Identification of an achiral analogue of J-113397 as potent nociceptin/orphanin FQ receptor antagonist.

abstract：:Two of the histone deacetylases, TbDAC1 and TbDAC3, have been reported to be essential genes in trypanosomes. Therefore, we tested the activity of a panel of human histone deacetylase inhibitors (HDACi) for their ability to block proliferation of Trypanosoma brucei brucei. Among the HDACi's, the hydroxamic acid deriva...

journal_title：Bioorganic & medicinal chemistry

authors： Carrillo AK,Guiguemde WA,Guy RK

更新日期：2015-08-15 00:00:00

abstract：:A sensitive chemiluminescence (CL) sensor for berberine combined with flow-injection (FI) technology is described. The analytical reagents involved in the CL reaction, including luminol and potassium ferricyanide, were both immobilized on an anion-exchange resin column. While a volume of sodium phosphate was passed th...

journal_title：Bioorganic & medicinal chemistry

authors： Song Z,Zhao T,Wang L,Xiao Z

更新日期：2001-07-01 00:00:00

abstract：:Cytochrome P450 (CYP) 1B1 catalyzes 17beta-estradiol (E(2)) to predominantly carcinogenic 4-hydroxy-E(2), whereas CYP1A1 and 1A2 convert E(2) to non-carcinogenic 2-hydroxy-E(2). Hence, selective inhibition of CYP1B1 is recognized to be beneficial for the prevention of E(2) related breast cancer. In this study, we firs...

journal_title：Bioorganic & medicinal chemistry

authors： Takemura H,Itoh T,Yamamoto K,Sakakibara H,Shimoi K

更新日期：2010-09-01 00:00:00

abstract：:Dipeptidyl peptidase IV (DPP-IV) inhibitors are promising antidiabetic drugs, and several drugs are in the developmental stage. We previously reported that the introduction of fluorine to the 4-position of 2-cyanopyrrolidine enhanced the DPP-IV inhibitory effect. In the present report, we examined the structure-activi...

journal_title：Bioorganic & medicinal chemistry

authors： Fukushima H,Hiratate A,Takahashi M,Mikami A,Saito-Hori M,Munetomo E,Kitano K,Chonan S,Saito H,Suzuki A,Takaoka Y,Yamamoto K

更新日期：2008-04-01 00:00:00

abstract：:Two hybrid analogues of the kainic acid receptor agonists, 2-amino-3-(5-tert-butyl-3-hydroxy-4-isoxazolyl)propionic acid (ATPA) and (2S,4R)-4-methylglutamic acid ((2S,4R)-4-Me-Glu), were designed, synthesized, and characterized in radioligand binding assays using cloned ionotropic and metabotropic glutamic acid recept...

journal_title：Bioorganic & medicinal chemistry

authors： Bunch L,Johansen TH,Bräuner-Osborne H,Stensbøl TB,Johansen TN,Krogsgaard-Larsen P,Madsen U

更新日期：2001-04-01 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：:CNS diseases such as Parkinson, schizophrenia, and attention deficit hyperactivity disorder (ADHD) are characterized by a significant alteration of dopamine transporter (DAT) density. Thus, the development of compounds that are able to selectively interact with DAT is of great interest. Herein we describe the design a...

journal_title：Bioorganic & medicinal chemistry

authors： Cini N,Danieli E,Menchi G,Trabocchi A,Bottoncetti A,Raspanti S,Pupi A,Guarna A

更新日期：2006-08-01 00:00:00

abstract：:The synthesis of a new minimum steric perturbing proxyl nitroxide, which is a derivative of glycerol and contains a stearic acid moiety, has been carried out. Its localization in model membrane L-alpha-dipalmitoyl phosphatidyl choline (DPPC) was ascertained with the help of ESR, DSC, 1H and 31P NMR techniques. The nit...

journal_title：Bioorganic & medicinal chemistry

authors： Katoch R,Trivedi GK,Phadke RS

更新日期：1999-12-01 00:00:00

abstract：:Synthesis and antimicrobial activity of squalamine analogue 2 are reported. The synthesis of 2 was accomplished from bisnoralcohol 3. The spermidine moiety was introduced via reductive amination of an appropriately functionalized 3beta-aminosterol with spermidinyl aldehyde 17 utilizing sodium triacetoxyborohydride as ...

journal_title：Bioorganic & medicinal chemistry

authors： Kim HS,Choi BS,Kwon KC,Lee SO,Kwak HJ,Lee CH

更新日期：2000-08-01 00:00:00

abstract：:A class of 5-trifluoroacetylamino-1,3-dioxacycloalkanes, 5-benzoylamino-1,3-dioxacycloalkanes, and 5-amino-1,3-dioxacycloalkane compounds were stereoselectively synthesized as potential anti-inflammatory drug candidates. The anti-inflammatory activities of these compounds were tested using the xylene-induced mouse ear...

