Evaluation of nitroalkenes as nitric oxide donors.

abstract：:In the study, we demonstrated that freezing was able to facilitate the short DNA strand T(4)G(4) to self-assemble into a tetramolecular G-quadruplex with a low DNA concentration in the absence of any ligand, providing a fast approach to configure intermolecular G-quadruplexes. The fast formation of intermolecular G-qu...

journal_title：Bioorganic & medicinal chemistry letters

authors： Zhai Q,Deng M,Xu L,Zhang X,Zhou X

更新日期：2012-01-15 00:00:00

abstract：:The design and profile of a series of adamantyl-containing long acting beta(2)-adrenoreceptor agonists are described. An optimal pharmacokinetic profile of low oral bioavailability was combined with a strong pharmacology profile when assessed using a guinea pig trachea tissue model. A focus was then placed on developi...

journal_title：Bioorganic & medicinal chemistry letters

authors： Brown AD,Bunnage ME,Glossop PA,James K,Jones R,Lane CA,Lewthwaite RA,Mantell S,Perros-Huguet C,Price DA,Trevethick M,Webster R

更新日期：2008-02-15 00:00:00

abstract：:Three C(60) derivatives [C(60) (NHCH(2)CH(2)COONa)(n)(H)(n)], n=1, 5, 9] (A, B, C) with different additional number of beta-alanine were synthesized by the control of relative amount of C(60) and beta-alanine added. Hydroxyl radical scavenging activity of the adducts was evaluated in a copper-catalyzed Haber-Weiss rea...

journal_title：Bioorganic & medicinal chemistry letters

authors： Sun T,Jia Z,Xu Z

更新日期：2004-04-05 00:00:00

abstract：:Pulvinone and several 3-fluoro-4-morpholino substituted pulvinone derivatives were synthesized in five steps from a common precursor, phenyl acetic acid. Most of synthetic morpholine substituted pulvinones showed inhibitory activity against Esherichia coli. For the first time, the inhibition of pulvinone and its deriv...

journal_title：Bioorganic & medicinal chemistry letters

authors： Xu HW,Xu C,Fan ZQ,Zhao LJ,Liu HM

更新日期：2013-02-01 00:00:00

abstract：:Molecular modeling studies performed on the two cyclooxygenase (COX) isozymes suggest that the cavity at the mouth of the active site on the membrane domain that may act as an actual binding site of COX ligands. Actual docking of different inhibitors at this site provides a structural basis to explain the dynamics of ...

journal_title：Bioorganic & medicinal chemistry letters

authors： Llorens O,Perez JJ,Palomer A,Mauleon D

更新日期：1999-10-04 00:00:00

abstract：:A pilot library of novel 4,4,5,5-tetramethyl-2-(4-substitutedstyrylphenyl)-1,3,2 dioxaborolane derivatives has been synthesized. 4-(4,4,5,5-Tetramethyl-1,3,2-dioxaboratophenyl)-methyl triphenylphosphonium bromide 3 was treated with various aldehydes in the presence of 3 equiv of (t)BuONa in DMF, and stirred at room te...

journal_title：Bioorganic & medicinal chemistry letters

authors： Das BC,Zhao X,Tang XY,Yang F

更新日期：2011-09-15 00:00:00

abstract：:The Hotoda's sequence substituted with TBDPS via 5'-end nucleobase existed as parallel quadruplex structure and exhibited inhibitory activities in an HIV-1 envelop proteins mediated cell-cell fusion assay. This result demonstrated that the 5'-aromatic groups of the Hotoda's sequence are allowed to have a large spatial...

journal_title：Bioorganic & medicinal chemistry letters

authors： Chen W,Xu L,Cai L,Zheng B,Wang K,He J,Liu K

更新日期：2011-10-01 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：:Several 1-[(2-hydroxy-ethoxy)methyl]-3-carbethoxy-4(1H)quinolones (2a-l) and l-[(2-hydroxy-ethoxy)methyl]-4(1H)quinolone-3-carboxylic acids (3a-j and 3l) were synthesized and 2a-j, 2l and 3a-j, 3l were evaluated against herpes simplex virus type 1 (HSV-1), employing a one-pot reaction: silylation of the desired quinol...

