Cyclic guanidines as dual 5-HT5A/5-HT7 receptor ligands: structure-activity relationship elucidation.

abstract：:A combination of isothermal titration calorimetry (ITC), topoisomerase I DNA unwinding assays, and ethidium bromide displacement studies were employed to investigate the binding of a homologous series of naphthalene diimides (NDI) to DNA. Our results suggest that the nature of the substituent plays a significant role ...

journal_title：Bioorganic & medicinal chemistry letters

authors： McKnight RE,Reisenauer E,Pintado MV,Polasani SR,Dixon DW

更新日期：2011-07-15 00:00:00

abstract：:In an effort to expand the spectrum of antibacterial activity associated with piperidin-4-one derivatives, we have synthesized two series of 3-carboxyethyl-2,6-diphenyl-4-hydroxy-Delta(3)-tetrahydropyridine derivatives bearing diversified heterocyclic and aromatic systems at the nitrogen atom through acetyl (6-18) and...

journal_title：Bioorganic & medicinal chemistry letters

authors： Aridoss G,Amirthaganesan S,Jeong YT

更新日期：2010-04-01 00:00:00

abstract：:We disclose a new compound class of potent and selective alpha-1A adrenergic receptor antagonists exemplified by the geminally, disubstituted cyclic imide 7. The optimization of lead compounds resulting in the cyclic imide motif is highlighted. The results of in vitro and in vivo studies of selected compounds are pres...

journal_title：Bioorganic & medicinal chemistry letters

authors： DiPardo RM,Patane MA,Newton RC,Price R,Broten TP,Chang RS,Ransom RW,Di Salvo J,Freidinger RM,Bock MG

更新日期：2001-07-23 00:00:00

abstract：:The elongation condensing enzymes in the bacterial fatty acid biosynthesis pathway represent desirable targets for the design of novel, broad-spectrum antimicrobial agents. A series of substituted benzoxazolinones was identified in this study as a novel class of elongation condensing enzyme (FabB and FabF) inhibitors ...

journal_title：Bioorganic & medicinal chemistry letters

authors： Zheng Z,Parsons JB,Tangallapally R,Zhang W,Rock CO,Lee RE

更新日期：2014-06-01 00:00:00

abstract：:With an insight that ligands possessing a N2S2 tetradentate array of donor atoms serve as ideal bifunctional chelating agents (BFCA) in the radiolabeling of target-specific agents, 5-hydroxy-3,7-diazanonan-1,9-dithiol (DAHPES) with a derivatizable substituent in the form of a hydroxyl group in the backbone was synthes...

journal_title：Bioorganic & medicinal chemistry letters

authors： Das T,Banerjee S,Samuel G,Bapat K,Subramanian S,Pillai MR,Venkatesh M

更新日期：2006-11-15 00:00:00

abstract：:Natural inhibitors of fatty acid synthase (FAS) are emerging as potential therapeutic agents to treat cancer and obesity. The bioassay-guided chemical investigation of the hulls of Garcinia mangostana led to the isolation of 13 phenolic compounds (1-13) mainly including xanthone and benzophenone, in which compounds 7,...

journal_title：Bioorganic & medicinal chemistry letters

authors： Jiang HZ,Quan XF,Tian WX,Hu JM,Wang PC,Huang SZ,Cheng ZQ,Liang WJ,Zhou J,Ma XF,Zhao YX

更新日期：2010-10-15 00:00:00

abstract：:The capabilities of 20 strains of fungi to transform acetyl-11-keto-β-boswellic (AKBA) were screened. And biotransformation of AKBA by Cunninghamella blakesleana AS 3.970 afforded five metabolites (1-5), while two metabolites (6, 7) were isolated from biotransformation of Cunninghamella elegans AS 3.1207. The chemical...

journal_title：Bioorganic & medicinal chemistry letters

authors： Sun Y,Liu D,Xi R,Wang X,Wang Y,Hou J,Zhang B,Wang C,Liu K,Ma X

更新日期：2013-03-01 00:00:00

abstract：:As part of our ongoing search for anti-inflammatory compounds from higher plants, we isolated and elucidated two new diterpenoid glycosides, kansuingol A (1) and kansuingol B (2), from the roots of Euphorbia kansui. These structures were elucidated by extensive spectroscopic methods such as NMR and MS. Compounds were ...

