Hydroxy- or methoxy-substituted benzaldoximes and benzaldehyde-O-alkyloximes as tyrosinase inhibitors.

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：:A series of substituted-isoxazole derivatives was prepared as candidate farnesoid X receptor (FXR) antagonists, based on our previously proposed ligand superfamily concept. Structure-activity relationship studies indicated that the shape and the structural bulkiness of the substituent at the 5-position of the isoxazol...

journal_title：Bioorganic & medicinal chemistry

authors： Kainuma M,Makishima M,Hashimoto Y,Miyachi H

更新日期：2007-04-01 00:00:00

abstract：:A new series of 11-keto-β-boswellic acid and 3-O-acetyl-11-keto-β-boswellic acid analogs (5, 7, 8, 10, 13, 18a-d, 27a-c, 28a-d) were synthesized by modification of hydroxyl and acid functional moieties of boswellic acids. The structures of these analogs were confirmed by spectral data analysis (1H, 13C NMR and mass). ...

journal_title：Bioorganic & medicinal chemistry

authors： Meka B,Ravada SR,Murali Krishna Kumar M,Purna Nagasree K,Golakoti T

更新日期：2017-02-15 00:00:00

abstract：:Aryl diketoacids (ADK) and their bioisosteres are among the most promising HIV-1 integrase (IN) inhibitors. Previously, we designed a series of ADK dimers as a new class of IN inhibitors that were hypothesized to target two divalent metal ions on the active site of IN. Herein we present a further structure-activity re...

journal_title：Bioorganic & medicinal chemistry

authors： Zeng LF,Jiang XH,Sanchez T,Zhang HS,Dayam R,Neamati N,Long YQ

更新日期：2008-08-15 00:00:00

abstract：:With the continuing interest in deciphering the interplay between protein function and conformational changes, small fluorescence probes will be especially useful for tracking changes in the crowded protein interior space. Presently, we describe the potential utility of six unnatural amino acid fluorescence donors str...

journal_title：Bioorganic & medicinal chemistry

authors： Talukder P,Chen S,Liu CT,Baldwin EA,Benkovic SJ,Hecht SM

更新日期：2014-11-01 00:00:00

abstract：:New 7-aryl or 7-heteroarylamino-2,3-dimethylbenzo[b]thiophenes were prepared by palladium-catalyzed Buchwald-Hartwig cross-coupling of 7-bromo or 7-amino-2,3-dimethylbenzo[b]thiophenes, previously prepared by us, with substituted (4-methoxy or 3,4-dimethoxy) anilines and 3-aminopyridine or with substituted (3-methoxy ...

journal_title：Bioorganic & medicinal chemistry

authors： Queiroz MJ,Ferreira IC,Calhelha RC,Estevinho LM

更新日期：2007-02-15 00:00:00

abstract：:Seven new nitrogen heterocycle porphyrins, 5,10,15,20-tetra[4-(N-pyrrolidinyl)phenyl]porphine (TBPPH(2)), 5,10,15,20-tetra[4-(4'-ethylpiperazinyl)phenyl]porphine (TEPPH(2)), 5,10,15,20-tetra [4-(4'-butylpiperazinyl)phenyl]porphine (TUPPH(2)), 5,10,15,20-tetra[4-(4'-heptylpiperazinyl) phenyl]porphine (THPPH(2)), 5-[4-(...

journal_title：Bioorganic & medicinal chemistry

authors： Guo CC,Li HP,Zhang XB

更新日期：2003-04-17 00:00:00

abstract：:A series of novel 1-methyl-3-substituted quinazoline-2,4-dione derivatives were designed, synthesized, and characterized by (1)H NMR, (13)C NMR and MS spectral data. Their inhibition against chitin synthase (CHS) and antifungal activities were evaluated in vitro. Results showed compounds 5b, 5c, 5e, 5f, 5j, 5k, 5l, an...

journal_title：Bioorganic & medicinal chemistry

authors： Ji Q,Yang D,Wang X,Chen C,Deng Q,Ge Z,Yuan L,Yang X,Liao F

更新日期：2014-07-01 00:00:00

abstract：:Paraoxonase1 (PON1) is a HDL bound enzyme and many of the anti-atherogenic properties of HDL are attributed to PON1. The enzyme precise mechanism of protective action and its endogenous substrate remain elusive. PON1 hydrolyzes organophosphates, arylesters and lactones, whereas the lactones activity is assumed as the ...

journal_title：Bioorganic & medicinal chemistry

authors： Tavori H,Khatib S,Aviram M,Vaya J

更新日期：2008-08-01 00:00:00

abstract：:Four palladium(II) and platinum(II) saccharinate (sac) complexes with 2-(hydroxymethyl)pyridine (2-hmpy) and 2-(2-hydroxyethyl)pyridine (2-hepy), namely trans-[Pd(2-hmpy)2(sac)2]·H2O (1), trans-[Pt(2-hmpy)2(sac)2]·3H2O (2), trans-[Pd(2-hepy)2(sac)2] (3) and trans-[Pt(2-hepy)2(sac)2] (4), have been synthesized and char...

