Synthesis and photophysical properties of new SNARF derivatives as dual emission pH sensors.

abstract：:Cyclophilins (Cyps) are ubiquitous proteins that effect the cis-trans isomerization of Pro amide bonds, and are thus crucial to protein folding. CypA is the most prevalent of the ~19 human Cyps, and plays a crucial role in viral infectivity, most notably for HIV-1 and HCV. Cyclophilins have been shown to play key role...

journal_title：Bioorganic & medicinal chemistry letters

authors： Peel M,Scribner A

更新日期：2013-08-15 00:00:00

abstract：:A facile synthesis of 7-epi-(-)-goniofufurone as well as the first synthesis of (-)-crassalactone C was achieved starting from D-xylose. A comparison of their in vitro antitumour activities with those observed for the corresponding naturally occurring enantiomers was provided. ...

journal_title：Bioorganic & medicinal chemistry letters

authors： Popsavin V,Benedeković G,Srećo B,Popsavin M,Francuz J,Kojić V,Bogdanović G

更新日期：2008-10-01 00:00:00

abstract：:A series of Sordarin derivatives bearing alkyl substituted tetrahydrofuran rings fused to C3'-C4' bond of the sugar moiety have been prepared and their antifungal properties evaluated. Most of them show remarkable antifungal activity against Candida spp and Cryptococcus neoformans. ...

journal_title：Bioorganic & medicinal chemistry letters

authors： Bueno JM,Chicharro J,Fiandor JM,Gómez de las Heras F,Huss S

更新日期：2002-07-08 00:00:00

abstract：:To design artificial restriction enzymes, synthetic catalytic centers that effectively hydrolyze linear double-stranded polydeoxyribonucleotides are needed. The Co(III) complex of cyclen (CoCyc) attached to polystyrene derivatives hydrolyzes linearized pUC18 DNA with half-lives as short as 30 min at 25 degrees C. The ...

journal_title：Bioorganic & medicinal chemistry letters

authors： Jeung CS,Song JB,Kim YH,Suh J

更新日期：2001-12-03 00:00:00

abstract：:Novel indole-3-heterocycles were designed and synthesized and found to be potent CB1 receptor agonists. Starting from a microsomally unstable lead 1, a bioisostere approach replacing a piperazine amide was undertaken. This was found to be a good strategy for improving stability both in vitro and in vivo. This led to t...

journal_title：Bioorganic & medicinal chemistry letters

authors： Morrison AJ,Adam JM,Baker JA,Campbell RA,Clark JK,Cottney JE,Deehan M,Easson AM,Fields R,Francis S,Jeremiah F,Keddie N,Kiyoi T,McArthur DR,Meyer K,Ratcliffe PD,Schulz J,Wishart G,Yoshiizumi K

更新日期：2011-01-01 00:00:00

abstract：:Several analogues of the potent anthelmintic praziquantel were prepared with variation in the aromatic ring. The biological activity of these analogues was evaluated and compared against known analogues. Amination of the ring was tolerated while other variations were not. These results have important implications for ...

journal_title：Bioorganic & medicinal chemistry letters

authors： Ronketti F,Ramana AV,Chao-Ming X,Pica-Mattoccia L,Cioli D,Todd MH

更新日期：2007-08-01 00:00:00

abstract：:Factor Xa, a critical serine protease in the blood coagulation cascade, has become a target for inhibition as a strategy for the invention of novel anti-thrombotic agents. Here we describe the development of phenylglycine containing benzamidine carboxamides as novel, potent and selective inhibitors of factor Xa. ...

journal_title：Bioorganic & medicinal chemistry letters

authors： Jones SD,Liebeschuetz JW,Morgan PJ,Murray CW,Rimmer AD,Roscoe JM,Waszkowycz B,Welsh PM,Wylie WA,Young SC,Martin H,Mahler J,Brady L,Wilkinson K

更新日期：2001-03-12 00:00:00

abstract：:We have synthesized a novel vitamin D receptor agonist VS-105 ((1R,3R)-5-((E)-2-((3αS,7αS)-1-((R)-1-((S)-3-hydroxy-2,3-dimethylbutoxy)ethyl)-7α-methyldihydro-1H-inden-4(2H,5H,6H,7H,7αH)-ylidene)ethylidene)-2-methylenecyclohexane-1,3-diol). Preparation of a-ring phenylphosphine oxide 11, followed by Wittig-Horner coupl...

