abstract：:It was determined, with a systematic mode, the carbonyl group frequency in the region of the infrared of N-[(dimethylamine)methyl] benzamides 4-substituted (set A) and their hydrochlorides (set B), that had its local anesthetical activity evaluated. The application of the Hammett equation considering the values of the...

journal_title：Bioorganic & medicinal chemistry

authors： Tavares LC,do Amaral AT

更新日期：2004-03-15 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：:Equol is a metabolite produced in vivo from the soy phytoestrogen daidzein by the action of gut microflora. It is known to be estrogenic, so human exposure to equol could have significant biological effects. Equol is a chiral molecule that can exist as the enantiomers R-equol and S-equol. To study the biological activ...

journal_title：Bioorganic & medicinal chemistry

authors： Muthyala RS,Ju YH,Sheng S,Williams LD,Doerge DR,Katzenellenbogen BS,Helferich WG,Katzenellenbogen JA

更新日期：2004-03-15 00:00:00

abstract：:A series of aryloxypropanolamines (5a-r) of different chalcones (3a-e) were synthesized and evaluated for antihyperglycemic activity in sucrose loaded (SLM) and streptozotocin (STZ) induced diabetic animal models. Among them compounds 5a, g, m, o, p and r showed significant reduction in blood glucose levels in both SL...

journal_title：Bioorganic & medicinal chemistry

authors： Satyanarayana M,Tiwari P,Tripathi BK,Srivastava AK,Pratap R

更新日期：2004-03-01 00:00:00

abstract：:Described here are the syntheses and preliminary biological evaluations of the first two enzymatically activated prodrugs of docetaxel (Taxotere) reported to date. These prodrugs were designed as potential candidates for selective chemotherapy in ADEPT or PMT. They are constituted of a glucuronic acid moiety, a double...

journal_title：Bioorganic & medicinal chemistry

authors： Bouvier E,Thirot S,Schmidt F,Monneret C

更新日期：2004-03-01 00:00:00

abstract：:Local excess of nitric oxide (NO) has been implicated in beta-cell damage, thus, a possible approach to the treatment of autoimmune IDDM is the selective inhibition of inducible nitric oxide synthase (iNOS). A series of variously substituted hexahydropyridazine-1-carbothioamides, -carbothioimidic acid esters and -carb...

journal_title：Bioorganic & medicinal chemistry

authors： Morgenstern O,Wanka H,Röser I,Steveling A,Kuttler B

更新日期：2004-03-01 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 amyloid-like fibril is considered to be a macromolecular self-assemblage with a highly-ordered quaternary structure, in which numerous beta-stranded polypeptide chains align regularly. Therefore, this kind of fibril has the potential to be engineered into proteinaceous materials, although conformational alteration...

journal_title：Bioorganic & medicinal chemistry

authors： Takahashi Y,Mihara H

更新日期：2004-02-15 00:00:00

abstract：:Recent studies have identified 2,3-dimethoxy-8,9-methylenedioxy-11-[(2-dimethylamino)ethyl]-11H-isoquino[4,3-c]cinnolin-12-one (1a) as a novel topoisomerase I-targeting agent with potent cytotoxic activity. The effect of varied substituents at the 11-position of 2,3-dimethoxy-8,9-methylenedioxy-11H-isoquino[4,3-c]cinn...

journal_title：Bioorganic & medicinal chemistry

authors： Ruchelman AL,Singh SK,Ray A,Wu X,Yang JM,Zhou N,Liu A,Liu LF,LaVoie EJ

更新日期：2004-02-15 00:00:00

abstract：:A series of catechol diazo dyes were synthesized and tested as substrates for the enzyme catechol-O-methyltransferase (COMT) with the aim of developing a sensitive HPLC assay method using visible wavelength light detection. A method was developed which allowed for the determination of the two regioisomeric methylated ...

