authors： Wang M,Gao M,Xu Z,Zheng QH

更新日期：2015-10-15 00:00:00

abstract：:An efficient synthesis of [D-lysine](8)cyclosporin A has been developed. Several analogs of [D-lysine](8)cyclosporin A have been synthesized and show promising anti-HCV activity, particularly compounds 39 and 43, which each exhibit an anti-HCV EC(50)<200 nM, and are each ≥50-fold less immunosuppressive than cyclospori...

journal_title：Bioorganic & medicinal chemistry letters

authors： Scribner A,Houck D,Huang Z,Mosier S,Peel M,Scorneaux B

更新日期：2010-11-15 00:00:00

abstract：:Glycogen synthase kinase-3 beta (GSK3β) kinase serves as a promising therapeutic target for the treatment of various human diseases, such as diabetes, obesity, and Alzheimer's disease. In this study, we report lead GSK3β inhibitors identified using a fragment-linking strategy. Through the systematic exploration, a six...

journal_title：Bioorganic & medicinal chemistry letters

authors： Kim J,Moon Y,Hong S

更新日期：2016-12-01 00:00:00

abstract：:Novel C-seco-taxoids were synthesized from 10-deacetylbaccatin III and their potencies evaluated against drug-sensitive and drug-resistant cancer cell lines. The drug-resistant cell lines include ovarian cancer cell lines resistant to cisplatin, topotecan, adriamycin and paclitaxel overexpressing class III beta-tubuli...

journal_title：Bioorganic & medicinal chemistry letters

authors： Pepe A,Sun L,Zanardi I,Wu X,Ferlini C,Fontana G,Bombardelli E,Ojima I

更新日期：2009-06-15 00:00:00

abstract：:An antibody-retinal assembly that mimics the opsin shift (OS) of the naturally occurring visual pigments is reported. Both experiments and calculations show that the aldolase antibody 33F12 covalently binds all-trans retinal via a protonated Schiff base with a lysine residue. This chromophore, which exhibits a remarka...

journal_title：Bioorganic & medicinal chemistry letters

authors： Grynszpan F,Keinan E

更新日期：1999-08-16 00:00:00

abstract：:Novel benzo[b]thiophene diamine thrombin inhibitors were investigated, focusing on a contracted C4'-side chain series. SAR studies identified compounds with either a pyrrolidino or morpholino group as potent, active site directed thrombin inhibitors when the amino group was connected to the C3-phenyl ring with a methy...

journal_title：Bioorganic & medicinal chemistry letters

authors： Takeuchi K,Kohn TJ,Harper RW,Lin HS,Gifford-Moore DS,Richett ME,Sall DJ,Smith GF,Zhang M

更新日期：2000-06-05 00:00:00

abstract：:Starting from our previously identified novel c-Met kinase inhibitors bearing 1H-imidazo[4,5-h][1,6]naphthyridin-2(3H)-one scaffold, a global structural exploration was conducted to furnish an optimal binding motif for further development, directed by the enzyme inhibitory mechanism. First round SAR study picked two i...

journal_title：Bioorganic & medicinal chemistry letters

authors： An XD,Liu H,Xu ZL,Jin Y,Peng X,Yao YM,Geng M,Long YQ

更新日期：2015-02-01 00:00:00

abstract：:The lead optimisation of the diaminopyrimidine carboxamide series of spleen tyrosine kinase inhibitors is described. The medicinal chemistry strategy was focused on optimising the human whole blood activity whilst achieving a sufficient margin over liability kinases and hERG activity. GSK143 is a potent and highly sel...

journal_title：Bioorganic & medicinal chemistry letters

authors： Liddle J,Atkinson FL,Barker MD,Carter PS,Curtis NR,Davis RP,Douault C,Dickson MC,Elwes D,Garton NS,Gray M,Hayhow TG,Hobbs CI,Jones E,Leach S,Leavens K,Lewis HD,McCleary S,Neu M,Patel VK,Preston AG,Ramirez-Molina

更新日期：2011-10-15 00:00:00

abstract：:This study describes the syntheses of di, tetra and hexa deuterated analogues of the NOD-like receptor pyrin domain-containing protein 3 (NLRP3) inflammasome inhibitor MCC950. In di and tetra deuterated analogues, deuteriums were incorporated into the 1,2,3,5,6,7-hexahydro-s-indacene moiety, whereas in the hexa deuter...

journal_title：Bioorganic & medicinal chemistry letters

authors： Salla M,Butler MS,Massey NL,Reid JC,Cooper MA,Robertson AAB

更新日期：2018-02-15 00:00:00

abstract：:Fast atom bombardment mass spectrometry that can directly analyze lysophospholipids was used to quantitatively determine the kinetics of phospholipase A2. This method is 1250 times more sensitive than the colorimetric assay. ...

journal_title：Bioorganic & medicinal chemistry letters

authors： Isomura S,Ito K,Haruna M

更新日期：1999-02-08 00:00:00