journal_title：Bioorganic & medicinal chemistry letters

authors： Lucero Bd,Gomes CR,Frugulhetti IC,Faro LV,Alvarenga L,de Souza MC,de Souza TM,Ferreira VF

更新日期：2006-02-15 00:00:00

abstract：:Stereoselective total synthesis of bioactive marine natural product crucigasterin A has been accomplished from commercially available and inexpensive L-(-)-malic acid as a starting material. Julia olefination and chelation controlled Grignard additions are the key steps involved in the present synthesis. Cytotoxic pro...

journal_title：Bioorganic & medicinal chemistry letters

authors： Kumar JN,Reddy PR,Das B,Kumar CG,Sujitha P

更新日期：2013-09-15 00:00:00

abstract：:Nobiletin, a major component of polymethoxyflavones in citrus fruits, has a broad spectrum of health beneficial properties including anti-inflammatory and anti-carcinogenic activities. The metabolite identification of nobiletin in mouse urine has concluded that it undergoes mono-demethylation (3'- and 4'-demethylnobil...

journal_title：Bioorganic & medicinal chemistry letters

authors： Li S,Sang S,Pan MH,Lai CS,Lo CY,Yang CS,Ho CT

更新日期：2007-09-15 00:00:00

abstract：:We report an SAR study of MC4R analogs containing spiroindane heterocyclic privileged structures. Compound 26 with N-Me-1,2,4-triazole moiety possesses exceptional potency at MC4R and potent anti-obesity efficacy in a mouse model. However, the efficacy is not completely mediated through MC4R. Additional SAR studies le...

journal_title：Bioorganic & medicinal chemistry letters

authors： He S,Ye Z,Dobbelaar PH,Bakshi RK,Hong Q,Dellureficio JP,Sebhat IK,Guo L,Liu J,Jian T,Lai Y,Franklin CL,Reibarkh M,Holmes MA,Weinberg DH,MacNeil T,Tang R,Tamvakopoulos C,Peng Q,Miller RR,Stearns RA,Chen HY,Chen

更新日期：2010-11-15 00:00:00

abstract：:Bis-(aryl)thioureas were found to be potent and selective inhibitors of cytomegalovirus (CMV) in cultured HFF cells. Of these, the thiazole analogue 38 was investigated as a potential development candidate. ...

journal_title：Bioorganic & medicinal chemistry letters

authors： Bloom JD,DiGrandi MJ,Dushin RG,Curran KJ,Ross AA,Norton EB,Terefenko E,Jones TR,Feld B,Lang SA

更新日期：2003-09-01 00:00:00

abstract：:Cyclic phosphatidic acid (CPA) is a naturally occurring analog of lysophosphatidic acid (LPA) in which the sn-2 hydroxy group forms a five-membered ring with the sn-3 phosphate. Here, we describe the synthesis of R-3-CCPA and S-3-CCPA along with their pharmacological properties as inhibitors of lysophospholipase D/aut...

journal_title：Bioorganic & medicinal chemistry letters

authors： Gupte R,Siddam A,Lu Y,Li W,Fujiwara Y,Panupinthu N,Pham TC,Baker DL,Parrill AL,Gotoh M,Murakami-Murofushi K,Kobayashi S,Mills GB,Tigyi G,Miller DD

更新日期：2010-12-15 00:00:00

abstract：:Structural features of the substituted 4-piperidinyl urea analogs 1, responsible for the H3 antagonist activity, have been identified. Structure-activity relationship of the H3 receptor affinity, hERG ion channel inhibitory activity and their separation is described. Preliminary pharmacokinetic evaluation of the compo...

journal_title：Bioorganic & medicinal chemistry letters

authors： Berlin M,Lee YJ,Boyce CW,Wang Y,Aslanian R,McCormick KD,Sorota S,Williams SM,West RE Jr,Korfmacher W

更新日期：2010-04-01 00:00:00

abstract：:New Lp-PLA(2) inhibitors were synthesized by the bioisosteric replacement of the amide group of Darapladib with an imidazole or a triazole. Unfortunately, the inhibitory activities of these derivatives were lower than that of Darapladib. But interestingly, a series of quaternary ammonium salts that were isolated as by...