journal_title：Bioorganic & medicinal chemistry

authors： Bailey K,Cowling R,Tan EW,Webb D

更新日期：2004-02-01 00:00:00

abstract：:Naltrexone (1), which is a member of the group of competitive opioid antagonists, shows a strong affinity for mu-receptors and its derivatives have been notable as novel receptor antagonists. In this paper, the preparation of several naltrexone derivatives is described; these were used to investigate the role of the o...

journal_title：Bioorganic & medicinal chemistry

authors： Uwai K,Uchiyama H,Sakurada S,Kabuto C,Takeshita M

更新日期：2004-01-15 00:00:00

abstract：:Three peptide amides, HPRK(Py)(4)HPRK-NH(2) (PyH-12), HPRK(Py)(3)HPRK-NH(2) (PyH-11) and HPRK(Py)(2)HPRK-NH(2) (PyH-10), incorporating two HPRK motifs and various 4-amino-1-methylpyrrole-2-carboxylic acid residues (Py) were synthesized by solid-phase peptide methodology. The binding of these three peptides to a 5'-32P...

journal_title：Bioorganic & medicinal chemistry

authors： Chang JC,Yang CH,Chou PY,Yang WH,Chou IC,Lu CT,Lin PH,Hou RC,Jeng KC,Cheng CC,Sheh L

更新日期：2004-01-02 00:00:00

abstract：:The interactions between 1-benzoyl-4-p-chlorphenyl thiosemicarbazide (BCPT) and bovine serum albumin (BSA) or human serum albumin (HSA) have been studied by fluorescence spectroscopy. By the analysis of fluorescence spectrum and fluorescence intensity, it was showed that BCPT has a strong ability to quench the intrins...

journal_title：Bioorganic & medicinal chemistry

authors： Cui FL,Fan J,Li JP,Hu ZD

更新日期：2004-01-02 00:00:00

abstract：:The permeability of dipeptide derivatives containing tryptophans and indole derivatives through Caco-2 cells was used as an in vitro intestinal absorption model in order to clarify structural factors which influence their intestinal epithelial permeation and metabolism. Most peptide derivatives were hydrolysed not onl...

journal_title：Bioorganic & medicinal chemistry

authors： Ano R,Kimura Y,Urakami M,Shima M,Matsuno R,Ueno T,Akamatsu M

更新日期：2004-01-02 00:00:00

abstract：:Glycosylated beta-amino acids (3-18, 38, 39), obtained by hydrolysis of glycosylated beta-amino esters on reaction with hydroxylamine hydrochloride in presence of DIC/DCC afforded glycosyl beta-amino hydroxamates (19-34, 40, 41) in fair to good yields. Compounds (19-34, 40, 41) were screened against human malarial par...

journal_title：Bioorganic & medicinal chemistry

authors： Mishra RC,Tripathi R,Katiyar D,Tewari N,Singh D,Tripathi RP

更新日期：2003-12-01 00:00:00

abstract：:A novel series of 6-hydroxy-3-morpholinones, in which the functional aldehyde and the hydroxy group of P(2) site form a cyclic hemiacetal, was identified as calpain inhibitors. The placement of isobutyl group at the 2-position of the 3-morpholinone was the most effective modification for inhibiting micro- and m-calpai...

journal_title：Bioorganic & medicinal chemistry

authors： Nakamura M,Miyashita H,Yamaguchi M,Shirasaki Y,Nakamura Y,Inoue J

更新日期：2003-12-01 00:00:00

abstract：:We describe the syntheses, physicochemical properties and biological evaluation of a novel series of complexones containing bis- or biazoles moieties and two iminodiacetic acid units as novel ligands for paramagnetic lanthanides. The complexones were prepared by reaction of the corresponding 1,1'-bishaloethylbi- or bi...

journal_title：Bioorganic & medicinal chemistry

authors： Mayoral EP,García-Amo M,López P,Soriano E,Cerdán S,Ballesteros P

更新日期：2003-12-01 00:00:00

abstract：:The potency of a series of eight compounds structurally related with 4,5,6,7-tetrahydroisoxazolo[5,4-c]pyridin-3-ol (THIP), a potent GABA(A) partial agonist exhibiting GABA(C) rho(1) antagonist effect (K(i)=25 microM), was determined electrophysiologically using homomeric human GABA(C) rho(1) receptors expressed in Xe...