journal_title：Bioorganic & medicinal chemistry

authors： Gu K,Bi L,Zhao M,Wang C,Dolan C,Kao MC,Tok JB,Peng S

更新日期：2006-03-01 00:00:00

abstract：:Four stereoisomers of roseoside (vomifoliol glucosides) were synthesized using glucose as a chiral resolving reagent. The four synthetic stereoisomers exhibited inhibitory activity on leukotriene release from mouse bone marrow-derived cultured mast cells (BMCMC). The (6S)-isomers of roseoside were about twice as activ...

journal_title：Bioorganic & medicinal chemistry

authors： Yajima A,Oono Y,Nakagawa R,Nukada T,Yabuta G

更新日期：2009-01-01 00:00:00

abstract：:The malarial parasite Plasmodium falciparum encodes for an alpha-carbonic anhydrase (CA) enzyme possessing catalytic properties distinct of that of the human host, which was only recently purified. A series of aromatic sulfonamides, most of which were Schiff's bases derived from sulfanilamide/homosulfanilamide/4-amino...

journal_title：Bioorganic & medicinal chemistry

authors： Krungkrai J,Scozzafava A,Reungprapavut S,Krungkrai SR,Rattanajak R,Kamchonwongpaisan S,Supuran CT

更新日期：2005-01-17 00:00:00

abstract：:In this work, we further investigated a previously introduced class of cholinesterase inhibitors. The removal of the carbamic function from the lead compound xanthostigmine led to a reversible cholinesterase inhibitors 3. Some new 3-[omega-(benzylmethylamino)alkoxy]xanthen-9-one analogs were designed, synthesized, and...

journal_title：Bioorganic & medicinal chemistry

authors： Piazzi L,Belluti F,Bisi A,Gobbi S,Rizzo S,Bartolini M,Andrisano V,Recanatini M,Rampa A

更新日期：2007-01-01 00:00:00

abstract：:We have recently reported the discovery of numerous new compounds that are selective inhibitors of all of the subtypes of the adenosine receptor family via a pharmacophore database searching and screening strategy. During the course of this work we made the unexpected discovery of a potent A(2B) receptor antagonist, 4...

journal_title：Bioorganic & medicinal chemistry

authors： Webb TR,Lvovskiy D,Kim SA,Ji Xd,Melman N,Linden J,Jacobson KA

更新日期：2003-01-02 00:00:00

abstract：:A series of new isoxazolyl, triazolyl and phenyl based 3-thiophen-2-yl-quinoline derivatives were synthesized adopting click chemistry approach. In addition, the synthesis of new useful synthon, (2-chloroquinolin-3-yl) (thiophen-2-yl) methanol, is reported. The obtained compounds were characterized by spectral data an...

journal_title：Bioorganic & medicinal chemistry

authors： Othman DIA,Selim KB,El-Sayed MA,Tantawy AS,Amen Y,Shimizu K,Okauchi T,Kitamura M

更新日期：2019-10-01 00:00:00

abstract：:The phosphate, uracil, and ribose moieties of uracil nucleotides were varied structurally for evaluation of agonist activity at the human P2Y(2), P2Y(4), and P2Y(6) receptors. The 2-thio modification, found previously to enhance P2Y(2) receptor potency, could be combined with other favorable modifications to produce n...

journal_title：Bioorganic & medicinal chemistry

authors： Ko H,Carter RL,Cosyn L,Petrelli R,de Castro S,Besada P,Zhou Y,Cappellacci L,Franchetti P,Grifantini M,Van Calenbergh S,Harden TK,Jacobson KA

更新日期：2008-06-15 00:00:00

abstract：:A series of ethyl 6-bromo-5-hydroxy-1H-indole-3-carboxylates, 8a-11v, were synthesized and evaluated for their anti-hepatitis B virus (HBV) activities in 2.2.15 cells. The selective indexes of inhibition on replication of HBV DNA of compounds 11s (>8.7) and 11t (10.8), which were introduced halogen on the phenyl ring ...

journal_title：Bioorganic & medicinal chemistry

authors： Chai H,Zhao Y,Zhao C,Gong P

更新日期：2006-02-15 00:00:00

abstract：:The synthesis of docetaxel esters of malic acid is described. These compounds were found to have greatly improved water solubility and are stable in solution at neutral pH. The C2' modified compounds 2a-c and 3a-c behave as prodrugs, that is, docetaxel is generated upon exposure to human plasma, whereas the C7 and C2'...

journal_title：Bioorganic & medicinal chemistry

authors： Du W,Hong L,Yao T,Yang X,He Q,Yang B,Hu Y

更新日期：2007-09-15 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：:5-Bromouracil ((Br)U) was incorporated into three types of synthetic RNA and the products of the photoirradiated (Br)U-containing RNAs were investigated using HPLC and MS analysis. The photoirradiation of r(GCA(Br)UGC)(2) and r(CGAA(Br)UUGC)/r(GCAAUUCG) in A-form RNA produced the corresponding 2'-keto adenosine ((keto...

journal_title：Bioorganic & medicinal chemistry

authors： Morinaga H,Kizaki S,Takenaka T,Kanesato S,Sannohe Y,Tashiro R,Sugiyama H

