Substituted 2-aminopyridines as inhibitors of nitric oxide synthases.

abstract：:This article describes the syntheses and SAR of a series of imidazolopyrimidine derivatives, which are evaluated as inhibitors of PI3-Kinase (PI3K) and mTOR. These compounds were found to be ATP competitive with good tumor cell growth inhibition, and suppression of pathway specific biomakers such as phosphorylation of...

journal_title：Bioorganic & medicinal chemistry letters

authors： Venkatesan AM,Dehnhardt CM,Chen Z,Santos ED,Dos Santos O,Bursavich M,Gilbert AM,Ellingboe JW,Ayral-Kaloustian S,Khafizova G,Brooijmans N,Mallon R,Hollander I,Feldberg L,Lucas J,Yu K,Gibbons J,Abraham R,Mansour TS

更新日期：2010-01-15 00:00:00

abstract：:The diacylglycerol acyltransferase enzyme, DGAT1, presents itself as a potential target for obesity as this enzyme is dedicated to the final committed step in triglyceride biosynthesis. Biphenyl ureas, exemplified by compound 4, have been reported to be potent hDGAT1 inhibitors. We have synthesized and evaluated 2-pyr...

journal_title：Bioorganic & medicinal chemistry letters

authors： Motiwala H,Kandre S,Birar V,Kadam KS,Rodge A,Jadhav RD,Mahesh Kumar Reddy M,Brahma MK,Deshmukh NJ,Dixit A,Doshi L,Gupte A,Gangopadhyay AK,Vishwakarma RA,Srinivasan S,Sharma M,Nemmani KV,Sharma R

更新日期：2011-10-01 00:00:00

abstract：:To improve the DNA hydrolytic activity of the zinc finger nuclease, we have created a new artificial zinc finger nuclease (ZWH4) by connecting two distinct zinc finger domains possessing different types of Zn(II) binding sites (Cys(2)His(2)- and His(4)-types). The overall fold of ZWH4 is similar to that of the wild-ty...

journal_title：Bioorganic & medicinal chemistry letters

authors： Negi S,Umeda Y,Masuyama S,Kano K,Sugiura Y

更新日期：2009-05-15 00:00:00

abstract：:A novel series of acylated omega-aminoalkyl 2-amino-2-deoxy-4-phosphono-beta-D-glucopyranosides (aminoalkyl glucosaminide 4-phosphates) was synthesized and screened for immunostimulant activity. Several of these compounds enhance the production of tetanus toxoid-specific antibodies in mice and augment vaccine-induced ...

journal_title：Bioorganic & medicinal chemistry letters

authors： Johnson DA,Sowell CG,Johnson CL,Livesay MT,Keegan DS,Rhodes MJ,Ulrich JT,Ward JR,Cantrell JL,Brookshire VG

更新日期：1999-08-02 00:00:00

abstract：:A library of conjugates of chromones and 2,4-thiazolidinedione has been synthesized by Knoevenagel condensation followed by reduction using hydrogen gas and Pd/C as a catalyst. Compounds 5c and 5e were most effective in lowering the blood glucose level comparable to standard drug pioglitazone. Compound 5e exhibited po...

journal_title：Bioorganic & medicinal chemistry letters

authors： Nazreen S,Alam MS,Hamid H,Yar MS,Dhulap A,Alam P,Pasha MA,Bano S,Alam MM,Haider S,Kharbanda C,Ali Y,Pillai KK

更新日期：2014-07-15 00:00:00

abstract：:A novel acromelic acid analogue containing a phenyl group possessing two different types of azido functional groups, of which one is the aromatic N3 acting as a photoaffinity group to bind to a target protein by photoirradiation and the other is alkyl N3 group which survives photolysis acting as a detecting group thro...

journal_title：Bioorganic & medicinal chemistry letters

authors： Sun P,Wang GX,Furuta K,Suzuki M

更新日期：2006-05-01 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：:A new cyclic heptapeptide, cyclonatsudamine A (1), cyclo (-Gly-Tyr-Leu-Leu-Pro-Pro-Ser-), has been isolated from the peels of Citrus natsudaidai and the structure was elucidated by 2D NMR analysis and chemical degradation. Cyclonatsudamine A (1) relaxed norepinephrine-induced contractions of rat aorta, which may be me...

journal_title：Bioorganic & medicinal chemistry letters

authors： Morita H,Enomoto M,Hirasawa Y,Iizuka T,Ogawa K,Kawahara N,Goda Y,Matsumoto T,Takeya K

更新日期：2007-10-01 00:00:00

abstract：:An efficient synthesis of [D-lysine](8)cyclosporin A has been developed. Several analogs of [D-lysine](8)cyclosporin A have been synthesized and show promising anti-HCV activity, particularly compounds 39 and 43, which each exhibit an anti-HCV EC(50)<200 nM, and are each ≥50-fold less immunosuppressive than cyclospori...