journal_title：Bioorganic & medicinal chemistry

authors： Krehan D,Frølund B,Ebert B,Nielsen B,Krogsgaard-Larsen P,Johnston GA,Chebib M

更新日期：2003-11-17 00:00:00

abstract：:To develop technetium and rhenium-labeled imaging agents for estrogen receptor (ER) positive breast tumors, we have prepared tridentate metal tricarbonyl chelates substituted at the 7alpha- and 17alpha-positions of estradiol. Some of the Re(CO)(3) conjugates have high binding for the ER in vitro. The in vivo biodistri...

journal_title：Bioorganic & medicinal chemistry

authors： Luyt LG,Bigott HM,Welch MJ,Katzenellenbogen JA

更新日期：2003-11-17 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：:1,3,5,6-tetrahydroxyxanthone was synthesized. The relationship between protective effect of xanthone on endothelial cells and endogenous nitric oxide synthase inhibitors was investigated. Endothelial cells were treated with ox-LDL (100 microg/mL) for 48 h. Adhesion of monocytes to endothelial cells and release of lact...

journal_title：Bioorganic & medicinal chemistry

authors： Jiang DJ,Hu GY,Jiang JL,Xiang HL,Deng HW,Li YJ

更新日期：2003-11-17 00:00:00

abstract：:Novel 2-phenyl-2,5-dihydropyrazolo[4,3-c]quinolin-3-(3H)-ones (PQs) endowed with high affinity for central benzodiazepine receptor (BzR) were synthesized. In particular, 9-fluoro-2-(2-fluorophenyl)-2,5-dihydro-3H-pyrazolo[4,3-c]quinolin-3-one (2(2)) showed binding affinity in the subnanomolar concentration range and p...

journal_title：Bioorganic & medicinal chemistry

authors： Carotti A,Altomare C,Savini L,Chiasserini L,Pellerano C,Mascia MP,Maciocco E,Busonero F,Mameli M,Biggio G,Sanna E

更新日期：2003-11-17 00:00:00

abstract：:A new class of cardiotonic agents characterized by a 2-pyridone structure was synthesized. Appropriate sym-2-dimethylaminomethylene-1,3-diones reacted with methylcyanoacetate to afford the desired compounds. These derivatives were evaluated for their ability in inducing cardiotonic response on guinea pig isolated myoc...

journal_title：Bioorganic & medicinal chemistry

authors： Fossa P,Menozzi G,Dorigo P,Floreani M,Mosti L

更新日期：2003-11-03 00:00:00

abstract：:Members of the Artemisia genus are important medicinal plants found throughout the world. Arteminolides A-D (1-4), isolated from the aerial parts of Artemisia, have an inhibitory activity on farnesyl-protein transferase (FPTase; EC 2.5.1.29) in in vitro assay. This study was carried out with the purpose of validating ...

journal_title：Bioorganic & medicinal chemistry

authors： Lee SH,Lee MY,Kang HM,Han DC,Son KH,Yang DC,Sung ND,Lee CW,Kim HM,Kwon BM

更新日期：2003-10-15 00:00:00

abstract：:Bovine plasma amine oxidase (BPAO) was previously shown to be irreversibly inhibited by propargylamine and 2-chloroallylamine. 1,4-Diamine versions of these two compounds are here shown to be highly potent inactivators, with IC50 values near 20 microM. Mono-N-alkylation or N,N-dialkylation greatly lowered the inactiva...

journal_title：Bioorganic & medicinal chemistry

authors： Jeon HB,Lee Y,Qiao C,Huang H,Sayre LM

更新日期：2003-10-15 00:00:00

abstract：:2-Amino-3-[3-hydroxy-5-(2-thiazolyl)-4-isoxazolyl]propionic acid (1) is a potent AMPA receptor agonist with moderate affinity for native kainic acid (KA) receptors, whereas (S)-E-4-(2,2-dimethylpropylidene)glutamic acid (3) show high affinity for the GluR5 subtype of KA receptors and much lower affinity for the GluR2 ...

