Melanocortin subtype-4 receptor agonists containing a piperazine core with substituted aryl sulfonamides.

abstract：:A series of flavonoid analogues were synthesized and screened for the in vitro antioxidant activity through their ability to quench 1,1-diphenyl-2-picryl hydrazyl (DPPH) radical. The activity of these compounds, measured in comparison to the well-known standard antioxidants (29-32), their precursors (38-42) and other ...

journal_title：Bioorganic & medicinal chemistry letters

authors： Das S,Mitra I,Batuta S,Niharul Alam M,Roy K,Begum NA

更新日期：2014-11-01 00:00:00

abstract：:The increase in the prevalence of multi drug-resistant and extensively drug-resistant strains of Mycobacteriumtuberculosis case demonstrates the urgent need of discovering new promising compounds with antimycobacterial activity. As part of our research program and with a aim of identifying new antitubercular drug cand...

journal_title：Bioorganic & medicinal chemistry letters

authors： Alegaon SG,Alagawadi KR,Sonkusare PV,Chaudhary SM,Dadwe DH,Shah AS

更新日期：2012-03-01 00:00:00

abstract：:A series of 6-hydroxy-7-methoxy-4-chromanone- (2a-e) and chroman-2-carboxamides (3a-e) were synthesized and their antioxidant activities were evaluated. While compounds 2a-e were less active, compounds 3a-e exhibited more potent inhibition of lipid peroxidation initiated by Fe(2+) and ascorbic acid in rat brain homoge...

journal_title：Bioorganic & medicinal chemistry letters

authors： Lee H,Lee K,Jung JK,Cho J,Theodorakis EA

更新日期：2005-06-02 00:00:00

abstract：:Analysis of the enantiomers of rosiglitazone in a PPAR gamma binding assay suggests that the (S)-(-)-isomer is responsible for the antidiabetic activity. ...

journal_title：Bioorganic & medicinal chemistry letters

authors： Parks DJ,Tomkinson NC,Villeneuve MS,Blanchard SG,Willson TM

更新日期：1998-12-15 00:00:00

abstract：:Four new lanostane triterpenes, butyl lucidenate P (1), butyl lucidenate D(2) (2), butyl lucidenate E(2) (3) and butyl lucidenate Q (4) along with 11 known compounds (5-15) were isolated from the fruiting bodies of Ganoderma lucidum. Their chemical structures were established mainly by 1D and 2D NMR techniques and mas...

journal_title：Bioorganic & medicinal chemistry letters

authors： Tung NT,Cuong TD,Hung TM,Lee JH,Woo MH,Choi JS,Kim J,Ryu SH,Min BS

更新日期：2013-03-01 00:00:00

abstract：:The reaction between methanethiosulfonate reagents and cysteine mutants of subtilisin is quantitative and can be used to prepare chemically modified mutant enzymes (CMMs) with novel properties. The virtually unrestricted structural variations possible for CMMs presents a preparative and screening challenge. To address...

journal_title：Bioorganic & medicinal chemistry letters

authors： Plettner E,Khumtaveeporn K,Shang X,Jones JB

更新日期：1998-09-08 00:00:00

abstract：:The synthesis of bis-ortho-alkoxy-para-piperazinesubstituted-2,4-dianilinopyrimidines is described and their structure-activity-relationship to anaplastic lymphoma kinase (ALK) is presented. KRCA-0008 is selective and potent to ALK and Ack1, and displays drug-like properties without hERG liability. KRCA-0008 demonstra...

journal_title：Bioorganic & medicinal chemistry letters

authors： Park CH,Choe H,Jang IY,Kwon SY,Latif M,Lee HK,Lee HJ,Yang EH,Yun JI,Chae CH,Cho SY,Choi SU,Ha JD,Jung H,Kim HR,Kim P,Lee CO,Yun CS,Lee K

更新日期：2013-11-15 00:00:00

abstract：:In continuation of our efforts to find new antimicrobial compounds, series of fatty N-acyldiamines were prepared from fatty methyl esters and 1,2-ethylenediamine, 1,3-propanediamine or 1,4-butanediamine. The synthesized compounds were screened for their antibacterial activity against Gram-positive bacteria (Staphyloco...

