Salicylanilide diethyl phosphates: synthesis, antimicrobial activity and cytotoxicity.

abstract：:SARS-CoV papain-like protease (PLpro) is an important antiviral target due to its key roles in SARS virus replication. The MeOH extracts of the fruits of the Paulownia tree yielded many small molecules capable of targeting PLpro. Five of these compounds were new geranylated flavonoids, tomentin A, tomentin B, tomentin...

journal_title：Bioorganic & medicinal chemistry

authors： Cho JK,Curtis-Long MJ,Lee KH,Kim DW,Ryu HW,Yuk HJ,Park KH

更新日期：2013-06-01 00:00:00

abstract：:Based on general SARs previously described for anti-HIV-1 diarylsulfone derivatives, a series of 2-amino- and 2-carboxamido-3-arylsulfonylthiophenes has been prepared and evaluated as potential antiviral and antitumor agents. In cell culture, some of the 2-aminothiophenes exhibited moderate and selective activity agai...

journal_title：Bioorganic & medicinal chemistry

authors： Stephens CE,Felder TM,Sowell JW Sr,Andrei G,Balzarini J,Snoeck R,De Clercq E

更新日期：2001-05-01 00:00:00

abstract：:As one of our ongoing research project concerning development of a novel anti-influenza virus agent, dihydrofuran-fused perhydrophenanthrenes were derivatized by means of Williamson ether synthesis and Suzuki-Miyaura cross coupling reactions. Newly synthesized compounds were subjected to evaluation of anti-influenza v...

journal_title：Bioorganic & medicinal chemistry

authors： Matsuya Y,Suzuki N,Kobayashi SY,Miyahara T,Ochiai H,Nemoto H

更新日期：2010-02-15 00:00:00

abstract：:This paper reports the synthesis of new derivatives (formed by two indole systems separated by a central moiety) analogous of potent antitumor agents previously described. The activity of the bis-indoles bearing a pyridine core confirms the good result described in the previous paper and compound 4c was chosen for the...

journal_title：Bioorganic & medicinal chemistry

authors： Andreani A,Burnelli S,Granaiola M,Leoni A,Locatelli A,Morigi R,Rambaldi M,Varoli L,Landi L,Prata C,Dalla Sega FV,Caliceti C,Shoemaker RH

更新日期：2010-05-01 00:00:00

abstract：:We have recently communicated that DNA oligonucleotide d(G(3)T(4)G(4)) forms a dimeric G-quadruplex in the presence of K(+) ions [J. Am. Chem. Soc.2003, 125, 7866-7871]. The high-resolution NMR structure of d(G(3)T(4)G(4))(2) G-quadruplex exhibits G-quadruplex core consisting of three stacked G-quartets. The two overh...

journal_title：Bioorganic & medicinal chemistry

authors： Sket P,Crnugelj M,Plavec J

更新日期：2004-11-15 00:00:00

abstract：:Selective proteinase inhibitors have demonstrated utility in the investigation of cartilage degeneration mechanisms and may have clinical use in the management of osteoarthritis. The cysteine protease cathepsin K (CatK) is an attractive target for arthritis therapy. Here we report the synthesis of two cathepsin K inhi...

journal_title：Bioorganic & medicinal chemistry

authors： Yuan XY,Ren Z,Wu Y,Bougault C,Brizuela L,Magne D,Buchet R,Mebarek S

更新日期：2019-03-15 00:00:00

abstract：:We herein describe the synthesis and anti-inflammatory properties of a small library of imidazoline-based NF-kappaB inhibitors. The structure-activity relationship of various substituents on an imidazoline core structure was evaluated for the ability to inhibit NF-kappaB mediated IL-6 production. Optimization of the s...

journal_title：Bioorganic & medicinal chemistry

authors： Kahlon DK,Lansdell TA,Fisk JS,Tepe JJ

更新日期：2009-04-15 00:00:00

abstract：:Twelve optically pure enantiomers were obtained using either crystallization or chiral high performance liquid chromatography (HPLC) separation methodologies to resolve six racemic sigma-1 (σ1) receptor ligands. The in vitro binding affinities of each enantiomer for σ1, σ2 receptors and vesicular acetylcholine transpo...