journal_title：Bioorganic & medicinal chemistry letters

authors： Kim YM,Ahn J,Chae HS,Choi YH,Kim J,Chin YW

更新日期：2018-04-15 00:00:00

abstract：:A series of substituted 2-aminopyridines was prepared and evaluated as inhibitors of human nitric oxide synthases (NOS). 4,6-Disubstitution enhanced both potency and specificity for the inducible NOS with the most potent compound having an IC50 of 28 nM. ...

journal_title：Bioorganic & medicinal chemistry letters

authors： Hagmann WK,Caldwell CG,Chen P,Durette PL,Esser CK,Lanza TJ,Kopka IE,Guthikonda R,Shah SK,MacCoss M,Chabin RM,Fletcher D,Grant SK,Green BG,Humes JL,Kelly TM,Luell S,Meurer R,Moore V,Pacholok SG,Pavia T,Williams H

更新日期：2000-09-04 00:00:00

abstract：:Diaryl-(4-piperidinyl)-pyrrole derivatives bearing cyclic amine substituents have been synthesized and evaluated as anticoccidial agents. Improvements in potency of Et-PKG inhibition, such as azetidine derivative 3a, and broad spectrum anticoccidial activities in feed, such as morpholine derivative 8c, have been achie...

journal_title：Bioorganic & medicinal chemistry letters

authors： Liang GB,Qian X,Feng D,Fisher M,Crumley T,Darkin-Rattray SJ,Dulski PM,Gurnett A,Leavitt PS,Liberator PA,Misura AS,Samaras S,Tamas T,Schmatz DM,Wyvratt M,Biftu T

更新日期：2008-03-15 00:00:00

abstract：:In the search of new antihyperglycemic agents and following rational approach of drug designing here new 2-hydrazolyl-4-thiazolidinone-5-carboxylic acids (4a-g) with pyrazolyl pharmacophore have been synthesized via thia Michael addition reaction of 1-((3-(4-substituted phenyl)-1-phenyl-1H-pyrazol-4-yl)methylene)thios...

journal_title：Bioorganic & medicinal chemistry letters

authors： Bhosle MR,Mali JR,Pal S,Srivastava AK,Mane RA

更新日期：2014-06-15 00:00:00

abstract：:The synthesis and biological evaluation of a series of novel isobenzofuran-based compounds are described. The compounds were evaluated for their immunosuppressive effects of T-cell proliferation and IMPDH type II inhibitor activity in vitro, as well as their structure-activity relationships were assessed. Several comp...

journal_title：Bioorganic & medicinal chemistry letters

authors： Yang N,Wang QH,Wang WQ,Wang J,Li F,Tan SP,Cheng MS

更新日期：2012-01-01 00:00:00

abstract：:We identified and tested bisphosphonates as inhibitors of a protozoan molecular target. Computational modeling studies demonstrated that these compounds are mimics of the natural substrate of the enzyme. The most potent bisphosphonates in vitro are pamidronate and risedronate, which inhibit the purine transferase from...

journal_title：Bioorganic & medicinal chemistry letters

authors： Fernández D,Wenck MA,Craig SP 3rd,Delfino JM

更新日期：2004-09-06 00:00:00

abstract：:Peptide-based alpha-ketoamides, alpha-ketoesters and alpha-diketones were designed, synthesized and evaluated against HCV NS3 protease. Alpha-ketoamides have the highest affinity among the three classes, with 8 being the most potent inhibitor with an IC50 of 340 nM. ...

journal_title：Bioorganic & medicinal chemistry letters

authors： Han W,Hu Z,Jiang X,Decicco CP

更新日期：2000-04-17 00:00:00

abstract：:A series of SYK inhibitors based on the phenylamino pyrimidine thiazole lead 4 were prepared and evaluated for biological activity. Lead optimization provided compounds with nanomolar K(i)'s against SYK and potent inhibition in mast cell degranulation assays. ...

