Novel BACE1 inhibitors with a non-acidic heterocycle at the P1' position.

abstract：:We report the synthesis and the functional studies of multiple crown alpha-helical peptides designed to form artificial ion channels. The approach combines the versatility of solid phase peptide synthesis, the conformational predictability of peptidic molecules, and the solution synthesis of crown ethers with engineer...

journal_title：Bioorganic & medicinal chemistry

authors： Biron E,Otis F,Meillon JC,Robitaille M,Lamothe J,Van Hove P,Cormier ME,Voyer N

更新日期：2004-03-15 00:00:00

abstract：:By means of QSAR algorithms we model the potency pIC(90) [mM] of 154 non-nucleoside reverse transcriptase inhibitors (NNRTI) of the wild-type HIV-1 virus, considered as the second generation analogues of Efavirenz. In addition, 56 inhibitors of the K-103N viral mutant form are also investigated. A pool of 1494 theoret...

journal_title：Bioorganic & medicinal chemistry

authors： Duchowicz PR,Fernández M,Caballero J,Castro EA,Fernández FM

更新日期：2006-09-01 00:00:00

abstract：:A series of novel pyrroles, pyrrolopyrimidines, pyrazolopyrrolopyrimidine, triazolopyrrolopyrimidines, tetrazolopyrrolopyrimidine, triazinopyrrolopyrimidines and pyrrolopyrimidotriazepines bearing the biologically active benzenesulfonamide moiety were synthesized by using pyrrole-o-amino-carbonitrile as key intermedia...

journal_title：Bioorganic & medicinal chemistry

authors： Ghorab MM,Alsaid MS,Ceruso M,Nissan YM,Supuran CT

更新日期：2014-07-15 00:00:00

abstract：:Carbonic anhydrases (CAs, EC 4.2.1.1) are zinc enzymes acting as efficient catalysts for the reversible hydration of carbon dioxide to bicarbonate. 16 different alpha-CA isoforms were isolated in mammals, where they play crucial physiological roles. Some of them are cytosolic (CA I, CA II, CA III, CA VII, CA XIII), ot...

journal_title：Bioorganic & medicinal chemistry

authors： Supuran CT,Scozzafava A

更新日期：2007-07-01 00:00:00

abstract：:FAAH inhibitors offer safety advantages by augmenting the anandamide levels "on demand" to promote neuroprotective mechanisms without the adverse psychotropic effects usually seen with direct and chronic activation of the CB1 receptor. FAAH is an enzyme implicated in the hydrolysis of the endocannabinoid N-arachidonoy...

journal_title：Bioorganic & medicinal chemistry

authors： Lamani M,Malamas MS,Farah SI,Shukla VG,Almeida MF,Weerts CM,Anderson J,Wood JT,Farizatto KLG,Bahr BA,Makriyannis A

更新日期：2019-12-01 00:00:00

abstract：:Glucose flux through glucokinase (GK) controls insulin release from the pancreas in response to high levels of glucose. Flux through GK is also responsible for reducing hepatic glucose output. Since many individuals with type 2 diabetes appear to have an inadequacy or defect in one or both of these processes, identify...

journal_title：Bioorganic & medicinal chemistry

authors： Hinklin RJ,Baer BR,Boyd SA,Chicarelli MD,Condroski KR,DeWolf WE Jr,Fischer J,Frank M,Hingorani GP,Lee PA,Neitzel NA,Pratt SA,Singh A,Sullivan FX,Turner T,Voegtli WC,Wallace EM,Williams L,Aicher TD

更新日期：2020-01-01 00:00:00

abstract：:Despite the serious public health problems caused by Chagas disease in several countries, the available therapy remains with only two drugs that are poorly active during the chronic phase of the disease in addition to having severe side effects. In search of new trypanocidal agents, herein we describe the synthesis an...

journal_title：Bioorganic & medicinal chemistry

authors： Ribeiro JLS,Soares JCAV,Portapilla GB,Providello MV,Lima CHS,Muri EMF,de Albuquerque S,Dias LRS

更新日期：2021-01-01 00:00:00

abstract：:The role of novel triazine derivatives against oxidative stress exerted by hydrogen peroxide on differentiated rat pheochromocytoma (PC12) cell line was examined and a consistent protection from H(2)O(2)-induced cell death, associated with a marked reduction in caspase-3 activation, was observed. Moreover, activation ...

