Selection of genomic target RNAs by iterative screening.

abstract：:A series of novel hybrids of metronidazole and berberine as new type of antimicrobial agents were synthesized and characterized by (1)H NMR, (13)C NMR, IR, MS and HRMS spectra. Bioactive assay manifested that most of the prepared compounds exhibited effective antibacterial and antifungal activities and some showed com...

journal_title：Bioorganic & medicinal chemistry

authors： Zhang L,Chang JJ,Zhang SL,Damu GL,Geng RX,Zhou CH

更新日期：2013-07-15 00:00:00

abstract：:A series of 1,2,3-triazolylsalicylamide derivatives has been developed from the antiproliferative agent 7 and was evaluated for their Aurora kinase inhibitory activity. The novel 1,2,3-triazolylsalicylamide scaffold could be readily assembled by Cu(I)-catalyzed azide-alkyne 1,3-dipolar cycloaddition, allowing rapid ac...

journal_title：Bioorganic & medicinal chemistry

authors： Song D,Park Y,Yoon J,Aman W,Hah JM,Ryu JS

更新日期：2014-09-01 00:00:00

abstract：:2,3-Dihydro-6,7-dichloro-pyrido[2,3-b]pyrazine-8-oxide was synthesized and evaluated for in vitro/in vivo antagonistic activity at the strychnine insensitive glycine binding site on the NMDA receptor revealing it to be a useful tool to evaluate the effectiveness of glycine antagonists in vivo. ...

journal_title：Bioorganic & medicinal chemistry

authors： Micheli F,Cugola A,Donati D,Missio A,Pecunioso A,Reggiani A,Tarzia G

更新日期：1997-12-01 00:00:00

abstract：:Guanase is an important enzyme of the purine salvage pathway of nucleic acid metabolism and its inhibition has beneficial implications in viral, bacterial, and cancer therapy. The work described herein is based on a hypothesis that azepinomycin, a heterocyclic natural product and a purported transition state analog in...

journal_title：Bioorganic & medicinal chemistry

authors： Tantravedi S,Chakraborty S,Shah NH,Fishbein JC,Hosmane RS

更新日期：2013-09-01 00:00:00

abstract：:We previously identified dibenzooxepine derivative 1 as a potent PPARγ ligand with a unique binding mode owing to its non-thiazolidinedione scaffold. However, while 1 showed remarkably potent MKN-45 gastric cancer cell aggregation activity, an indicator of cancer differentiation-inducing activity induced by PPARγ acti...

journal_title：Bioorganic & medicinal chemistry

authors： Yamamoto K,Tamura T,Nakamura R,Hosoe S,Matsubara M,Nagata K,Kodaira H,Uemori T,Takahashi Y,Suzuki M,Saito JI,Ueno K,Shuto S

更新日期：2019-11-15 00:00:00

abstract：:A codrug approach for simultaneous treatment of alcohol abuse and tobacco dependence is considered as very desirable because of substantial evidence that smoking is increased significantly during drinking, and that smoking is regarded as a behavioral 'cue' for the urge to consume alcohol. The purpose of this study was...

journal_title：Bioorganic & medicinal chemistry

authors： Hamad MO,Kiptoo PK,Stinchcomb AL,Crooks PA

更新日期：2006-10-15 00:00:00

abstract：:A series of acridine derivatives were synthesised and their in vitro antimalarial activity was evaluated against one chloroquine-susceptible strain (3D7) and three chloroquine-resistant strains (W2, Bre1 and FCR3) of Plasmodium falciparum. Structure-activity relationship showed that two positives charges as well as 6-...

journal_title：Bioorganic & medicinal chemistry

authors： Guetzoyan L,Yu XM,Ramiandrasoa F,Pethe S,Rogier C,Pradines B,Cresteil T,Perrée-Fauvet M,Mahy JP

更新日期：2009-12-01 00:00:00

abstract：:Analogs of nantenine were docked into a modeled structure of the human 5-HT(2A) receptor using ICM Pro, GLIDE, and GOLD docking methods. The resultant docking scores were used to correlate with observed in vitro apparent affinity (K(e)) data. The GOLD docking algorithm when used with a homology model of 5-HT(2A), base...

