Novel dammarane-type triterpenes isolated from hydrolyzate of total Gynostemma pentaphyllum saponins.

abstract：:A novel, potent, and orally bioavailable class of product-like inhibitors of the HCV NS3 protease was discovered by constraining the P2-P3 amide bond and the P3 hydrocarbon substituent to the protease-bound conformation. This preorganization was accomplished by incorporation of the P2-P3 amide into a six-membered ring...

journal_title：Bioorganic & medicinal chemistry letters

authors： Clarke MO,Byun D,Chen X,Doerffler E,Leavitt SA,Sheng XC,Yang CY,Kim CU

更新日期：2012-01-15 00:00:00

abstract：:Novel dimers of triphenylethylene-coumarin hybrid containing one amino side chain were designed and synthesized by the condensation of four dicarboxylic acids with the amino monomeric hybrids catalyzed by HATU and DIPEA at room temperature. The adding order of the reactants had a significant effect on the condensation...

journal_title：Bioorganic & medicinal chemistry letters

authors： Tan G,Yao Y,Gu Y,Li S,Lv M,Wang K,Chen H,Li X

更新日期：2014-07-01 00:00:00

abstract：:Elevation of glycine levels and activation of the NMDA receptor by inhibition of the glycine transporter 1 (GlyT-1) is a potential strategy for the treatment of schizophrenia. A novel series of GlyT-1 inhibitors have been identified containing the 2-arylsulfanyl-phenylpiperazine motif. The most prominent member of thi...

journal_title：Bioorganic & medicinal chemistry letters

authors： Smith G,Ruhland T,Mikkelsen G,Andersen K,Christoffersen CT,Alifrangis LH,Mørk A,Wren SP,Harris N,Wyman BM,Brandt G

更新日期：2004-08-02 00:00:00

abstract：:The potency and selectivity of a series of 5-hetero-2-iminohexahydroazepines were examined as inhibitors of the three human NOS isoforms. The effect of ring substitution of the 5-carbon for a heteroatom is presented. Potencies (IC(50)'s) for these inhibitors are in the low micromolar range for hi-NOS with some example...

journal_title：Bioorganic & medicinal chemistry letters

authors： Moormann AE,Metz S,Toth MV,Moore WM,Jerome G,Kornmeier C,Manning P,Hansen DW Jr,Pitzele BS,Webber RK

更新日期：2001-10-08 00:00:00

abstract：:We describe an efficient method for the synthesis of alkyl lysophosphatidic acid (LPA) analogs as well as alkyl LPA mono- and difluoromethylene phosphonate analogs. Each alkyl LPA analog was evaluated for subtype-specific LPA receptor agonist activity using a cell migration assay for LPA(1) activation in cancer cells ...

journal_title：Bioorganic & medicinal chemistry letters

authors： Xu Y,Tanaka M,Arai H,Aoki J,Prestwich GD

更新日期：2004-11-01 00:00:00

abstract：:A new class of non-ionic amphiphilic molecules suitable for biological purposes, especially extraction of membrane proteins, is reported. Such surfactants were prepared in two steps: addition of alkyl or fluoroalkyl mercaptan on Tris(hydroxymethyl)acrylamidomethane (THAM) derivatives, followed by the oxydation of sulf...

journal_title：Bioorganic & medicinal chemistry letters

authors： Barthélémy P,Maurizis JC,Lacombe JM,Pucci B

更新日期：1998-06-16 00:00:00

abstract：:Two series of novel gemcitabine-nucleoside analogue dimers were synthesized using the 'click' chemistry approach. In the first series of dimers (21-30), the nucleoside units were connected with a stable methyltriazole 4N-3'(or 5')C linker whereas in the second series (31-40) with a cleavable ester-methyltriazole 4N-3'...

journal_title：Bioorganic & medicinal chemistry letters

authors： Trznadel R,Singh A,Kleczewska N,Liberska J,Ruszkowski P,Celewicz L

更新日期：2019-09-15 00:00:00

abstract：:Benzalacetone synthase (BAS) and chalcone synthase (CHS) are plant-specific type III polyketide synthases (PKSs), sharing 70% amino acid sequence identity and highly homologous overall protein structures. BAS catalyzes the decarboxylative coupling of 4-coumaroyl-CoA with malonyl-CoA to produce the diketide benzalaceto...

