Recent progresses on synthesized LuxS inhibitors: A mini-review.


:Design and synthesis of LuxS enzyme inhibitors otherwise known as S-ribosylhomocysteine analogues, to target quorum sensing in bacteria, has been considerably developed within the last decade. This review presents which molecules have been synthesized to target LuxS enzyme in other words inhibitors of S-ribosylhomocysteinase. It reports their tested biological activity as LuxS inhibitors when available. A systematic overview has been conducted by searching PubMed, Medline, and The Cochrane Library and data extraction of all synthesized S-ribosylhomocysteine analogues has been collected. This mini-review shows limited data to date on this area and should continue to be studied.


Bioorg Med Chem


Mina G,Chbib C




Has Abstract


2019-01-01 00:00:00














  • Discovery and SAR study of c-Met kinase inhibitors bearing an 3-amino-benzo[d]isoxazole or 3-aminoindazole scaffold.

    abstract::A series of 3-amino-benzo[d]isoxazole-/3-aminoindazole-based compounds were designed, synthesized and pharmacologically evaluated as tyrosine kinase c-Met inhibitors. The SAR study was conducted leading to identification of nine compounds (8d, 8e, 12, 28a-d, 28h and 28i) with IC50s less than 10nM against c-Met. Compou...

    journal_title:Bioorganic & medicinal chemistry

    pub_type: 杂志文章


    authors: Jiang X,Liu H,Song Z,Peng X,Ji Y,Yao Q,Geng M,Ai J,Zhang A

    更新日期:2015-02-01 00:00:00

  • Preparation and biological properties of biotinylated PhTX derivatives.

    abstract::We report the synthesis of several highly functionalized biotinylated philanthotoxin (PhTX) analogues (7, 8, 10, 13-16) designed on the basis of earlier structure-activity relationship studies. Despite the extensive modifications, the binding to nicotinic acetylcholine receptor (nAChR) is in the low micromolar range a...

    journal_title:Bioorganic & medicinal chemistry

    pub_type: 杂志文章


    authors: Hashimoto M,Liu Y,Fang K,Li HY,Campiani G,Nakanishi K

    更新日期:1999-06-01 00:00:00

  • Design, synthesis, and activity of caffeoyl pyrrolidine derivatives as potential gelatinase inhibitors.

    abstract::The synthesis and biological evaluation of caffonyl pyrrolidine derivatives as MMPs inhibitors are reported in this paper. Inhibiting activities of synthesized compounds on gelatinase (MMP-2 and -9) were tested by using succinylated gelatin as substrate. Structure-activity relationship results from these tested compou...

    journal_title:Bioorganic & medicinal chemistry

    pub_type: 杂志文章


    authors: Li YL,Xu WF

    更新日期:2004-10-01 00:00:00

  • 000Synthesis of new α-aminophosphonates: Evaluation as anti-inflammatory agents and QSAR studies.

    abstract::In this paper, we report the synthesis of a new series of α-aminophosphonates derivatives based in an efficient three-component reaction. All compounds prepared showed significant anti-inflammatory activity, being the compounds 1a, 1c, 1d, 1f, 2b and 2c the most promising ones, in terms of maximal efficacy (over 95%),...

    journal_title:Bioorganic & medicinal chemistry

    pub_type: 杂志文章


    authors: Romero-Estudillo I,Viveros-Ceballos JL,Cazares-Carreño O,González-Morales A,de Jesús BF,López-Castillo M,Razo-Hernández RS,Castañeda-Corral G,Ordóñez M

    更新日期:2019-06-15 00:00:00

  • Synthesis and structure-activity data of some new epibatidine analogues.

    abstract::The high-pressure Diels-Alder reaction of N-carbomethyoxypyrroles and phenyl vinyl sulfone affords versatile intermediates for the palladium-catalyzed preparation of new epibatidine analogues. Structure-activity relationships of new epibatidine analogues are presented. High affinities of Ki = 0.81 and 2.6 nM for the [...

    journal_title:Bioorganic & medicinal chemistry

    pub_type: 杂志文章


    authors: Seerden JP,Tulp MT,Scheeren HW,Kruse CG

    更新日期:1998-11-01 00:00:00

  • 1-Methylpyridinium-4-(4-phenylmethanethiosulfonate) iodide, MTS-MPP+, a novel scanning cysteine accessibility method (SCAM) reagent for monoamine transporter studies.