journal_title：Bioorganic & medicinal chemistry letters

authors： Ferreira BDS,de Almeida AM,Nascimento TC,de Castro PP,Silva VL,Diniz CG,Le Hyaric M

更新日期：2014-10-01 00:00:00

abstract：:A new abietane, namely, 20-hydroxyferruginol (1), together with known ferruginol (2), 18-hydroxyferruginol (3), sugiol (4), and 6alpha-hydroxysugiol (5), were isolated from the cones of Sequoia sempervirens. Their structures were elucidated through spectral data. Compounds 1 and 5 strongly inhibited colon, lung, and b...

journal_title：Bioorganic & medicinal chemistry letters

authors： Son KH,Oh HM,Choi SK,Han DC,Kwon BM

更新日期：2005-04-15 00:00:00

abstract：:Benz[b]oxepines 4a-g and 12-oxobenzo[c]phenanthridines 5a-d were designed and synthesized as constrained forms of 3-arylisoquinolines through an intramolecular radical cyclization reaction. Radical cyclization of O-vinyl compounds preferentially led to the 7-endo-trig cyclization pathway to the benz[b]oxepines and 12-...

journal_title：Bioorganic & medicinal chemistry letters

authors： Lee SH,Van HT,Yang SH,Lee KT,Kwon Y,Cho WJ

更新日期：2009-05-01 00:00:00

abstract：:A series of 6,7-diphenyl-2,3,8,8a-tetrahydro-1H-indolizin-5-one analogues were synthesized and evaluated for cytotoxic activity against eight human cancer cell lines. Compounds 18, 21, 28, 29, 30 and 31 showed cytotoxic activity with GI(50) values in the range of 2.1-8.1 microM concentration. Among these, compounds 21...

journal_title：Bioorganic & medicinal chemistry letters

authors： Sharma VM,Adi Seshu KV,Vamsee Krishna C,Prasanna P,Chandra Sekhar V,Venkateswarlu A,Rajagopal S,Ajaykumar R,Deevi DS,Rao Mamidi NV,Rajagopalan R

更新日期：2003-05-19 00:00:00

abstract：:Retinoids are analogues of all-trans-retinoic acid, a powerful hormone that mediates many fundamental biological processes. Cancer and other serious hyperproliferative diseases are attractive therapeutic targets for retinoids, but the therapeutic use of retinoids is limited due to severe toxicity. We report here the d...

journal_title：Bioorganic & medicinal chemistry letters

authors： Beard RL,Duong TT,Teng M,Klein ES,Standevan AM,Chandraratna RA

更新日期：2002-11-04 00:00:00

abstract：:A series of (N-benzyl-N-phenylsulfonamido)alkyl amides were developed from classic and parallel synthesis strategies. Compounds with good in vitro and in vivo γ-secretase activity were identified and described. ...

journal_title：Bioorganic & medicinal chemistry letters

authors： Parker MF,Barten DM,Bergstrom CP,Bronson JJ,Corsa JA,Dee MF,Gai Y,Guss VL,Higgins MA,Keavy DJ,Loo A,Mate RA,Marcin LR,McElhone KE,Polson CT,Roberts SB,Macor JE

更新日期：2012-11-15 00:00:00

abstract：:A novel conjugate of Hoechst 33258, pyrene and neomycin was synthesized and examined for its binding and stabilization of A-T rich DNA duplexes using spectroscopic and viscometric techniques. The conjugate, containing three well known ligands that bind nucleic acids albeit in different binding modes, was found to sign...

journal_title：Bioorganic & medicinal chemistry letters

authors： Willis B,Arya DP

更新日期：2009-09-01 00:00:00

abstract：:The structural modification of the benzylic ether region of oxime 1 has resulted in the identification of several novel aryl amides as selective or dual NK(1)/NK(2) antagonists. ...

journal_title：Bioorganic & medicinal chemistry letters

authors： Shih NY,Albanese M,Anthes JC,Carruthers NI,Grice CA,Lin L,Mangiaracina P,Reichard GA,Schwerdt J,Seidl V,Wong SC,Piwinski JJ