journal_title：Bioorganic & medicinal chemistry letters

authors： Shimokawa Y,Morita H,Abe I

更新日期：2010-09-01 00:00:00

abstract：:A group of sixteen iridoids isolated from plants used as anti-inflammatory remedies in Mexican folk medicine were evaluated for their potential to inhibit cyclooxygenase-1 (COX-1) and cyclooxygenase-2 (COX-2) enzymes. From these assays, loganic acid (10) was identified as the most promising compound with both COX-1 (3...

journal_title：Bioorganic & medicinal chemistry letters

authors： Ramírez-Cisneros MÁ,Rios MY,Aguilar-Guadarrama AB,Rao PP,Aburto-Amar R,Rodríguez-López V

更新日期：2015-10-15 00:00:00

abstract：:A series of pyrimidine derivatives as acid pump antagonists (APAs) was synthesized and the inhibitory activities against H(+)/K(+) ATPase isolated from hog gastric mucosa were determined. After elaborating on substituents at C2 and C4 position of the pyrimidine scaffold, we have observed that the compound 7h is a pote...

journal_title：Bioorganic & medicinal chemistry letters

authors： Yoon YA,Park CS,Cha MH,Choi H,Sim JY,Kim JG

更新日期：2010-10-01 00:00:00

abstract：:The purpose of the present study was the synthesis and the biological screening of new analogues of N/OFQ(1-13)NH2, the minimal sequence maintaining the same activity as the natural peptide nociceptin. In order to investigate the role of Lys, we substituted Lys at positions 9 and/or 13 by Orn, Dab (diaminobutanoic aci...

journal_title：Bioorganic & medicinal chemistry letters

authors： Naydenova ED,Zhivkova VI,Zamfirova RN,Vezenkov LT,Dobrinova YG,Mateeva PI

更新日期：2006-08-01 00:00:00

abstract：:3-O-tert-Butyldimethylsilyl-17 alpha-(6-mesyloxyhexynyl)estradiol was converted to the azide in 60-70% yield with NaN3/DMPU, then reduced to the corresponding amine (> 95% yield). Acylation with the N-hydroxysuccinimide esters of biotin, 5-carboxyfluorescein and 10-(3-sulfopropyl)-N-tosyl-N-(3- carboxypropyl)acridiniu...

journal_title：Bioorganic & medicinal chemistry letters

authors： Adamczyk M,Chen YY,Moore JA,Mattingly PG

更新日期：1998-06-02 00:00:00

abstract：:A vitamin D analogue containing an affinity and a photoaffinity probe (affinity-driven cross-linker, Double Label) was synthesized. An unknown factor, associated with vitamin D receptor (VDR), was isolated from rat liver nuclear extract using a GST-VDR-ligand-binding domain fusion protein (GST-VDR-LBD), affinity label...

journal_title：Bioorganic & medicinal chemistry letters

authors： Swamy N,Addo JK,Ray R

更新日期：2000-02-21 00:00:00

abstract：:Novel arylethynyltriazole acyclonucleosides were synthesized and assessed for their anticancer activity on drug-resistant pancreatic cancer MiaPaCa-2 cells. One lead compound was found to have much more potent apoptosis-related antiproliferative effects than gemcitabine, the current first-line treatment for pancreatic...

journal_title：Bioorganic & medicinal chemistry letters

authors： Wang M,Xia Y,Fan Y,Rocchi P,Qu F,Iovanna JL,Peng L

更新日期：2010-10-15 00:00:00

abstract：:Poor prognosis coupled with significant economic burden makes heart failure (HF) one of the largest issues currently facing the world population. Although a significant number of new therapies have emerged over the past 20 years to treat the underlying physiological risk factors, only two new medications specifically ...