journal_title：Bioorganic & medicinal chemistry letters

authors： Farmer LJ,Bemis G,Britt SD,Cochran J,Connors M,Harrington EM,Hoock T,Markland W,Nanthakumar S,Taslimi P,Ter Haar E,Wang J,Zhaveri D,Salituro FG

更新日期：2008-12-01 00:00:00

abstract：:Huisgen [3+2] dipolar cycloaddition of 6″-azido-6″-deoxy-α-galactosyl ceramide 11 with a range of alkynes (or a benzyne precursor) yielded a series of triazole-containing α-galactosyl ceramide (α-GalCer) analogues in high yield. These α-GalCer analogues and the precursor azide 11 were tested for their ability to activ...

journal_title：Bioorganic & medicinal chemistry letters

authors： Jervis PJ,Graham LM,Foster EL,Cox LR,Porcelli SA,Besra GS

更新日期：2012-07-01 00:00:00

abstract：:A series of 7-diethylaminocoumarin compounds were synthesized and the cytotoxicities were tested against human umbilical vein endothelial cell (HUVEC) and some cancer cells. We found that the introduction of cyano groups at the 4-position will promote the bioactivity. In particular, compounds 9 and 10 strongly inhibit...

journal_title：Bioorganic & medicinal chemistry letters

authors： Lee S,Sivakumar K,Shin WS,Xie F,Wang Q

更新日期：2006-09-01 00:00:00

abstract：:Myelin associated glycoprotein (Siglec-4) is a myelin adhesion receptor, that is, well established for its role as an inhibitor of axonal outgrowth in nerve injury, mediated by binding to sialic acid containing ligands on the axonal membrane. Because disruption of myelin-ligand interactions promotes axon outgrowth, we...

journal_title：Bioorganic & medicinal chemistry letters

authors： Zeng Y,Rademacher C,Nycholat CM,Futakawa S,Lemme K,Ernst B,Paulson JC

更新日期：2011-09-01 00:00:00

abstract：:Poly(ADP-ribose) (PAR) is an important biopolymer, which is involved in various life processes such as DNA repair and replication, modulation of chromatin structure, transcription, cell differentiation, and in pathogenesis of various diseases such as cancer, diabetes, ischemia and inflammations. PAR is the most electr...

journal_title：Bioorganic & medicinal chemistry letters

authors： Drenichev MS,Mikhailov SN

更新日期：2016-08-01 00:00:00

abstract：:Treatment of diseases such as African sleeping sickness and leishmaniasis often depends on relatively expensive or toxic drugs, and resistance to current chemotherapeutics is an issue in treating these diseases and malaria. In this study, a new semi-synthetic berberine analogue, 5,6-didehydro-8,8-diethyl-13-oxodihydro...

journal_title：Bioorganic & medicinal chemistry letters

authors： Bahar M,Deng Y,Zhu X,He S,Pandharkar T,Drew ME,Navarro-Vázquez A,Anklin C,Gil RR,Doskotch RW,Werbovetz KA,Kinghorn AD

更新日期：2011-05-01 00:00:00

abstract：:A structure-activity relationship study of dorsomorphin, a previously identified inhibitor of SMAD 1/5/8 phosphorylation by bone morphogenetic protein (BMP) type 1 receptors ALK2, 3, and 6, revealed that increased inhibitory activity could be accomplished by replacing the pendent 4-pyridine ring with 4-quinoline. The ...

journal_title：Bioorganic & medicinal chemistry letters

authors： Cuny GD,Yu PB,Laha JK,Xing X,Liu JF,Lai CS,Deng DY,Sachidanandan C,Bloch KD,Peterson RT

更新日期：2008-08-01 00:00:00

abstract：:Benzofuran-5-ol derivatives were synthesized and tested for in vitro antifungal activity against Candida, Aspergillus species, and Cryptococcus neoformans. Among them tested, many benzofuran-5-ols showed good antifungal activity. The results suggest that benzofuran-5-ols would be promising antifungal agents. ...

journal_title：Bioorganic & medicinal chemistry letters

authors： Ryu CK,Song AL,Lee JY,Hong JA,Yoon JH,Kim A

更新日期：2010-11-15 00:00:00

abstract：:We designed and synthesized strobilurin analogues as hypoxia-inducible factor (HIF) inhibitors based on the molecular structure of kresoxim-methyl. Biological evaluation in human colorectal cancer HCT116 cells showed that most of the synthesized kresoxim-methyl analogues possessed moderate to potent inhibitory activit...