更新日期：2013-01-15 00:00:00

abstract：:The cellular penetration (CP) activity of functional molecules has attracted significant attention as one of the most promising new approaches for drug delivery. In particular, cell-penetrating peptides (CPPs) have been studied extensively in cellular engineering. Because there have been few large-scale systematic stu...

journal_title：Bioorganic & medicinal chemistry

authors： Usui K,Kikuchi T,Mie M,Kobatake E,Mihara H

更新日期：2013-05-01 00:00:00

abstract：:Analogues of mitoQ and idebenone were synthesized to define the structural elements that support oxygen consumption in the mitochondrial respiratory chain. Eight analogues were prepared and fully characterized, then evaluated for their ability to support oxygen consumption in the mitochondrial respiratory chain. While...

journal_title：Bioorganic & medicinal chemistry

authors： Duveau DY,Arce PM,Schoenfeld RA,Raghav N,Cortopassi GA,Hecht SM

更新日期：2010-09-01 00:00:00

abstract：:Aminosteroid derivatives represent a new family of compounds with promising antiproliferative activity over different cancer cell lines. Among all the aminosteroid derivatives synthesised in our laboratory, we have identified E-37P as one of the more potent when tested in vitro. Unfortunately, the pharmacokinetic prop...

journal_title：Bioorganic & medicinal chemistry

authors： Ayan D,Maltais R,Hospital A,Poirier D

更新日期：2014-11-01 00:00:00

abstract：:Tyrosinase inhibitors are important agents for cosmetic products. We examined here the inhibitory effects of three isomers of thujaplicins (α, β and γ) on mushroom tyrosinase and analyzed their binding modes using a homology model from the crystal structure of Streptomyces castaneoglobisporus tyrosinase (PDB ID: 1wx2)...

journal_title：Bioorganic & medicinal chemistry

authors： Takahashi S,Kamiya T,Saeki K,Nezu T,Takeuchi S,Takasawa R,Sunaga S,Yoshimori A,Ebizuka S,Abe T,Tanuma S

更新日期：2010-11-15 00:00:00

abstract：:Large series of O-alkyl derivatives (methyl and benzyl) of silybin and 2,3-dehydrosilybin was prepared. Selective alkylation of the silybin molecule was systematically investigated. For the first time we present here, for example, preparation of 19-nor-2,3-dehydrosilybin. All prepared silybin/2,3-dehydrosilybin deriva...

journal_title：Bioorganic & medicinal chemistry

authors： Dzubák P,Hajdúch M,Gazák R,Svobodová A,Psotová J,Walterová D,Sedmera P,Kren V

更新日期：2006-06-01 00:00:00

abstract：:A series of 40 7-(O-substituted)-2-morpholino-8-aryl-4H-benzo[e][1,3]oxazin-4-one derivatives was synthesized. They were prepared via synthesis of a key precursor, 8-bromo-7-hydroxy-2-morpholino-4H-benzo[e][1,3]oxazin-4-one 13 which was amenable to ether synthesis at the 7-position and Suzuki coupling at the 8-positio...

journal_title：Bioorganic & medicinal chemistry

authors： Saifuzzaman M,Morrison R,Zheng Z,Orive S,Hamilton J,Thompson PE,Al-Rawi JMA

更新日期：2017-10-15 00:00:00

abstract：:The purpose of this study was to synthesize two new positron emission tomography (PET) probes, N-(4-(2-(1,2,3,4-tetrahydro-6,7-dimethoxy-2-isoquinolinyl)ethyl)phenyl)-9,10-dihydro-5-[¹⁸F]fluoroethoxy-9-oxo-4-acridine carboxamide ([¹⁸F]3) and quinoline-3-carboxylic acid [2-(4-{2-[7-(2-[¹⁸F]fluoroethoxy)-6-methoxy-3,4-d...

journal_title：Bioorganic & medicinal chemistry

authors： Kawamura K,Yamasaki T,Konno F,Yui J,Hatori A,Yanamoto K,Wakizaka H,Ogawa M,Yoshida Y,Nengaki N,Fukumura T,Zhang MR

更新日期：2011-01-15 00:00:00

abstract：:Triterpene sapogenins are a group of biologically active compounds with antibacterial activity. However, the limited solubility and poor bioavailability of triterpene sapogenins restrict their therapeutic application. Polyarginine peptides are small cationic peptides with high affinities for multiple negatively charge...

journal_title：Bioorganic & medicinal chemistry

authors： Na H,Li X,Zou C,Wang C,Wang C,Liu K

更新日期：2016-07-01 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：:Peroxynitrite, a reactive nitrogen species generated from nitric oxide and superoxide anion radical, is an endogenous potential risk factor for human cancer. When 2'-deoxycytidine was incubated with peroxynitrite at neutral pH and 37 degrees C, the reaction was greatly enhanced by the addition of ammonium bromide. Bot...

journal_title：Bioorganic & medicinal chemistry

authors： Suzuki T,Ida K,Uchibe S,Inukai M

更新日期：2008-05-01 00:00:00