Pyridine alkaloids with activity in the central nervous system.

abstract：:Aggregation of amyloid peptide (Abeta) has been identified as a major feature of the pathogenesis of Alzheimer's disease. Increased risk for disease is associated with increased formation of polymerized Abeta. Inhibition of formation of toxic (aggregated) form of Abeta is one of the therapeutic possibilities. Beta she...

journal_title：Bioorganic & medicinal chemistry

authors： Hetényi C,Körtvélyesi T,Penke B

更新日期：2002-05-01 00:00:00

abstract：:Deoxyhypusine synthase catalyzes the first step in the posttranslational biosynthesis of the unusual amino acid hypusine [N epsilon-(4-amino-2-hydroxybutyl)lysine] in eukaryotic translation initiation factor 5A (eIF-5A). eIF-5A and its single hypusine residue are essential for cell proliferation. Two series of 1,7-dia...

journal_title：Bioorganic & medicinal chemistry

authors： Lee YB,Folk JE

更新日期：1998-03-01 00:00:00

abstract：:The farnesoid X receptor (FXR) belonging to the metabolic subfamily of nuclear receptors is a ligand-induced transcriptional activator. Its central function is the physiological maintenance of bile acid homeostasis including the regulation of glucose and lipid metabolism. Accessible structural information about its li...

journal_title：Bioorganic & medicinal chemistry

authors： Grienke U,Mihály-Bison J,Schuster D,Afonyushkin T,Binder M,Guan SH,Cheng CR,Wolber G,Stuppner H,Guo DA,Bochkov VN,Rollinger JM

更新日期：2011-11-15 00:00:00

abstract：:A series of analogs were synthesized in a straightforward manner from naturally available sesquiterpenes ilicic acid and tessaric acid. The in vitro antiproliferative activities were examined in the human solid tumor cell lines A2780, HBL-100, HeLa, SW1573, T-47D and WiDr. The most potent analog induced considerably g...

journal_title：Bioorganic & medicinal chemistry

authors： León LG,Donadel OJ,Tonn CE,Padrón JM

更新日期：2009-09-01 00:00:00

abstract：:The synthesis of a new minimum steric perturbing proxyl nitroxide, which is a derivative of glycerol and contains a stearic acid moiety, has been carried out. Its localization in model membrane L-alpha-dipalmitoyl phosphatidyl choline (DPPC) was ascertained with the help of ESR, DSC, 1H and 31P NMR techniques. The nit...

journal_title：Bioorganic & medicinal chemistry

authors： Katoch R,Trivedi GK,Phadke RS

更新日期：1999-12-01 00:00:00

abstract：:Conformationally constrained analogue synthesis was undertaken to aid in pharmacophore mapping and 3D-QSAR analysis of nitrobenzylmercaptopurine riboside (NBMPR) congeners as equilibriative nucleoside transporter 1 (ENT1) inhibitors. In our previous study [J. Med. Chem. 2003, 46, 831-837], novel regioisomeric nitro-1,...

journal_title：Bioorganic & medicinal chemistry

authors： Zhu Z,Buolamwini JK

更新日期：2008-04-01 00:00:00

abstract：:Previously, we reported 2-N-carbamoylguanine (cmG) as a guanine analog. We further studied the synthetic protocol and hybridization properties of oligodeoxynucleotides (ODNs) incorporating cmG. These ODNs were synthesized using the phosphoramidite of cmG without protection of the 6-O position. However, the isolated pr...

journal_title：Bioorganic & medicinal chemistry

authors： Sasami T,Odawara Y,Ohkubo A,Sekine M,Seio K

更新日期：2009-02-01 00:00:00

abstract：:Novel benzimidazolium salts were synthesized as N-heterocyclic carbene (NHC) precursors, these NHC precursors were metallated with Ag2O in dichloromethane at room temperature to give novel silver(I)-NHC complexes. Structures of these benzimidazolium salts and silver(I)-NHC complexes were characterized on the basis of ...

