Synthesis and antihyperglycemic activity of suitably functionalized 3H-quinazolin-4-ones.

abstract：:Lamin A contributes to the structure of nuclei in all mammalian cells and plays an important role in cell division and migration. Mature lamin A is derived from a farnesylated precursor protein, known as prelamin A, which undergoes post-translational cleavage catalyzed by the zinc metalloprotease STE24 (ZPMSTE24). Acc...

journal_title：Bioorganic & medicinal chemistry

authors： Matralis AN,Xanthopoulos D,Huot G,Lopes-Paciencia S,Cole C,de Vries H,Ferbeyre G,Tsantrizos YS

更新日期：2018-11-01 00:00:00

abstract：:Antisense oligonucleotides (AS-ODNs) specifically hybridize with target mRNAs, resulting in interference with the splicing mechanism or the regulation of protein translation. In our previous reports, we demonstrated that β-glucan schizophyllan (SPG) can form a complex with AS-ODNs attached with oligo deoxyadenosine dA...

journal_title：Bioorganic & medicinal chemistry

authors： Sasaki S,Izumi H,Morimoto Y,Sakurai K,Mochizuki S

更新日期：2020-09-15 00:00:00

abstract：:Isoflavones are bioactive compounds that have been shown to decrease lipid accumulation in vitro. However, the knowledge of the isoflavone formononetin is limited. The aim of the study was to assess the effects of formononetin and its two synthetic analogues, 2-(2-bromophenyl)-formononetin and 2-heptyl-formononetin, o...

journal_title：Bioorganic & medicinal chemistry

authors： Andersen C,Kotowska D,Tortzen CG,Kristiansen K,Nielsen J,Petersen RK

更新日期：2014-11-01 00:00:00

abstract：:In continuation of our efforts toward identification and optimization of novel non-nucleoside reverse transcriptase inhibitors (NNRTIs), we have employed a structure-based bioisosterism strategy, with which a new series of diarylpyridazine (DAPD) derivatives were synthesized and evaluated for their anti-HIV-1 (human i...

journal_title：Bioorganic & medicinal chemistry

authors： Li D,Zhan P,Liu H,Pannecouque C,Balzarini J,De Clercq E,Liu X

更新日期：2013-04-01 00:00:00

abstract：:Novel 4-amino-2-phenylpyrimidine derivatives were synthesized and evaluated as GPR119 agonists. Optimization of the substituents on the phenyl ring at the 2-position and the amino group at the 4-position led to the identification of 3,4-dihalogenated and 2,4,5-trihalogenated phenyl derivatives showing potent GPR119 ag...

journal_title：Bioorganic & medicinal chemistry

authors： Negoro K,Yonetoku Y,Misawa-Mukai H,Hamaguchi W,Maruyama T,Yoshida S,Takeuchi M,Ohta M

更新日期：2012-09-01 00:00:00

abstract：:A novel scaffold system for the generation of diversity libraries has been designed which allows for rapid modification not only of functional groups, but their spatial arrangements as well. The biphenyl scaffold allows for display of three or four diverse functional groups in a wide variety of spatial arrangements de...

journal_title：Bioorganic & medicinal chemistry

authors： Pavia MR,Cohen MP,Dilley GJ,Dubuc GR,Durgin TL,Forman FW,Hediger ME,Milot G,Powers TS,Sucholeiki I,Zhou S,Hangauer DG

更新日期：1996-05-01 00:00:00

abstract：:Multidrug-resistant bacterial infections continue to be a rising global health concern. Herein is described the development of a class of novel 2-aminobenzimidazoles with antibiotic activity. These active 2-aminobenzimidazoles retain their antibiotic activity against several strains of multidrug-resistant Staphylococc...

journal_title：Bioorganic & medicinal chemistry

authors： Huigens RW 3rd,Reyes S,Reed CS,Bunders C,Rogers SA,Steinhauer AT,Melander C

更新日期：2010-01-15 00:00:00

abstract：:A novel series of 6-hydroxy-3-morpholinones, in which the functional aldehyde and the hydroxy group of P(2) site form a cyclic hemiacetal, was identified as calpain inhibitors. The placement of isobutyl group at the 2-position of the 3-morpholinone was the most effective modification for inhibiting micro- and m-calpai...

