In vitro characterization of the Gd complex of [2,6-pyridinediylbis(methylene nitrilo)] tetraacetic acid (PMN-tetraacetic acid) and of its Eu analogue, suitable bimodal contrast agents for MRI and optical imaging.

abstract：:A dynamic target-based pharmacophoric model mapping the CD4 binding site on HIV-1 gp120 was built and used to identify new hits able to inhibit gp120-CD4 protein-protein interactions. Two compounds showed micromolar inhibition of HIV-1 replication in cells attributable to an interference with the entry step of infecti...

journal_title：Bioorganic & medicinal chemistry letters

authors： Caporuscio F,Tafi A,González E,Manetti F,Esté JA,Botta M

更新日期：2009-11-01 00:00:00

abstract：:Poly(ADP-ribose)polymerase-I (PARP-1) enzyme is involved in maintaining DNA integrity and programmed cell death. A virtual screening of commercial libraries led to the identification of five novel scaffolds with inhibitory profile in the low nanomolar range. A hit-to-lead optimization led to the identification of a gr...

journal_title：Bioorganic & medicinal chemistry letters

authors： Giannini G,Battistuzzi G,Vesci L,Milazzo FM,De Paolis F,Barbarino M,Guglielmi MB,Carollo V,Gallo G,Artali R,Dallavalle S

更新日期：2014-01-15 00:00:00

abstract：:The B(6) vitamers have been shown to display beneficial therapeutic effects in cardiovascular related disorders. The design of novel antiplatelet agents using pyridoxine as a template has led to the discovery of a class of novel cardio- and cerebro-protective agents. The present study describes the synthesis of severa...

journal_title：Bioorganic & medicinal chemistry letters

authors： Zhang W,Yao J,Pham V,Whitney T,Froese D,Friesen A,Stang L,Xu C,Shuaib A,Diakur JM,Haque W

更新日期：2004-09-20 00:00:00

abstract：:We previously identified o-carborane bisphenol BE360 (4) as a selective estrogen receptor modulator (SERM), which ameliorated bone loss without inducing estrogenic action in uterus of OVX and ORX mice. Here, we synthesized a fluorinated derivative, B-fluorinated o-carborane bisphenol BE310 (5) by means of S(N)Ar react...

journal_title：Bioorganic & medicinal chemistry letters

authors： Ohta K,Ogawa T,Endo Y

更新日期：2012-07-15 00:00:00

abstract：:Highly potent and novel derivatives of doxorubicin were linked to monoclonal antibodies (mAbs) for site-specific drug delivery. Drug linker 5 consisted of a dipeptide linker attached directly to the daunosamine nitrogen of the n-butyldiacetate doxorubicin derivative 2a. Upon hydrolysis of the peptide linker and acetat...

journal_title：Bioorganic & medicinal chemistry letters

authors： Jeffrey SC,Nguyen MT,Andreyka JB,Meyer DL,Doronina SO,Senter PD

更新日期：2006-01-15 00:00:00

abstract：:Peptides containing Nepsilon-thioacetyl-lysine and Nepsilon-acetyl-lysine were evaluated for their de(thio)acetylation catalyzed by human HDAC8 and SIRT1, two distinct protein deacetylases. Nepsilon-Thioacetyl-lysine was found to be a mimic of Nepsilon-acetyl-lysine for HDAC8-catalyzed reaction, but to confer inhibiti...

journal_title：Bioorganic & medicinal chemistry letters

authors： Fatkins DG,Monnot AD,Zheng W

更新日期：2006-07-15 00:00:00

abstract：:Current therapy for blood vessel thrombosis has the risk of leading to gastrointestinal bleeding and thrombocytopenia. We previously reported that a new derivative of diosgenin, compound 5, had significant anti-inflammatory activity superior to that of aspirin, prolonged bleeding time, and inhibited platelet aggregati...

