Development of benzo[d]oxazol-2(3H)-ones derivatives as novel inhibitors of Mycobacterium tuberculosis InhA.

abstract：:Since NSAIDs are commonly used anti-inflammatory agents that produce adverse effects, there have been ongoing efforts to develop more effective and less toxic compounds. Based on the structure of the anti-inflammatory pyrrolizines licofelone and ketorolac, a series of 1-arylpyrrolizin-3-ones was synthesized. Also prep...

journal_title：Bioorganic & medicinal chemistry

authors： Madrigal DA,Escalante CH,Gutiérrez-Rebolledo GA,Cristobal-Luna JM,Gómez-García O,Hernández-Benitez RI,Esquivel-Campos AL,Pérez-Gutiérrez S,Chamorro-Cevallos GA,Delgado F,Tamariz J

更新日期：2019-10-15 00:00:00

abstract：:The N-demethylation of 3-deoxymorphine (1) was investigated using methyl chloroformate and hydrazine. 3-Deoxynormorphine (2) was obtained in 70% yield, and 3-deoxydihydronormorphine (3) was also obtained as a side product. The mu, delta, and kappa receptor binding affinity of a series of N-substituted 3-deoxynormorphi...

journal_title：Bioorganic & medicinal chemistry

authors： Csutoras C,Zhang A,Bidlack JM,Neumeyer JL

更新日期：2004-05-15 00:00:00

abstract：:We designed a phenylglycine (Phg)-incorporated ascidiacyclamide (ASC) analogue, cyclo(-Phg-oxazoline-d-Val-thiazole-Ile-oxazoline-d-Val-thiazole- ([Phg]ASC), with the aim of stabilizing the square conformation of ASC through interactions between amino acid side chains. X-ray diffraction analysis showed that [Phg]ASC h...

journal_title：Bioorganic & medicinal chemistry

authors： Asano A,Yamada T,Doi M

更新日期：2011-06-01 00:00:00

abstract：:Cell division cycle 7 (Cdc7) is a serine/threonine kinase that plays important roles in the regulation of DNA replication process. A genetic study indicates that Cdc7 inhibition can induce selective tumor-cell death in a p53-dependent manner, suggesting that Cdc7 is an attractive target for the treatment of cancers. I...

journal_title：Bioorganic & medicinal chemistry

authors： Kurasawa O,Oguro Y,Miyazaki T,Homma M,Mori K,Iwai K,Hara H,Skene R,Hoffman I,Ohashi A,Yoshida S,Ishikawa T,Cho N

更新日期：2017-04-01 00:00:00

abstract：:Peptides are limited in their use as drugs due to low cell permeability and vulnerability to proteases. In contrast, peptoids are immune to enzymatic degradation and some peptoids have been shown to be relatively cell permeable. In order to facilitate future design of peptoid libraries for screening experiments, it wo...

journal_title：Bioorganic & medicinal chemistry

authors： Tan NC,Yu P,Kwon YU,Kodadek T

更新日期：2008-06-01 00:00:00

abstract：:The structure elucidation and biological activity of novel YM-254890 (1) analogues and semi-synthetic derivatives are described. Three natural analogues, YM-254891 (2), YM-254892 (3), and YM-280193 (4), were isolated from the fermentation broth of Chromobacterium sp. QS3666, and two hydrogenated derivatives, YM-385780...

journal_title：Bioorganic & medicinal chemistry

authors： Taniguchi M,Suzumura K,Nagai K,Kawasaki T,Takasaki J,Sekiguchi M,Moritani Y,Saito T,Hayashi K,Fujita S,Tsukamoto S,Suzuki K

更新日期：2004-06-15 00:00:00

abstract：:A series of thiosugar derivatives (thiolevomannosans) derived from mannose were synthesized and their inhibitory activity was tested against alpha-mannosidase (jack bean). These inhibitors were found to be more potent than the well-known inhibitors like kifunensine and deoxymannojirimycin based on docking and biochemi...

journal_title：Bioorganic & medicinal chemistry

authors： Sivapriya K,Hariharaputran S,Suhas VL,Chandra N,Chandrasekaran S

更新日期：2007-09-01 00:00:00

abstract：:Antibiotic resistance among clinically significant bacterial pathogens, such as methicillin-resistant Staphylococcus aureus (MRSA) and vancomycin-resistant S. aureus (VRSA) is becoming a prevalent threat to public health, and new antibacterial agents with novel mechanisms of action hence are in an urgent need. As a pa...