journal_title：Bioorganic & medicinal chemistry

authors： Ari F,Aztopal N,Icsel C,Yilmaz VT,Guney E,Buyukgungor O,Ulukaya E

更新日期：2013-11-01 00:00:00

abstract：:Synthetic modification of cyclosporin A at P3-P4 positions led to the discovery of NIM258, a next generation cyclophilin inhibitor with excellent anti-hepatitis C virus potency, with decreased transporter inhibition, and pharmacokinetics suitable for coadministration with other drugs. Herein is disclosed the evolution...

journal_title：Bioorganic & medicinal chemistry

authors： Fu J,Becker C,Cao L,Capparelli M,Denay R,Fujimoto R,Gai Y,Gao Z,Guenat C,Karur S,Kim H,Li W,Li X,Li W,Lochmann T,Lu A,Lu P,Luneau A,Meier N,Mergo W,Ng S,Parker D,Peng Y,Riss B,Rivkin A,Roggo S,Schroede

更新日期：2018-02-15 00:00:00

abstract：:A new meso-2,4,6-trimethoxyphenyl porphyrin covalently linked to a 2',6'-dinitro-4'-trifluoromethylphenyl group by an amine bond 5 and its metal complex with Cd(II) 6 was prepared. The photodynamic activities of 5 and 6 were evaluated in vitro on Hep-2 cells. A considerable increase in the photocytotoxic effect was fo...

journal_title：Bioorganic & medicinal chemistry

authors： Milanesio ME,Morán FS,Yslas EI,Alvarez MG,Rivarola V,Durantini EN

更新日期：2001-08-01 00:00:00

abstract：:Structural features and hydrogen-bond interactions of dinotefuran (DIN), imidacoloprid (IMI) and acetamiprid (ACE) have been investigated experimentally through analyses of new crystal structures and observations in structural databases, as well as by Density Functional Theory quantum chemical calculations. Several co...

journal_title：Bioorganic & medicinal chemistry

authors： Le Questel JY,Graton J,Cerón-Carrasco JP,Jacquemin D,Planchat A,Thany SH

更新日期：2011-12-15 00:00:00

abstract：:The synthesis and in vitro vasodilating properties of hybrid compounds in which furoxan (1,2,5-oxadiazole 2-oxide) moieties, endowed with different NO-donor properties, were substituted for the nitroxy function of Nicorandil are reported. The corresponding cyanoguanidine analogues are also considered. This approach ha...

journal_title：Bioorganic & medicinal chemistry

authors： Boschi D,Cena C,Di Stilo A,Fruttero R,Gasco A

更新日期：2000-07-01 00:00:00

abstract：:A series of acridine derivatives were synthesised and their in vitro antimalarial activity was evaluated against one chloroquine-susceptible strain (3D7) and three chloroquine-resistant strains (W2, Bre1 and FCR3) of Plasmodium falciparum. Structure-activity relationship showed that two positives charges as well as 6-...

journal_title：Bioorganic & medicinal chemistry

authors： Guetzoyan L,Yu XM,Ramiandrasoa F,Pethe S,Rogier C,Pradines B,Cresteil T,Perrée-Fauvet M,Mahy JP

更新日期：2009-12-01 00:00:00

abstract：:Verticipyrone has recently been isolated from the culture broth of Verticillium sp. and shown to inhibit NADH fumarate reductase, as well as NADH oxidoreductase (complex I) of the mitochondrial electron transport chain. In order to assess the structural elements in verticipyrone essential for complex I inhibitor, 15 s...

journal_title：Bioorganic & medicinal chemistry

authors： Leiris SJ,Khdour OM,Segerman ZJ,Tsosie KS,Chapuis JC,Hecht SM

更新日期：2010-05-15 00:00:00

abstract：:A labeling probe containing a pyrenecarboxamide-tethered modified DNA base, (Py)U, has been developed for fluorometric detection of RNA poly(A) tracts, in which the fluorescence emission intensity was controlled by the microstructural change around (Py)U caused by binding with the target RNA. ...

journal_title：Bioorganic & medicinal chemistry

authors： Tanaka K,Okamoto A

更新日期：2008-01-01 00:00:00

abstract：:The activity-structure relationships (ASR) of phenolic compounds as hydroxyl-radical scavengers have mostly been studied and discussed with regard to their iron-chelating and hydrogen-donation properties in Fenton-type system, but extensive elucidation of multiple mechanisms underlying the hydroxyl radical scavenging ...

journal_title：Bioorganic & medicinal chemistry

authors： Cheng Z,Ren J,Li Y,Chang W,Chen Z

更新日期：2002-12-01 00:00:00

abstract：:The scorpion toxin AmmTx3 is a specific blocker of Kv4 channels. It was shown to have interesting potential for neurological disorders. In this study, we report the first chemical synthesis of AmmTx3 by using the native chemical ligation strategy and validate its biological activity. We determined its 3D structure by ...