journal_title：Bioorganic & medicinal chemistry

authors： Kaloğlu M,Kaloğlu N,Özdemir İ,Günal S,Özdemir İ

更新日期：2016-08-15 00:00:00

abstract：:Methicillin resistant Staphylococcus aureus (MRSA) is a major health problem that has created a pressing need for new antibiotics. Compounds that inhibit the S. aureus SrtA sortase may function as potent anti-infective agents as this enzyme attaches virulence factors to the cell wall. Using high-throughput screening, ...

journal_title：Bioorganic & medicinal chemistry

authors： Suree N,Yi SW,Thieu W,Marohn M,Damoiseaux R,Chan A,Jung ME,Clubb RT

更新日期：2009-10-15 00:00:00

abstract：:Green tea and (-)-epigallocatechin gallate (EGCG: one of the main components of green tea) are reported to have cancer-preventive activity in humans. A previous SAR study of EGCG and derivatives indicated that a galloyl group is essential for the activity. To test this hypothesis, we synthesized various alkyl gallate ...

journal_title：Bioorganic & medicinal chemistry

authors： Dodo K,Minato T,Noguchi-Yachide T,Suganuma M,Hashimoto Y

更新日期：2008-09-01 00:00:00

abstract：:Derivatives of chlorogenic acid or its analogues were synthesized by coupling protected chlorogenic acid or its analogues with p-octyloxyaniline and selected amino acids. Most of the compounds exhibited significant potency against Cryptococcus neoformans and Candida species with low toxicity to brine shrimps. The 4,5-...

journal_title：Bioorganic & medicinal chemistry

authors： Ma CM,Kully M,Khan JK,Hattori M,Daneshtalab M

更新日期：2007-11-01 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：:Bromodomain-containing protein 4 (BRD4) is a key epigenetic regulator in cancer, and inhibitors targeting BRD4 exhibit great anticancer activity. By replacing the methyltriazole ring of the BRD4 inhibitor I-BET-762 with an N-methylthiazolidone heterocyclic ring, fifteen novel BRD4 inhibitors were designed and synthesi...

journal_title：Bioorganic & medicinal chemistry

authors： Li Q,Li J,Cai Y,Zou Y,Chen B,Zou F,Mo J,Han T,Guo W,Huang W,Qiu Q,Qian H

更新日期：2020-08-01 00:00:00

abstract：:Acute myeloid leukemia (AML) is characterized by fast progression and low survival rates, in which Fms-like tyrosine kinase 3 (FLT3) receptor mutations have been identified as a driver mutation in cancer progression in a subgroup of AML patients. Clinical trials have shown emergence of drug resistant mutants, emphasiz...

journal_title：Bioorganic & medicinal chemistry

authors： Grimm SH,Gagestein B,Keijzer JF,Liu N,Wijdeven RH,Lenselink EB,Tuin AW,van den Nieuwendijk AMCH,van Westen GJP,van Boeckel CAA,Overkleeft HS,Neefjes J,van der Stelt M

更新日期：2019-03-01 00:00:00

abstract：:Enantiomerically pure (S)-atenolol was prepared by using (R,R) salen Co(III) complex for the resolution of terminal epoxide. This process was carried out at room temperature in excellent enantio selectivity. The method can be applied for large-scale preparation of (S)-atenolol without any problem. ...

journal_title：Bioorganic & medicinal chemistry

authors： Bose DS,Venkat Narsaiah A

更新日期：2005-02-01 00:00:00

abstract：:The enantioselective recognition of 'remote' stereogenic centers represents a scientific task in organic chemistry being also of current interest in the pharmaceutical industry. This is due to a range of pharmaceutically relevant molecules or intermediates thereof bearing a stereogenic center, which is separated from ...