journal_title：Bioorganic & medicinal chemistry

authors： Song D,Bi F,Zhang N,Qin Y,Liu X,Teng Y,Ma S

更新日期：2020-11-01 00:00:00

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

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

abstract：:The optimization of a series of benzimidazole glucokinase activators is described. We identified a novel and potent achiral benzimidazole derivative as an allosteric GK activator. This activator was designed and synthesized via removal of the chiral center of the lead compound, 6-(N-acylpyrrolidin-2-yl)benzimidazole. ...

journal_title：Bioorganic & medicinal chemistry

authors： Takahashi K,Hashimoto N,Nakama C,Kamata K,Sasaki K,Yoshimoto R,Ohyama S,Hosaka H,Maruki H,Nagata Y,Eiki J,Nishimura T

更新日期：2009-10-01 00:00:00

abstract：:Several analogues of (Z)-8-dodecenyl acetate (1a), the major pheromone component of the Oriental fruit moth, Cydia molesta, with chloroformate and lactone functional groups in place of the acetate moiety, were synthesized and investigated for their biological activity at four evaluation levels, i.e. by electroantennog...

journal_title：Bioorganic & medicinal chemistry

authors： Hoskovec M,Hovorka O,Kalinová B,Koutek B,Streinz L,Svatos A,Sebek P,Saman D,Vrkoc J

更新日期：1996-03-01 00:00:00

abstract：:Natural (-)-huperzine B (HupB), isolated from Chinese medicinal herb, displayed moderate inhibitory activity of acetylcholinesterase (AChE). Based on the active dual-site of AChE, a series of novel derivatives of bis- and bifunctional HupB were designed and synthesized. The AChE inhibition potency of most derivatives ...

journal_title：Bioorganic & medicinal chemistry

authors： He XC,Feng S,Wang ZF,Shi Y,Zheng S,Xia Y,Jiang H,Tang XC,Bai D

更新日期：2007-02-01 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：:N-[(18)F]Fluoroethyl-4-piperidyl acetate ([(18)F]FEtP4A) was synthesized and evaluated as a PET tracer for imaging brain acetylcholinesterase (AchE) in vivo. [(18)F]FEtP4A was previously prepared by reacting 4-piperidyl acetate (P4A) with 2-[(18)F]fluoroethyl bromide ([(18)F]FEtBr) at 130 degrees C for 30 min in 37% r...

journal_title：Bioorganic & medicinal chemistry

authors： Zhang MR,Furutsuka K,Maeda J,Kikuchi T,Kida T,Okauchi T,Irie T,Suzuki K

更新日期：2003-06-12 00:00:00

abstract：:Synthesis of new 6-ureido-4-anilinoquinazolines have been accomplished and their in vitro antimalarial activity against chloroquine-sensitive P. falciparum have been examined. Out of 64 compounds evaluated, the IC(50) of 16 compounds which have displayed MIC of 0.25 microg/mL were also recorded. One of the compounds (...

journal_title：Bioorganic & medicinal chemistry

authors： Madapa S,Tusi Z,Mishra A,Srivastava K,Pandey SK,Tripathi R,Puri SK,Batra S

更新日期：2009-01-01 00:00:00

abstract：:Experimental and theoretical physico-chemical methods were used to investigate the interaction between several reversible monoamine oxidase A inhibitors in the oxazolidinone series and the active site of the enzyme. Phenyloxazolidinones include toloxatone and analogues, among which befloxatone was selected as drug can...

journal_title：Bioorganic & medicinal chemistry

authors： Wouters J,Moureau F,Evrard G,Koenig JJ,Jegham S,George P,Durant F

更新日期：1999-08-01 00:00:00

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：:New phenothiazine derivatives 6-20 have been designed, synthesized and evaluated in vitro for their ability to inhibit tubulin polymerization and antiproliferative activity against 60 cancer cell lines, including several multi-drug resistant (MDR) tumor cell lines. The phenothiazine unit may successfully replace the c...

journal_title：Bioorganic & medicinal chemistry

authors： Ghinet A,Moise IM,Rigo B,Homerin G,Farce A,Dubois J,Bîcu E

更新日期：2016-05-15 00:00:00

abstract：:In this study, a number of 2',4'-BNA- and 2',4'-BNA(NC)-modified siRNAs were designed and synthesized. Their thermal stability, nuclease resistance and gene silencing properties against cultured mammalian cells were evaluated and compared with those of natural siRNAs. The 2',4'-BNA- and 2',4'-BNA(NC)-modified siRNAs (...

journal_title：Bioorganic & medicinal chemistry

authors： Abdur Rahman SM,Sato H,Tsuda N,Haitani S,Narukawa K,Imanishi T,Obika S

更新日期：2010-05-15 00:00:00

abstract：:Based on an established 3D pharmacophore, a series of quinoline derivatives were synthesized. The opioidergic properties of these compounds were determined by a competitive binding assay using (125)I-Dynorphine, (3)H-DAMGO and (125)I-DADLE for kappa, mu, and delta receptors, respectively. Results showed varying degree...

