Properties of diacetyl (acetoin) reductase from Bacillus stearothermophilus.

abstract：:Leinamycin (1) is a Streptomyces-derived natural product that displays nanomolar IC(50) values against human cancer cell lines. In the work described here, we report the synthesis and characterization of a small leinamycin analogue 19 that closely resembles the 'upper-right quadrant' of the natural product, consisting...

journal_title：Bioorganic & medicinal chemistry

authors： Keerthi K,Rajapakse A,Sun D,Gates KS

更新日期：2013-01-01 00:00:00

abstract：:This study aimed to investigate the relationships between structures of gene carrier molecules and their activities for gene delivery into cells. We compared 2 types of poly(L-lysine) as carriers, that is, dendritic poly(L-lysine) (KG6) and linear poly(L-lysine) (PLL). KG6 formed a neutral DNA complex, and its DNA com...

journal_title：Bioorganic & medicinal chemistry

authors： Yamagata M,Kawano T,Shiba K,Mori T,Katayama Y,Niidome T

更新日期：2007-01-01 00:00:00

abstract：:Concise total syntheses of (R)- and (S)-argentilactone have been developed via enantioselective catalytic allylation (ECA) and ring-closing metathesis pathways (four steps, 39% overall yield and 82-84% ee) from 2-octynal and their in vitro activity against cancer cells is described. ...

journal_title：Bioorganic & medicinal chemistry

authors： de Fatima A,Kohn LK,Antônio MA,de Carvalho JE,Pilli RA

更新日期：2004-10-15 00:00:00

abstract：:We investigated the carbonic anhydrase (CA, EC 4.2.1.1) inhibitory activity of the clinically used antitumor agent bortezomib, a marketed proteasome inhibitor, against all the catalytically active mammalian isoforms CA I-VII, IX, XII-XV. Bortezomib effectively inhibited all these CAs in the micromolar range. hCA II, t...

journal_title：Bioorganic & medicinal chemistry

authors： Supuran CT

更新日期：2017-10-01 00:00:00

abstract：:A series of allosteric kidney-type glutaminase (GLS) inhibitors possessing a mercaptoethyl (SCH2CH2) linker were synthesized in an effort to further expand the structural diversity of chemotypes derived from bis-2-(5-phenylacetamido-1,3,4-thiadiazol-2-yl)ethyl sulfide (BPTES), a prototype allosteric inhibitor of GLS. ...

journal_title：Bioorganic & medicinal chemistry

authors： Duvall B,Zimmermann SC,Gao RD,Thomas AG,Kalčic F,Veeravalli V,Elgogary A,Rais R,Rojas C,Le A,Slusher BS,Tsukamoto T

更新日期：2020-10-15 00:00:00

abstract：:A series of halogen-substituted tricyclic flavonoids containing a 1,3-dithiol-2-ylium moiety has been synthesized from the corresponding 3-dithiocarbamic flavanones. The influence of halogen substituents on the antibacterial properties of the tricyclic flavonoids has been investigated against Staphylococcus aureus and...

journal_title：Bioorganic & medicinal chemistry

authors： Bahrin LG,Sarbu LG,Hopf H,Jones PG,Babii C,Stefan M,Birsa ML

更新日期：2016-07-15 00:00:00

abstract：:Forty-five novel cephalosporin derivatives with activity against methicillin-resistant Staphylococcus aureus (MRSA) are described. The compounds contain novel cinnamic acid moieties at C-7 that were synthesized using a key Heck reaction followed by nucleophilic aromatic substitution reactions. The most active compound...

journal_title：Bioorganic & medicinal chemistry

authors： Springer DM,Luh BY,Goodrich J,Bronson JJ

更新日期：2003-01-17 00:00:00

abstract：:The chemical cross-linking of complexes of proteins with nucleic acids is often used in structural and mechanistic studies of these oftentimes unstable and transient complexes. To date, no method has been reported for the thiol-based conjugation of proteins with an RNA backbone, mainly because of instability of the mo...

journal_title：Bioorganic & medicinal chemistry

authors： Hyjek-Składanowska M,Stasińska AR,Napiórkowska-Gromadzka A,Bartłomiejczak A,Seth PP,Chmielewski MK,Nowotny M