journal_title：Bioorganic & medicinal chemistry letters

authors： Malinowski JT,St Jean DJ Jr

更新日期：2018-05-15 00:00:00

abstract：:A series of N-alkyl-N-arylmethylpiperidin-4-amines have been prepared and are demonstrated to be inhibitors of both serotonin and norepinephrine reuptake. ...

journal_title：Bioorganic & medicinal chemistry letters

authors： Boot JR,Boulet SL,Clark BP,Cases-Thomas MJ,Delhaye L,Diker K,Fairhurst J,Findlay J,Gallagher PT,Gilmore J,Harris JR,Masters JJ,Mitchell SN,Naik M,Simmonds RG,Smith SM,Richards SJ,Timms GH,Whatton MA,Wolfe CN,Wood

更新日期：2006-05-15 00:00:00

abstract：:A series of pyrrolo[3,2,1-ij]quinoline derivatives was synthesized, evaluated for their activity against the 5-HT2c and 5-HT2a, receptors and found to be agonists at 5-HT2c with selectivity over 5-HT2a. ...

journal_title：Bioorganic & medicinal chemistry letters

authors： Isaac M,Slassi A,O'Brien A,Edwards L,MacLean N,Bueschkens D,Lee DK,McCallum K,De Lannoy I,Demchyshyn L,Kamboj R

更新日期：2000-05-01 00:00:00

abstract：:We report the results of our study into a series of simple phenyl and alkyl sulfamates and alkyl methanesulfonates as potential inhibitors of the enzyme estrone sulfatase (ES). The results of the study show that the substituted phenyl sulfamates are good irreversible inhibitors; the alkyl sulfamate compounds were foun...

journal_title：Bioorganic & medicinal chemistry letters

authors： Ahmed S,James K,Owen CP,Patel CK,Sampson L

更新日期：2002-05-06 00:00:00

abstract：:The synthesis of a series of new antitumour agents, the benzothiazole substituted quinol ethers and esters, is reported via the hypervalent iodine mediated oxidation of hydroxylated 2-phenylbenzothiazoles. The products were found to be active in vitro against human colon and breast cancer cell lines with IC50 values i...

journal_title：Bioorganic & medicinal chemistry letters

authors： Wells G,Bradshaw TD,Diana P,Seaton A,Shi DF,Westwell AD,Stevens MF

更新日期：2000-03-06 00:00:00

abstract：:Two new trichothecene sesquiterpenes, trichobreols D (1) and E (2), were isolated from the culture broth of marine-derived Trichoderma cf. brevicompactum together with trichobreol A (3). The structures of 1 and 2 were assigned on the basis of their spectroscopic data. Compound 1 inhibited the growth of two yeast-like ...

journal_title：Bioorganic & medicinal chemistry letters

authors： Yamazaki H,Yagi A,Takahashi O,Yamaguchi Y,Saito A,Namikoshi M,Uchida R

更新日期：2020-09-01 00:00:00

abstract：:The discovery of genotoxic amino acids derived from phenylglycine, and possessing halogen substituents, is described. The utility of hypervalent iodine reagents in the synthesis of this class of compounds is highlighted. The mechanism of action of the (haloaryl)glycines was studied in Saccharomyces cerevisiae. ...

journal_title：Bioorganic & medicinal chemistry letters

authors： Boto A,Gallardo JA,Hernández R,Ledo F,Muñoz A,Murguía JR,Menacho-Márquez M,Orjales A,Saavedra CJ

更新日期：2006-12-01 00:00:00

abstract：:A series of novel ethyl 5-(4-aminophenyl)-1H-pyrazole-3-carboxylate derivatives were designed and synthesized and their in vitro acrosin inhibitory activities were evaluated. Most of the compounds exhibited acrosin inhibitory activities. Among them, three compounds (5l, 5n, and 5v) were more potent than that of the co...