journal_title：Bioorganic & medicinal chemistry

authors： Nakamura M,Miyashita H,Yamaguchi M,Shirasaki Y,Nakamura Y,Inoue J

更新日期：2003-12-01 00:00:00

abstract：:Here we describe the design, synthesis, and pharmacological evaluation of a set of compounds structurally related to the high affinity serotonin 5-HT7 receptor agonist N-(4-cyanophenylmethyl)-4-(2-diphenyl)-1-piperazinehexanamide (6, LP-211). Specific structural modifications were performed in order to maintain affini...

journal_title：Bioorganic & medicinal chemistry

authors： Lacivita E,Niso M,Hansen HD,Di Pilato P,Herth MM,Lehel S,Ettrup A,Montenegro L,Perrone R,Berardi F,Colabufo NA,Leopoldo M,Knudsen GM

更新日期：2014-03-01 00:00:00

abstract：:Tryprostatin A is an inhibitor of breast cancer resistance protein, consequently a series of structure-activity studies on the cell cycle inhibitory effects of tryprostatin A analogues as potential antitumor antimitotic agents have been carried out. These analogues were assayed for their growth inhibition properties a...

journal_title：Bioorganic & medicinal chemistry

authors： Jain HD,Zhang C,Zhou S,Zhou H,Ma J,Liu X,Liao X,Deveau AM,Dieckhaus CM,Johnson MA,Smith KS,Macdonald TL,Kakeya H,Osada H,Cook JM

更新日期：2008-04-15 00:00:00

abstract：:Three new derivatives of 2-substituted 1,3,4-thiadiazole-5-sulfonamide have been synthesized. These compounds are 2-(3-chloropropionylamino)-1,3,4-thiadiazole-5-sulfonamide (1); 2-(2,2-dichloroacetylamino)-1,3,4-thiadiazole-5-sulfonamide (2); and 2-(3-phenylpropionylamino)-1,3,4-thiadiazole-5-sulfonamide (3). Inhibiti...

journal_title：Bioorganic & medicinal chemistry

authors： Arslan O,Küfrevioĝlu OI,Nalbantoĝlu B

更新日期：1997-03-01 00:00:00

abstract：:3-Amino-2-hydroxy-propionaldehydes [H2NCH(R)CHOHCHO with R = H, i-Bu, CH2Ph] were designed as metallo-aminopeptidase inhibitors based on the metal active site chelation concept. These compounds were found to be micromolar inhibitors of aminopeptidase-M (AP-M, EC 3.4.11.2) with potencies similar to bestatin (Ki = 3.5 m...

journal_title：Bioorganic & medicinal chemistry

authors： Tarnus C,Rémy JM,d'Orchymont H

更新日期：1996-08-01 00:00:00

abstract：:2-Guanadino-3-cyanopyridines 8-33 and pyrido[2,3-d]-pyrimidines 35-52 were synthesized by nucleophilic displacement and cyclization of the chloroamidines 6a-d easily obtained by reaction of 2-aminocyanopyridines 5a-d with phosgene iminium chloride and their action on the release of histamine by mast cells examined und...

journal_title：Bioorganic & medicinal chemistry

authors： Quintela JM,Peinador C,Botana L,Estévez M,Riguera R

更新日期：1997-08-01 00:00:00

abstract：:Protein tyrosine phosphatases (PTPs) are important in the regulation of signal transduction processes. Certain enzymes of this class are considered as potential therapeutic targets in the treatment of a variety of diseases such as diabetes, inflammation, and cancer. However, many PTP inhibitors identified to date are ...

journal_title：Bioorganic & medicinal chemistry

authors： Huang P,Ramphal J,Wei J,Liang C,Jallal B,McMahon G,Tang C

更新日期：2003-04-17 00:00:00

abstract：:A series of ophiobolins were isolated from a fungal extract based on their nematocidal activity. These compounds are non-competitive inhibitors of ivermectin binding to membranes prepared from the free-living nematode, Caenorhabditis elegans, with an inhibition constant of 15 microM. The ophiobolins which were most po...