journal_title：Bioorganic & medicinal chemistry letters

authors： Chen B,Kawai M,Wu-Wong JR

更新日期：2013-11-01 00:00:00

abstract：:The first inhibitors of fungal protein: mannosyl transferase 1 (PMT1) are described. They are based upon rhodanine-3-acetic acid and several compounds have been identified, for example, 5-[[3-(1-phenylethoxy)-4-(2-phenylethoxy)phenyl]methylene]-4-oxo-2-thioxo-3-thiazolidineacetic acid (5a), which inhibit Candida albic...

journal_title：Bioorganic & medicinal chemistry letters

authors： Orchard MG,Neuss JC,Galley CM,Carr A,Porter DW,Smith P,Scopes DI,Haydon D,Vousden K,Stubberfield CR,Young K,Page M

更新日期：2004-08-02 00:00:00

abstract：:The Hedgehog (Hh-) signalling pathway is a key developmental pathway and there is a growing body of evidence showing that this pathway is aberrantly reactivated in a number of human tumors. Novel agents capable of inhibiting this pathway are sought, and an entirely novel series of smoothened (Smo) antagonists capable ...

journal_title：Bioorganic & medicinal chemistry letters

authors： Ontoria JM,Bufi LL,Torrisi C,Bresciani A,Giomini C,Rowley M,Serafini S,Bin H,Hao W,Steinkühler C,Jones P

更新日期：2011-09-15 00:00:00

abstract：:We report the discovery of a novel series of ATP-competitive Janus kinase 3 (JAK3) inhibitors based on the 5H-pyrrolo[2,3-b]pyrazine scaffold. The initial leads in this series, compounds 1a and 1h, showed promising potencies, but a lack of selectivity against other isoforms in the JAK family. Computational and crystal...

journal_title：Bioorganic & medicinal chemistry letters

authors： Jaime-Figueroa S,De Vicente J,Hermann J,Jahangir A,Jin S,Kuglstatter A,Lynch SM,Menke J,Niu L,Patel V,Shao A,Soth M,Vu MD,Yee C

更新日期：2013-05-01 00:00:00

abstract：:Alpha-keto ester and amides were found to be potent inhibitors of histone deacetylase. Nanomolar inhibitors against the isolated enzyme and sub-micromolar inhibitors of cellular proliferation were obtained. The alpha-keto amide 30 also exhibited significant anti-tumor effects in an in vivo tumor model. ...

journal_title：Bioorganic & medicinal chemistry letters

authors： Wada CK,Frey RR,Ji Z,Curtin ML,Garland RB,Holms JH,Li J,Pease LJ,Guo J,Glaser KB,Marcotte PA,Richardson PL,Murphy SS,Bouska JJ,Tapang P,Magoc TJ,Albert DH,Davidsen SK,Michaelides MR

更新日期：2003-10-06 00:00:00

abstract：:A series of human carbonic anhydrase (hCA) IX inhibitors conjugated to various near-infrared fluorescent dyes was synthesized with the aim of imaging hypoxia-induced hCA IX expression in tumor cells in vitro, ex vivo and in vivo. The resulting compounds were profiled for inhibition of transmembrane hCA IX showing a ra...

journal_title：Bioorganic & medicinal chemistry letters

authors： Groves K,Bao B,Zhang J,Handy E,Kennedy P,Cuneo G,Supuran CT,Yared W,Peterson JD,Rajopadhye M

更新日期：2012-01-01 00:00:00

abstract：:Synthesis of a symmetrically branched diglycerol (BGL002, involving one iminodiacetic residue) as a G2 dendron, and the tetradecaglycerol (BGL014, involving one iminodiacetic residue) as a G4 dendron, is described. Several members of the BGL family of G2-G4 dendrons were assembled, with G2 bearing four hydroxyl groups...

journal_title：Bioorganic & medicinal chemistry letters

authors： Nemoto H,Ishihara A,Araki T,Katagiri A,Kamiya M,Matsushita T,Hattori H,Mimura Y,Tomoda Y,Yamasaki M

更新日期：2011-08-15 00:00:00

abstract：:In this study, we investigated the anti-inflammatory effects and mechanisms of cirsimaritin isolated from an ethanol extract of the aerial parts of Cirsium japonicum var. maackii Maxim. using RAW264.7 cells. The extract and its flavonoid cirsimaritin inhibited nitric oxide (NO) production and inducible nitric oxide sy...

journal_title：Bioorganic & medicinal chemistry letters

authors： Shin MS,Park JY,Lee J,Yoo HH,Hahm DH,Lee SC,Lee S,Hwang GS,Jung K,Kang KS

