BIOORGANIC & MEDICINAL CHEMISTRY LETTERS文献大全第2页

Synthesis and pharmacological evaluation of bivalent tethered ligands to target the mGlu2/4 heterodimeric receptor results in a compound with mGlu2/2 homodimer selectivity.
abstract：:This Letter details our ongoing efforts to develop selective positive allosteric modulators (PAMs) of the mGlu2/4 heterodimeric receptor that exists in the CNS and may represent a novel drug target to modulate the glutamatergic system. As multiple hit-to-lead campaigns from HTS hits failed to produce selective small m...

journal_title：Bioorganic & medicinal chemistry letters

pub_type： 杂志文章

doi：10.1016/j.bmcl.2020.127212

authors： Fulton MG,Loch MT,Rodriguez AL,Lin X,Javitch JA,Conn PJ,Niswender CM,Lindsley CW

更新日期：2020-07-01 00:00:00
Design, synthesis and biological evaluation of N-hydroxy-aminobenzyloxyarylamide analogues as novel selective κ opioid receptor antagonists.
abstract：:Aminobenzyloxyarylamide derivatives 1a-i and 2a-t were designed and synthesized as novel selective κ opioid receptor (KOR) antagonists. The benzoyl amide moiety of LY2456302 was changed into N-hydroxybenzamide and benzisoxazole-3(2H)-one to investigate whether it could increase the binding affinity or selectivity for ...

journal_title：Bioorganic & medicinal chemistry letters

pub_type： 杂志文章

doi：10.1016/j.bmcl.2020.127236

authors： He G,Song Q,Wang J,Xu A,Peng K,Zhu Q,Xu Y

更新日期：2020-07-01 00:00:00
Synthesis of morpholine derivatives using the Castagnoli-Cushman reaction as BACE1 inhibitors: Unexpected binding activity of cyclic thioamides.
abstract：:The Castagnoli-Cushman reaction between diglycolic anhydride and imines was applied for the synthesis of morpholine derivatives containing a thioamide or an amidino group. Enzyme inhibition assays towards BACE1 revealed an unexpected role of the cyclic thioamide group in providing inhibition in the micromolar range. M...

journal_title：Bioorganic & medicinal chemistry letters

pub_type： 杂志文章

doi：10.1016/j.bmcl.2020.127211

authors： Calugi L,Lenci E,Innocenti R,Trabocchi A

更新日期：2020-07-01 00:00:00
Discovery of δ opioid receptor full agonists lacking a basic nitrogen atom and their antidepressant-like effects.
abstract：:We have recently reported that the elaboration of the N-substituent in the δ opioid receptor (DOR) antagonist naltrindole (NTI) enabled the regulation of the DOR activities from full inverse agonists to weak partial agonists. The investigations of amide-type NTI derivatives revealed that N-phenylacetyl and N-dihydroci...

journal_title：Bioorganic & medicinal chemistry letters

pub_type： 杂志文章

doi：10.1016/j.bmcl.2020.127176

authors： Fujii H,Uchida Y,Shibasaki M,Nishida M,Yoshioka T,Kobayashi R,Honjo A,Itoh K,Yamada D,Hirayama S,Saitoh A

更新日期：2020-06-15 00:00:00
Enhancing the activity of membrane remodeling epsin-peptide by trimerization.
abstract：:Modulating the structural dynamics of biomembranes by inducing bilayer curvature and lipid packing defects has been highlighted as a practical tool to modify membrane-dependent cellular processes. Previously, we have reported on an amphipathic helical peptide derived from the N-terminal segment (residues 1-18, EpN18) ...

journal_title：Bioorganic & medicinal chemistry letters

pub_type： 杂志文章

doi：10.1016/j.bmcl.2020.127190

authors： Hsu WY,Masuda T,Afonin S,Sakai T,Arafiles JVV,Kawano K,Hirose H,Imanishi M,Ulrich AS,Futaki S

更新日期：2020-06-15 00:00:00
Substituted sulfonamide bioisosteres of 8-hydroxyquinoline as zinc-dependent antibacterial compounds.
abstract：:A series of substituted sulfonamide bioisosteres of 8-hydroxyquinoline were evaluated for their antibacterial activity against the common mastitis causative pathogens Streptococcus uberis, Staphylococcus aureus and Escherichia coli, both in the presence and absence of supplementary zinc. Compounds 9a-e, 10a-c, 11a-e, ...