journal_title：Bioorganic & medicinal chemistry

authors： Deb I,Paira P,Hazra A,Banerjee S,Dutta PK,Mondal NB,Das S

更新日期：2009-08-15 00:00:00

abstract：:The β-lactam antibiotic resistance of Gram-negative bacteria has shown to be a critical global health problem. One of the primary reasons for the drug resistance is the existence of β-lactamases especially metallo-β-lactamases such as New Delhi metallo-β-lactamase (NDM-1) and Verona Integron-encoded metallo-β-lactamas...

journal_title：Bioorganic & medicinal chemistry

authors： Zhang J,Wang S,Wei Q,Guo Q,Bai Y,Yang S,Song F,Zhang L,Lei X

更新日期：2017-10-01 00:00:00

abstract：:Petrosaspongiolides M-R (PM-PR, 1-5) are marine sesterterpenes structurally characterised by a gamma-hydroxybutenolide moiety. They have shown an in vitro and in vivo potent anti-inflammatory activity, mediated by specific inhibition of secretory phospholipase A(2) (sPLA(2) enzymes). The molecular mechanism underlying...

journal_title：Bioorganic & medicinal chemistry

authors： Monti MC,Casapullo A,Riccio R,Gomez-Paloma L

更新日期：2004-03-15 00:00:00

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

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

abstract：:A set of phosphonic acid derivatives (1-4) of pyridoxal 5'-phosphate (PLP) was synthesized and characterized biochemically using purified murine pyridoxal phosphatase (PDXP), also known as chronophin. The most promising compound 1 displayed primarily competitive PDXP inhibitory activity with an IC50 value of 79μM, whi...

journal_title：Bioorganic & medicinal chemistry

authors： Knobloch G,Jabari N,Stadlbauer S,Schindelin H,Köhn M,Gohla A

更新日期：2015-06-15 00:00:00

abstract：:This review discusses all pyridine alkaloids with CNS activity, their therapeutic potential, and the interesting array of sources whence they originate. ...

journal_title：Bioorganic & medicinal chemistry

authors： Lin SX,Curtis MA,Sperry J

更新日期：2020-12-15 00:00:00

abstract：:Herein, we describe the design, synthesis, and structure-activity relationships of novel benzylpyrazole acylsulfonamides as non-thiazolidinedione (TZD), non-carboxylic-acid-based peroxisome proliferator-activated receptor (PPAR) γ agonists. Docking model analysis of in-house weak agonist 2 bound to the reported PPARγ ...

journal_title：Bioorganic & medicinal chemistry

authors： Rikimaru K,Wakabayashi T,Abe H,Imoto H,Maekawa T,Ujikawa O,Murase K,Matsuo T,Matsumoto M,Nomura C,Tsuge H,Arimura N,Kawakami K,Sakamoto J,Funami M,Mol CD,Snell GP,Bragstad KA,Sang BC,Dougan DR,Tanaka T,Katayama

更新日期：2012-01-15 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：:An activation study of mammalian carbonic anhydrase (CA, EC 4.2.1.1) isoforms I-XIV with D- and L-tryptophan has been performed both by means of kinetic and X-ray crystallographic techniques. These compounds show a time dependent activity against isozyme CA II, with activation constants of 1.13 microM for L-Trp and 0....

journal_title：Bioorganic & medicinal chemistry

authors： Temperini C,Innocenti A,Scozzafava A,Supuran CT

更新日期：2008-09-15 00:00:00

abstract：:Two novel ligands 2-(1'-phenyl-2'-carboxyl-3'-aza-n-butyl)-1,10-phenanthroline (L1) and 2-(1'-p-phenol-2'-carboxyl-3'-aza-butyl)-1,10-phenanthroline (L2), and their La(III) complexes of La(III)L1, La(III)(L1)(2), La(III)L2, and La(III)(L2)(2), were synthesized and characterized by (1)H NMR, elemental analysis, IR, the...

journal_title：Bioorganic & medicinal chemistry

authors： Zhao G,Li F,Lin H,Lin H

更新日期：2007-01-01 00:00:00

abstract：:The design, synthesis, and biological evaluation of a series of pyrrole and pyrazole congeners 2 of suramin, directed toward the development and identification of new ligands that complex the human fibroblast growth factor (bFGF), thereby inhibiting tumor-promoted angiogenesis, is reported. Compounds 2 were evaluated ...

journal_title：Bioorganic & medicinal chemistry

authors： Manetti F,Cappello V,Botta M,Corelli F,Mongelli N,Biasoli G,Borgia AL,Ciomei M

更新日期：1998-07-01 00:00:00