更新日期：2002-01-21 00:00:00

abstract：:Polysulfides typically react readily with thiols, thus, reactions of endogenous cellular thiols with the polysulfide linkage in naturally-occuring pentathiepin cytotoxins are likely to be an important aspect of their biological chemistry. Here, it is reported that the reaction of thiols with the pentathiepin ring syst...

journal_title：Bioorganic & medicinal chemistry letters

authors： Chatterji T,Gates KS

更新日期：2003-04-07 00:00:00

abstract：:Clausenamide, isolated from aqueous extract of dry leaves of Clausena lansium, a Chinese folk medicine, was found to have potent activity in enhancing LTP and show nootropic activity in animal tests. In order to discovery more potent stereoisomers and to analyze the relationship of structure-activity, the synthesis of...

journal_title：Bioorganic & medicinal chemistry letters

authors： Feng Z,Li X,Zheng G,Huang L

更新日期：2009-04-15 00:00:00

abstract：:We report a fluorinated and iodinated radiotracer as a probe for PET/SPECT to detect of β-amyloid (Aβ) plaques in the brain of patients with Alzheimer's disease (AD). We successfully designed and synthesized the fluorinated and iodinated aurone derivative (3) and its radiolabels ([(125)I]3 and [(18)F]3). In binding ex...

journal_title：Bioorganic & medicinal chemistry letters

authors： Watanabe H,Ono M,Kimura H,Kagawa S,Nishii R,Fuchigami T,Haratake M,Nakayama M,Saji H

更新日期：2011-11-01 00:00:00

abstract：:Current techniques for the identification of DNA adduct-inducing and DNA interstrand crosslinking agents include electrophoretic crosslinking assays, electrophoretic gel shift assays, DNA and RNA stop assays, mass spectrometry-based methods and 32P-post-labelling. While these assays provide considerable insight into t...

journal_title：Bioorganic & medicinal chemistry letters

authors： Medan J,Sleebs BE,Lackovic K,Watson KG,Evison BJ,Phillips DR,Cutts SM

更新日期：2021-01-21 00:00:00

abstract：:Four platinum(II) complexes of N-cyclobutyl-1R,2R-diaminocyclohexane with different bidentate dicarboxylates (1 oxalate, 2 malonate, 3 1,1-cyclobutanedicarboxylate and 4 3-hydroxy-1,1-cyclobutanedicarboxylate) as leaving groups were synthesized and characterized by elemental analyses, IR and (1)HNMR spectra together w...

journal_title：Bioorganic & medicinal chemistry letters

authors： Xu G,Zhao J,Gou S,Pang J

更新日期：2015-01-15 00:00:00

abstract：:2-Octyl gamma-bromoacetoacetate (O gamma Br), an endogenous compound originally isolated from human cerebrospinal fluid (CSF), has previously been demonstrated to increase REM sleep duration in cats. Based on the chemical structure of O gamma Br and its reported sleep-inducing effects, we synthesized O gamma Br along ...

journal_title：Bioorganic & medicinal chemistry letters

authors： Patricelli MP,Patterson JE,Boger DL,Cravatt BF

更新日期：1998-03-17 00:00:00

abstract：:A series of 1-isoquinolinylguanidines are shown to be potent inhibitors of uPA with selectivity over tPA and plasmin. Potency is enhanced by the presence of a 4-halo and a 7-aryl substituent, particularly when substituted by a 3-carboxylic acid group. Compound 13j (UK-356,202) combines excellent potency and selectivit...

journal_title：Bioorganic & medicinal chemistry letters

authors： Barber CG,Dickinson RP,Fish PV

更新日期：2004-06-21 00:00:00

abstract：:A series of alisol A derivatives were synthesized and evaluated for their anti-hepatitis B virus (HBV) activities and cytotoxicities in vitro. The preliminary investigation demonstrates that simple modifications of the parent structure of alisol A can produce a number of potentially important derivatives against HBV. ...