journal_title：Bioorganic & medicinal chemistry

authors： Irannejad H,Amini M,Khodagholi F,Ansari N,Tusi SK,Sharifzadeh M,Shafiee A

更新日期：2010-06-15 00:00:00

abstract：:Three carboranyltetraphenylporphyrins containing 40 or 80 boron atoms were synthesized and evaluated for their biodistribution and toxicity in EMT-6 tumor-bearing mice. Copper (II) meso-5,10,15,20-tetrakis[3-methoxy-4-(o-carboranylmethoxy)phenyl]porphyrin, 6, and copper (II) meso-5,10,15,20-tetrakis[3-hydroxy-4-(o-car...

journal_title：Bioorganic & medicinal chemistry

authors： Wu H,Micca PL,Makar MS,Miura M

更新日期：2006-08-01 00:00:00

abstract：:We have previously found that T22 ([Tyr(5,12), Lys7]-polyphemusin II) has strong anti-human immunodeficiency virus (HIV) activity, and that T22 inhibits T cell-line-tropic HIV-1 infection mediated by CXCR4/fusin. T22 is an 18-residue peptide amide, which takes an antiparallel beta-sheet structure that is maintained by...

journal_title：Bioorganic & medicinal chemistry

authors： Tamamura H,Imai M,Ishihara T,Masuda M,Funakoshi H,Oyake H,Murakami T,Arakaki R,Nakashima H,Otaka A,Ibuka T,Waki M,Matsumoto A,Yamamoto N,Fujii N

更新日期：1998-07-01 00:00:00

abstract：:Aromatic alpha-amino-alpha-methyl acids and alpha-hydrazino-alpha-methyl acids are known aromatic amino acid decarboxylase inhibitors. Specific derivatives such as 2-amino-2-methyl-3-(3,4- dihydroxyphenyl)propanoate, Aldomet, and 2-hydrazino-2-methyl-3-(3,4- dihydroxyphenyl)propanoate, Lodosyn, have been developed as ...

journal_title：Bioorganic & medicinal chemistry

authors： Kallwass HK,Yee C,Blythe TA,McNabb TJ,Rogers EE,Shames SL

更新日期：1994-07-01 00:00:00

abstract：:A chemoenzymatic glycosylation remodeling method for the synthesis of selectively fluorinated glycoproteins is described. The method consists of chemical synthesis of a fluoroglycan oxazoline and its use as donor substrate for endoglycosidase (ENGase)-catalyzed transglycosylation to a GlcNAc-protein to form a homogene...

journal_title：Bioorganic & medicinal chemistry

authors： Orwenyo J,Huang W,Wang LX

更新日期：2013-08-15 00:00:00

abstract：:A series of 2-(3-aryl-2-propenoyl)-3-methylquinoxaline-1,4-dioxides 3a-l were prepared by condensation of various aryl aldehydes with 2-acetyl-3-methylquinoxaline-1,4-dioxide 2. These compounds inhibit the growth of human Molt 4/C8 and CEM T-lymphocytes and the IC(50) values are mainly in the 5-30 microM range. The qu...

journal_title：Bioorganic & medicinal chemistry

authors： Das U,Pati HN,Panda AK,De Clercq E,Balzarini J,Molnár J,Baráth Z,Ocsovszki I,Kawase M,Zhou L,Sakagami H,Dimmock JR

更新日期：2009-06-01 00:00:00

abstract：:The signal transducer and activator of transcription 3 (STAT3) is constitutively activated in cancer cells. Therefore, blocking the aberrant activity of STAT3 in tumor cells is a validated therapeutic strategy. To discover novel inhibitors of STAT3 activity, we screened against microbial natural products using a dual-...

journal_title：Bioorganic & medicinal chemistry

authors： Kim J,Lee YJ,Shin DS,Jeon SH,Son KH,Han DC,Jung SN,Oh TK,Kwon BM

更新日期：2011-12-15 00:00:00

abstract：:To streamline the preclinical phase of pharmaceutical development, we have explored the utility of structural data on the molecular target and synergy between computational and medicinal chemistry. We have concentrated on parasitic infectious diseases with a particular emphasis on the development of specific noncovale...