更新日期：2020-12-01 00:00:00

abstract：:A series of new Luotonin A derivatives with substituents at rings A and E was synthesized, together with some E-ring-unsubstituted derivatives. Subsequently, the compound library was examined in silico for their binding into a previously proposed site in the DNA/topoisomerase I binary complex. Whereas no convincing co...

journal_title：Bioorganic & medicinal chemistry

authors： Ibric A,Battisti V,Deckardt S,Haller AV,Lee C,Prötsch C,Langer T,Heffeter P,Schueffl HH,Marian B,Haider N

更新日期：2020-05-01 00:00:00

abstract：:Metabolic disorders such as diabetes are known risk factors for developing cholesterol gallstone disease (CGD). Cholesterol gallstone disease is one of the most prevalent digestive diseases, leading to considerable financial and social burden worldwide. Ursodeoxycholic acid (UDCA) is the only bile acid drug approved b...

journal_title：Bioorganic & medicinal chemistry

authors： Yu DD,Andrali SS,Li H,Lin M,Huang W,Forman BM

更新日期：2016-09-15 00:00:00

abstract：:Mycobacterium tuberculosis glutamate racemase is an essential enzyme involved in peptidoglycan synthesis and conserved in most bacteria. Small molecule inhibitors were reported on other bacterial species whereas in M. tuberculosis it wasn't explored much. In this study we have screened in house compound library using ...

journal_title：Bioorganic & medicinal chemistry

authors： Malapati P,Siva Krishna V,Nallangi R,Meda N,Reshma Srilakshmi R,Sriram D

更新日期：2018-01-01 00:00:00

abstract：:Twenty manzamine amides were synthesized and evaluated for in vitro antimalarial and antimicrobial activities. The amides of manzamine A (1) showed significantly reduced cytotoxicity against Vero cells, although were less active than 1. The structure-activity analysis showed that linear, short alkyl groups adjacent to...

journal_title：Bioorganic & medicinal chemistry

authors： Wahba AE,Peng J,Kudrimoti S,Tekwani BL,Hamann MT

更新日期：2009-11-15 00:00:00

abstract：:MGAT2 (monoacylglycerol acyltransferase 2) is expected to be an attractive target for the drug treatment of obesity, diabetes, and other disease. We describe our exploration and structure-activity relationship (SAR) study of 2,3-dihydro-1H-isoindole-5-sulfonamide derivatives. In this study, we identified 29 as an oral...

journal_title：Bioorganic & medicinal chemistry

authors： Busujima T,Tanaka H,Shirasaki Y,Munetomo E,Saito M,Kitano K,Minagawa T,Yoshida K,Osaki N,Sato N

更新日期：2015-09-01 00:00:00

abstract：:Human enterovirus (EV) belongs to the picornavirus family, which consists of over 200 medically relevant viruses. A peptidomimetic inhibitor AG7088 was developed to inhibit the 3C protease of rhinovirus (a member of the family), a chymotrypsin-like protease required for viral replication, by forming a covalent bond wi...

journal_title：Bioorganic & medicinal chemistry

authors： Kuo CJ,Shie JJ,Fang JM,Yen GR,Hsu JT,Liu HG,Tseng SN,Chang SC,Lee CY,Shih SR,Liang PH

更新日期：2008-08-01 00:00:00

abstract：:A facile, one-pot enzymatic glycan remodeling of antibody rituximab to produce homogeneous high-mannose and hybrid type antibody glycoforms is described. This method was based on the unique substrate specificity of the endoglycosidase S (Endo-S) from Streptococcus pyogenes. While Endo-S efficiently hydrolyzes the bi-a...

journal_title：Bioorganic & medicinal chemistry

authors： Tong X,Li T,Orwenyo J,Toonstra C,Wang LX

更新日期：2018-04-01 00:00:00

abstract：:The chemistries of S-nitroso-DL-penicillamine (SNAP) and S-nitrosoglutathione (GSNO) in relation to their ability to relax vascular smooth muscle and prevent platelet aggregation have been investigated. Metal ion catalysis greatly accelerates the decomposition of SNAP, but has little effect on GSNO. Instead, NO releas...