journal_title：Bioorganic & medicinal chemistry letters

pub_type： 杂志文章

doi：10.1016/j.bmcl.2020.127110

authors： McGowan JE,Harper AD,Davison EK,Jeong JY,Mros S,Harbison-Price N,Van Zuylen EM,Knottenbelt MK,Heikal A,Ferguson SA,McConnell MA,Cook GM,Krittaphol W,Walker GF,Brimble MA,Rennison D

更新日期：2020-06-01 00:00:00
A hypoxia-activated antibacterial prodrug.
abstract：:A prodrug based on a known antibacterial compound is reported to target Staphylococcus aureus and Escherichia coli under reductive conditions. The prodrug was prepared by masking the N-terminus and side chain amines of a component lysine residue as 4-nitrobenzyl carbamates. Activation to liberate the antibacterial was...

journal_title：Bioorganic & medicinal chemistry letters

pub_type： 杂志文章

doi：10.1016/j.bmcl.2020.127140

authors： Yeoh YQ,Horsley JR,Polyak SW,Abell AD

更新日期：2020-06-01 00:00:00
Novel pyridone EP4 agonists featuring allylic alcohol ω-chains.
abstract：:Novel prostaglandin E2 receptor 4 (EP4) agonists featuring a pyridone core and an allylic alcohol ω-chain were discovered. These agonists were shown to be selective over EP1, EP2 and EP3. Analogs harboring a 4-carboxylic acid phenethyl α-chain displayed improved potency over those containing an n-heptanoic acid chain....

journal_title：Bioorganic & medicinal chemistry letters

pub_type： 杂志文章

doi：10.1016/j.bmcl.2020.127104

authors： Dorich S,Cox JH,Burch JD,Chagnon F,Chen B,Léger S,St-Onge M,Fader LD

更新日期：2020-05-15 00:00:00
Discovery and optimization of 2-aminopyridine derivatives as novel and selective JAK2 inhibitors.
abstract：:Janus kinases (JAKs) including JAK1, JAK2, JAK3, and TYK2 are members of a family of intracellular nonreceptor tyrosine kinases, which have been demonstrated to be critical in the cell signaling pathway and involved in inflammatory diseases and cancer. V617F mutation in JAK2 has been implicated in polycythaemia vera (...

journal_title：Bioorganic & medicinal chemistry letters

pub_type： 杂志文章

doi：10.1016/j.bmcl.2020.127048

authors： Ma X,Diao Y,Ge H,Xu F,Zhu L,Zhao Z,Li H

更新日期：2020-04-15 00:00:00
Novel 1,3,4-oxadiazole thioether derivatives containing flexible-chain moiety: Design, synthesis, nematocidal activities, and pesticide-likeness analysis.
abstract：:Seventy-two novel 1,3,4-oxadiazole thioether derivatives containing different flexible-chain moieties were designed and synthesized. The nematicidal activities of all the title compounds were evaluated, and some compounds showed excellent nematicidal activities against citrus nematodes. The compounds 15, 16, 18, 27, 4...

journal_title：Bioorganic & medicinal chemistry letters

pub_type： 杂志文章

doi：10.1016/j.bmcl.2020.127028

authors： Chen J,Wei C,Wu S,Luo Y,Wu R,Hu D,Song B

更新日期：2020-04-15 00:00:00
Study on structure-activity relationship of vitamin K derivatives: Conversion of the naphthoquinone part into another aromatic ring and evaluation of their neuronal differentiation-inducing activity.
abstract：:We synthesized novel vitamin K derivatives by converting the naphthoquinone group to benzene derivatives and benzoquinone. We evaluated their neuronal differentiation activities to investigate the effect of the quinone moiety on this process. We observed that the 1,4-quinone as well as the side chain part play importa...

journal_title：Bioorganic & medicinal chemistry letters

pub_type： 杂志文章

doi：10.1016/j.bmcl.2020.127059

authors： Yoshimura H,Hirota Y,Soda S,Okazeri M,Takagi Y,Takeuchi A,Tode C,Kamao M,Osakabe N,Suhara Y