journal_title：Bioorganic & medicinal chemistry

authors： Pecic S,Makkar P,Chaudhary S,Reddy BV,Navarro HA,Harding WW

更新日期：2010-08-01 00:00:00

abstract：:We reported previously that octadecyloxyethyl 9-(S)-[3-hydroxy-2-(phosphonomethoxy)-propyl]adenine (ODE-(S)-HPMPA) was active against genotype 1b and 2a hepatitis C virus (HCV) replicons. This is surprising because acyclic nucleoside phosphonates have been regarded as having antiviral activity only against double stra...

journal_title：Bioorganic & medicinal chemistry

authors： Valiaeva N,Wyles DL,Schooley RT,Hwu JB,Beadle JR,Prichard MN,Hostetler KY

更新日期：2011-08-01 00:00:00

abstract：:Three C terminal His6-tagged recombinant microbial CMP-sialic acid synthetases [EC 2.7.7.43] cloned from Neisseria meningitidis group B, Streptococcus agalactiae serotype V, and Escherichia coli K1, respectively, were evaluated for their ability in the synthesis of CMP-sialic acid derivatives in a one-pot two-enzyme s...

journal_title：Bioorganic & medicinal chemistry

authors： Yu H,Yu H,Karpel R,Chen X

更新日期：2004-12-15 00:00:00

abstract：:Human dipeptidyl peptidase I (hDPPI, cathepsin C, EC 3.4.14.1) is a novel putative drug target for the treatment of inflammatory diseases. Using 1 as a starting point (IC50>10 microM), we have improved potency by more than 500-fold and successfully identified novel inhibitors of DPPI via screening of a one-bead-two-co...

journal_title：Bioorganic & medicinal chemistry

authors： Bondebjerg J,Fuglsang H,Valeur KR,Kaznelson DW,Hansen JA,Pedersen RO,Krogh BO,Jensen BS,Lauritzen C,Petersen G,Pedersen J,Naerum L

更新日期：2005-07-15 00:00:00

abstract：:The synthesis of a range of 2-amido-3-hydroxypyridin-4-ones as bidentate iron(III) chelators with potential for oral administration is described. The pKa values of the ligands together with the stability constants of their iron(III) complexes have been determined. Results indicate that the introduction of an amido sub...

journal_title：Bioorganic & medicinal chemistry

authors： Liu ZD,Piyamongkol S,Liu DY,Khodr HH,Lu SL,Hider RC

更新日期：2001-03-01 00:00:00

abstract：:We examined the properties of RNA analogues containing 2'-deoxy-2'-alpha-fluorouridine (1) or 2'-O-methyluridine (2) as inhibitors against human RNase L, that cleaves a single-stranded RNA in the presence of 2',5'-linked oligoadenylate (2-5A). The RNA analogue, FF, containing two molecules of 1 in place of uridine eff...

journal_title：Bioorganic & medicinal chemistry

authors： Ueno Y,Yamada Y,Nakanishi M,Kitade Y

更新日期：2003-11-17 00:00:00

abstract：:Aromatic alpha-amino-alpha-methyl acids and alpha-hydrazino-alpha-methyl acids are known aromatic amino acid decarboxylase inhibitors. Specific derivatives such as 2-amino-2-methyl-3-(3,4- dihydroxyphenyl)propanoate, Aldomet, and 2-hydrazino-2-methyl-3-(3,4- dihydroxyphenyl)propanoate, Lodosyn, have been developed as ...

journal_title：Bioorganic & medicinal chemistry

authors： Kallwass HK,Yee C,Blythe TA,McNabb TJ,Rogers EE,Shames SL

更新日期：1994-07-01 00:00:00

abstract：:1,4,7-Trisubstituted isoquinolines were designed, synthesized and evaluated for their inhibition against Plasmodium falciparum cysteine protease falcipain-2. The 1-benzyloxyphenyl-dihydroisoquinoline and -isoquinoline derivatives were found to exhibit better activity against falcipain-2 than their corresponding 1-hydr...