journal_title：Bioorganic & medicinal chemistry letters

authors： Zhang Q,Jiang ZY,Luo J,Cheng P,Ma YB,Zhang XM,Zhang FX,Zhou J,Chen JJ

更新日期：2008-08-15 00:00:00

abstract：:The reaction mechanisms of hypochlorous acid (HOCl) with several tryptophan and tryptamine derivatives, previously reported to scavenge this powerful oxidant, was investigated to determine whether ionic or radical pathways were involved. For this purpose, the reaction of tryptamine and tryptophan derivatives with HOCl...

journal_title：Bioorganic & medicinal chemistry letters

authors： Carvalho LC,Estevão MS,Ferreira LM,Fernandes E,Marques MM

更新日期：2010-11-15 00:00:00

abstract：:Bacterial quorum sensing is mediated by autoinducers, small signaling molecules generated by bacteria. It has been proposed that the LuxS enzyme converts S-ribosyl-L-homocysteine to 4,5-dihydroxy-2,3-pentanedione, the precursor of autoinducer 2 (AI-2). We report here a chemical synthesis of S-ribosyl-L-homocysteine an...

journal_title：Bioorganic & medicinal chemistry letters

authors： Zhao G,Wan W,Mansouri S,Alfaro JF,Bassler BL,Cornell KA,Zhou ZS

更新日期：2003-11-17 00:00:00

abstract：:Four new polyphenols namely excoecariphenols A-D (1-4) were isolated from the Chinese mangrove plant Excoecaria agallocha L. together with 23 known phenolic compounds. The structures of new compounds were elucidated on the basis of extensive spectroscopic analyses including IR, MS, NMR, and CD data. Excoecariphenols A...

journal_title：Bioorganic & medicinal chemistry letters

authors： Li Y,Yu S,Liu D,Proksch P,Lin W

更新日期：2012-01-15 00:00:00

abstract：:4-(Substituted-benzylidine)-2-substituted-5,6-dihydrobenzo[h]quinazoline (5a-p) and 4-(substituted-benzylidine)-2-substituted-3, 4, 5, 6-tetrahydrobenzo[h]quinazoline (6a-p) have been synthesized from 2-(substituted-benzylidine)tetralone-1(3a-d) and several substituted guanidine sulfates(4a-d).These compounds were tes...

journal_title：Bioorganic & medicinal chemistry letters

authors： Agarwal KC,Sharma V,Shakya N,Gupta S

更新日期：2009-09-15 00:00:00

abstract：:Optimization of clearance of adenosine inhibitors of bacterial NAD(+)-dependent DNA ligase is discussed. To reduce Cytochrome P-450-mediated metabolic clearance, many strategies were explored; however, most modifications resulted in compounds with reduced antibacterial activity and/or unchanged total clearance. The al...

journal_title：Bioorganic & medicinal chemistry letters

authors： Stokes SS,Gowravaram M,Huynh H,Lu M,Mullen GB,Chen B,Albert R,O'Shea TJ,Rooney MT,Hu H,Newman JV,Mills SD

更新日期：2012-01-01 00:00:00

abstract：:Chimeric molecules which effect intracellular degradation of target proteins via E3 ligase-mediated ubiquitination (e.g., PROTACs) are currently of high interest in medicinal chemistry. However, these entities are relatively large compounds that often possess molecular characteristics which may compromise oral bioavai...

journal_title：Bioorganic & medicinal chemistry letters

authors： Dragovich PS,Adhikari P,Blake RA,Blaquiere N,Chen J,Cheng YX,den Besten W,Han J,Hartman SJ,He J,He M,Rei Ingalla E,Kamath AV,Kleinheinz T,Lai T,Leipold DD,Li CS,Liu Q,Lu J,Lu Y,Meng F,Meng L,Ng C,Peng K,Le

更新日期：2020-02-15 00:00:00

abstract：:Several strychnobrasiline derivatives have been synthesized to overcome the lack of in vivo reversal activity of the parent compound. In the present study, N(a)-deacetyl-ferrocenoyl-strychnobrasiline was synthesized by condensing N(a)-deacetyl-strychnobrasiline with ferrocenic acid previously treated with oxalyl chlor...

journal_title：Bioorganic & medicinal chemistry letters

authors： Razafimahefa D,Pélinski L,Martin MT,Ramanitrahasimbola D,Rasoanaivo P,Brocard J

更新日期：2005-02-15 00:00:00