journal_title：Bioorganic & medicinal chemistry

authors： Valgeirsson J,Christensen JK,Kristensen AS,Pickering DS,Nielsen B,Fischer CH,Bräuner-Osborne H,Nielsen EØ,Krogsgaard-Larsen P,Madsen U

更新日期：2003-10-01 00:00:00

abstract：:It was shown that a new taxane analogue 3, which exhibited both in vitro antitumor activity and in vivo efficacy by both i.v. and p.o. administration, was prone to be metabolized by human liver microsomes. We identified a major metabolite, M-1, generated by human liver microsomes as 20a, a hydroxylated compound at the...

journal_title：Bioorganic & medicinal chemistry

authors： Takeda Y,Uoto K,Chiba J,Horiuchi T,Iwahana M,Atsumi R,Ono C,Terasawa H,Soga T

更新日期：2003-10-01 00:00:00

abstract：:Inhibition of the isoforms of nitric oxide synthase (NOS) has important applications in therapy of several diseases, including cancer. Using 1400 W [N-(3-aminomethylbenzyl)acetamidine], thiocitrulline and N(delta)-(4,5-dihydrothiazol-2-yl)ornithine as lead compounds, series of N-benzyl- and N-phenyl-2-amino-4,5-dihydr...

journal_title：Bioorganic & medicinal chemistry

authors： Goodyer CL,Chinje EC,Jaffar M,Stratford IJ,Threadgill MD

更新日期：2003-09-15 00:00:00

abstract：:A set of new muscarinic antagonists, bridged bicyclic derivatives of 2,2-diphenyl-[1,3]-dioxolan-4-ylmethyl-dimethylamine (1), was synthesized and tested to evaluate their affinity and selectivity for M(1), M(2), M(3) and M(4) receptor subtypes. The conformational constraint of 1 in a bicyclic structure, and the varia...

journal_title：Bioorganic & medicinal chemistry

authors： Piergentili A,Gentili F,Ghelfi F,Marucci G,Pigini M,Quaglia W,Giannella M

更新日期：2003-09-01 00:00:00

abstract：:A set of thirty five molecules of 1,3-diaryl-4,5,6,7-tetrahydro-2H-isoindoles endowed with selective COX-2 inhibitory activity was analyzed using comparative molecular field analysis (CoMFA) and comparative molecular similarity indices analysis (CoMSIA). Besides conventional steric and electrostatic fields, seven addi...

journal_title：Bioorganic & medicinal chemistry

authors： Chakraborti AK,Thilagavathi R

更新日期：2003-09-01 00:00:00

abstract：:During the course of a collaborative screening program, a set of 1-phenyl-4-pyridyl-butadienes was found to exhibit in vitro activity against Eimeria tenella in a cell-based assay. Activity was dependent on the chain length and degree of unsaturation of the linker between the two aryl groups as well as substitution of...

journal_title：Bioorganic & medicinal chemistry

authors： Gage JL,Kirst HA,O'Neil D,David BA,Smith CK 2nd,Naylor SA

更新日期：2003-09-01 00:00:00

abstract：:The syntheses of four glyco-imidazoles, which are pentose-derivatives belonging to the D-series, as well as the syntheses of their L-enantiomers, are reported. Starting from the known linear xylo, lyxo, arabino, and ribo imidazolo-pentoses in both the L- and the D-series, intramolecular Walden inversion led to the cor...

journal_title：Bioorganic & medicinal chemistry

authors： Tschamber T,Gessier F,Dubost E,Newsome J,Tarnus C,Kohler J,Neuburger M,Streith J