journal_title：Bioorganic & medicinal chemistry

authors： Askew SC,Butler AR,Flitney FW,Kemp GD,Megson IL

更新日期：1995-01-01 00:00:00

abstract：:Eighteen derivatives of egonol (A-R) were synthesized and evaluated for their antimicrobial activities against Staphylococcus aureus ATCC 29213, Bacillus subtilis ATCC 6633, Candida albicans ATCC 10231 and Escherichia coli ATCC 8739 microorganisms comparing with egonol. The obtained data reported that compound B exhib...

journal_title：Bioorganic & medicinal chemistry

authors： Emirdağ-Öztürk S,Karayildirim T,Anil H

更新日期：2011-02-01 00:00:00

abstract：:The synthesis and the binding study of new 3-arylesters and 3-heteroarylpyrazolo[5,1-c][1,2,4]benzotriazine 5-oxide 8-substituted are reported. The nature of these substituents (in terms of lipophilic and electronic features) seems to influence the binding affinity. High-affinity ligands were studied in mice in vivo f...

journal_title：Bioorganic & medicinal chemistry

authors： Guerrini G,Costanzo A,Ciciani G,Bruni F,Selleri S,Costagli C,Besnard F,Costa B,Martini C,De Siena G,Malmberg-Aiello P

更新日期：2006-02-01 00:00:00

abstract：:Positron emission tomography (PET) using fluorine-18 (18F)-labeled 2-nitroimidazole radiotracers has proven useful for assessment of tumor oxygenation. However, the passive diffusion-driven cellular uptake of currently available radiotracers results in slow kinetics and low tumor-to-background ratios. With the aim to ...

journal_title：Bioorganic & medicinal chemistry

authors： Wanek T,Kreis K,Križková P,Schweifer A,Denk C,Stanek J,Mairinger S,Filip T,Sauberer M,Edelhofer P,Traxl A,Muchitsch VE,Mereiter K,Hammerschmidt F,Cass CE,Damaraju VL,Langer O,Kuntner C

更新日期：2016-11-01 00:00:00

abstract：:The synthesis and biological activity of a novel series of 2-alkyl-4-pyrrolidinylthio-beta-methylcarbapenems containing a variety of cationic heteroaromatic substituents linked via a C-C bond is described. As a result of these studies, we selected FR21818 (In) as a candidate compound for development. FR21818 exhibited...

journal_title：Bioorganic & medicinal chemistry

authors： Zam HA,Barrett D,Tanaka A,Sasaki H,Matsuda K,Sakurai M,Terasawa T,Shirai F,Chiba T,Matsumoto Y,Tawara S

更新日期：2001-04-01 00:00:00

abstract：:Several derivatives out of a series of antifungal agents exhibited a good inhibitory potency against aromatase as well as a fairly good selectivity toward CYP17, even if lacking H-bond accepting substituents. Their common structural feature is a flexible backbone that did not fit into previously reported CYP19 models....

journal_title：Bioorganic & medicinal chemistry

authors： Castellano S,Stefancich G,Ragno R,Schewe K,Santoriello M,Caroli A,Hartmann RW,Sbardella G

更新日期：2008-09-15 00:00:00

abstract：:The beta-amino acid, (S)-ethyl-3-amino-4-pentynoate, is a chiral synthon used in the synthesis of xemilofiban hydrochloride, an anti-platelet agent. A biocatalytic approach was developed to resolve (R)- and (S)-enantiomers of ethyl 3-amino-4-pentynoate in enantiomerically pure form employing the enzyme Penicillin acyl...

journal_title：Bioorganic & medicinal chemistry

authors： Topgi RS,Ng JS,Landis B,Wang P,Behling JR

更新日期：1999-10-01 00:00:00

abstract：:Alternaria brassicicola is a fungal pathogen of many agriculturally important cruciferous crops. Cyclobrassinin hydrolase (CH) is an enzyme produced by A. brassicicola that catalyzes the transformation of the cruciferous phytoalexin cyclobrassinin into S-methyl[(2-sulfanyl-1H-indolyl-3)methyl]carbamothioate. The purif...