journal_title：Bioorganic & medicinal chemistry

authors： Yue X,Jin H,Luo Z,Liu H,Zhang X,McSpadden ED,Tian L,Flores HP,Perlmutter JS,Parsons SM,Tu Z

更新日期：2017-02-15 00:00:00

abstract：:The dopamine D4 receptor has been shown to play key roles in certain CNS pathologies including addiction to cigarette smoking. Thus, selective D4 ligands may be useful in treating some of these conditions. Previous studies in our laboratory have indicated that the piperazine analog of haloperidol exhibits selective an...

journal_title：Bioorganic & medicinal chemistry

authors： Sampson D,Zhu XY,Eyunni SV,Etukala JR,Ofori E,Bricker B,Lamango NS,Setola V,Roth BL,Ablordeppey SY

更新日期：2014-06-15 00:00:00

abstract：:MARCH-INSIDE methodology was applied to the prediction of the bitter tasting threshold of 48 dipeptides by means of pattern recognition techniques, in this case linear discriminant analysis (LDA), and regression methods. The LDA models yielded a percentage of good classification higher than 80% with the two main famil...

journal_title：Bioorganic & medicinal chemistry

authors： Ramos de Armas R,González Díaz H,Molina R,Pérez González M,Uriarte E

更新日期：2004-09-15 00:00:00

abstract：:2-Phenyl-9-benzyl-8-azapurines, bearing at the 6 position an amido group interposed between the 8-azapurine moiety and an alkyl or a substituted phenyl group, have been synthesised and assayed as ligands for adenosine receptors. All the compounds show high affinity for the A(1) adenosine receptor, and many of them als...

journal_title：Bioorganic & medicinal chemistry

authors： Giorgi I,Leonardi M,Pietra D,Biagi G,Borghini A,Massarelli I,Ciampi O,Bianucci AM

更新日期：2009-03-01 00:00:00

abstract：:The effects of Brazilian green propolis ethanol extract on Cry j1-induced cys-leukotrienes and histamine release from peripheral leukocytes of patients with allergic rhinitis were investigated. One of the key mechanisms for the anti-allergic properties of the extract was revealed to be the suppression of cys-LTs relea...

journal_title：Bioorganic & medicinal chemistry

authors： Tani H,Hasumi K,Tatefuji T,Hashimoto K,Koshino H,Takahashi S

更新日期：2010-01-01 00:00:00

abstract：:Germanicane-type triterpenes allobetulin (3) and 28-oxoallobetulin (4) can be obtained by the Wagner-Meerwein rearrangement of the more available lupane-type triterpenes betulin (1) and betulinic acid (2), respectively. The medical uses of betulinic acid (2) and its derivatives are limited because of their poor hydros...

journal_title：Bioorganic & medicinal chemistry

authors： Thibeault D,Gauthier C,Legault J,Bouchard J,Dufour P,Pichette A

更新日期：2007-09-15 00:00:00

abstract：:The clinical success of covalent kinase inhibitors in the treatment of EGFR-dependent non-small cell lung cancer (NSCLC) has rejuvenated the appreciation of reactive small molecules. Acquired drug resistance against first-line EGFR inhibitors remains the major bottleneck in NSCLC and is currently addressed by the appl...

journal_title：Bioorganic & medicinal chemistry

authors： Basu D,Richters A,Rauh D

更新日期：2015-06-15 00:00:00

abstract：:The enantioselective recognition of 'remote' stereogenic centers represents a scientific task in organic chemistry being also of current interest in the pharmaceutical industry. This is due to a range of pharmaceutically relevant molecules or intermediates thereof bearing a stereogenic center, which is separated from ...

journal_title：Bioorganic & medicinal chemistry

authors： Alfaro Blasco M,Gröger H

更新日期：2014-10-15 00:00:00

abstract：:A new kaurane type diterpene lactone, neotripterifordin (1), has been isolated from the roots of Tripterygium wilfordii. The structure of 1 was elucidated by spectroscopic methods, which included the concerted application of a number of 2-D NMR techniques including 1H-1H COSY, phase-sensitive NOESY, HETCOR, and long-r...