更新日期：2020-04-15 00:00:00
Synthesis and biological evaluation of novel pyrazolo[3,4-b]pyridines as cis-restricted combretastatin A-4 analogues.
abstract：:Twenty-six novel pyrazolo[3,4-b]pyridine-bridged analogues of combretastatin A-4 possessing 3,4,5-trimethoxylphenyl groups, were synthesized and evaluated for their antiproliferative and tubulin polymerization inhibitory activities. Preliminary biological evaluation demonstrated that some of the target compounds displ...

journal_title：Bioorganic & medicinal chemistry letters

pub_type： 杂志文章

doi：10.1016/j.bmcl.2020.127025

authors： Jian XE,Yang F,Jiang CS,You WW,Zhao PL

更新日期：2020-04-15 00:00:00
Multi-step parallel synthesis enabled optimization of benzofuran derivatives as pan-genotypic non-nucleoside inhibitors of HCV NS5B.
abstract：:In a lead optimization effort towards NS5B NNI inhibitors, two multi-step parallel libraries were designed and successfully synthesized. Through this effort we discovered compound 9B, which achieved rigorous and delicate balance of inhibition across the common genotypes and mutants with <10 nM potency. In addition, th...

journal_title：Bioorganic & medicinal chemistry letters

pub_type： 杂志文章

doi：10.1016/j.bmcl.2020.127004

authors： Xiao D,Dai X,Liu H,He S,Shi ZC,Ludmerer SW,Li F,Nargund R,Palani A

更新日期：2020-04-01 00:00:00
Pro-apoptotic carboxamide analogues of natural fislatifolic acid targeting Mcl-1 and Bcl-2.
abstract：:A library of 26 novel carboxamides deriving from natural fislatifolic acid has been prepared. The synthetic strategy involved a bio-inspired Diels-Alder cycloaddition, followed by functionalisations of the carbonyl moiety. All the compounds were evaluated on Bcl-xL, Mcl-1 and Bcl-2 proteins. In this series of cyclohex...

journal_title：Bioorganic & medicinal chemistry letters

pub_type： 杂志文章

doi：10.1016/j.bmcl.2020.127003

authors： Gapil Tiamas S,Daressy F,Abou Samra A,Bignon J,Steinmetz V,Litaudon M,Fourneau C,Hoong Leong K,Ariffin A,Awang K,Desrat S,Roussi F

更新日期：2020-04-01 00:00:00
Design, synthesis and anti-TMV activities of novel chromone derivatives containing dithioacetal moiety.
abstract：:Thirty-five novel chromone derivatives containing dithioacetal moiety were designed, synthesized, and their anti-TMV activities were evaluated through half-leaf method. The results showed compound c23 illustrates highly curative, protective and inactivating activities against TMV at 500 mg/L, with the values of 68.8%,...

journal_title：Bioorganic & medicinal chemistry letters

pub_type： 杂志文章

doi：10.1016/j.bmcl.2019.126945

authors： Li M,Zan N,Huang M,Jiang D,Hu D,Song B

更新日期：2020-03-01 00:00:00
Design and synthesis of (E)-1,2-diphenylethene-based EZH2 inhibitors.
abstract：:Enhancer of zeste homolog 2 (EZH2) serves as the catalytic subunit of the polycomb repression complex 2 (PRC2), which is implicated in cancer progression metastasis and poor prognosis. Based on our EZH2 inhibitor SKLB1049 with low nanomolar activity, we extended the "tail" region to get a series of (E)-1,2-diphenyleth...

journal_title：Bioorganic & medicinal chemistry letters

pub_type： 杂志文章

doi：10.1016/j.bmcl.2020.126957

authors： He H,Hu X,Teng F,Liu Z,Zhang Q,Feng Z,Feng Q,Yu L

更新日期：2020-03-01 00:00:00
Discovery of a lead series of potent benzodiazepine 5-HT2C receptor agonists with high selectivity in functional and binding assays.
abstract：:A series of potential new 5-HT2 receptor scaffolds based on a simplification of the clinically studied, 5-HT2CR agonist vabicaserin, were designed. An in vivo feeding assay early in our screening process played an instrumental part in the lead identification process, leading us to focus on a 6,5,7-tricyclic scaffold. ...

journal_title：Bioorganic & medicinal chemistry letters

pub_type： 杂志文章

doi：10.1016/j.bmcl.2019.126929

authors： Ren A,Zhu X,Feichtinger K,Lehman J,Kasem M,Schrader TO,Wong A,Dang H,Le M,Frazer J,Unett DJ,Grottick AJ,Whelan KT,Morgan ME,Sage CR,Semple G

