2,3-Dihydro-6,7-dichloro-pyrido[2,3-b]pyrazine-8-oxide as selective glycine antagonist with in vivo activity.

abstract：:The synthesis of dihydronaphthofurandione and dihydrofuroquinolinedione derivatives 4-11 was performed through Diels-Alder reactions of dihydrobenzofurandione 1 with several carbodienes and acrolein N,N-dimethylhydrazone. Then, the use of 5-bromobenzofurandione 2 toward 1,3-pentadiene and the 1-azadiene afforded quino...

journal_title：Bioorganic & medicinal chemistry

authors： Tapia RA,Salas C,Morello A,Maya JD,Toro-Labbé A

更新日期：2004-05-01 00:00:00

abstract：:The emergence of multidrug-resistant bacterial and fungal strains poses a threat to human health that requires the design and synthesis of new classes of antimicrobial agents. We evaluated bis(N-amidinohydrazones) and N-(amidino)-N'-aryl-bishydrazones for their antibacterial and antifungal activities against panels of...

journal_title：Bioorganic & medicinal chemistry

authors： Shrestha SK,Kril LM,Green KD,Kwiatkowski S,Sviripa VM,Nickell JR,Dwoskin LP,Watt DS,Garneau-Tsodikova S

更新日期：2017-01-01 00:00:00

abstract：:Novel pyrazolyl-2,4-thiazolidinediones were prepared via the reaction of appropriate pyrazolecarboxaldehydes with 2,4-thiazolidinediones and substituted benzyl-2,4-thiazolidinediones. The resultant compounds were first evaluated for their anti-inflammatory and neuroprotective properties in vitro. The active compounds ...

journal_title：Bioorganic & medicinal chemistry

authors： Youssef AM,White MS,Villanueva EB,El-Ashmawy IM,Klegeris A

更新日期：2010-03-01 00:00:00

abstract：:We report a series of tubulin targeting agents, some of which demonstrate potent antiproliferative activities. These analogs were designed to optimize the antiproliferative activity of 1 by varying the heteroatom substituent at the 4'-position, the basicity of the 4-position amino moiety, and conformational restrictio...

journal_title：Bioorganic & medicinal chemistry

authors： Xiang W,Choudhary S,Hamel E,Mooberry SL,Gangjee A

更新日期：2018-05-15 00:00:00

abstract：:Cannabinoid receptor 2 (CB2) selective agonists and inverse agonists possess significant potential as therapeutic agents for regulating inflammation and immune function. Although CB2 agonists have received the greatest attention, it is emerging that inverse agonists also manifest anti-inflammatory activity. In process...

journal_title：Bioorganic & medicinal chemistry

authors： Presley CS,Mustafa SM,Abidi AH,Moore BM 2nd

更新日期：2015-09-01 00:00:00

abstract：:The emergence of multidrug-resistant bacteria has created an urgent need for antibiotics with a novel mechanism of action. The bacterial cell division protein FtsZ is an attractive target for the development of novel antibiotics. The benzo[c]phenanthridinium sanguinarine and the dibenzo[a,g]quinolizin-7-ium berberine ...

journal_title：Bioorganic & medicinal chemistry

authors： Kelley C,Zhang Y,Parhi A,Kaul M,Pilch DS,LaVoie EJ

更新日期：2012-12-15 00:00:00

abstract：:In this paper, we report the NMR structural study of two quadruplex structures formed by truncations of the human telomeric sequence and containing a modified base, namely d(AprGGGT) and d(TAprGGGT), where Apr indicates 2'-deoxy-8-(propyn-1-yl)adenosines. Both oligonucleotides have been found to form 4-fold symmetric ...

journal_title：Bioorganic & medicinal chemistry

authors： Esposito V,Randazzo A,Galeone A,Varra M,Mayol L

更新日期：2004-03-01 00:00:00

abstract：:The cells of Bacillus stearothermophilus contain an NADH-dependent diacetyl (acetoin) reductase. The enzyme was easily purified to homogeneity, partially characterised, and found to be composed of two subunits with the same molecular weight. In the presence of NADH, it catalyses the stereospecific reduction of diacety...

journal_title：Bioorganic & medicinal chemistry

authors： Giovannini PP,Medici A,Bergamini CM,Rippa M

更新日期：1996-08-01 00:00:00

abstract：:Antagonizing transcriptional activity of farnesoid X receptor (FXR) in the intestine has been reported as an effective means for the treatment of nonalcoholic fatty liver disease, type 2 diabetes and obesity. We describe herein that the building blocks necessary to maintain the antagonism of our chemotype were investi...

journal_title：Bioorganic & medicinal chemistry

authors： Teno N,Yamashita Y,Masuda A,Iguchi Y,Oda K,Fujimori K,Hiramoto T,Nishimaki-Mogami T,Une M,Gohda K

