A facile 1,3-dipolar cycloaddition of azomethine ylides to 2-arylidene-1,3-indanediones: synthesis of dispiro-oxindolylpyrrolothiazoles and their antimycobacterial evaluation.

abstract：:Considering the complex etiology of Alzheimer's disease (AD), multifunctional agents may be beneficial for the treatment of this disease. A series of DL-3-n-butylphthalide-Edaravone hybrids were designed, synthesized and evaluated as novel dual inhibitors of amyloid-β aggregation and monoamine oxidases. Among them, co...

journal_title：Bioorganic & medicinal chemistry letters

authors： Qiang X,Li Y,Yang X,Luo L,Xu R,Zheng Y,Cao Z,Tan Z,Deng Y

更新日期：2017-02-15 00:00:00

abstract：:The essential oils from leaves of Piper malacophyllum (Piperaceae) showed to be mainly composed by two alkenylphenol derivatives: gibbilimbols A and B. After isolation and structural characterization by NMR and MS data analysis, both compounds were evaluated against promastigote/amastigote forms of Leishmania (L.) inf...

journal_title：Bioorganic & medicinal chemistry letters

authors： Varela MT,Dias RZ,Martins LF,Ferreira DD,Tempone AG,Ueno AK,Lago JH,Fernandes JP

更新日期：2016-02-15 00:00:00

abstract：:Primaquine (PQ) is the only commercially available drug that clears dormant liver stages of malaria and blocks transmission to mosquito vectors. Although an old drug, much remains to be known about the mechanism(s) of action. Herein we develop a fluorescent tagged PQ to discover cellular localization in the human mala...

journal_title：Bioorganic & medicinal chemistry letters

authors： McQueen A,Blake LD,Azhari A,Kemp MT,McGaha TW Jr,Namelikonda N,Larsen RW,Manetsch R,Kyle DE

更新日期：2017-10-15 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：:A new glucuronylated prodrug of nornitrogen mustard, incorporating the same spacer group as the doxorubicin prodrug HMR 1826, has been prepared. Upon exposure to E. coli beta-glucuronidase, fast hydrolysis occurs but a lower cytotoxicity against LoVo cancer cells is observed compared to the nornitrogen mustard alone. ...

journal_title：Bioorganic & medicinal chemistry letters

authors： Papot S,Combaud D,Bosslet K,Gerken M,Czech J,Gesson JP

更新日期：2000-08-21 00:00:00

abstract：:Water is an essential part of protein binding sites and mediates interactions to ligands. Its displacement by ligand parts affects the free binding energy of resulting protein-ligand complexes. Therefore the characterization of solvation properties is important for design. Of particular interest is the propensity of l...

journal_title：Bioorganic & medicinal chemistry letters

authors： Matter H,Güssregen S

更新日期：2018-08-01 00:00:00

abstract：:Retinoid X receptor (RXR) and Histone deacetylase (HDAC) are considered important targets for anti-cancer therapy due to their crucial roles in genetic or epigenetic regulations of cancer development and progression. Here, we have designed and synthesized a novel compound which targets both RXR and HADC. This dual-tar...

journal_title：Bioorganic & medicinal chemistry letters

authors： Chen GL,Wang LH,Wang J,Chen K,Zhao M,Sun ZZ,Wang S,Zheng HL,Yang JY,Wu CF

更新日期：2013-07-01 00:00:00

abstract：:A series of (N-benzyl-N-phenylsulfonamido)alkyl amides were developed from classic and parallel synthesis strategies. Compounds with good in vitro and in vivo γ-secretase activity were identified and described. ...

journal_title：Bioorganic & medicinal chemistry letters

authors： Parker MF,Barten DM,Bergstrom CP,Bronson JJ,Corsa JA,Dee MF,Gai Y,Guss VL,Higgins MA,Keavy DJ,Loo A,Mate RA,Marcin LR,McElhone KE,Polson CT,Roberts SB,Macor JE