更新日期：2020-03-01 00:00:00
Antibody-mediated delivery of chimeric protein degraders which target estrogen receptor alpha (ERα).
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

pub_type： 杂志文章

doi：10.1016/j.bmcl.2019.126907

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
The synthesis of trifluoromethylated N-nitroaryl-2-amino-1,3-dichloropropane derivatives and their evaluation as potential anti-cancer agents.
abstract：:Six N-nitroaryl-2-amino-1,3-dichloropropane derivatives have been prepared and evaluated against 18 cancer cell lines and two non-cancerous cell lines. Analysis of cell viability data and IC50 values indicated that the presence of a trifluoromethyl group in the nitroaryl moiety is an important structural feature assoc...

journal_title：Bioorganic & medicinal chemistry letters

pub_type： 杂志文章

doi：10.1016/j.bmcl.2019.126910

authors： Chappel L,Wong LC,Leong CO,Mai CW,Meikle IT,Stanforth SP,Truong TV

更新日期：2020-02-15 00:00:00
Mariannamides A and B, new cyclic octapeptides isolated from Mariannaea elegans NBRC102301.
abstract：:Two new cyclic octapeptides, mariannamides A (1) and B (2), have been isolated from Mariannaea elegans NBRC102301, a Pinus densiflora-derived filamentous fungus. Their structures were elucidated to be cyclo-(l-Leu1-l-Pro1-l-Pro2-l-Leu2-l-Ile1-l-Pro3-l-Val1-l-Ile2) and cyclo-(l-Leu1-l-Pro1-l-Pro2-l-Leu2-l-Ile1-l-Pro3-l...

journal_title：Bioorganic & medicinal chemistry letters

pub_type： 杂志文章

doi：10.1016/j.bmcl.2019.126946

authors： Ishiuchi K,Hirose D,Kondo T,Watanabe K,Terasaka K,Makino T

更新日期：2020-02-15 00:00:00
Selective acetylcholinesterase inhibitors derived from muscle relaxant dantrolene.
abstract：:Dantrolene, the only therapeutic agent for malignant hyperthermia, is known to have not only a muscle relaxant effect, but also a neuroprotective effect and Alzheimer's disease improving effect. Recently, it has been reported that dantrolene has a weak inhibitory effect on acetylcholinesterase (AChE), which is a thera...

journal_title：Bioorganic & medicinal chemistry letters

pub_type： 杂志文章

doi：10.1016/j.bmcl.2019.126888

authors： Aoyama H,Doura T

更新日期：2020-02-15 00:00:00
An amide-based sulfenamide prodrug of gamma secretase inhibitor BMS-708163 delivers parent drug from an oral conventional solid dosage form in male beagle dog.
abstract：:The objective of this Letter is to report the first (to our knowledge) in vivo proof of concept for a sulfenamide prodrug to orally deliver a poorly soluble drug containing a weakly-acidic NH-acid from a conventional solid dosage formulation. This proof of concept was established using BMS-708163 (1), a gamma secretas...

journal_title：Bioorganic & medicinal chemistry letters

pub_type： 杂志文章

doi：10.1016/j.bmcl.2019.126856

authors： Guarino VR,Olson RE,Everlof JG,Wang N,McDonald I,Haskell R,Clarke W,Lentz KA

更新日期：2020-02-01 00:00:00
Discovery of a novel 2,3-dimethylimidazo[1,2-a]pyrazine-6-carboxamide M4 positive allosteric modulator (PAM) chemotype.
abstract：:This Letter details our efforts to discover structurally unique M4 PAMs containing 5,6-heteroaryl ring systems. In an attempt to improve the DMPK profiles of the 2,3-dimethyl-2H-indazole-5-carboxamide and 1-methyl-1H-benzo[d][1,2,3]triazole-6-carboxamide cores, we investigated a plethora of core replacements. This exe...

journal_title：Bioorganic & medicinal chemistry letters

pub_type： 杂志文章

doi：10.1016/j.bmcl.2019.126812

authors： Temple KJ,Engers JL,Long MF,Watson KJ,Chang S,Luscombe VB,Jenkins MT,Rodriguez AL,Niswender CM,Bridges TM,Conn PJ,Engers DW,Lindsley CW