更新日期：2019-06-01 00:00:00

abstract：:A set of 8-methylene-, 8-methyl-, and 8-methyl-9-dihydro-oleandomycin derivatives having different combinations of stereochemistries at positions C-8 and/or C-9 have been prepared in a chemoselective and stereoselective manner and tested in vitro for antibacterial activity and inhibition of IL-6 production. Configurat...

journal_title：Bioorganic & medicinal chemistry

authors： Bauer J,Vine M,Corić I,Bosnar M,Pašalić I,Turkalj G,Lazarevski G,Culić O,Kragol G

更新日期：2012-04-01 00:00:00

abstract：:3,4-Dihydro-2H,6H-pyrimido[1,2-c][1,3]benzothiazin-6-imine (PD 404182) is an antiretroviral agent with submicromolar inhibitory activity against human immunodeficiency virus-1 (HIV-1) and HIV-2 infection. In the current study, the structure-activity relationships of accessory groups at the 3- and 9-positions of pyrimi...

journal_title：Bioorganic & medicinal chemistry

authors： Mizuhara T,Oishi S,Ohno H,Shimura K,Matsuoka M,Fujii N

更新日期：2012-11-01 00:00:00

abstract：:Thymidylate synthase (TS) (EC 2.1.1.45), an enzyme involved in the DNA synthesis of both prokaryotic and eukaryotic cells, is a potential target for the development of anticancer and antinfective agents. Recently, we described a series of phthalein and naphthalein derivatives as TS inhibitors. These compounds have str...

journal_title：Bioorganic & medicinal chemistry

authors： Ghelli S,Rinaldi M,Barlocco D,Gelain A,Pecorari P,Tondi D,Rastelli G,Costi MP

更新日期：2003-03-20 00:00:00

abstract：:This paper describes and illustrates the use of ensemble-based docking, i.e., using a collection of protein structures in docking calculations for hit discovery, the exploration of biochemical pathways and toxicity prediction of drug candidates. We describe the computational engineering work necessary to enable large ...

journal_title：Bioorganic & medicinal chemistry

authors： Evangelista W,Weir RL,Ellingson SR,Harris JB,Kapoor K,Smith JC,Baudry J

更新日期：2016-10-15 00:00:00

abstract：:4-{[2-[(2-Furylsulfonyl)(isobutyl)amino]-5-(trifluoromethyl)phenoxy]methyl}benzoic acid analogs 2a and b and a series of the acid analogs, in which the carboxylic acid residue of 2b was replaced with various kinds of carboxylic acid bioisosteres, were synthesized and evaluated as EP1 receptor antagonists. Compound 2b ...

journal_title：Bioorganic & medicinal chemistry

authors： Naganawa A,Matsui T,Ima M,Saito T,Murota M,Aratani Y,Kijima H,Yamamoto H,Maruyama T,Ohuchida S,Nakai H,Toda M

更新日期：2006-11-01 00:00:00

abstract：:The design and synthesis of novel 14- to 16-membered 11-azalides starting from 16-membered macrolides are reported. A linear 9-formylcarboxylic acid was isolated via a mobile dialdehyde previously reported. Sequential macrocyclization of the formylcarboxylic acid with amino alcohol followed by deprotection afforded co...

journal_title：Bioorganic & medicinal chemistry

authors： Miura T,Kanemoto K,Natsume S,Atsumi K,Fushimi H,Yoshida T,Ajito K

更新日期：2008-12-01 00:00:00

abstract：:On the basis of potent and selective binding affinity of truncated 4'-thioadenosine derivatives at the human A(3) adenosine receptor (AR), their bioisosteric 4'-oxo derivatives were designed and synthesized from commercially available 2,3-O-isopropylidene-D-erythrono lactone. The derivatives tested in AR binding assay...

journal_title：Bioorganic & medicinal chemistry

authors： Pal S,Choi WJ,Choe SA,Heller CL,Gao ZG,Chinn M,Jacobson KA,Hou X,Lee SK,Kim HO,Jeong LS

更新日期：2009-05-15 00:00:00

abstract：:Protein tyrosine phosphatases (PTPs) are important in the regulation of signal transduction processes. Certain enzymes of this class are considered as potential therapeutic targets in the treatment of a variety of diseases such as diabetes, inflammation, and cancer. However, many PTP inhibitors identified to date are ...

journal_title：Bioorganic & medicinal chemistry

authors： Huang P,Ramphal J,Wei J,Liang C,Jallal B,McMahon G,Tang C

更新日期：2003-04-17 00:00:00

abstract：:A series of novel tetrahydropyrazolopyridone derivatives containing 1,3,4-triazole, triazolylmethyl, and partially saturated heterocyclic moieties as P2 binding element was designed, synthesized, and evaluated in vitro for anticoagulant activity in human and rabbit plasma. All compounds showed moderate to significant ...