更新日期：2012-11-15 00:00:00

abstract：:The discovery and optimization of novel pyrrolo[3,4-b]pyridin-7(6H)-one MCH-R1 antagonists are described. A systematic SAR study probing the effects of aryl-, benzyl- and arylthio-substituents at the 2-position of the pyrrolo[3,4-b]pyridin-7(6H)-ones led to identification of the 2-[(4-fluorophenyl)thio] derivative 7b ...

journal_title：Bioorganic & medicinal chemistry letters

authors： Lim CJ,Kim JY,Lee BH,Oh KS,Yi KY

更新日期：2013-03-15 00:00:00

abstract：:Imidazo[1,2-a]pyrimidines and imidazo[1,2-b][1,2,4]triazines are ligands for the benzodiazepine binding site of GABA(A) receptors that are functionally selective for the alpha2/alpha3 subtypes over the alpha1 subtype. SAR studies to optimise this functional selectivity, pharmacokinetic and behavioural data are describ...

journal_title：Bioorganic & medicinal chemistry letters

authors： Jennings AS,Lewis RT,Russell MG,Hallett DJ,Street LJ,Castro JL,Atack JR,Cook SM,Lincoln R,Stanley J,Smith AJ,Reynolds DS,Sohal B,Pike A,Marshall GR,Wafford KA,Sheppard WF,Tye SJ

更新日期：2006-03-15 00:00:00

abstract：:A catalyst-free synthesis of 6,9-dihydro-[1,3]dioxolo[4,5-g]thieno[3,4-b]quinolin-8(5H)-ones as novel analogues of podophyllotoxins was developed by a three-component reaction of aldehydes, ethyl 2,4-dioxotetrahydrothiophene-3-carboxylate and 3,4-(methylenedioxy)aniline. This methodology not only provides new chemical...

journal_title：Bioorganic & medicinal chemistry letters

authors： Li T,Lu T,Yu C,Yao C

更新日期：2015-04-01 00:00:00

abstract：:The eryA gene of the bacterial pathogen Brucella abortus has been functionally expressed in Escherichia coli. The resultant EryA was shown to catalyze the ATP-dependent conversion of erythritol to L-erythritol-4-phosphate (L-E4P). The steady state kinetic parameters of this reaction were determined and the enzyme was ...

journal_title：Bioorganic & medicinal chemistry letters

authors： Lillo AM,Tetzlaff CN,Sangari FJ,Cane DE

更新日期：2003-02-24 00:00:00

abstract：:We previously showed that fluorination of the carborane-containing selective estrogen receptor modulator (SERM) BE360 altered the agonist/antagonist activity balance and the estrogen receptor (ER) α/β subtype selectivity. Here, we designed and synthesized a series of fluorinated carboranyl phenols as candidate ERβ-sel...

journal_title：Bioorganic & medicinal chemistry letters

authors： Ohta K,Ogawa T,Kaise A,Endo Y

更新日期：2013-12-15 00:00:00

abstract：:Natural or synthetic coumarins showed gastroprotective and antiulcer activity in animal models. In this study, we have synthetized twenty coumarins using classic methods to evaluate their gastroprotective effects on the ethanol/HCl-induced gastric lesion model in mice at 20mg/kg. Among the coumarins synthetized, compo...

journal_title：Bioorganic & medicinal chemistry letters

authors： Sepulveda B,Quispe C,Simirgiotis M,Torres-Benítez A,Reyes-Ortíz J,Areche C,García-Beltrán O

更新日期：2016-12-01 00:00:00

abstract：:Although Au(I) complexes have been used to treat rheumatoid arthritis for over 75 years, their mechanism of action is still poorly understood. A family of enzymes responsible for joint destruction in rheumatoid arthritis, the cathepsins, has been discussed as a possible biological target of Au(I). In this study, inhib...