journal_title：Bioorganic & medicinal chemistry letters

authors： Zheng H,Wei Z,Xin G,Ji C,Wen L,Xia Q,Niu H,Huang W

更新日期：2016-07-15 00:00:00

abstract：:This study describes the syntheses of di, tetra and hexa deuterated analogues of the NOD-like receptor pyrin domain-containing protein 3 (NLRP3) inflammasome inhibitor MCC950. In di and tetra deuterated analogues, deuteriums were incorporated into the 1,2,3,5,6,7-hexahydro-s-indacene moiety, whereas in the hexa deuter...

journal_title：Bioorganic & medicinal chemistry letters

authors： Salla M,Butler MS,Massey NL,Reid JC,Cooper MA,Robertson AAB

更新日期：2018-02-15 00:00:00

abstract：:Glycosyldisulfides can interact efficiently with carbohydrate-binding entities. This has been shown for a range of thiosaccharide dimers when tested for their effects against the lectin Concanavalin A using a modified quartz crystal microbalance-technique. Contrary to the thiosaccharide monomers, showing no significan...

journal_title：Bioorganic & medicinal chemistry letters

authors： Pei Z,Aastrup T,Anderson H,Ramström O

更新日期：2005-06-02 00:00:00

abstract：:A new series of triazole-imidazo[2,1-b][1,3,4]thiadiazole hybrids (6a-s, 7a) were designed by a molecular hybridisation approach and the target molecules were synthesized via one pot click chemistry protocol. All the intermediates and final molecules were characterised using spectral methods and one of the target comp...

journal_title：Bioorganic & medicinal chemistry letters

authors： Ramprasad J,Nayak N,Dalimba U,Yogeeswari P,Sriram D

更新日期：2015-10-01 00:00:00

abstract：:Janus kinases (JAKs) including JAK1, JAK2, JAK3, and TYK2 are members of a family of intracellular nonreceptor tyrosine kinases, which have been demonstrated to be critical in the cell signaling pathway and involved in inflammatory diseases and cancer. V617F mutation in JAK2 has been implicated in polycythaemia vera (...

journal_title：Bioorganic & medicinal chemistry letters

authors： Ma X,Diao Y,Ge H,Xu F,Zhu L,Zhao Z,Li H

更新日期：2020-04-15 00:00:00

abstract：:The highly selective agonists of the A(3) adenosine receptor (AR), Cl-IB-MECA (2-chloro-N(6)-(3-iodobenzyl)-5'-N-methylcarboxamidoadenosine), and its 4'-thio analogue, were successfully converted into selective antagonists simply by appending a second N-methyl group on the 5'-uronamide position. The 2-chloro-5'-(N,N-d...

journal_title：Bioorganic & medicinal chemistry letters

authors： Gao ZG,Joshi BV,Klutz AM,Kim SK,Lee HW,Kim HO,Jeong LS,Jacobson KA

更新日期：2006-02-01 00:00:00

abstract：:The synthesis and SAR of a series of 6-(4-(substituted)phenyl)-2-aminopyridines as inhibitors of nitric oxide synthase are described. Compound 3a from this series shows potent and selective inhibition of the human nNOS isoform, with pharmacokinetics sufficient to provide in vivo inhibition of nNOS activity. ...

journal_title：Bioorganic & medicinal chemistry letters

authors： Lowe JA 3rd,Qian W,Volkmann RA,Heck S,Nowakowski J,Nelson R,Nolan C,Liston D,Ward K,Zorn S,Johnson C,Vanase M,Faraci WS,Verdries KA,Baxter J,Doran S,Sanders M,Ashton M,Whittle P,Stefaniak M

更新日期：1999-09-06 00:00:00

abstract：:A novel series of kappa (kappa) opioid receptor agonists were synthesized by incorporating the key structural features of known kappa opioid agonists while replacing the aryl acetamide portion with substituted amino acid conjugates. Compounds 3j (Ki = 6.7 nM), 3k (Ki = 3.6 nM), 3l (Ki = 4.6 nM), 3m (Ki = 0.83 nM) and ...