journal_title：Bioorganic & medicinal chemistry

authors： Sun X,Hong Z,Liu M,Guo S,Yang D,Wang Y,Lan T,Gao L,Qi H,Gong P,Liu Y

更新日期：2017-05-15 00:00:00

abstract：:Carbonic anhydrases (CAs) catalyze the reversible hydration of carbon dioxide to bicarbonate and are abundantly distributed in prokaryotes and eukaryotes. There are five classes (α,β,γ,δ,ζ) with no significant sequence or structural identity among them, a remarkable example of convergent evolution. The β and γ classes...

journal_title：Bioorganic & medicinal chemistry

authors： Ferry JG

更新日期：2013-03-15 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：:Selenium-incorporated fucoses (seleno-fucoses) differing in the position of the seleno-substituent were synthesized and applied to the X-ray structural determination of a carbohydrate-lectin complex using single/multi-wavelength anomalous dispersion (SAD/MAD) phasing. The hydroxyl groups at the C-1, -2, -3 and -4 posi...

journal_title：Bioorganic & medicinal chemistry

authors： Shimabukuro J,Makyio H,Suzuki T,Nishikawa Y,Kawasaki M,Imamura A,Ishida H,Ando H,Kato R,Kiso M

更新日期：2017-02-01 00:00:00

abstract：:Two novel hybrid molecules 3-O-sulfo-alpha/beta-galactosylceramide 3 and 4, which are derived from an immunostimulatory agent alpha-GalCer 1 and self-glycolipid ligand sulfatide 2, were designed and synthesized. Compound 3 was shown to efficiently stimulate human NKT cells to secret IL-4 and IFN-gamma, with activities...

journal_title：Bioorganic & medicinal chemistry

authors： Xing GW,Wu D,Poles MA,Horowitz A,Tsuji M,Ho DD,Wong CH

更新日期：2005-04-15 00:00:00

abstract：:Highly regioselective electrophilic substitution of dibenzofluorene was achieved and the nitro derivative was transformed to a variety of new anticancer agents. ...

journal_title：Bioorganic & medicinal chemistry

authors： Becker FF,Mukhopadhyay C,Hackfeld L,Banik I,Banik BK

更新日期：2000-12-01 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：:Grapefruit juice has been shown to increase the oral bioavailability of several clinically important drugs by inhibiting first pass metabolism. Several compounds in grapefruit juice have shown different biological activities. Unique among them are furocoumarins with potent inhibitory activity against cytochrome P450 e...

journal_title：Bioorganic & medicinal chemistry

authors： Girennavar B,Jayaprakasha GK,Jadegoud Y,Nagana Gowda GA,Patil BS

更新日期：2007-06-01 00:00:00

abstract：:Synthesis of a range of indomethacin analogues, required for investigation in combination toxicity assays, bearing both N-benzyl and N-benzoyl groups, is described. ...

journal_title：Bioorganic & medicinal chemistry

authors： Maguire AR,Plunkett SJ,Papot S,Clynes M,O'Connor R,Touhey S

更新日期：2001-03-01 00:00:00

abstract：:The donor-acceptor interaction between a tertiary amine and an aldehyde, first observed among a select class of alkaloids, was deliberately established in a peptidomimetic (1a-c) to mimic features of the two principal transition states of peptide hydrolysis. Compounds 1a-c show preferential adoption in methanol and wa...

journal_title：Bioorganic & medicinal chemistry

authors： Gautier A,Pitrat D,Hasserodt J

更新日期：2006-06-01 00:00:00

abstract：:A series of fifteen N4-benzyl substituted 5-nitroisatin-3-thiosemicarbazones 5a-o was synthesized and evaluated for urease inhibitory, phytotoxic and cytotoxic influences. All the compounds proved to be highly potent inhibitors of the enzyme, showing inhibitory activity (IC50=0.87±0.25-8.09±0.23μM) much better than th...

journal_title：Bioorganic & medicinal chemistry

authors： Pervez H,Khan N,Zaib S,Yaqub M,Naseer MM,Tahir MN,Iqbal J

更新日期：2017-02-01 00:00:00

abstract：:G protein-coupled receptors (GPCRs) constitute the largest protein superfamily in the human genome. GPCRs play key roles in mediating a wide variety of physiological events including proliferation and cancer metastasis. Given the major roles that GPCRs play in mediating cancer growth, they present promising targets fo...

journal_title：Bioorganic & medicinal chemistry

authors： Paciaroni NG,Norwood VM 4th,Ratnayake R,Luesch H,Huigens RW 3rd

更新日期：2020-07-15 00:00:00

abstract：:Fourteen hybrids of farnesylthiosalicylic acid (FTS) with various diamines were synthesized and biologically evaluated. It was found that FTS-monoamide molecules (10a-g) displayed strong anti-proliferative activity against seven human cancer cell lines, superior to FTS and FTS-bisamide compounds (11a-g). The mono-amid...

journal_title：Bioorganic & medicinal chemistry

authors： Ling Y,Wang Z,Zhu H,Wang X,Zhang W,Wang X,Chen L,Huang Z,Zhang Y

更新日期：2014-01-01 00:00:00