journal_title：Bioorganic & medicinal chemistry

authors： Tsipouras A,Adefarati AA,Tkacz JS,Frazier EG,Rohrer SP,Birzin E,Rosegay A,Zink DL,Goetz MA,Singh SB,Schaeffer JM

更新日期：1996-04-01 00:00:00

abstract：:Matrix metalloproteinases are implicated in a wide range of pathophysiological processes and potent selective inhibitors for these enzymes continue to be eagerly sought. 5,5-Disubstituted barbiturates hold promise as inhibitor types being stable in vivo and relatively selective for the gelatinases (MMP-2 and MMP-9). I...

journal_title：Bioorganic & medicinal chemistry

authors： Wang J,Medina C,Radomski MW,Gilmer JF

更新日期：2011-08-15 00:00:00

abstract：:A new structural scaffold for antiestrogens was identified from the cell-based screening of transcriptional regulation properties of a 67-member library of homoallylic amides, allylic amides, and C-cyclopropylalkylamides. C-Cyclopropylalkylamide 3a (O-ethyl-N-{2-[(1S*,2R*)-2-{(R*)-[(diphenylphosphinoyl)amino](phenyl)m...

journal_title：Bioorganic & medicinal chemistry

authors： Janjic JM,Mu Y,Kendall C,Stephenson CR,Balachandran R,Raccor BS,Lu Y,Zhu G,Xie W,Wipf P,Day BW

更新日期：2005-01-03 00:00:00

abstract：:With the aim of finding new chemical entities selective for fish pathogens to avoid drug resistance in humans, a series of coumarin-chalcone hybrid compounds with different patterns of substitution were designed and synthesized. Their antibacterial activity was evaluated against important types of human bacteria strai...

journal_title：Bioorganic & medicinal chemistry

authors： Vazquez-Rodriguez S,Lama López R,Matos MJ,Armesto-Quintas G,Serra S,Uriarte E,Santana L,Borges F,Muñoz Crego A,Santos Y

更新日期：2015-11-01 00:00:00

abstract：:The physiology of the oxytocin receptor has increasingly become a focus of scientific investigation due to its connection with social behavior and psychiatric disorders with impairments in social funciton. Experimental utilization of small molecule and peptide antagonists for the oxytocin receptor has played a role in...

journal_title：Bioorganic & medicinal chemistry

authors： Smith AL,Walum H,Connor-Stroud F,Freeman SM,Inoue K,Parr LA,Goodman MM,Young LJ

更新日期：2017-01-01 00:00:00

abstract：:Four palladium(II) and platinum(II) saccharinate (sac) complexes with 2-(hydroxymethyl)pyridine (2-hmpy) and 2-(2-hydroxyethyl)pyridine (2-hepy), namely trans-[Pd(2-hmpy)2(sac)2]·H2O (1), trans-[Pt(2-hmpy)2(sac)2]·3H2O (2), trans-[Pd(2-hepy)2(sac)2] (3) and trans-[Pt(2-hepy)2(sac)2] (4), have been synthesized and char...

journal_title：Bioorganic & medicinal chemistry

authors： Ari F,Aztopal N,Icsel C,Yilmaz VT,Guney E,Buyukgungor O,Ulukaya E

更新日期：2013-11-01 00:00:00

abstract：:A series of 1-substituted-3(5)-(6-methylpyridin-2-yl)-4-(quinolin-6-yl)pyrazoles 14a-e, 15a-e, 17a-c, and 18a-d have been synthesized and evaluated for their ALK5 inhibitory activity in an enzyme assay and in a cell-based luciferase reporter assay. The 6-quinolinyl pyrazole analogue 14b inhibited ALK5 phosphorylation ...

journal_title：Bioorganic & medicinal chemistry

authors： Jin CH,Krishnaiah M,Sreenu D,Rao KS,Subrahmanyam VB,Park CY,Son JY,Sheen YY,Kim DK

更新日期：2011-04-15 00:00:00

abstract：:This article has been withdrawn at the request of the author(s) and/or editor. The Publisher apologizes for any inconvenience this may cause. The full Elsevier Policy on Article Withdrawal can be found at http://www.elsevier.com/locate/withdrawalpolicy. ...