journal_title：Bioorganic & medicinal chemistry

authors： Li R,Chen X,Gong B,Selzer PM,Li Z,Davidson E,Kurzban G,Miller RE,Nuzum EO,McKerrow JH,Fletterick RJ,Gillmor SA,Craik CS,Kuntz ID,Cohen FE,Kenyon GL

更新日期：1996-09-01 00:00:00

abstract：:Research in recent years has demonstrated that the Trypanosoma cruzi cysteine protease cruzain (TCC) is a valid chemotherapeutic target, since inhibitors of this protease affect the pathology appropriately. By exploring the N-acylhydrazones (NAH) as privileged structures usually present in antiparasitic agents, we inv...

journal_title：Bioorganic & medicinal chemistry

authors： dos Santos Filho JM,Leite AC,de Oliveira BG,Moreira DR,Lima MS,Soares MB,Leite LF

更新日期：2009-09-15 00:00:00

abstract：:Bilirubin, biliverdin and their serum albumin complexes were tested as oxyradical scavengers (superoxide generated by the xanthine/xanthine oxidase system and peroxyl radical-trapping antioxidant ability). As superoxide scavengers the free bile pigments showed activities near to that of serum albumin, higher than the ...

journal_title：Bioorganic & medicinal chemistry

authors： Farrera JA,Jaumà A,Ribó JM,Peiré MA,Parellada PP,Roques-Choua S,Bienvenue E,Seta P

更新日期：1994-03-01 00:00:00

abstract：:Cancer is a major cause of death, and the development of new anticancer drugs is urgently needed. Invasion and metastasis are the primary causes of death due to cancer rather than growth of the primary tumor. In the current study, we examined the anti-invasive effects of p-dodecylaminophenol (1), which was developed b...

journal_title：Bioorganic & medicinal chemistry

authors： Takahashi N,Takeda K,Imai M

更新日期：2013-10-01 00:00:00

abstract：:We synthesized modified 2'-deoxyuridine triphosphates bearing amino acids at the C5 position and investigated their substrate properties for KOD Dash DNA polymerase during polymerase chain reaction (PCR). PCR using C5-modified dUTP having an amino acyl group (arginyl, histidyl, lysyl, phenylalanyl, tryptophanyl, leucy...

journal_title：Bioorganic & medicinal chemistry

authors： Kuwahara M,Hanawa K,Ohsawa K,Kitagata R,Ozaki H,Sawai H

更新日期：2006-04-15 00:00:00

abstract：:Sensing technologies based on Peptide Nucleic Acids (PNAs) and oligonucleotide-templated chemistry are perfectly suited for biomedical applications (e.g., diagnosis, prognosis and stratification of diseases) and could compete well with more traditional amplification technologies using expensive dual-labelled oligonucl...

journal_title：Bioorganic & medicinal chemistry

authors： Choi Y,Metcalf G,Sleiman MH,Vair-Turnbull D,Ladame S

更新日期：2014-08-15 00:00:00

abstract：:Microsomal prostaglandin E(2) synthase-1 (mPGES-1) has been recognized as novel, promising drug target for anti-inflammatory and anticancer drugs. mPGES-1 catalyzes the synthesis of the inducible prostaglandin E(2) in response to pro-inflammatory stimuli, rendering this enzyme extremely interesting in drug discovery p...

journal_title：Bioorganic & medicinal chemistry

authors： De Simone R,Bruno I,Riccio R,Stadler K,Bauer J,Schaible AM,Laufer S,Werz O

更新日期：2012-08-15 00:00:00

abstract：:A series of 5-(2-hydroxyphenyl)-3-substituted-2,3-dihydro-1,3,4-oxadiazole-2-thione derivatives was synthesized and 13 of them were selected by the National Cancer Institute (NCI) and evaluated for their in vitro anticancer activity. Seven of the investigated compounds, 3i, 3j, 3k, 3o, 3p, 3q, and 3r, displayed high a...

journal_title：Bioorganic & medicinal chemistry

authors： Aboraia AS,Abdel-Rahman HM,Mahfouz NM,El-Gendy MA

更新日期：2006-02-15 00:00:00

abstract：:A series of benzyloxybenzaldehyde derivatives were prepared and tested against the HL-60 cell line for anticancer activity. Preliminary structure-activity relationships were established. It was discovered that 2-(benzyloxy)benzaldehyde (17), 2-(benzyloxy)-4-methoxybenzaldehyde (26), 2-(benzyloxy)-5-methoxybenzaldehyde...