journal_title：Bioorganic & medicinal chemistry letters

authors： Chircorian A,Barrios AM

更新日期：2004-10-18 00:00:00

abstract：:Human 5-lipoxygenase (5-LOX) is responsible for the formation of leukotriene (LT)A4, a pivotal intermediate in the biosynthesis of the leukotrienes, a family of proinflammatory lipid mediators. 5-LOX has thus gained attention as a potential drug target. However, details of the kinetic mechanism of 5-LOX are still obsc...

journal_title：Bioorganic & medicinal chemistry letters

authors： Mittal M,Kumar RB,Balagunaseelan N,Hamberg M,Jegerschöld C,Rådmark O,Haeggström JZ,Rinaldo-Matthis A

更新日期：2016-08-01 00:00:00

abstract：:In a continuing effort to discover novel PDE5 inhibitors, we have successfully found quinazolines with 4-benzylamino substitution as potent and selective PDE5 inhibitors. Initial lead compound (1) was found to be easily metabolized when incubated with human liver microsomes mainly through C6 amide hydrolysis. Blocking...

journal_title：Bioorganic & medicinal chemistry letters

authors： Choi H,Lee J,Kim YH,Im DS,Hwang IC,Kim SJ,Moon SK,Lee HW,Lee SS,Ahn SK,Kim SW,Choi NS,Lee KJ

更新日期：2010-01-01 00:00:00

abstract：:Previously we reported the optimization of antiviral scaffolds containing benzimidazole and related heterocycles possessing activity against a variety of arenaviruses. These series of compounds were discovered through an HTS campaign of a 400,000 small molecule library using lentivirus-based pseudotypes incorporated w...

journal_title：Bioorganic & medicinal chemistry letters

authors： Burgeson JR,Gharaibeh DN,Moore AL,Larson RA,Amberg SM,Bolken TC,Hruby DE,Dai D

更新日期：2013-11-01 00:00:00

abstract：:Tyrosine kinase inhibitor (TKI) therapy is the standard treatment for chronic phase (CP)-chronic myeloid leukemia (CML), yet patients in blast crisis (BC) phase of CML are unlikely to respond to TKI therapy. The transcription factor E2F1 is a down-stream target of the tyrosine kinase BCR-ABL1 and is up-regulated in TK...

journal_title：Bioorganic & medicinal chemistry letters

authors： Hayatigolkhatmi K,Padroni G,Su W,Fang L,Gómez-Castañeda E,Hsieh YC,Jackson L,Pellicano F,Burley GA,Jørgensen HG

更新日期：2019-09-15 00:00:00

abstract：:The discovery and optimization of a new class of non-peptidyl, pyridazinone derived melanocortin subtype-4 receptor agonists is disclosed. ...

journal_title：Bioorganic & medicinal chemistry letters

authors： Ujjainwalla F,Warner D,Walsh TF,Wyvratt MJ,Zhou C,Yang L,Kalyani RN,MacNeil T,Van der Ploeg LH,Rosenblum CI,Tang R,Vongs A,Weinberg DH,Goulet MT

更新日期：2003-12-15 00:00:00

abstract：:The Letter describes the preparation and characterization of a conjugate of isoniazid (INH) with magnetic nanoparticles Fe3O4@SiO2 115±60 nm in size. The INH molecules were attached to the surface of nanoparticles by a covalent pH-sensitive amidine bond. The conjugate was characterized by X-ray diffraction, SEM, dynam...

journal_title：Bioorganic & medicinal chemistry letters

authors： Sedlák M,Bhosale DS,Beneš L,Palarčík J,Kalendová A,Královec K,Imramovský A

更新日期：2013-08-15 00:00:00

abstract：:Eukaryotic mRNA contains a 3' poly(A) tail, which plays important roles in the regulation of mRNA stability and translation. Well-characterized enzymes involved in the shortening of the poly(A) tail include the multi-subunit Ccr4-Not deadenylase, which contains the Caf1 (Pop2) and Ccr4 catalytic components, and poly(A...