journal_title：Bioorganic & medicinal chemistry letters

authors： Kumar V,Guo D,Daubert JD,Cassel JA,DeHaven RN,Mansson E,DeHaven-Hudkins DL,Maycock AL

更新日期：2005-03-01 00:00:00

abstract：:Aberrant expansion of GGGGCC (G4C2) hexanucleotide repeat (HNR) in the first intron of C9ORF72 has been found in frontotemporal dementia and amyotrophic lateral sclerosis (FTD/ALD). The non-canonical DNA structures of the expanded repeats are causative to repeat instability leading to contraction and expansion. We dem...

journal_title：Bioorganic & medicinal chemistry letters

authors： Shibata T,Murakami E,Nakatani K

更新日期：2018-08-01 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：:Considering the therapeutic potential of fatty acid amides, the present study aimed to evaluate their in vitro activity against Toxocara canis larvae and their cytotoxicity for the first time. Linoleylpyrrolidilamide was the most potent, with a minimal larvicidal concentration (MLC) of 0.05 mg/mL and 27% cytotoxicity ...

journal_title：Bioorganic & medicinal chemistry letters

authors： Mata-Santos T,D'Oca CDRM,Mata-Santos HA,Fenalti J,Pinto N,Coelho T,Berne ME,da Silva PEA,D'Oca MGM,Scaini CJ

更新日期：2016-02-01 00:00:00

abstract：:Novel ligands, NBEA, NBPA, NETA, NE3TA, and NE3TA-Bn, were synthesized and evaluated as potential chelators of copper radioisotopes for use in targeted positron emission tomography (PET) imaging or radiation therapy. The new ligands were radiolabeled with (64)Cu, and in vitro stability of the radiolabeled complexes wa...

journal_title：Bioorganic & medicinal chemistry letters

authors： Chong HS,Mhaske S,Lin M,Bhuniya S,Song HA,Brechbiel MW,Sun X

更新日期：2007-11-15 00:00:00

abstract：:Cage amines 1-4 are potent peripheral anionic site-bound reversible inhibitors of both acetylcholinesterase and butyrylcholinesterase. Cage amines 1-3 are selective butyrylcholinesterase inhibitor versus acetylcholinesterase. For both enzymes, the -log K(i) values linearly correlate with the difference of substituted ...

journal_title：Bioorganic & medicinal chemistry letters

authors： Lin G,Tsai HJ,Tsai YH

更新日期：2003-09-01 00:00:00

abstract：:Considering the complex etiology of Alzheimer's disease (AD), multifunctional agents may be beneficial for the treatment of this disease. A series of DL-3-n-butylphthalide-Edaravone hybrids were designed, synthesized and evaluated as novel dual inhibitors of amyloid-β aggregation and monoamine oxidases. Among them, co...

journal_title：Bioorganic & medicinal chemistry letters

authors： Qiang X,Li Y,Yang X,Luo L,Xu R,Zheng Y,Cao Z,Tan Z,Deng Y

更新日期：2017-02-15 00:00:00

abstract：:A 70% EtOH extract from the bark of Syringareticulata has shown significant antioxidant activity. Chemical study on the extract resulted in the isolation of seventeen compounds (1-17), including a novel oleoside-type secoiridoid glucoside, reticuloside (1), and the structures were elucidated on the basis of extensive ...

journal_title：Bioorganic & medicinal chemistry letters

authors： Bi X,Li W,Sasaki T,Li Q,Mitsuhata N,Asada Y,Zhang Q,Koike K

更新日期：2011-11-01 00:00:00

abstract：:The present work reports on the preparation of glass surfaces coated with NPPOC-protected aminooxy groups and their use for the patterning of oligonucleotides on glass slides and in capillary tubes. The method involves the use of surfaces coated with amino groups using (gamma-aminopropyl)triethoxy silane and subsequen...