journal_title：Bioorganic & medicinal chemistry

authors： Lin CF,Yang JS,Chang CY,Kuo SC,Lee MR,Huang LJ

更新日期：2005-03-01 00:00:00

abstract：:Naphthalene melatoninergic ligands with alkyl groups (Me, Et, Pr, Bz) in the beta position of the ethylamido chain were synthesised. The affinity of the compounds for chicken brain melatonin receptors was evaluated using 2-[125I]-iodomelatonin as the radioligand. An increase in the affinity was observed with the beta-...

journal_title：Bioorganic & medicinal chemistry

authors： Mathé-Allainmat M,Le Gall M,Jellimann C,Andrieux J,Langlois M

更新日期：1999-12-01 00:00:00

abstract：:Using 3β-hydroxychol-5-en-24-oic acid (4) as starting material, the diastereoisomeric allylic alcohols (24E)-26-hydroxydesmosterol (2) and (24Z)-26-hydroxydesmosterol (3) have been synthesised in six steps with 67% and 12% overall yield, respectively. Both of these isomers are found in newborn mouse brain where sterol...

journal_title：Bioorganic & medicinal chemistry

authors： Saini R,Kataeva O,Schmidt AW,Wang Y,Meljon A,Griffiths WJ,Knölker HJ

更新日期：2013-09-15 00:00:00

abstract：:Selective targeting of RNA has become a recent priority in drug design strategies due to the emergence of retroviruses, the need for new antibiotics to counter drug resistance, and our increased awareness of the essential role RNA and RNA structures play in the progression of disease. Most organic compounds known to s...

journal_title：Bioorganic & medicinal chemistry

authors： Li K,Fernandez-Saiz M,Rigl CT,Kumar A,Ragunathan KG,McConnaughie AW,Boykin DW,Schneider HJ,Wilson WD

更新日期：1997-06-01 00:00:00

abstract：:Reverse chemical proteomics using T7 phage display is a powerful technique for identifying cellular receptors of biologically active small molecules. However, to date this method has generally been limited to cDNA libraries constructed from mRNA isolated from eukaryotes. In this paper, we describe the construction of ...

journal_title：Bioorganic & medicinal chemistry

authors： Piggott AM,Kriegel AM,Willows RD,Karuso P

更新日期：2009-10-01 00:00:00

abstract：:Maslinic acid (1) has been coupled at C-28 with several alpha- and omega-amino acids by using solution- and solid-phase synthetic procedures. Twelve derivatives (2-13) with a single amino acid residue were prepared in solution phase, whereas a dipeptide (14), a tripeptide (15), and a series of conjugate dipeptides (16...

journal_title：Bioorganic & medicinal chemistry

authors： Parra A,Rivas F,Lopez PE,Garcia-Granados A,Martinez A,Albericio F,Marquez N,Muñoz E

更新日期：2009-02-01 00:00:00

abstract：:L,L-Diaminopimelate aminotransferase (DapL) is an enzyme required for the biosynthesis of meso-diaminopimelate (m-DAP) and L-lysine (Lys) in some bacteria and photosynthetic organisms. m-DAP and Lys are both involved in the synthesis of peptidoglycan (PG) and protein synthesis. DapL is found in specific eubacterial an...

journal_title：Bioorganic & medicinal chemistry

authors： McKinnie SM,Rodriguez-Lopez EM,Vederas JC,Crowther JM,Suzuki H,Dobson RC,Leustek T,Triassi AJ,Wheatley MS,Hudson AO

更新日期：2014-01-01 00:00:00

abstract：:There is currently interest in the metabolism of the various compounds which make up the vitamin E family, especially with regards to the possible use of vitamin E metabolites as markers of oxidative stress and adequate vitamin E supply. A number of vitamin E metabolites have been described to date and we have recentl...

journal_title：Bioorganic & medicinal chemistry

authors： Pope SA,Burtin GE,Clayton PT,Madge DJ,Muller DP

更新日期：2001-05-01 00:00:00