journal_title：Bioorganic & medicinal chemistry

authors： Batra S,Sabnis YA,Rosenthal PJ,Avery MA

更新日期：2003-05-15 00:00:00

abstract：:12-O-β-D-glucopyranosyl jasmonic acid (JAG) shows unique biological activities, including leaf-closing of Samanea saman. It is expected that the mode of action for such regulation is distinct from that of other jasmonates. We developed high-performance compact molecular probes (CMPs) based on JAG that can be used for ...

journal_title：Bioorganic & medicinal chemistry

authors： Ueda M,Yang G,Ishimaru Y,Itabashi T,Tamura S,Kiyota H,Kuwahara S,Inomata S,Shoji M,Sugai T

更新日期：2012-10-01 00:00:00

abstract：:Avermectin B1a (1) is a potent anthelmintic, insecticide, miticide and chloride channel activator on interaction with a specific nerve membrane site analyzed by binding assays with [3H]1. Candidate photoaffinity probes were prepared replacing the dioleandrosyl substituent with potential isosteric esters and ethers app...

journal_title：Bioorganic & medicinal chemistry

authors： Tsukamoto Y,Cole LM,Casida JE

更新日期：2000-01-01 00:00:00

abstract：:Efficient preparations of the titled compounds are described, their antimicrobial activity and mutagenic properties being evaluated. Some of the studied compounds are nonmutagenic and present a MIC as low as some of the usual standards in the field. ...

journal_title：Bioorganic & medicinal chemistry

authors： Arredondo Y,Moreno-Mañas M,Pleixats R,Palacín C,Raga MM,Castelló JM,Ortiz JA

更新日期：1997-10-01 00:00:00

abstract：:The 10 analogous bis-xylosylated dihydroxynaphthalenes have been synthesized and their chemical and biological properties investigated. The yield of the xylosylation reactions can be correlated to the electrostatic potential, and thus to the nucleophilicity, for the oxygen atoms of the dihydroxynaphthalenes. The bis-x...

journal_title：Bioorganic & medicinal chemistry

authors： Johnsson R,Mani K,Ellervik U

更新日期：2007-04-15 00:00:00

abstract：:Nuclear factor-kappaB (NF-kappaB) has been considered as a good target for the treatment of many diseases. Although a lot of NF-kappaB inhibitors have already been reported, many of them have several common problems. Thus, we attempted to identify novel NF-kappaB inhibitors to be unique lead compounds for creating new...

journal_title：Bioorganic & medicinal chemistry

authors： Kobayashi T,Yoshimori A,Kino K,Komori R,Miyazawa H,Tanuma SI

更新日期：2009-07-15 00:00:00

abstract：:The 1,2,4-triazolo[1,5-a]quinoxaline (TQX) scaffold was extensively investigated in our previously reported studies and recently, our attention was focused at position 5 of the tricyclic nucleus where different acyl and carboxylate moieties were introduced (compounds 2-15). This study produced some interesting compoun...

journal_title：Bioorganic & medicinal chemistry

authors： Catarzi D,Varano F,Poli D,Squarcialupi L,Betti M,Trincavelli L,Martini C,Dal Ben D,Thomas A,Volpini R,Colotta V

更新日期：2015-01-01 00:00:00

abstract：:The design, synthesis, and biological evaluation of new phosphodiesterase type 4 inhibitors, which possess new templates instead of a cyclohexane ring, are described. The mode of interaction with the enzyme is discussed based on the structure-activity relationship (SAR) data obtained for the synthesized inhibitors. Fu...

journal_title：Bioorganic & medicinal chemistry

authors： Ochiai H,Odagaki Y,Ohtani T,Ishida A,Kusumi K,Kishikawa K,Yamamoto S,Takeda H,Obata T,Kobayashi K,Nakai H,Toda M