    abstract::A novel substituted cysteine accessibility method (SCAM) reagent was developed for monoamine uptake transporters. The new reagent, MTS-MPP(+), was a derivative of the neurotoxin and transporter substrate MPP(+). MTS-MPP(+) labeled cysteine residues introduced into the serotonin transporter protein. Although it did not...

    journal_title:Bioorganic & medicinal chemistry

    pub_type: 杂志文章


    authors: Gallardo-Godoy A,Torres-Altoro MI,White KJ,Barker EL,Nichols DE

    更新日期:2007-01-01 00:00:00

  • Biased and unbiased strategies to identify biologically active small molecules.

    abstract::Small molecules are central players in chemical biology studies. They promote the perturbation of cellular processes underlying diseases and enable the identification of biological targets that can be validated for therapeutic intervention. Small molecules have been shown to accurately tune a single function of plurip...

    journal_title:Bioorganic & medicinal chemistry

    pub_type: 杂志文章,评审


    authors: Abet V,Mariani A,Truscott FR,Britton S,Rodriguez R

    更新日期:2014-08-15 00:00:00

  • Synthesis and binding affinities of methylvesamicol analogs for the acetylcholine transporter and sigma receptor.

    abstract::We synthesized methylvesamicol analogs 13-16 and investigated the binding characteristics of 2-[4-phenylpiperidino]cyclohexanol (vesamicol) and methylvesamicol analogs 13-16, with a methyl group introduced into the 4-phenylpiperidine moiety, to sigma receptors (sigma-1, sigma-2) and to vesicular acetylcholine transpor...

    journal_title:Bioorganic & medicinal chemistry

    pub_type: 杂志文章


    authors: Shiba K,Ogawa K,Ishiwata K,Yajima K,Mori H

    更新日期:2006-04-15 00:00:00

  • Inhibition of the β-carbonic anhydrase from Streptococcus pneumoniae by inorganic anions and small molecules: Toward innovative drug design of antiinfectives?

    abstract::The Gram-positive bacterium Streptococcus pneumoniae is a human respiratory tract pathogen that contributes significantly to global mortality and morbidity. It was recently shown that this bacterial pathogen depends on a conserved β-carbonic anhydrase (CA, EC for in vitro growth in environmental ambient air a...

    journal_title:Bioorganic & medicinal chemistry

    pub_type: 杂志文章


    authors: Burghout P,Vullo D,Scozzafava A,Hermans PW,Supuran CT

    更新日期:2011-01-01 00:00:00

  • Carbonic anhydrase inhibitors: Synthesis, molecular docking, cytotoxic and inhibition of the human carbonic anhydrase isoforms I, II, IX, XII with novel benzenesulfonamides incorporating pyrrole, pyrrolopyrimidine and fused pyrrolopyrimidine moieties.

    abstract::A series of novel pyrroles, pyrrolopyrimidines, pyrazolopyrrolopyrimidine, triazolopyrrolopyrimidines, tetrazolopyrrolopyrimidine, triazinopyrrolopyrimidines and pyrrolopyrimidotriazepines bearing the biologically active benzenesulfonamide moiety were synthesized by using pyrrole-o-amino-carbonitrile as key intermedia...

    journal_title:Bioorganic & medicinal chemistry

    pub_type: 杂志文章


    authors: Ghorab MM,Alsaid MS,Ceruso M,Nissan YM,Supuran CT

    更新日期:2014-07-15 00:00:00

  • Chemiluminescence flow sensor for berberine with immobilized reagents.

    abstract::A sensitive chemiluminescence (CL) sensor for berberine combined with flow-injection (FI) technology is described. The analytical reagents involved in the CL reaction, including luminol and potassium ferricyanide, were both immobilized on an anion-exchange resin column. While a volume of sodium phosphate was passed th...

    journal_title:Bioorganic & medicinal chemistry

    pub_type: 杂志文章


    authors: Song Z,Zhao T,Wang L,Xiao Z

    更新日期:2001-07-01 00:00:00

  • Synthesis and in vitro anti-hepatitis B virus activities of some ethyl 6-bromo-5-hydroxy-1H-indole-3-carboxylates.