journal_title：Bioorganic & medicinal chemistry letters

authors： Wang K,Xu W,Liu Y,Zhang W,Wang W,Shen J,Wang Y

更新日期：2013-03-01 00:00:00

abstract：:In our search for potent inhibitors of the enzyme estrone sulfatase (ES), we have undertaken the synthesis and biochemical evaluation of a range of straight chain alkyl esters of 4-[(aminosulfonyl)oxy] benzoic acid. The results of the study show that the synthesised compounds possess greater inhibitory activity when c...

journal_title：Bioorganic & medicinal chemistry letters

authors： Ahmed S,James K,Owen CP

更新日期：2002-09-02 00:00:00

abstract：:A novel series of compounds derived from the previously reported N-type calcium channel blocker NP118809 (1-(4-benzhydrylpiperazin-1-yl)-3,3-diphenylpropan-1-one) is described. Extensive SAR studies resulted in compounds with IC(50) values in the range of 10-150 nM and selectivity over the L-type channels up to nearly...

journal_title：Bioorganic & medicinal chemistry letters

authors： Pajouhesh H,Feng ZP,Ding Y,Zhang L,Pajouhesh H,Morrison JL,Belardetti F,Tringham E,Simonson E,Vanderah TW,Porreca F,Zamponi GW,Mitscher LA,Snutch TP

更新日期：2010-02-15 00:00:00

abstract：:Group A streptococcus is a Gram-positive bacteria that causes a range of infectious diseases. Targeting the bacteria, a new self-adjuvanting vaccine candidate, incorporating a carbohydrate carrier and an amino acid-based adjuvant, was synthesised utilising carbohydrate chemistry and solid-phase peptide synthesis proce...

journal_title：Bioorganic & medicinal chemistry letters

authors： Simerska P,Lu H,Toth I

更新日期：2009-02-01 00:00:00

abstract：:A novel series of potent histamine H(3) receptor inverse agonists based on the 3,4-dihydro-2H-pyrazino[1,2-a]indol-1-one scaffold has been discovered. Several compounds display high selectivity over other histamine receptor subtypes and have favorable physicochemical properties, low potential for CYP450 enzyme inhibit...

journal_title：Bioorganic & medicinal chemistry letters

authors： Richter HG,Freichel C,Huwyler J,Nakagawa T,Nettekoven M,Plancher JM,Raab S,Roche O,Schuler F,Taylor S,Ullmer C,Wiegand R

更新日期：2010-10-01 00:00:00

abstract：:Starting from a non-selective pyrazolo-pyrimidone lead, the sequential use of parallel medicinal chemistry and directed synthesis led to the discovery of potent, highly selective, and orally bioavailable PDE9 inhibitors. The availability of these tools allowed for a thorough evaluation of the therapeutic potential of ...

journal_title：Bioorganic & medicinal chemistry letters

authors： Deninno MP,Andrews M,Bell AS,Chen Y,Eller-Zarbo C,Eshelby N,Etienne JB,Moore DE,Palmer MJ,Visser MS,Yu LJ,Zavadoski WJ,Michael Gibbs E

更新日期：2009-05-01 00:00:00

abstract：:A group of novel quinoxalinone derivatives (4a-h) were prepared and investigated for their inhibitory activity against ALR2 and antioxidant activity. Most of them were found to be potent aldose reductase inhibitors with IC50 values ranging from 0.019 to 0.982 μM. The most active compound 2-(3-(4-hydroxyphenoxy)-6-fluo...

journal_title：Bioorganic & medicinal chemistry letters

authors： Zou Y,Qin X,Hao X,Zhang W,Yang S,Yang Y,Han Z,Ma B,Zhu C

更新日期：2015-09-15 00:00:00

abstract：:Modifications at C6 and C7 positions of 3-cyanoquinolines 6 and 7 led to potent inhibitors of the ErbB family of kinases particularly against EGFRWT and Her4 enzymes in the radioisotope filter binding assay. The lead (4, SAB402) displayed potent dual biochemical activities with EGFRWT/Her4 IC50 ratio of 80 due to its ...

journal_title：Bioorganic & medicinal chemistry letters

authors： Mansour TS,Pallepati RR,Basetti V

更新日期：2020-08-15 00:00:00

abstract：:A series of 6-hydroxy-7-methoxy-4-chromanone- (2a-e) and chroman-2-carboxamides (3a-e) were synthesized and their antioxidant activities were evaluated. While compounds 2a-e were less active, compounds 3a-e exhibited more potent inhibition of lipid peroxidation initiated by Fe(2+) and ascorbic acid in rat brain homoge...