journal_title：Bioorganic & medicinal chemistry

authors： Alfaro Blasco M,Gröger H

更新日期：2014-10-15 00:00:00

abstract：:5-HT(3A) receptor antagonists have been used mainly for the treatment of nausea and vomiting. These days, the antagonists are of special interest due to their therapeutic potential to treat other diseases such as depression, psychotic disorder, drug abuse, and irritable bowel syndrome. To discover novel 5-HT(3A) recep...

journal_title：Bioorganic & medicinal chemistry

authors： Lee BH,Choi MJ,Jo MN,Seo HJ,Nah SY,Cho YS,Nam G,Pae AN,Rhim H,Choo H

更新日期：2009-07-01 00:00:00

abstract：:A new efficient approach to the synthesis of 6-alkenyl substituted pyridoxine derivatives has been developed. A series of 31 novel alkenyl pyridoxine derivatives, stilbene-based bioisosteric analogs of estradiol, were synthesized. In vitro cytotoxicity of the obtained compounds against MCF-7 (ER+) breast cancer tumor ...

journal_title：Bioorganic & medicinal chemistry

authors： Pugachev MV,Pavelyev RS,Nguyen TNT,Gabbasova RR,Bulatov TM,Iksanova AG,Aljondi B,Bondar OV,Grishaev DY,Yamaleeva ZR,Kataeva ON,Nikishova TV,Balakin KV,Shtyrlin YG

更新日期：2021-01-15 00:00:00

abstract：:The multi-step ligand action to a target protein is an important aspect when understanding mechanisms of ligand binding and discovering new drugs. However, structurally capturing such complex mechanisms is challenging. This is particularly true for interactions between large membrane proteins and small molecules. One ...

journal_title：Bioorganic & medicinal chemistry

authors： Niitsu A,Egawa A,Ikeda K,Tachibana K,Fujiwara T

更新日期：2018-11-15 00:00:00

abstract：:A series of 5-chloro-N-aryl-1H-indole-2-carboxamide derivatives were prepared and evaluated as inhibitors of human liver glycogen phosphorylase a (hLGPa). One compound, 5-chloro-N-[4-(1,2-dihydroxyethyl)phenyl]-1H-indole-2-carboxamide (2f), inhibited hLGPa with an IC(50) of 0.90microM. The pyridine analogue of 2f show...

journal_title：Bioorganic & medicinal chemistry

authors： Onda K,Suzuki T,Shiraki R,Yonetoku Y,Negoro K,Momose K,Katayama N,Orita M,Yamaguchi T,Ohta M,Tsukamoto S

更新日期：2008-05-15 00:00:00

abstract：:A series of mechanism-based inhibitors designed to interact with the S' subsites of serine proteases was synthesized and their inhibitory activity toward the closely-related serine proteases human neutrophil elastase (HNE) and proteinase 3 (PR 3) was investigated. The compounds were found to be time-dependent inhibito...

journal_title：Bioorganic & medicinal chemistry

authors： Li Y,Dou D,He G,Lushington GH,Groutas WC

更新日期：2009-05-15 00:00:00

abstract：:The solution-phase parallel synthesis involving reactions of Baylis-Hillman products of 3-substituted-5-isoxazolecarbaldehydes with nucleophiles and their in vivo antithrombotic evaluations are described along with the results of in vitro platelet aggregation inhibition assay of a few compounds. Results of the detaile...

journal_title：Bioorganic & medicinal chemistry

authors： Batra S,Roy AK,Patra A,Bhaduri AP,Surin WR,Raghavan SA,Sharma P,Kapoor K,Dikshit M

更新日期：2004-05-01 00:00:00

abstract：:Although cancer cells often harbor supernumerary centrosomes, they form pseudo-bipolar spindles via centrosome clustering, instead of lethal multipolar spindles, and thus avoid cell death. Kinesin-14 HSET/KIFC1 is a crucial protein involved in centrosome clustering. Accordingly, a compound that targets HSET could pote...