更新日期：2020-02-01 00:00:00
Synthesis and immunostimulatory activity of sugar-conjugated TLR7 ligands.
abstract：:Toll-like receptors (TLRs) are a type of pattern recognition receptors (PRRs), which are activated by recognizing pathogen-associated molecular patterns (PAMPs). The activation of TLRs initiates innate immune responses and subsequently leads to adaptive immune responses. TLR agonists are effective immuomodulators in v...

journal_title：Bioorganic & medicinal chemistry letters

pub_type： 杂志文章

doi：10.1016/j.bmcl.2019.126840

authors： Baba A,Wakao M,Shinchi H,Chan M,Hayashi T,Yao S,Cottam HB,Carson DA,Suda Y

更新日期：2020-02-01 00:00:00
Design, synthesis and biological evaluation of Proteolysis Targeting Chimeras (PROTACs) as a BTK degraders with improved pharmacokinetic properties.
abstract：:A new series of Proteolysis Targeting Chimeras (PROTACs) targeting Bruton's Tyrosine Kinase (BTK) was synthesized, with the goal of improving the pharmacokinetic properties of our previously reported PROTAC, MT802. We recently described the ability of MT802 to induce degradation of both wild-type and C481S mutant BTK ...

journal_title：Bioorganic & medicinal chemistry letters

pub_type： 杂志文章

doi：10.1016/j.bmcl.2019.126877

authors： Jaime-Figueroa S,Buhimschi AD,Toure M,Hines J,Crews CM

更新日期：2020-02-01 00:00:00
Design, synthesis and antitumor activity of a novel PEG-A6-conjugated irinotecan derivative.
abstract：:A novel PEG-A6-conjugated irinotecan derivative 8 was designed and synthesized as antitumor agent by the PEGylation and A6-peptide modification of irinotecan. In vivo antitumor activity screening assay revealed that 8 exhibited better in vivo antiproliferation activity than irinotecan and its previous PEG-cRGD-conjuga...

journal_title：Bioorganic & medicinal chemistry letters

pub_type： 杂志文章

doi：10.1016/j.bmcl.2019.126847

authors： Huang YQ,Yuan JD,Ding HF,Song YS,Qian G,Wang JL,Ji M,Zhang Y

更新日期：2020-01-15 00:00:00
Structural insights for producing CK2α1-specific inhibitors.
abstract：:Casein kinase 2 catalytic subunit (CK2α) is classified into two subtypes CK2α1 and CK2α2. CK2α1 is a drug discovery target, whereas CK2α2 is an off-target of CK2α1 inhibitors. High amino acid sequence homology between these subtypes hampers efforts to produce ATP competitive inhibitors that are highly selective to CK2...

journal_title：Bioorganic & medicinal chemistry letters

pub_type： 杂志文章

doi：10.1016/j.bmcl.2019.126837

authors： Tsuyuguchi M,Nakaniwa T,Hirasawa A,Nakanishi I,Kinoshita T

更新日期：2020-01-15 00:00:00
Structure-based design of guanosine analogue inhibitors targeting GTP cyclohydrolase IB towards a new class of antibiotics.
abstract：:GTP cyclohydrolase (GCYH-I) is an enzyme in the folate biosynthesis pathway that has not been previously exploited as an antibiotic target, although several pathogens including N. gonorrhoeae use a form of the enzyme GCYH-IB that is structurally distinct from the human homologue GCYH-IA. A comparison of the crystal st...

journal_title：Bioorganic & medicinal chemistry letters

pub_type： 杂志文章

doi：10.1016/j.bmcl.2019.126818

authors： Samaan GN,Paranagama N,Haque A,Hecht DA,Swairjo MA,Purse BW

更新日期：2020-01-15 00:00:00
Serendipitous discovery of aryl boronic acids as β-lactamase inhibitors.
abstract：:High throughput screening for β-lactamase inhibitors afforded biphenyl hits such as 1. Hit confirmation and X-ray soaking experiments with Pseudomonas Aeruginosa AmpC enzyme led to the identification of an aryl boronic acid-serine complex 4, which was formed from phenyl boronic acid 8 (an impurity in compound 1) and e...