journal_title：Bioorganic & medicinal chemistry letters

authors： Qi J,Zhu J,Liu X,Ding L,Zheng C,Han G,Lv J,Zhou Y

更新日期：2011-10-01 00:00:00

abstract：:A series of novel 3-substituted isocoumarins was prepared via Pd-catalysed coupling processes and screened in vitro for antifungal activity against Candida species. The study revealed antifungal potential of isocoumarins possessing the azole substituents, which, in some cases, showed biological properties equal to tho...

journal_title：Bioorganic & medicinal chemistry letters

authors： Simic M,Paunovic N,Boric I,Randjelovic J,Vojnovic S,Nikodinovic-Runic J,Pekmezovic M,Savic V

更新日期：2016-01-01 00:00:00

abstract：:In our efforts to identify potent CRF(1) antagonists with proper physicochemical properties, a series of 3-phenylpyrazolo[1,5-a]pyrimidines bearing polar groups, such as amino, hydroxyl, methoxy, sulfoxide, were designed and synthesized. Several positions of the core structure were identified, where a polar group was ...

journal_title：Bioorganic & medicinal chemistry letters

authors： Chen C,Wilcoxen KM,Huang CQ,McCarthy JR,Chen T,Grigoriadis DE

更新日期：2004-07-16 00:00:00

abstract：:Two series of 1-alkyl-2-aryl-4-(1-naphthoyl)pyrroles were synthesized and their affinities for the cannabinoid CB(1) and CB(2) receptors were determined. In the 2-phenyl series (5) the N-alkyl group was varied from n-propyl to n-heptyl. A second series of 23 1-pentyl-2-aryl-4-(1-naphthoyl)-pyrroles (6) was also prepar...

journal_title：Bioorganic & medicinal chemistry letters

authors： Huffman JW,Padgett LW,Isherwood ML,Wiley JL,Martin BR

更新日期：2006-10-15 00:00:00

abstract：:New polyphenol classes have been tested against amyloid-beta peptide aggregation. We have identified four novel polyphenols which could be efficient fibril inhibitors in Alzheimer's disease: malvidin and its glucoside and curculigosides B and D. We suggest that molecules with the particular C(6)-linkers-C(6) structure...

journal_title：Bioorganic & medicinal chemistry letters

authors： Rivière C,Richard T,Vitrac X,Mérillon JM,Valls J,Monti JP

更新日期：2008-01-15 00:00:00

abstract：:A 2-pyrrolidinone ring containing a single hydroxymethyl side chain effectively replaces the N-acetylamino group of 4-(N-acetylamino)-3-guanidinobenzoic acid, a low micromolar inhibitor of influenza neuraminidase. This novel structural template affords new opportunities to evolve more potent benzoic acid inhibitors. ...

journal_title：Bioorganic & medicinal chemistry letters

authors： Brouillette WJ,Atigadda VR,Luo M,Air GM,Babu YS,Bantia S

更新日期：1999-07-19 00:00:00

abstract：:2,6-Diamino-4,N-diarylpyridines were identified as potent, isoform selective inhibitors of the enzymatic activity of lysophosphatidic acid acyltransferase-beta (LPAAT-beta). ...

journal_title：Bioorganic & medicinal chemistry letters

authors： Hong F,Hollenback D,Singer JW,Klein P

更新日期：2005-11-01 00:00:00

abstract：:This paper documents a serious problem met during the testing of Gi protein-activating properties of a new series of synthetic compounds by measuring the induced binding of [(35)S]GTPgammaS to different subtypes of Gi protein. The problem arose from the strong affinity between [(35)S]GTPgammaS and the tested compounds...

journal_title：Bioorganic & medicinal chemistry letters

authors： Manetti D,Di Cesare Mannelli L,Dei S,Guandalini L,Martini E,Banchelli M,Ghelardini C

更新日期：2009-04-15 00:00:00

abstract：:Ceramides are the major lipid components of the stratum corneum, the major permeability barrier of the skin. Here we report a chemical synthesis of ceramide analogs covalently bonded on the silica particles, that can be used to predict the skin permeability of chemicals via HPLC methods. ...

journal_title：Bioorganic & medicinal chemistry letters

authors： Yin J,Liu H,Pidgeon C

更新日期：1998-01-20 00:00:00