journal_title：Bioorganic & medicinal chemistry letters

authors： Lee H,Lee K,Jung JK,Cho J,Theodorakis EA

更新日期：2005-06-02 00:00:00

abstract：:Following the discovery of N-acyl-1,4-diazepan-2-one as a novel pharmacophore for potent and selective DPP-4 inhibitors, optimization of this new lead with different substitution on the seven-membered ring resulted in several highly potent and selective, orally bioavailable, and efficacious DPP-4 inhibitors, such as 3...

journal_title：Bioorganic & medicinal chemistry letters

authors： Liang GB,Qian X,Feng D,Biftu T,Eiermann G,He H,Leiting B,Lyons K,Petrov A,Sinha-Roy R,Zhang B,Wu J,Zhang X,Thornberry NA,Weber AE

更新日期：2007-04-01 00:00:00

abstract：:A series of SYK inhibitors based on the phenylamino pyrimidine thiazole lead 4 were prepared and evaluated for biological activity. Lead optimization provided compounds with nanomolar K(i)'s against SYK and potent inhibition in mast cell degranulation assays. ...

journal_title：Bioorganic & medicinal chemistry letters

authors： Farmer LJ,Bemis G,Britt SD,Cochran J,Connors M,Harrington EM,Hoock T,Markland W,Nanthakumar S,Taslimi P,Ter Haar E,Wang J,Zhaveri D,Salituro FG

更新日期：2008-12-01 00:00:00

abstract：:An HTS campaign of our corporate compound library resulted in thieno[2,3-b]pyridines derivative hits with mGluR5 negative allosteric modulator effects. During the hit-to-lead development our objective was to improve affinity, and to keep the ligand efficiency values at an acceptable level. After different modification...

journal_title：Bioorganic & medicinal chemistry letters

authors： Nógrádi K,Wágner G,Domány G,Bobok A,Magdó I,Kiss B,Kolok S,Fónagy K,Gyertyán I,Háda V,Kóti J,Gál K,Farkas S,Keserű GM,Greiner I,Szombathelyi Z

更新日期：2014-08-15 00:00:00

abstract：:Eight stilbenoids, 1-(p-hydroxybenzyl)-4,8-dimethoxyphenanthrene-2,7-diol (1), 2,7-dihydroxy-1,3-bis(p-hydroxybenzyl)-4-methoxy-9,10-dihydrophenanthrene (2), 4,7-dihydroxy-1-(p-hydroxybenzyl)-2-methoxy-9,10-dihydrophenanthrene (3), 3,3'-dihydroxy-2',6'-bis(p-hydroxybenzyl)-5-methoxybibenzyl (4), 3',5-dihydroxy-2-(p-hy...

journal_title：Bioorganic & medicinal chemistry letters

authors： Morita H,Koyama K,Sugimoto Y,Kobayashi J

更新日期：2005-02-15 00:00:00

abstract：:T-type calcium channel is one of therapeutic targets for the treatment of cardiovascular diseases and neuropathic pain. In this study, as a part of our ongoing efforts to develop potent T-type calcium channel blockers, we designed oxazole derivatives substituted with arylpiperazinylalkylamines. The oxazoles were synth...

journal_title：Bioorganic & medicinal chemistry letters

authors： Lee JE,Koh HY,Seo SH,Baek YY,Rhim H,Cho YS,Choo H,Pae AN

更新日期：2010-07-15 00:00:00

abstract：:A new class of kappa-opioid receptor agonists is described. The design of these agents was based upon energy minimization and structural overlay studies of the generic azepin-2-one structure 3 with the crystal structure of arylacetamide kappa agonist 1, ICI 199441. The most active compound identified was ligand 4a (K(...

journal_title：Bioorganic & medicinal chemistry letters

authors： Tuthill PA,Seida PR,Barker W,Cassel JA,Belanger S,DeHaven RN,Koblish M,Gottshall SL,Little PJ,DeHaven-Hudkins DL,Dolle RE

更新日期：2004-11-15 00:00:00