journal_title：Bioorganic & medicinal chemistry

authors： Pedras MS,Minic Z

更新日期：2014-01-01 00:00:00

abstract：:We have previously employed cyclization of a linear peptide as a strategy to modulate peptide function and properties, but cleavage to regenerate the linear peptide left parts of the linker structure on the peptide, interfering with its activity. Here, we focused on cyclization of a linear peptide via a "traceless" di...

journal_title：Bioorganic & medicinal chemistry

authors： Amano Y,Umezawa N,Sato S,Watanabe H,Umehara T,Higuchi T

更新日期：2017-02-01 00:00:00

abstract：:Lead compounds 5-fluoro-2-methyl-N-[2-methyl-4-(2-methyl-[1,3']bipyrrolidinyl-1'-yl)-phenyl]-benzamide (1), tetrahydro-pyran-4-carboxylic acid [((2S,3'S)-2-methyl-[1,3']bipyrrolidinyl-1'-yl)-phenyl]-amide (2), and 3,5-dimethyl-isoxazole-4-carboxylic acid [((2S,3'S)-2-methyl-[1,3']bipyrrolidinyl-1'-yl)-phenyl]-amide (3...

journal_title：Bioorganic & medicinal chemistry

authors： Gao Z,Hurst WJ,Hall D,Hartung R,Reynolds W,Kang J,Nagorny R,Hendrix JA,George PG

更新日期：2015-02-01 00:00:00

abstract：:Synthesis of [(11)C]celecoxib, a selective COX-2 inhibitor, and [(11)C]SC-62807, a major metabolite of celecoxib, were achieved and the potential of these PET probes for assessing the function of drug transporter in biliary excretion was evaluated. The synthesis of [(11)C]celecoxib was achieved in one-pot by reacting ...

journal_title：Bioorganic & medicinal chemistry

authors： Takashima-Hirano M,Takashima T,Katayama Y,Wada Y,Sugiyama Y,Watanabe Y,Doi H,Suzuki M

更新日期：2011-05-01 00:00:00

abstract：:An iduronic acid-containing trisaccharide, methyl-O-(4-O-methyl-2,3,6-tri-O-sulfo-alpha-D-glucopyranosyl-(1-->4)-O- (2-O-sulfo-alpha-L-idopyranosyluronic acid)-(1-->4)-O-2,6-di-O-sulfo-alpha-D-glucopyranoside, related to antithrombotic heparin fragments has been subjected to a combined NMR and molecular modeling inves...

journal_title：Bioorganic & medicinal chemistry

authors： Cros S,Petitou M,Sizun P,Pérez S,Imberty A

更新日期：1997-07-01 00:00:00

abstract：:A series of novel 9(10H)-acridinone derivatives with terminal amino substituents at C2 position on the acridinone ring were synthesized and studied for their antiproliferative activity and underlying mechanisms. These compounds demonstrated promising cytotoxicity to leukemia cells CCRF-CEM, displaying IC(50) values in...

journal_title：Bioorganic & medicinal chemistry

authors： Gao C,Liu F,Luan X,Tan C,Liu H,Xie Y,Jin Y,Jiang Y

更新日期：2010-11-01 00:00:00

abstract：:3-Amino-2-hydroxy-propionaldehydes [H2NCH(R)CHOHCHO with R = H, i-Bu, CH2Ph] were designed as metallo-aminopeptidase inhibitors based on the metal active site chelation concept. These compounds were found to be micromolar inhibitors of aminopeptidase-M (AP-M, EC 3.4.11.2) with potencies similar to bestatin (Ki = 3.5 m...

journal_title：Bioorganic & medicinal chemistry

authors： Tarnus C,Rémy JM,d'Orchymont H

更新日期：1996-08-01 00:00:00

abstract：:A series of hydroxycarbazole derivatives were synthesized and evaluated for PPAR alpha/gamma dual agonist as well as antioxidant activities. While most compounds showed good antioxidant activity, some compounds were identified as potential PPAR alpha/gamma dual agonists as well. Compounds 10a and 16 were found to be a...

journal_title：Bioorganic & medicinal chemistry

authors： Kumar R,Ramachandran U,Srinivasan K,Ramarao P,Raichur S,Chakrabarti R

更新日期：2005-07-01 00:00:00