journal_title：Bioorganic & medicinal chemistry

authors： Kurisawa N,Yukawa M,Koshino H,Onodera T,Toda T,Kimura KI

更新日期：2020-01-01 00:00:00

abstract：:Synthesis and base-pairing studies of two 2'-deoxyribonucleosides, containing a common heterocyclic base, 7(4)-amino-5(6)H-imidazo[4,5-d]pyridazin-4(7)one (1 and 2), have been reported. The synthesis was accomplished by base-promoted deoxyribosylation of ethyl 5(4)-cyanoimidazole-4(5)-carboxylate (6), followed by ring...

journal_title：Bioorganic & medicinal chemistry

authors： Ujjinamatada RK,Paulman RL,Ptak RG,Hosmane RS

更新日期：2006-09-15 00:00:00

abstract：:Glycamino acids, a family of sugar amino acids, are derivatives of C-glycosides that possesses a carboxyl group at the C-1 position and an amino group replacing one of the hydroxyl groups at either the C-2, 3, 4, or 6 position. We have prepared a series of glucose-type glycamino acids as monomeric building blocks: the...

journal_title：Bioorganic & medicinal chemistry

authors： Suhara Y,Yamaguchi Y,Collins B,Schnaar RL,Yanagishita M,Hildreth JE,Shimada I,Ichikawa Y

更新日期：2002-06-01 00:00:00

abstract：:1,11-Didechloro-6-methyl-4'-O-demethyl rebeccamycin (JDC-108), a rebeccamycin analog possessing potent anti-tumor activities, was prepared via a concise one-pot strategy in good yield. The interaction between JDC-108 and human serum albumin (HSA) was studied by spectroscopic methods including fluorescence spectroscopy...

journal_title：Bioorganic & medicinal chemistry

authors： Cui F,Qin L,Zhang G,Liu X,Yao X,Lei B

更新日期：2008-08-15 00:00:00

abstract：:The reaction mechanism of 12 antimalarial artemisinin compounds with two competitive pathways was studied by means of quantum chemical calculations using the IMOMO(B3LYP/6-31(d,p):HF/3-21G) method. The oxygen-centered radicals, carbon-centered radicals, and transition states (TS) in both pathways were geometrically op...

journal_title：Bioorganic & medicinal chemistry

authors： Tonmunphean S,Parasuk V,Kokpol S

更新日期：2006-04-01 00:00:00

abstract：:The present study describes the chemical synthesis and pharmacological evaluation of a new series of eleven compounds stereoisomers of imidobenzenesulfonylaziridines in the forced-swimming test (FST) in mice. The pharmacological results of these compounds show that six of them, given intraperitoneally, reduced the imm...

journal_title：Bioorganic & medicinal chemistry

authors： Duarte FS,Andrade Eda S,Vieira RA,Uieara M,Nunes RJ,de Lima TC

更新日期：2006-08-01 00:00:00

abstract：:The intestinal absorption of an intact oligopeptide was investigated in rats using a synthetic cationic peptide, 001-C8 (H-MeTyr-Arg-MeArg-D-Leu-NH(CH2)8NH2). The peptide was coupled with 4-nitrobenzo-2-oxa-1,3-diazole (NBD) to prepare a fluorescence-labeled derivative 001-C8-NBD (H-MeTyr-Arg-MeArg-D-Leu-NH(CH2)8NH-NB...

journal_title：Bioorganic & medicinal chemistry

authors： Sai Y,Kajita M,Tamai I,Kamata M,Wakama J,Wakamiya T,Tsuji A

更新日期：1998-06-01 00:00:00

abstract：:The activity of 17 beta-HSD type 1, the enzyme that converts estrone into its more potent metabolite estradiol, has been demonstrated in all classical steroidogenic tissues and almost all peripheral tissues from both rat and human. Since 17 beta-HSD is one of the most important enzymes involved in active steroid hormo...

journal_title：Bioorganic & medicinal chemistry

authors： Tremblay MR,Auger S,Poirier D

更新日期：1995-05-01 00:00:00