journal_title：Bioorganic & medicinal chemistry letters

authors： Scribner A,Houck D,Huang Z,Mosier S,Peel M,Scorneaux B

更新日期：2010-11-15 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：:Catalytic disulfenylation reaction of alkenes by common Lewis acids has been investigated in detail. While reactions by FeCl(3) were feasible with cycloalkenes and other simple alkenes, much faster and excellent conversions were possible by AlCl(3) even with the substrates less reactive toward FeCl(3). ...

journal_title：Bioorganic & medicinal chemistry letters

authors： Yamagiwa N,Suto Y,Torisawa Y

更新日期：2007-11-15 00:00:00

abstract：:A series of dihydropyrazolopyrimidine inhibitors of K(V)1.5 (I(Kur)) have been identified. The synthesis, structure-activity relationships and selectivity against several other ion channels are described. ...

journal_title：Bioorganic & medicinal chemistry letters

authors： Vaccaro W,Huynh T,Lloyd J,Atwal K,Finlay HJ,Levesque P,Conder ML,Jenkins-West T,Shi H,Sun L

更新日期：2008-12-15 00:00:00

abstract：:Novel imidazole frameworks have been identified as potent partial agonists of the alpha(1A) adrenergic receptor, with good selectivity over the alpha(1B), alpha(1D) and alpha(2A) receptor sub-types. Nitrile 28 possessed attractive CNS drug-like properties with good membrane permeability and no P-pg mediated efflux. 28...

journal_title：Bioorganic & medicinal chemistry letters

authors： Whitlock GA,Brennan PE,Roberts LR,Stobie A

更新日期：2009-06-01 00:00:00

abstract：:Five-coordinated oxovanadium(IV) complexes with ciprofloxacin and various uninegative bidentate amino acids have been prepared. The structure of complexes has been investigated using spectral, physicochemical, mass spectroscopy, and elemental analyses. The antimicrobial activities (MIC) of the complexes, ligands, meta...

journal_title：Bioorganic & medicinal chemistry letters

authors： Patel MN,Patel SH,Chhasatia MR,Parmar PA

更新日期：2008-12-15 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 have synthesized and tested novel quinuclidinone analogs to assay the effects on H1299 lung cancer cell lines alone or with gamma-radiation. We have found two series of quinuclidinone analogs that act as anti-cancer agents. Of these, four interesting analogs significantly decreased cell viability in H1299 lung canc...

journal_title：Bioorganic & medicinal chemistry letters

authors： Malki A,Pulipaka AB,Evans SC,Bergmeier SC

更新日期：2006-03-01 00:00:00

abstract：:Triple-negative breast cancer (TNBC) has been reported to be correlated with high expression of proliferation markers as well as constitutive activation of metastasis-relevant signaling pathways. For many years, breast cancer researchers have been investigating specific and effective methods to treat or to control the...

journal_title：Bioorganic & medicinal chemistry letters

authors： Chen L,Long C,Nguyen J,Kumar D,Lee J

更新日期：2018-02-01 00:00:00

abstract：:The discovery and optimization of a novel series of prolinol-derived GHSR agonists is described. This series emerged from a 11,520-member solid-phase library targeting the GPCR protein superfamily, and the rapid optimization of low micromolar hits into single-digit nanomolar leads can be attributed to the solid-phase ...

journal_title：Bioorganic & medicinal chemistry letters

authors： Zhai W,Flynn N,Longhi DA,Tino JA,Murphy BJ,Slusarchyk D,Gordon DA,Pendri A,Shi S,Stoffel R,Ma B,Sofia MJ,Gerritz SW

更新日期：2008-09-15 00:00:00

abstract：:Nineteen new 2-pyrazoline bearing benzenesulfonamide derivatives were synthesized by condensing chalcones with 4-hydrazinonbenzenesulfonamide hydrochloride. Their chemical structures were proved by means of IR, (1)H NMR, (13)C NMR, mass spectroscopic and elemental analyses data. These compounds were tested at dose of ...

journal_title：Bioorganic & medicinal chemistry letters

authors： Rathish IG,Javed K,Ahmad S,Bano S,Alam MS,Pillai KK,Singh S,Bagchi V

更新日期：2009-01-01 00:00:00

abstract：:Water is an essential part of protein binding sites and mediates interactions to ligands. Its displacement by ligand parts affects the free binding energy of resulting protein-ligand complexes. Therefore the characterization of solvation properties is important for design. Of particular interest is the propensity of l...