journal_title：Bioorganic & medicinal chemistry

authors： Zoukimian C,Meudal H,De Waard S,Ouares KA,Nicolas S,Canepari M,Béroud R,Landon C,De Waard M,Boturyn D

更新日期：2019-01-01 00:00:00

abstract：:6-N-(Benzothiazol-2-yl)deoxyadenosine (A(BT)) was synthesized and incorporated into DNAs. Although, the multipoint benzothiazole (BT) modification of oligodeoxynucleotides reduced the stability of duplexes with their complementary strands, it induced the strong exciton coupling between BT moieties. The circular dichro...

journal_title：Bioorganic & medicinal chemistry

authors： Masaki Y,Ohkubo A,Seio K,Sekine M

更新日期：2010-01-15 00:00:00

abstract：:Mainly driven by the needs of antisense research, a large number of oligonucleotide analogues have been prepared and evaluated over the last 15 years. Besides minor structural modifications of the building blocks of DNA and RNA itself, a considerable effort has been devoted to the de novo design of nucleoside analogue...

journal_title：Bioorganic & medicinal chemistry

authors： Leumann CJ

更新日期：2002-04-01 00:00:00

abstract：:A new series of 5-glycylamino-2-substituted-phenyl-1,3-dioxacycloalkanes were designed and synthesized. The anti-inflammatory activities of these compounds were tested using the xylene-induced mouse ear edema model. Sixteen of these new compounds exhibited comparable or better anti-inflammatory activities than aspirin...

journal_title：Bioorganic & medicinal chemistry

authors： Bi L,Zhao M,Gu K,Wang C,Ju J,Peng S

更新日期：2008-02-15 00:00:00

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

authors： Schoonover M,Kerwin SM

更新日期：2012-12-15 00:00:00

abstract：:Indole beta-cyclodextrin (beta-1) was found to be able to prevent aggregation of citrate synthase (CS) on heating condition. As a result, beta-1 showed anti-CS aggregation in this system by regulating in early stage. The depression mechanism of beta-1 for aggregation of CS is as follows: the beta-1 formed a complex wi...

journal_title：Bioorganic & medicinal chemistry

authors： Toda M,Itoh H,Kondo Y,Hamada F

更新日期：2007-03-01 00:00:00

abstract：:In the light of known HDAC inhibitors, 33 carboxylic acid derivatives were tested to understand the structural requirements for HDAC inhibition activity. Several modifications were applied to develop the structure-activity relationships of carboxylic acid HDAC inhibitors. HDAC inhibition activities were investigated i...

journal_title：Bioorganic & medicinal chemistry

authors： Bora-Tatar G,Dayangaç-Erden D,Demir AS,Dalkara S,Yelekçi K,Erdem-Yurter H

更新日期：2009-07-15 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：:We described the synthesis of a new congener series of 1,2,3-triazolyl-4-oxoquinolines and evaluated their ability to inhibit oseltamivir (OST)-resistant influenza strains. Oxoquinoline derivative 1i was the most potent compound within this series, inhibiting 94% of wild-type (WT) influenza neuraminidase (NA) activity...

journal_title：Bioorganic & medicinal chemistry

authors： Boechat Fda C,Sacramento CQ,Cunha AC,Sagrillo FS,Nogueira CM,Fintelman-Rodrigues N,Santos-Filho O,Riscado CS,Forezi Lda S,Faro LV,Brozeguini L,Marques IP,Ferreira VF,Souza TM,de Souza MC

更新日期：2015-12-15 00:00:00

abstract：:We isolated the 4 kinds of flavonoids from strawberry 'Nohime' and examined the effect of these flavonoids on the degranulation in RBL-2H3 cells. The flavonoids were found to suppress the degranulation from Ag-stimulated RBL-2H3 cells to different extents. To disclose the inhibitory mechanism of degranulation by flavo...

journal_title：Bioorganic & medicinal chemistry

authors： Itoh T,Ninomiya M,Yasuda M,Koshikawa K,Deyashiki Y,Nozawa Y,Akao Y,Koketsu M

更新日期：2009-08-01 00:00:00

abstract：:The outcomes of breast cancer patients are still poor although new compounds have recently been introduced into the clinic. Therefore, novel chemical approaches are required. In the present study, palladium(II) and corresponding platinum(II) complexes containing bis(2-pyridylmethyl)amine (bpma) and saccharine were syn...

journal_title：Bioorganic & medicinal chemistry

authors： Ari F,Ulukaya E,Sarimahmut M,Yilmaz VT

更新日期：2013-06-01 00:00:00

abstract：:Combinatorial biocatalysis, based on a principle of the combinatorial use of biosynthetic steps rather than the combinatorial use of reagents, offers a complementary approach to combinatorial chemistry, which, used individually or in connection with synthetic organic transformations, provides access to analogues not r...

journal_title：Bioorganic & medicinal chemistry

authors： Krstenansky JL,Khmelnitsky Y

更新日期：1999-10-01 00:00:00