journal_title：Bioorganic & medicinal chemistry

authors： Chen K,Shi Q,Fujioka T,Nakano T,Hu CQ,Jin JQ,Kilkuskie RE,Lee KH

更新日期：1995-10-01 00:00:00

abstract：:We report structure-activity investigations in a series of tripeptide amide inhibitors of thrombin, and the development of a series of highly potent active site directed alpha-keto carbonyl inhibitors having the side chain of lysine at P1. Compounds of this class are unstable by virtue of reactivity at the electrophil...

journal_title：Bioorganic & medicinal chemistry

authors： Brady SF,Sisko JT,Stauffer KJ,Colton CD,Qiu H,Lewis SD,Ng AS,Shafer JA,Bogusky MJ,Veber DF

更新日期：1995-08-01 00:00:00

abstract：:Two new daphne diterpene esters Yuanhuajine (2) and Yuanhuagine (4), together with three known daphne diterpene esters yuanhuacine (1), yuanhuadine (3), and yuanhuapine (5), were isolated and identified from Daphne genkwa, a traditional Chinese medicine. Their structures were elucidated by a combination of UV, IR, MS ...

journal_title：Bioorganic & medicinal chemistry

authors： Zhang S,Li X,Zhang F,Yang P,Gao X,Song Q

更新日期：2006-06-01 00:00:00

abstract：:γ-Aminobutyric acid (GABA) receptors are important targets of parasiticides/insecticides. Several 4-substituted analogs of the partial GABAA receptor agonist 5-(4-piperidyl)-3-isothiazolol (Thio-4-PIOL) were synthesized and examined for their antagonism of insect GABA receptors expressed in Drosophila S2 cells or Xeno...

journal_title：Bioorganic & medicinal chemistry

authors： Liu G,Furuta K,Nakajima H,Ozoe F,Ozoe Y

更新日期：2014-09-01 00:00:00

abstract：:Further structure-activity relationship (SAR) studies with the 1,2,3,4-tetrahydroisoquinoline (THIQ) class of 5-HT(1A) ligands led to the synthesis of new 1-adamantoyloaminoalkyl derivatives. The impact of substituent variations in the aromatic part of THIQ moiety on 5-HT(1A) and 5-HT(2A) receptor affinities, as well ...

journal_title：Bioorganic & medicinal chemistry

authors： Bojarski AJ,Mokrosz MJ,Minol SC,Kozioł A,Wesołowska A,Tatarczyńska E,Kłodzińska A,Chojnacka-Wójcik E

更新日期：2002-01-01 00:00:00

abstract：:High specificity has been an important feature in affinity labeling for target profiling. Especially, to label targets via rapidly progressing reactions with consumption of ligand (probe), high specificity of reaction with common functional groups of target protein should be achieved without reactions with similar gro...

journal_title：Bioorganic & medicinal chemistry

authors： Tomohiro T,Nakabayashi M,Sugita Y,Morimoto S

更新日期：2016-08-01 00:00:00

abstract：:A series of formylchromone derivatives were synthesized as PTP1B inhibitors and some of them were potent against PTP1B with IC50 values as low as 1.0 microM. They exhibited remarkable selectivity for PTP1B over other human PTPases. Kinetic studies revealed that formylchromone derivatives are irreversible and active si...

journal_title：Bioorganic & medicinal chemistry

authors： Shim YS,Kim KC,Lee KA,Shrestha S,Lee KH,Kim CK,Cho H

更新日期：2005-02-15 00:00:00

abstract：:N(1)-Phenyl-3,5-dinitro-N(4),N(4)-di-n-propylsulfanilamide (1) and N(1)-phenyl-3,5-dinitro-N(4),N(4)-di-n-butylsulfanilamide (2) show potent in vitro antimitotic activity against kinetoplastid parasites but display poor in vivo activity. Seventeen new dinitroaniline sulfonamide and eleven new benzamide analogs of thes...