更新日期：2004-10-01 00:00:00

abstract：:Many therapeutically-relevant protein-protein interactions (PPIs) have been reported that feature a helix and helix-binding cleft at the interface. Given this, different approaches to disrupting such PPIs have been developed. While short peptides (<15 amino acids) typically do not fold into a stable helix, researchers...

journal_title：Bioorganic & medicinal chemistry

authors： Tennyson RL,Walker SN,Ikeda T,Harris RS,McNaughton BR

更新日期：2018-03-15 00:00:00

abstract：:Breast cancer is the second most common cancer worldwide after lung cancer with the vast majority of early stage breast cancers being hormone-dependent. One of the major therapeutic advances in the clinical treatment of breast cancer has been the introduction of selective estrogen receptor modulators (SERMs). We descr...

journal_title：Bioorganic & medicinal chemistry

authors： Kelly PM,Bright SA,Fayne D,Pollock JK,Zisterer DM,Williams DC,Meegan MJ

更新日期：2016-09-15 00:00:00

abstract：:A quantitative structure-activity relationship (QSAR) study has been made on two different series of tetrahydropyrimidinones acting as HIV-1 protease inhibitors. A structural parameter, the first order valence molecular connectivity index ((1)chi(v)), has been used to account for the variation in the activity. The pro...

journal_title：Bioorganic & medicinal chemistry

authors： Gayathri P,Pande V,Sivakumar R,Gupta SP

更新日期：2001-11-01 00:00:00

abstract：:A new intercalating nucleic acid monomer M comprising a 4-(1-indole)-butane-1,2-diol moiety was synthesized via a classical alkylation reaction of indole-3-carboxaldehyde followed by a condensation reaction with phenanthrene-9,10-dione in the presence of ammonium acetate to form a phenanthroimidazole moiety linked to ...

journal_title：Bioorganic & medicinal chemistry

authors： Fatthalla MI,Elkholy YM,Abbas NS,Mandour AH,Jørgensen PT,Bomholt N,Pedersen EB

更新日期：2012-01-01 00:00:00

abstract：:The present study was designed to synthesize and evaluate pyrrolo-isoxazole benzoic acid derivatives as potential acetylcholinesterase (AChE) inhibitors for the management of Alzheimer's disease. The synthesis of pyrrolo-isoxazole benzoic acid derivatives involved ring opening cyclization of p-aminobenzoic acid with m...

journal_title：Bioorganic & medicinal chemistry

authors： Anand P,Singh B

更新日期：2012-01-01 00:00:00

abstract：:Leu-enkephalin is an endogenous pain modulating opioid pentapeptide. Its development as a potential pharmaceutic has been hampered by poor membrane permeability and susceptibility to enzymatic degradation. The addition of an unnatural amino acid containing a lipidic side chain at the N-terminus and the modification of...

journal_title：Bioorganic & medicinal chemistry

authors： Cros CD,Toth I,Blanchfield JT

更新日期：2011-02-15 00:00:00

abstract：:Combretastatin A-4 (CA-4) is a highly cytotoxic natural product and several derivatives have been prepared which underwent clinical trial. These investigations revealed that the cis-stilbene moiety of the natural product is prone to undergo cis/trans isomerization under physiological conditions, reducing the overall a...

journal_title：Bioorganic & medicinal chemistry

authors： Nowikow C,Fuerst R,Kauderer M,Dank C,Schmid W,Hajduch M,Rehulka J,Gurska S,Mokshyna O,Polishchuk P,Zupkó I,Dzubak P,Rinner U

更新日期：2019-10-01 00:00:00

abstract：:2,6-Bis(4-anilino)-4-(4-N,N-dimethylanilino)thiopyrylium chloride (AA1) and -selenopyrylium chloride (AA1-Se) and 2,6-bis(4-anilino)-4-(4-N-morpholinophenyl)thiopyrylium chloride (1) and -selenopyrylium chloride (2) were prepared via the addition of 4-N,N-dimethylanilino magnesium bromide and 4-N-morpholinophenyl magn...

journal_title：Bioorganic & medicinal chemistry

authors： Detty MR,Gibson SL,Hilf R

更新日期：2004-05-15 00:00:00