journal_title：Bioorganic & medicinal chemistry letters

authors： Lee S,Kwon OS,Lee CS,Won M,Ban HS,Ra CS

更新日期：2017-07-01 00:00:00

abstract：:The enzymatic synthesis of Gal-beta 1,3[GlcNAc-beta 1,6]-GalNAc-alpha 1-OBn (core 2-Bn) using a multi-enzyme system consisting of a beta-galactosidase (EC 3.2.1.23) from bovine testes and a recombinant core 2 beta 1,6-GlcNAc transferase (C2GnT, EC 2.4.1.102) was empirically optimized by the use of a genetic algorithm....

journal_title：Bioorganic & medicinal chemistry letters

authors： Hoh C,Dudziak G,Liese A

更新日期：2002-04-08 00:00:00

abstract：:A novel class of 2,3-tri- and tetrasubstituted γ-butyrolactones analogous to paraconic acids has been synthesized in one step using a straightforward three-component reaction among aryl bromides, dimethyl itaconate and carbonyl compounds. The in vitro cytotoxic activity of representative compounds has been evaluated a...

journal_title：Bioorganic & medicinal chemistry letters

authors： Le Floch C,Le Gall E,Léonel E,Martens T,Cresteil T

更新日期：2011-12-01 00:00:00

abstract：:Several shortened peptide analogues of the N-terminal domain of GPR1, an orphan G protein-coupled receptor (GPCR), were prepared and their anti-HIV-1 activities were evaluated. Some of the prepared compounds, especially sulfated derivatives, showed potent inhibitory activity against a broad range of HIV-1, including T...

journal_title：Bioorganic & medicinal chemistry letters

authors： Ikeda K,Konishi K,Sato M,Hoshino H,Tanaka K

更新日期：2001-10-08 00:00:00

abstract：:Four new peptidyl aldehydes bearing proline mimetics at the P(2)-position were synthesized and studied as inhibitors of calpain I, cathepsin B, and selected serine proteases. The ring size of the P(2)-constraining residue influenced the inhibitory potency and selectivity of the compounds for calpain I compared to the ...

journal_title：Bioorganic & medicinal chemistry letters

authors： Donkor IO,Korukonda R,Huang TL,LeCour L Jr

更新日期：2003-03-10 00:00:00

abstract：:Multivalent interactions play an essential role in molecular recognition in living systems. These effects were employed to target tumor cells using albumin clusters bearing ∼10 molecules of asparagine-linked glycans (N-glycans). Noninvasive near-infrared fluorescence imaging clearly revealed A431 tumors implanted in B...

journal_title：Bioorganic & medicinal chemistry letters

authors： Ogura A,Tahara T,Nozaki S,Onoe H,Kurbangalieva A,Watanabe Y,Tanaka K

更新日期：2016-05-01 00:00:00

abstract：:To obtain modulators for reducing mitochondrial damage by the inhibition of Aβ oligomer formation, 2-phenylbenzofuran derivatives were designed and prepared. Their inhibitory activity against Aβ fibril formation was screened using ThT fluorescence assay, and the effect of derivatives on mitochondrial function was eval...

journal_title：Bioorganic & medicinal chemistry letters

authors： Lee YS,Kim HY,Youn HM,Seo JH,Kim Y,Shin KJ

更新日期：2013-11-01 00:00:00

abstract：:A series of trans-4-phenylpyrrolidine-3-carboxamides were synthesized and characterized as potent ligands of the human melanocortin-4 receptor. Interestingly, a pair of diastereoisomers 13b displayed potent functional agonist and antagonist activity, respectively. Thus, the 3S,4R-pyrrolidine 13b-1 possessed a Ki of 1....

journal_title：Bioorganic & medicinal chemistry letters

authors： Chen C,Jiang W,Tran JA,Tucci FC,Fleck BA,Markison S,Wen J,Madan A,Hoare SR,Foster AC,Marinkovic D,Chen CW,Arellano M,Saunders J

更新日期：2008-01-01 00:00:00