更新日期：2017-07-15 00:00:00

abstract：:Based on lead compound 1 identified from the patent literature, we developed novel patentable BACE-1 inhibitors by introducing a cyclic amine scaffold. Extensive SAR studies on both pyrrolidines and piperidines ultimately led to inhibitor 2f, one of the most potent inhibitors synthesized to date. ...

journal_title：Bioorganic & medicinal chemistry letters

authors： Iserloh U,Wu Y,Cumming JN,Pan J,Wang LY,Stamford AW,Kennedy ME,Kuvelkar R,Chen X,Parker EM,Strickland C,Voigt J

更新日期：2008-01-01 00:00:00

abstract：:VanX, a Zn(II)-dependent D-ala-D-ala dipeptidase, is essential for vancomycin resistance in Enterococcus faecium. The enzymatic activity of VanX was previously found to be inhibited competitively by 2-{[(1-aminoethyl) (hydroxy) phosphoryl]oxy} propanoic acid (1B). Here we report the synthesis and characterization of s...

journal_title：Bioorganic & medicinal chemistry letters

authors： Jia C,Yang KW,Liu CC,Feng L,Xiao JM,Zhou LS,Zhang YL

更新日期：2012-01-01 00:00:00

abstract：:Analogues of BIBP 3226, (R)-N(alpha)-diphenylacetyl-N-(4-hydroxybenzyl)argininamide, were synthesized and investigated for Y1 antagonism (Ca2+-assay, HEL cells) and binding on Y1, Y2 and Y5 receptors. Replacing the benzylamino by a tetrahydrobenzazepinyl group preserves most of the Y1 activity. Combination with a N(G)...

journal_title：Bioorganic & medicinal chemistry letters

authors： Aiglstorfer I,Hendrich I,Moser C,Bernhardt G,Dove S,Buschauer A

更新日期：2000-07-17 00:00:00

abstract：:In the search of new antihyperglycemic agents and following rational approach of drug designing here new 2-hydrazolyl-4-thiazolidinone-5-carboxylic acids (4a-g) with pyrazolyl pharmacophore have been synthesized via thia Michael addition reaction of 1-((3-(4-substituted phenyl)-1-phenyl-1H-pyrazol-4-yl)methylene)thios...

journal_title：Bioorganic & medicinal chemistry letters

authors： Bhosle MR,Mali JR,Pal S,Srivastava AK,Mane RA

更新日期：2014-06-15 00:00:00

abstract：:This study aims to develop novel azatyrosinamide compounds structurally modified from ras-specific antioncogenic azatyrosine. Analogues 4-15 were prepared and their inhibition on the growth of wild-type and ras-transformed NIH 3T3 cell lines was compared. Compound 12 was found to be the most active with IC50 16.5+/-2....

journal_title：Bioorganic & medicinal chemistry letters

authors： Wang HP,Hwang TL,Lee O,Tseng YJ,Shu CY,Lee SJ

更新日期：2005-10-01 00:00:00

abstract：:We report here the development of a novel fluorescein-based probe which shows selective fluorescence enhancement on binding to a hexahistidine-tagged protein. No fluorescence change was observed with untagged protein. This probe is excitable with visible light and is considered to be suitable for use in biological app...

journal_title：Bioorganic & medicinal chemistry letters

authors： Kamoto M,Umezawa N,Kato N,Higuchi T

更新日期：2009-04-15 00:00:00

abstract：:A series of tripeptidic acylsulfonamide inhibitors of HCV NS3 protease were prepared that explored structure-activity relationships (SARs) at the P4 position, and their in vitro and in vivo properties were evaluated. Enhanced potency was observed in a series of P4 ureas; however, the PK profiles of these analogues wer...

journal_title：Bioorganic & medicinal chemistry letters

authors： Venables BL,Sin N,Wang AX,Sun LQ,Tu Y,Hernandez D,Sheaffer A,Lee M,Dunaj C,Zhai G,Barry D,Friborg J,Yu F,Knipe J,Sandquist J,Falk P,Parker D,Good AC,Rajamani R,McPhee F,Meanwell NA,Scola PM

更新日期：2018-06-01 00:00:00

abstract：:Benzylidene-2,4-thiazolidinedione derivatives with substitutions at both the ortho and para-positions of the phenyl group were synthesized as PTP1B inhibitors with IC(50) values in a low micromolar range. Compound 18l, the lowest, bore an IC(50) of 1.3 μM. In a peroxisome proliferator-activated receptor-γ (PPAR-γ) pro...