journal_title：Bioorganic & medicinal chemistry letters

authors： Matter H,Güssregen S

更新日期：2018-08-01 00:00:00

abstract：:New hybrid molecules of isothiocyanate and progesterone and their metal complexes were synthesized exhibiting promising anti-proliferative and pro-apoptotic activity against breast and prostate cancer cells. These metal complex compounds exploited an existing cellular transport pathway for delivery of cytotoxic isothi...

journal_title：Bioorganic & medicinal chemistry letters

authors： Adsule S,Banerjee S,Ahmed F,Padhye S,Sarkar FH

更新日期：2010-02-01 00:00:00

abstract：:We report the identification of a novel biaryl template for H(+)/K(+) ATPase inhibition. Evaluation of critical SAR features within the biaryl imidazole framework and the use of pharmacophore modelling against known imidazopyridine and azaindole templates suggested that the geometry of the molecule is key to achieving...

journal_title：Bioorganic & medicinal chemistry letters

authors： Garton N,Bailey N,Bamford M,Demont E,Farre-Gutierrez I,Hutley G,Bravi G,Pickering P

更新日期：2010-02-01 00:00:00

abstract：:In an effort to discover potent antitumor agents, a series of novel C-7-heteroaryl-substituted camptothecin derivatives were designed and synthesized via microwave-promoted Suzuki coupling reaction. These analogs were then assessed for cytotoxicity against three human tumor cell lines, A549, HCT116, HT-29, and inhibit...

journal_title：Bioorganic & medicinal chemistry letters

authors： Wang L,Huang Y,Zhang J,Tong L,Chen Y,Lu W,Huang Q

更新日期：2014-03-15 00:00:00

abstract：:DNA polymerases can efficiently and sequence selectively incorporate oligonucleotide (ODN)-modified nucleotides and the incorporated oligonucleotide strand can be employed as primer in rolling circle amplification (RCA). The effective amplification of the DNA primer by Φ29 DNA polymerase allows the sequence-selective ...

journal_title：Bioorganic & medicinal chemistry letters

authors： Verga D,Welter M,Marx A

更新日期：2016-02-01 00:00:00

abstract：:Glutathione reductase (GR), is responsible for the existence of GSH molecule, a crucial antioxidant against oxidative stress reagents. The antimalarial activities of some redox active compounds are attributed to their inhibition of antioxidant flavoenzyme glutathione reductase, and inhibitors are therefore expected to...

journal_title：Bioorganic & medicinal chemistry letters

authors： Sentürk M,Talaz O,Ekinci D,Cavdar H,Küfrevioğlu OI

更新日期：2009-07-01 00:00:00

abstract：:The synthesis and biological properties of a novel water-soluble echinocandin-like lipopeptide, FR131535, are described. This compound displayed potent in vitro and in vivo antifungal activities. The hemolytic activity of FR901379 was reduced by replacing the acyl side chain. This compound showed good water-solubility...

journal_title：Bioorganic & medicinal chemistry letters

authors： Fujie A,Iwamoto T,Sato B,Muramatsu H,Kasahara C,Furuta T,Hori Y,Hino M,Hashimoto S

更新日期：2001-02-12 00:00:00

abstract：:C-Mannosyl residue-containing trimannose ManC alpha(1,6)[Man alpha(1,3)Man] (2) and 5-thio-C mannosyl residue-containing trimannose 5SManC alpha(1,6)[Man alpha(1,3)Man] (3) were synthesized via a glycosyl radical addition to enone derivative of mannose (6). Dissociation constants for the binding of these trisaccharide...

journal_title：Bioorganic & medicinal chemistry letters

authors： Tsuruta O,Yuasa H,Kurono S,Hashimoto H

更新日期：1999-03-22 00:00:00

abstract：:The DBU-promoted intramolecular aldol condensation of two partially protected L-lyxo-hexos-5-ulose derivatives (8 and 9), in turn obtained starting from methyl beta-D-galactopyranoside, takes place with fairly good yield and complete diastereoselectivity to give 2L-(2,3,6/4,5)-pentahydroxycyclohexanone derivatives, 10...

journal_title：Bioorganic & medicinal chemistry letters

authors： Catelani G,Corsaro A,D'Andrea F,Mariani M,Pistarà V

更新日期：2002-11-18 00:00:00

abstract：:A series of new HIV-1 protease inhibitors with the hydroxyethylamine core and different hydroxyprolinamide P2 ligands were designed and synthesized. Variation of substitutions at the P2 significantly affected the enzyme inhibitory potency of the inhibitors. Compounds 2a and 2d showed excellent enzyme inhibitory activi...

journal_title：Bioorganic & medicinal chemistry letters

authors： Gao BL,Zhang CM,Yin YZ,Tang LQ,Liu ZP

更新日期：2011-06-15 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