    abstract::A series of ethyl 6-bromo-5-hydroxy-1H-indole-3-carboxylates, 8a-11v, were synthesized and evaluated for their anti-hepatitis B virus (HBV) activities in 2.2.15 cells. The selective indexes of inhibition on replication of HBV DNA of compounds 11s (>8.7) and 11t (10.8), which were introduced halogen on the phenyl ring ...

    journal_title:Bioorganic & medicinal chemistry

    pub_type: 杂志文章


    authors: Chai H,Zhao Y,Zhao C,Gong P

    更新日期:2006-02-15 00:00:00

  • Design, synthesis and evaluation of phthalide alkyl tertiary amine derivatives as promising acetylcholinesterase inhibitors with high potency and selectivity against Alzheimer's disease.

    abstract::A series of phthalide alkyl tertiary amine derivatives were designed, synthesized and evaluated as potential multi-target agents against Alzheimer's disease (AD). The results indicated that almost all the compounds displayed significant AChE inhibitory and selective activities. Besides, most of the derivatives exhibit...

    journal_title:Bioorganic & medicinal chemistry

    pub_type: 杂志文章


    authors: Luo L,Song Q,Li Y,Cao Z,Qiang X,Tan Z,Deng Y

    更新日期:2020-04-15 00:00:00

  • New sensible method to quantize the intestinal absorption of receptor ligands.

    abstract::In recent years, special attention has been paid to the A3 adenosine receptor (A3AR) as a possible pharmacological target to treat intestinal inflammation. In this work, it was set up a novel method to quantify the concentration of a promising anti-inflammatory agent inside and outside of intestinal barrier using the ...

    journal_title:Bioorganic & medicinal chemistry

    pub_type: 杂志文章


    authors: Buccioni M,Dal Ben D,Lambertucci C,Martí Navia A,Ricciutelli M,Spinaci A,Volpini R,Marucci G

    更新日期:2019-08-01 00:00:00

  • Protein linear indices of the 'macromolecular pseudograph alpha-carbon atom adjacency matrix' in bioinformatics. Part 1: prediction of protein stability effects of a complete set of alanine substitutions in Arc repressor.

    abstract::A novel approach to bio-macromolecular design from a linear algebra point of view is introduced. A protein's total (whole protein) and local (one or more amino acid) linear indices are a new set of bio-macromolecular descriptors of relevance to protein QSAR/QSPR studies. These amino-acid level biochemical descriptors ...

    journal_title:Bioorganic & medicinal chemistry

    pub_type: 杂志文章


    authors: Marrero-Ponce Y,Medina-Marrero R,Castillo-Garit JA,Romero-Zaldivar V,Torrens F,Castro EA

    更新日期:2005-04-15 00:00:00

  • Structure-activity relationship at alpha-adrenergic receptors within a series of imidazoline analogues of cirazoline.

    abstract::Several analogues of cirazoline (2), a selective alpha1-adrenoreceptor agonist, were prepared and their pharmacological profiles studied. Although at the alpha1-adrenoreceptor all the compounds displayed a significant agonist activity, at the alpha2-adrenoreceptor they showed either agonist or antagonist activity depe...

    journal_title:Bioorganic & medicinal chemistry

    pub_type: 杂志文章


    authors: Pigini M,Quaglia W,Gentili F,Marucci G,Cantalamessa F,Franchini S,Sorbi C,Brasili L

    更新日期:2000-05-01 00:00:00

  • Synthesis, structural elucidation and in vitro antiparasitic activity against Trypanosoma cruzi and Leishmania chagasi parasites of novel tetrahydro-1-benzazepine derivatives.

    abstract::Forty six new 1,4-epoxy-2-exo-aryl- and cis-2-aryl-4-hydroxytetrahydro-1-benzazepine derivatives were synthesized and fully characterized. All compounds were tested in vitro against both Trypanosoma cruzi and Leishmania chagasi parasites and also for cytotoxicity using Vero and THP-1 mammalian cell lines. Many of the ...

    journal_title:Bioorganic & medicinal chemistry

    pub_type: 杂志文章


    authors: Gómez-Ayala S,Castrillón JA,Palma A,Leal SM,Escobar P,Bahsas A

    更新日期:2010-07-01 00:00:00

  • Antiproliferative activities of halogenated pyrrolo[3,2-d]pyrimidines.