journal_title：Bioorganic & medicinal chemistry letters

pub_type： 杂志文章

doi：10.1016/j.bmcl.2019.126795

authors： Yang SW,Pan J,Root Y,Scapin G,Xiao L,Su J

更新日期：2020-01-15 00:00:00
The bioisosteric modification of pyrazinamide derivatives led to potent antitubercular agents: Synthesis via click approach and molecular docking of pyrazine-1,2,3-triazoles.
abstract：:Tuberculosis remains as a major public health risk which causes the highest mortality rate globally and an improved regimen is required to treat the drug-resistant strains. Pyrazinamide is a first-line antitubercular drug used in combination therapy with other anti-TB drugs. Herein, we describe the modification of pyr...

journal_title：Bioorganic & medicinal chemistry letters

pub_type： 杂志文章

doi：10.1016/j.bmcl.2019.126846

authors： Reddyrajula R,Dalimba U

更新日期：2020-01-15 00:00:00
Discovery of a potent and selective adenylyl cyclase type 8 agonist by docking-based virtual screening.
abstract：:Adenylyl cyclases (ACs), which are responsible for catalyzing the conversion of adenosine triphosphate (ATP) into the second messenger cyclic adenosine monophosphate (cAMP), play a critical role in cell signal transduction. In this study, a combined approach involving docking-based virtual screening, with the combinat...

journal_title：Bioorganic & medicinal chemistry letters

pub_type： 杂志文章

doi：10.1016/j.bmcl.2019.126823

authors： Weng Z,Xu G,Chen D,Yang Y,Song G,Shen W,Zhang S,Wang L,Yang W,Zuo Z

更新日期：2020-01-15 00:00:00
Therapeutic potential of coumarin bearing metal complexes: Where are we headed?
abstract：:The successfully application of some metallodrugs such as salvarsan, silver sulfadiazine and cisplatin in modern medicine launched the biological investigation of organometallic and metal-organic complexes. The availability and tunability of various ligands including N-heterocycles, phosphines, N-heterocyclic carbenes...

journal_title：Bioorganic & medicinal chemistry letters

pub_type： 杂志文章,评审

doi：10.1016/j.bmcl.2019.126805

authors： Balcıoğlu S,Olgun Karataş M,Ateş B,Alıcı B,Özdemir İ

更新日期：2020-01-15 00:00:00
Synthesis, anti-plasmodial and cytotoxic evaluation of 1H-1,2,3-triazole/acyl hydrazide integrated tetrahydro-β-carboline-4-aminoquinoline conjugates.
abstract：:A series of 1H-1,2,3-triazole/acylhydrazide-tethered tetrahydro-β-carboline-4-aminoquinoline conjugates was synthesized with an aim to study their anti-plasmodial structure-activity relationship. The presence of 1H-1,2,3-triazole-core along with a flexible alkyl chain length on aminoquinoline core has favourable influ...

journal_title：Bioorganic & medicinal chemistry letters

pub_type： 杂志文章

doi：10.1016/j.bmcl.2019.126810

authors： Sharma B,Kaur S,Legac J,Rosenthal PJ,Kumar V

更新日期：2020-01-15 00:00:00
Hydroxyl substituted benzoic acid/cinnamic acid derivatives: Tyrosinase inhibitory kinetics, anti-melanogenic activity and molecular docking studies.
abstract：:The inhibition of tyrosinase is an established strategy for treating hyperpigmentation. Our previous findings demonstrated that cinnamic acid and benzoic acid scaffolds can be effective tyrosinase inhibitors with low toxicity. The hydroxyl substituted benzoic and cinnamic acid moieties of these precursors were incorpo...

journal_title：Bioorganic & medicinal chemistry letters

pub_type： 杂志文章

doi：10.1016/j.bmcl.2019.126722

authors： Nazir Y,Saeed A,Rafiq M,Afzal S,Ali A,Latif M,Zuegg J,Hussein WM,Fercher C,Barnard RT,Cooper MA,Blaskovich MAT,Ashraf Z,Ziora ZM

更新日期：2020-01-01 00:00:00
Design, synthesis, and biological evaluation of 2-amino-N-(2-methoxyphenyl)-6-((4-nitrophenyl)sulfonyl)benzamide derivatives as potent HIV-1 Vif inhibitors.
abstract：:Viral infectivity factor (Vif) is one of the accessory protein of human immunodeficiency virus type I (HIV-1) that inhibits host defense factor, APOBEC3G (A3G), mediated viral cDNA hypermutations. Previous work developed a novel Vif inhibitor 2-amino-N-(2-methoxyphenyl)-6-((4-nitrophenyl)thio)benzamide (1) with strong...