journal_title：Bioorganic & medicinal chemistry

authors： George TG,Johnsamuel J,Delfín DA,Yakovich A,Mukherjee M,Phelps MA,Dalton JT,Sackett DL,Kaiser M,Brun R,Werbovetz KA

更新日期：2006-08-15 00:00:00

abstract：:Peptide-semicarbazones derived from Z-Trp-Trp-Phe-aldehyde inhibit the chymotryptic activity of the human proteasome at nanomolar concentrations, but are less active in a NFkappaB reporter gene assay. Cyclic semicarbazones, in contrast, combine a strong inhibitory effect on the enzyme with an inhibition of NFkappaB si...

journal_title：Bioorganic & medicinal chemistry

authors： Leban J,Blisse M,Krauss B,Rath S,Baumgartner R,Seifert MH

更新日期：2008-04-15 00:00:00

abstract：:One of the grand challenges in chemical biology is identifying a small-molecule modulator for each individual function of all human proteins. Instead of targeting one protein at a time, an efficient approach to address this challenge is to target entire protein families by taking advantage of the relatively high level...

journal_title：Bioorganic & medicinal chemistry

authors： Areias FM,Brea J,Gregori-Puigjané E,Zaki ME,Carvalho MA,Domínguez E,Gutiérrez-de-Terán H,Proença MF,Loza MI,Mestres J

更新日期：2010-05-01 00:00:00

abstract：:A series of potential DNA-binding antitumor agents, 2-[omega-(alkylamino)alkyl]-9-methoxy-5-nitro-2,6-dihydroindazolo[4,3-bc][1,5]naphthyridines (2a-f), 10-aza derivatives of PZA, has been prepared by condensation of 9-chloro-2-methoxy-6-nitro-5,10-dihydrobenzo[b][1,5]naphthyridin-10-one (6) with the appropriate (omeg...

journal_title：Bioorganic & medicinal chemistry

authors： Magnano A,Sparapani S,Lucciarini R,Michela M,Amantini C,Santoni G,Antonini I

更新日期：2004-11-15 00:00:00

abstract：:Endogenous opioid peptides consist of a conserved amino acid residue of Phe(3) and Phe(4), although their binding modes for opioid receptors have not been elucidated in detail. Endomorphin-2, which is highly selective and specific for the mu opioid receptor, possesses two Phe residues at the consecutive positions 3 an...

journal_title：Bioorganic & medicinal chemistry

authors： Honda T,Shirasu N,Isozaki K,Kawano M,Shigehiro D,Chuman Y,Fujita T,Nose T,Shimohigashi Y

更新日期：2007-06-01 00:00:00

abstract：:Amyotrophic lateral sclerosis (ALS) is an orphan neurodegenerative disease currently without a cure. Mutations in copper/zinc superoxide dismutase 1 (SOD1) have been implicated in the pathophysiology of this disease. Using a high-throughput screening assay expressing mutant G93A SOD1, two bioactive chemical hit compou...

journal_title：Bioorganic & medicinal chemistry

authors： Chen T,Benmohamed R,Arvanites AC,Ralay Ranaivo H,Morimoto RI,Ferrante RJ,Watterson DM,Kirsch DR,Silverman RB

更新日期：2011-01-01 00:00:00

abstract：:Synthesis and pharmacological characterisation of a series of compounds in which the oxime substructure present in imoproxifan was constrained in the pentatomic NO-donor furoxan ring, as well as their structurally related furazan analogues devoid of NO-donating properties, are described. The whole series of products d...

journal_title：Bioorganic & medicinal chemistry

authors： Tosco P,Bertinaria M,Di Stilo A,Cena C,Sorba G,Fruttero R,Gasco A

更新日期：2005-08-01 00:00:00

abstract：:The boronic acid group is widely used in chemosensor design due to its ability to reversibly bind diol-containing compounds. The thermodynamic properties of the boronic acid-diol binding process have been investigated extensively. However, there are few studies of the kinetic properties of such binding processes. In t...

journal_title：Bioorganic & medicinal chemistry

authors： Ni N,Laughlin S,Wang Y,Feng Y,Zheng Y,Wang B

更新日期：2012-05-01 00:00:00