    abstract::In vitro evaluation of the halogenated pyrrolo[3,2-d]pyrimidines identified antiproliferative activities in compounds 1 and 2 against four different cancer cell lines. Upon screening of a series of pyrrolo[3,2-d]pyrimidines, the 2,4-Cl compound 1 was found to exhibit antiproliferative activity at low micromolar concen...

    journal_title:Bioorganic & medicinal chemistry

    pub_type: 杂志文章


    authors: Temburnikar KW,Ross CR,Wilson GM,Balzarini J,Cawrse BM,Seley-Radtke KL

    更新日期:2015-08-01 00:00:00

  • Investigating the activity of 2-substituted alkyl-6-(2,5-dioxopyrrolidin-1-yl)hexanoates as skin penetration enhancers.

    abstract::Skin penetration enhancers are used in the formulation of transdermal delivery systems for drugs that are otherwise not sufficiently skin-permeable. We generated two series of esters by multi-step synthesis with substituted 6-aminohexanoic acid as potential transdermal penetration enhancers by multi-step synthesis. Th...

    journal_title:Bioorganic & medicinal chemistry

    pub_type: 杂志文章


    authors: Brychtova K,Opatrilova R,Raich I,Kalinowski DS,Dvorakova L,Placek L,Csollei J,Richardson DR,Jampilek J

    更新日期:2010-12-15 00:00:00

  • Cyclopentitol as a scaffold for a natural product-like compound library for drug discovery.

    abstract::A concise and efficient synthesis of cyclopentitols as a scaffold for a two-dimensional compound library for drug discovery is described. Starting from d-mannose, the key steps are Wittig olefination and ring-closing metathesis (RCM) followed by a [3,3]-sigmatropic Overmann rearrangement to form an sp(3)-rich, natural...

    journal_title:Bioorganic & medicinal chemistry

    pub_type: 杂志文章


    authors: Padwal JD,Filippov DV,Narhe BD,Aertssen S,Beuving RJ,Benningshof JC,van der Marel GA,Overkleeft HS,van der Stelt M

    更新日期:2015-06-01 00:00:00

  • Conjugation of a 3-(1H-phenanthro[9,10-d]imidazol-2-yl)-1H-indole intercalator to a triplex oligonucleotide and to a three-way junction.

    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

    pub_type: 杂志文章


    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

  • G-quadruplex DNA cleavage preference and identification of a perylene diimide G-quadruplex photocleavage agent using a rapid fluorescent assay.

    abstract::A rapid fluorescence assay for G-quadruplex DNA cleavage was used to investigate the preference of TMPyP4 photochemical and Mn·TMPyP4 oxidative cleavage. Both agents most efficiently cleave the c-Myc promoter G-quadruplex. Direct PAGE analysis of selected assay samples showed that for a given cleavage agent, different...

    journal_title:Bioorganic & medicinal chemistry

    pub_type: 杂志文章


    authors: Schoonover M,Kerwin SM

    更新日期:2012-12-15 00:00:00

  • Design and synthesis of novel androgen receptor antagonists with sterically bulky icosahedral carboranes.

    abstract::Carboranes (dicarba-closo-dodecaboranes) are a class of carbon-containing polyhedral boron-cluster compounds having remarkable chemical and thermal stability, and hydrophobic character. These features may allow application of carboranes as a new hydrophobic core structure in biologically active molecules that interact...

    journal_title:Bioorganic & medicinal chemistry

    pub_type: 杂志文章


    authors: Goto T,Ohta K,Suzuki T,Ohta S,Endo Y

    更新日期:2005-12-01 00:00:00

  • Nucleosides with self-complementary hydrogen-bonding motifs: synthesis and base-pairing studies of two nucleosides containing the imidazo[4,5-d]pyridazine ring system.

    abstract::Synthesis and base-pairing studies of two 2'-deoxyribonucleosides, containing a common heterocyclic base, 7(4)-amino-5(6)H-imidazo[4,5-d]pyridazin-4(7)one (1 and 2), have been reported. The synthesis was accomplished by base-promoted deoxyribosylation of ethyl 5(4)-cyanoimidazole-4(5)-carboxylate (6), followed by ring...

    journal_title:Bioorganic & medicinal chemistry

    pub_type: 杂志文章


    authors: Ujjinamatada RK,Paulman RL,Ptak RG,Hosmane RS

    更新日期:2006-09-15 00:00:00

  • Synthesis of new chemical entities from paracetamol and NSAIDs with improved pharmacodynamic profile.