journal_title：Bioorganic & medicinal chemistry letters

pub_type： 杂志文章

doi：10.1016/j.bmcl.2019.126638

authors： Zhang RH,Wang S,Luo RH,Zhou M,Zhang H,Xu GB,Zhao YL,Li YJ,Wang YL,Yan G,Liao SG,Zheng YT,Li R

更新日期：2019-12-15 00:00:00
Synthesis, 3D-structure and stability analyses of NRPa-308, a new promising anti-cancer agent.
abstract：:We report herein the synthesis of a newly described anti-cancer agent, NRPa-308. This compound antagonizes Neuropilin-1, a multi-partners transmembrane receptor overexpressed in numerous tumors, and thereby validated as promising target in oncology. The preparation of NRPa-308 proved challenging because of the orthogo...

journal_title：Bioorganic & medicinal chemistry letters

pub_type： 杂志文章

doi：10.1016/j.bmcl.2019.126710

authors： Brachet E,Dumond A,Liu WQ,Fabre M,Selkti M,Raynaud F,Hermine O,Benhida R,Belmont P,Garbay C,Lepelletier Y,Ronco C,Pagès G,Demange L

更新日期：2019-12-15 00:00:00
Design, synthesis and biological evaluation of novel semicarbazone-selenochroman-4-ones hybrids as potent antifungal agents.
abstract：:A series of novel 2,3-dihydro-4H-1-benzoselenin-4-one (thio)semicarbazone derivatives were designed and synthesized by using molecular hybridization approach. All the target compounds were characterized by HRMS and NMR and evaluated in vitro antifungal activity against five pathogenic strains. In comparison with precu...

journal_title：Bioorganic & medicinal chemistry letters

pub_type： 杂志文章

doi：10.1016/j.bmcl.2019.126726

authors： Xu H,Su X,Liu XQ,Zhang KP,Hou Z,Guo C

更新日期：2019-12-01 00:00:00
Synthesis and biological evaluation of 9-fluorenone derivatives for SPECT imaging of α7-nicotinic acetylcholine receptor.
abstract：:The α7-nicotinic acetylcholine receptor (α7-nAChR) subtype, is found to have a connection with the pathogenesis of a variety of psychiatric and neurological disorders. Herein, we report the development of radioiodinated 9-fluorenone derivatives as single-photon emission computed tomography (SPECT) imaging tracers for ...

journal_title：Bioorganic & medicinal chemistry letters

pub_type： 杂志文章

doi：10.1016/j.bmcl.2019.126724

authors： Gao H,Wang S,Qi Y,He G,Qiang B,Wang S,Zhang H

更新日期：2019-12-01 00:00:00
Austalides V and W, new meroterpenoids from the fungus Aspergillus ustus and their antitumor activities.
abstract：:Two new austalide meroterpenoids, named austalides V and W (1 and 2), were isolated from the fungus Aspergillus ustus VKM F-4692. Their structures were elucidated by extensive spectroscopic analysis and by comparison with related known compounds. The main structural feature of both compounds is a tetrahydrofuranyl rin...

journal_title：Bioorganic & medicinal chemistry letters

pub_type： 杂志文章

doi：10.1016/j.bmcl.2019.126708

authors： Antipova TV,Zaitsev KV,Oprunenko YF,Ya Zherebker A,Rystsov GK,Zemskova MY,Zhelifonova VP,Ivanushkina NE,Kozlovsky AG

更新日期：2019-11-15 00:00:00
Inhaled Janus Kinase (JAK) inhibitors for the treatment of asthma.
abstract：:Multiple asthma-relevant cytokines including IL-4, IL-5, IL-13, and TSLP depend upon JAKs for signaling. JAK inhibition may, therefore, offer a novel intervention strategy for patients with disease refractory to current standards of care. Multiple systemically delivered JAK inhibitors have been approved for human use ...

journal_title：Bioorganic & medicinal chemistry letters

pub_type： 杂志文章,评审

doi：10.1016/j.bmcl.2019.126658

authors： Zak M,Dengler HS,Rajapaksa NS

更新日期：2019-10-15 00:00:00

2410 条记录 2/61 页 « 123 4 5 6 7 8...60 61 »

在线工具