journal_title：Bioorganic & medicinal chemistry

authors： Tandon V,Chhikara BS,Chandra R,Mishra AK

更新日期：2006-02-21 00:00:00

abstract：:RNA cleavage by enediyne anticancer antibiotics was shown to occur with no apparent sequence selectivity, but RNA structure appears to be important in those substrates where cleavage was observed. Neocarzinostatin (NCS) cleaved a wider variety of RNA substrates than either esperamicin (ESP) or calicheamicin (CAL), and...

journal_title：Bioorganic & medicinal chemistry

authors： Battigello JM,Cui M,Roshong S,Carter BJ

更新日期：1995-06-01 00:00:00

abstract：:The function of acid ceramidase (ACDase), whose congenital deficiency leads to Farber disease, has been recognized to be vital to tumor cell biology, and inhibition of its activity may be beneficial in cancer therapy. Therefore, manipulation of the activity of this enzyme may have significant effect, especially on can...

journal_title：Bioorganic & medicinal chemistry

authors： Bai A,Bielawska A,Rahmaniyan M,Kraveka JM,Bielawski J,Hannun YA

更新日期：2018-12-15 00:00:00

abstract：:Chronic hepatitis C virus (HCV) infections are a significant medical problem worldwide. The NS5B Polymerase of HCV plays a central role in virus replication and is a prime target for the discovery of new treatment options. We recently disclosed 1H-benzo[de]isoquinoline-1,3(2H)-diones as allosteric inhibitors of NS5B P...

journal_title：Bioorganic & medicinal chemistry

authors： Malancona S,Donghi M,Ferrara M,Martin Hernando JI,Pompei M,Pesci S,Ontoria JM,Koch U,Rowley M,Summa V

更新日期：2010-04-15 00:00:00

abstract：:The syntheses of four glyco-imidazoles, which are pentose-derivatives belonging to the D-series, as well as the syntheses of their L-enantiomers, are reported. Starting from the known linear xylo, lyxo, arabino, and ribo imidazolo-pentoses in both the L- and the D-series, intramolecular Walden inversion led to the cor...

journal_title：Bioorganic & medicinal chemistry

authors： Tschamber T,Gessier F,Dubost E,Newsome J,Tarnus C,Kohler J,Neuburger M,Streith J

更新日期：2003-08-15 00:00:00

abstract：:A new series of 2-thioether-benzothiazoles has been synthesized and evaluated for JNK inhibition. The SAR studies led to the discovery of potent, allosteric JNK inhibitors with selectivity against p38. ...

journal_title：Bioorganic & medicinal chemistry

authors： De SK,Chen LH,Stebbins JL,Machleidt T,Riel-Mehan M,Dahl R,Chen V,Yuan H,Barile E,Emdadi A,Murphy R,Pellecchia M

更新日期：2009-04-01 00:00:00

abstract：:Aryl diketoacids (ADK) and their bioisosteres are among the most promising HIV-1 integrase (IN) inhibitors. Previously, we designed a series of ADK dimers as a new class of IN inhibitors that were hypothesized to target two divalent metal ions on the active site of IN. Herein we present a further structure-activity re...

journal_title：Bioorganic & medicinal chemistry

authors： Zeng LF,Jiang XH,Sanchez T,Zhang HS,Dayam R,Neamati N,Long YQ

更新日期：2008-08-15 00:00:00

abstract：:C1027 is a potent antitumor agent that damages DNA. It has the unusual ability to produce double strand breaks and interstrand cross-links (ICLs) intracellularly, which enable it to initiate concurrent ataxia-telangiestasia mutated (ATM) and Rad-3 related (ATR) independent damage responses. The latter form of damage i...

journal_title：Bioorganic & medicinal chemistry

authors： San Pedro JM,Beerman TA,Greenberg MM

更新日期：2012-08-01 00:00:00

abstract：:The organoselenium antioxidant 1 was previously found to act as a catalytic antioxidant in a two-phase lipid peroxidation system. In aqueous environment, selenide 1 quenched ABTS-radicals more efficiently than Trolox and ascorbic acid. The selenide dose-dependently scavenged reactive oxygen and nitrogen species more e...

journal_title：Bioorganic & medicinal chemistry

authors： Johansson H,Svartström O,Phadnis P,Engman L,Ott MK

更新日期：2010-03-01 00:00:00