journal_title：Bioorganic & medicinal chemistry letters

authors： Dendane N,Hoang A,Defrancq E,Vinet F,Dumy P

更新日期：2008-04-15 00:00:00

abstract：:During the course of our investigations in the field of azole antimicrobial agents, we have identified BM212 a pyrrole derivative with good in vitro activity against mycobacteria and candidae. These findings prompted us to prepare new pyrrole derivatives 2-6 in the hope of increasing the activity. The microbiological ...

journal_title：Bioorganic & medicinal chemistry letters

authors： Biava M,Fioravanti R,Porretta GC,Deidda D,Maullu C,Pompei R

更新日期：1999-10-18 00:00:00

abstract：:In this study, we investigated the anti-inflammatory effects and mechanisms of cirsimaritin isolated from an ethanol extract of the aerial parts of Cirsium japonicum var. maackii Maxim. using RAW264.7 cells. The extract and its flavonoid cirsimaritin inhibited nitric oxide (NO) production and inducible nitric oxide sy...

journal_title：Bioorganic & medicinal chemistry letters

authors： Shin MS,Park JY,Lee J,Yoo HH,Hahm DH,Lee SC,Lee S,Hwang GS,Jung K,Kang KS

更新日期：2017-07-15 00:00:00

abstract：:The synthesis and inhibitory activity against MraY of a series of simplified analogues of liposidomycins are described. These compounds were mainly obtained by performing parallel synthesis in the 6'-position of a scaffold that gathers key features found necessary for the binding to MraY. Thus, inhibitory activity was...

journal_title：Bioorganic & medicinal chemistry letters

authors： Dini C,Didier-Laurent S,Drochon N,Feteanu S,Guillot JC,Monti F,Uridat E,Zhang J,Aszodi J

更新日期：2002-04-22 00:00:00

abstract：:A methyl group at the 2-position of methyl mesopyropheophorbide-a was transformed to the 2-formyl group to give methyl mesopyropheophorbide-f, one of the chlorophyll-f analogs. The 2-formylation moved the redmost electronic absorption band in a solution to a longer wavelength and the bathochromic shift was comparable ...

journal_title：Bioorganic & medicinal chemistry letters

authors： Xu M,Kinoshita Y,Tamiaki H

更新日期：2014-08-15 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：:In HEK293 cells stably expressing alpha4beta2 nAChRs, naltrexone, but not naloxone, blocked alpha4beta2 nAChRs via an open-channel blocking mechanism. In primary hippocampal cultures, naltrexone inhibited alpha7 nAChRs up-regulated by nicotine, and in organotypic hippocampal cultures naltrexone caused a time-dependent...

journal_title：Bioorganic & medicinal chemistry letters

authors： Almeida LE,Pereira EF,Camara AL,Maelicke A,Albuquerque EX

更新日期：2004-04-19 00:00:00

abstract：:In an effort to find potential anxiolytic and/or antipsychotic agents with selective 5-HT(2C) affinity a series of new pyrimidine derivatives was prepared and the binding affinities for 5-HT(2A) and 5-HT(2C) receptors were determined. ...

journal_title：Bioorganic & medicinal chemistry letters

authors： Bózsing D,Simonek I,Simig G,Jakóczi I,Gacsályi I,Lévay G,Tihanyi K,Schmidt E

更新日期：2002-11-04 00:00:00

abstract：:A serendipitous discovery that the metalloprotease binding profile of a novel class of 2-carboxamide-3-hydroxamic acid piperidines could be significantly attenuated by the modification of the unexplored P1 substituent enabled the design and synthesis of a novel 2-carboxamide-1-hydroxamic acid cyclohexyl scaffold core ...

journal_title：Bioorganic & medicinal chemistry letters

authors： Burns DM,Li YL,Shi E,He C,Xu M,Zhuo J,Zhang C,Qian DQ,Li Y,Wynn R,Covington MB,Katiyar K,Marando CA,Fridman JS,Scherle P,Friedman S,Metcalf B,Yao W

更新日期：2009-07-01 00:00:00