journal_title：Bioorganic & medicinal chemistry letters

authors： Jadhav GP,Kaur I,Maryati M,Airhihen B,Fischer PM,Winkler GS

更新日期：2015-10-01 00:00:00

abstract：:Tritiated opioid radioligands have proven valuable in exploring opioid binding sites. However, tritium has many limitations. Its low specific activity and limited counting efficiency makes it difficult to examine low abundant, high affinity sites and its disposal is problematic due to the need to use organic scintilla...

journal_title：Bioorganic & medicinal chemistry letters

authors： Majumdar S,Burgman M,Haselton N,Grinnell S,Ocampo J,Pasternak AR,Pasternak GW

更新日期：2011-07-01 00:00:00

abstract：:Novel fused 1H-benzo[f]chromen-indole derivatives were synthesized regioselectivly in good to high yields by triethyl amine catalyzed condensation of 3-cyanoacetylindoles, β-naphthol and aryl aldehydes in methanol under ultrasounic irradiations and conventional conditions. The easy work-up of the products, rapidity, a...

journal_title：Bioorganic & medicinal chemistry letters

authors： Hossein nia R,Mamaghani M,Tabatabaeian K,Shirini F,Rassa M

更新日期：2012-09-15 00:00:00

abstract：:Thienylpyrimidines substituted at position 2 of the pyrimidine with a chiral aminoalkoxy group were synthesized. Upon interaction with duplex DNA, the unfused heteroaromatic system of these compounds intercalates with DNA base pairs and the protonated side chain is located in the major groove. The S-enantiomers bind m...

journal_title：Bioorganic & medicinal chemistry letters

authors： Strekowski L,Cegla MT,Honkan V,Buczak H,Winkeljohn WR,Baumstark AL,Wilson WD

更新日期：2005-06-02 00:00:00

abstract：:Starting from the known FXR agonist GW 4064 1a, a series of alternately 3,5-substituted isoxazoles was prepared. Several of these analogs were potent full FXR agonists. A subset of this series, with a tether between the isoxazole ring and the 3-position aryl substituent, were equipotent FXR agonists to GW 4064 1a, wit...

journal_title：Bioorganic & medicinal chemistry letters

authors： Bass JY,Caldwell RD,Caravella JA,Chen L,Creech KL,Deaton DN,Madauss KP,Marr HB,McFadyen RB,Miller AB,Parks DJ,Todd D,Williams SP,Wisely GB

更新日期：2009-06-01 00:00:00

abstract：:We report the solution structure of T140, a truncated polyphemusin peptide analogue that efficiently inhibits infection of target cells by T-cell line-tropic strains of HIV-1 through its specific binding to a chemokine receptor, CXCR4. Nuclear magnetic resonance analysis and molecular dynamic calculations revealed tha...

journal_title：Bioorganic & medicinal chemistry letters

authors： Tamamura H,Sugioka M,Odagaki Y,Omagari A,Kan Y,Oishi S,Nakashima H,Yamamoto N,Peiper SC,Hamanaka N,Otaka A,Fujii N

更新日期：2001-02-12 00:00:00

abstract：:We proposed a novel QSAR (quantitative structure-activity relationship) procedure called LERE (linear expression by representative energy terms)-QSAR involving molecular calculations such as ab initio fragment molecular orbital and generalized Born/surface area ones. We applied LERE-QSAR to two datasets for the free-e...

journal_title：Bioorganic & medicinal chemistry letters

authors： Munei Y,Shimamoto K,Harada M,Yoshida T,Chuman H

更新日期：2011-01-01 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：:Protein tyrosine phosphatase 1B (PTP1B) is a major negative regulator in insulin- and leptin-signaling cascades as well as a positive regulator in tumorigenesis, and much attention has been paid to PTP1B inhibitors as potential therapies for diabetes, obesity, and cancer. In the present study, the screening of a compo...

journal_title：Bioorganic & medicinal chemistry letters

authors： Li W,Li S,Higai K,Sasaki T,Asada Y,Ohshima S,Koike K

更新日期：2013-11-01 00:00:00