    abstract::It was envisaged to combine high antipyretic activity of paracetamol into commonly used NSAIDs. To achieve this goal new chemical entities were synthesized by chemically combining paracetamol and NSAIDs, and biologically evaluated for their antipyretic, analgesic, anti-inflammatory and ulcerogenic potential. The acid ...

    journal_title:Bioorganic & medicinal chemistry

    pub_type: 杂志文章


    authors: Yadav MR,Nimekar DM,Ananthakrishnan A,Brahmkshatriya PS,Shirude ST,Giridhar R,Parmar A,Balaraman R

    更新日期:2006-12-15 00:00:00

  • Discovery and structural analyses of S-adenosyl-L-homocysteine hydrolase inhibitors based on non-adenosine analogs.

    abstract::Optimization of a new series of S-adenosyl-L-homocysteine hydrolase (AdoHcyase) inhibitors based on non-adenosine analogs led to very potent compounds 14n, 18a, and 18b with IC50 values of 13 ± 3, 5.0 ± 2.0, and 8.5 ± 3.1 nM, respectively. An X-ray crystal structure of AdoHcyase with NAD(+) and 18a showed a novel open...

    journal_title:Bioorganic & medicinal chemistry

    pub_type: 杂志文章


    authors: Nakao A,Suzuki H,Ueno H,Iwasaki H,Setsuta T,Kashima A,Sunada S

    更新日期:2015-08-01 00:00:00

  • Small-molecules that bind to the ubiquitin-binding motif of REV1 inhibit REV1 interaction with K164-monoubiquitinated PCNA and suppress DNA damage tolerance.

    abstract::REV1 protein is a mutagenic DNA damage tolerance (DDT) mediator and encodes two ubiquitin-binding motifs (i.e., UBM1 and UBM2) that are essential for the DDT function. REV1 interacts with K164-monoubiquitinated PCNA (UbPCNA) in cells upon DNA-damaging stress. By using AlphaScreen assays to detect inhibition of REV1 an...

    journal_title:Bioorganic & medicinal chemistry

    pub_type: 杂志文章


    authors: Vanarotti M,Evison BJ,Actis ML,Inoue A,McDonald ET,Shao Y,Heath RJ,Fujii N

    更新日期:2018-05-15 00:00:00

  • An artificial CuII complex with intriguing oxygen radical-quenching profile. X-ray structure, cytochrome c assay, and ESR study.

    abstract::A novel artificial peptide named HPH-Pep, comprising a pyridine and two histidine units, was synthesized. The HPH-Pep-CuII complex had unique pentacoordinated structure as shown by X-ray crystallography and exhibited superoxide-scavenging activity as indicated by ESR spectroscopy. The superoxide-quenching profile of H...

    journal_title:Bioorganic & medicinal chemistry

    pub_type: 杂志文章


    authors: Otsuka M,Satake H,Murakami S,Doi M,Ishida T,Shibasaki M,Sugiura Y

    更新日期:1996-10-01 00:00:00

  • Synthesis, biological evaluation and molecular docking studies of benzyloxyacetohydroxamic acids as LpxC inhibitors.

    abstract::The inhibition of the UDP-3-O-[(R)-3-hydroxymyristoyl]-N-acetylglucosamine deacetylase (LpxC) represents a promising strategy to combat infections caused by multidrug-resistant Gram-negative bacteria. In order to elucidate the functional groups being important for the inhibition of LpxC, the structure of our previousl...

    journal_title:Bioorganic & medicinal chemistry

    pub_type: 杂志文章


    authors: Szermerski M,Melesina J,Wichapong K,Löppenberg M,Jose J,Sippl W,Holl R

    更新日期:2014-02-01 00:00:00

  • Antitumor activity of some natural flavonoids and synthetic derivatives on various human and murine cancer cell lines.

    abstract::The effect of various natural flavonoids, cinnamic acid derivatives, and a series of synthetic flavones on cell proliferation was evaluated in vitro in a panel of established human and murine tumor cell lines. The most potent antiproliferative agents were caffeic acid n-butyl ester (12) > 2'-nitroflavone (26) > caffei...

    journal_title:Bioorganic & medicinal chemistry

    pub_type: 杂志文章


    authors: Cárdenas M,Marder M,Blank VC,Roguin LP

    更新日期:2006-05-01 00:00:00