更新日期：2003-08-15 00:00:00

abstract：:Three fluoroalkylated derivatives (1-3) of the selective estrogen receptor modulator (SERM), raloxifene, have been synthesized. The key step in the synthesis is the C-C bond formation of benzo[b]thiophene and a substituted phenyl group (ring C) using a Stille reaction. The in vitro binding affinities of the substitute...

journal_title：Bioorganic & medicinal chemistry

authors： Lee KC,Moon BS,Lee JH,Chung KH,Katzenellenbogen JA,Chi DY

更新日期：2003-08-15 00:00:00

abstract：:The quantitative structure-activity relationship of a set of 40 octopaminergic agonists against receptor 2 in cockroach nervous tissue, was analyzed using molecular-field analysis (MFA). MFA on the study set of those compounds evaluated effectively the energy between a probe and a molecular model at a series of points...

journal_title：Bioorganic & medicinal chemistry

authors： Hirashima A,Morimoto M,Kuwano E,Eto M

更新日期：2003-08-15 00:00:00

abstract：:The synthesis and structure-activity relationships of a series of simple biphenyls is described. Optimization of the 4-hydroxy-biphenyl template led to compounds with ERbeta selectivity on the order of 20-70-fold. ...

journal_title：Bioorganic & medicinal chemistry

authors： Edsall RJ Jr,Harris HA,Manas ES,Mewshaw RE

更新日期：2003-08-05 00:00:00

abstract：:An efficient and practical strategy for the synthesis of N-hydroxyethyl-1-deoxy-homonojirimycins 4 and 5 and N-hydroxyethyl-pyrrolidine homoazasugars 6 and 7 with full stereocontrol is being reported. The key step involved is the intermolecular Michael addition of benzylamine to D-glucose derived alpha,beta-unsaturate...

journal_title：Bioorganic & medicinal chemistry

authors： Dhavale DD,Matin MM,Sharma T,Sabharwal SG

更新日期：2003-07-31 00:00:00

abstract：:Xestoquinone isolated from a marine sponge binds to skeletal muscle myosin and inhibits its Ca(2+) ATPase activity. In this study, we first examined xestoquinone and its analogues to assess the relationships between structure and myosin Ca(2+) ATPase inhibitory activity. On the basis of the resultant data, we then des...

journal_title：Bioorganic & medicinal chemistry

authors： Nakamura M,Kakuda T,Oba Y,Ojika M,Nakamura H

更新日期：2003-07-17 00:00:00

abstract：:Based on two lead cytotoxic spongiane diterpenes, a new series of C7-oxygenated derivatives were synthesized and evaluated for their antitumor activity in vitro against the cancer cell lines HeLa and HEp-2. In general, introduction of either hydroxyl or acetoxy groups at C-7 did not improve the resultant cytotoxicity,...

journal_title：Bioorganic & medicinal chemistry

authors： Arnó M,Betancur-Galvis L,González MA,Sierra J,Zaragozá RJ

更新日期：2003-07-17 00:00:00

abstract：:This review addresses key pharmacology and virology issues relevant in discovery and development of CCR5 antagonists as anti-HIV drugs, such as target validation, receptor internalization, allosterism, viral resistance and tropism. Recent progress in the discovery and development of CCR5 antagonists, SAR and clinical ...

journal_title：Bioorganic & medicinal chemistry

authors： Kazmierski W,Bifulco N,Yang H,Boone L,DeAnda F,Watson C,Kenakin T

更新日期：2003-07-03 00:00:00

abstract：:Several cis and trans bis-steroidal 1,2,4,5-tetraoxanes possessing amide terminus were synthesised and evaluated as antimalarials and antiproliferatives. The compounds exhibited submicromolar antimalarial activity against Plasmodium falciparum D6 and W2 strains. The existence of HN-C(O) moiety was found necessary for ...

journal_title：Bioorganic & medicinal chemistry

authors： Opsenica D,Angelovski G,Pocsfalvi G,Juranić Z,Zizak Z,Kyle D,Milhous WK,Solaja BA

更新日期：2003-07-03 00:00:00