journal_title：Bioorganic & medicinal chemistry letters

authors： Bhattarai BR,Kafle B,Hwang JS,Ham SW,Lee KH,Park H,Han IO,Cho H

更新日期：2010-11-15 00:00:00

abstract：:A series of 1-(quinoliloxypropyl)-4-aryl-piperazines has been synthesized and the target compounds evaluated for atypical antipsychotic activity in apomorphine induced mesh climbing and stereotypic behaviour in mice. The 8-hydroxyquinoline ether derivative 14 has emerged as an important lead compound showing a potenti...

journal_title：Bioorganic & medicinal chemistry letters

authors： Bali A,Malhotra S,Dhir H,Kumar A,Sharma A

更新日期：2009-06-01 00:00:00

abstract：:A series of bis(indolyl) hydrazide-hydrazones 5a-n were synthesized and evaluated for their cytotoxicity against selected human cancer cell lines. The reaction of indole-3-carboxaldehyde 2 with indole-3-carbohydrazide 4 in presence of catalytic amount of acetic acid afforded 5a-n in good yields. Among the synthesized ...

journal_title：Bioorganic & medicinal chemistry letters

authors： Kumar D,Maruthi Kumar N,Ghosh S,Shah K

更新日期：2012-01-01 00:00:00

abstract：:To make full use both of optical properties of quantum dots (QDs) and of specific interactions between aptamers and their ligands of interest, we employed QD-conjugated RNA aptamer interactions with histidine tag. QDs offer revolutionary fluorescence performance due to their long-term photostability, brilliant colors,...

journal_title：Bioorganic & medicinal chemistry letters

authors： Shin S,Kim IH,Kang W,Yang JK,Hah SS

更新日期：2010-06-01 00:00:00

abstract：:(3-tert-Butyl-7-(5-methylisoxazol-3-yl)-2-(1-methyl-1H-1,2,4-triazol-5-ylmethoxy)pyrazolo[1,5-d][1,2,4]triazine (1) was recently identified as a functionally selective, inverse agonist at the benzodiazepine site of GABA(A) alpha5 receptors and enhances performance in animal models of cognition. The routes of metabolis...

journal_title：Bioorganic & medicinal chemistry letters

authors： Jones P,Atack JR,Braun MP,Cato BP,Chambers MS,O'Connor D,Cook SM,Hobbs SC,Maxey R,Szekeres HJ,Szeto N,Wafford KA,MacLeod AM

更新日期：2006-02-15 00:00:00

abstract：:The paper describes the SAR/SPR studies that led to the discovery of phenoxy cyclopropyl phenyl acetamide derivatives as potent and selective GPR119 agonists. Based on a cis cyclopropane scaffold discovered previously, phenyl acetamides such as compound 17 were found to have excellent GPR119 potency and improved physi...

journal_title：Bioorganic & medicinal chemistry letters

authors： Zhu C,Wang L,Zhu Y,Guo ZZ,Liu P,Hu Z,Szewczyk JW,Kang L,Chicchi G,Ehrhardt A,Woods A,Seo T,Woods M,van Heek M,Dingley KH,Pang J,Salituro GM,Powell J,Terebetski JL,Hornak V,Campeau LC,Orr RK,Ujjainwalla F,Mil

更新日期：2017-03-01 00:00:00

abstract：:A series of new voltage-gated sodium channel blockers were prepared based on the screening lead succinic diamide BPBTS. Replacement of the succinimide linker with the more rigid cyclic 1,2-trans-diamide linker was well tolerated. N-Methylation on the biphenylsulfonamide side of the amide moiety significantly reduced t...

journal_title：Bioorganic & medicinal chemistry letters

authors： Shao PP,Ok D,Fisher MH,Garcia ML,Kaczorowski GJ,Li C,Lyons KA,Martin WJ,Meinke PT,Priest BT,Smith MM,Wyvratt MJ,Ye F,Parsons WH

更新日期：2005-04-01 00:00:00

abstract：:Microsomal prostaglandin E(2) synthase-1 (mPGES-1) is a novel therapeutic target for the treatment of inflammation and pain. In the preceding letter, we detailed the discovery of clinical candidate PF-04693627, a potent mPGES-1 inhibitor possessing a novel benzoxazole structure. While PF-04693627 was undergoing furthe...

journal_title：Bioorganic & medicinal chemistry letters

authors： Walker DP,Arhancet GB,Lu HF,Heasley SE,Metz S,Kablaoui NM,Franco FM,Hanau CE,Scholten JA,Springer JR,Fobian YM,Carter JS,Xing L,Yang S,Shaffer AF,Jerome GM,Baratta MT,Moore WM,Vazquez ML

更新日期：2013-02-15 00:00:00