Abstract：
:Advanced glycation end products (AGEs) are implicated to be the key players in most of the diabetic complications. The AGE's interfere with the proteins heterogeneously, thereby rendering denaturation and the consequent loss of function and accumulation. Thus, a novel natural product inspired indeno[2,1-c]pyridinone (4a-4ad) molecular templates with AGE's trapping potential was designed through scaffold hopping approach and synthesized via facile two-step synthetic route. Amongst the tested indeno[2,1-c]pyridinone hybrids, 4i, 4x and 4aa exhibited excellent efficiency in trapping the AGE's. The percentage of antiglycation is measured by the analytical model system, i.e. via MG trapping capacity; here the compounds 4i, 4x and 4aa with 50.03%, 69.58%, and 93.37% respectively has displayed promising efficiency. In particular, 4aa demonstrated better activity than the positive control aminoguanidine (79.82%). The in-vitro toxicity of compounds was tested on L6 rat skeletal muscle cell lines revealed that none of the compounds showed any significant toxicity at concentrations up to 1000 μM.
journal_name
Bioorg Chemjournal_title
Bioorganic chemistryauthors
Anaga N,D B,Abraham B,Nisha P,Varughese S,Jayamurthy P,Somappa SBdoi
10.1016/j.bioorg.2020.104375subject
Has Abstractpub_date
2020-12-01 00:00:00pages
104375eissn
0045-2068issn
1090-2120pii
S0045-2068(20)31673-4journal_volume
105pub_type
杂志文章abstract：:We reported an useful protocol for the labeling of the second domain of the Vascular Endothelial Growth Factor Receptor 1 (VEGFR1D2), a small protein ligand able to bind VEGF, the main regulator of angiogenesis. We developed a bioconjugation strategy based on the use of oxime-ligation reaction conjugating an aldehyde ...
journal_title：Bioorganic chemistry
pub_type： 杂志文章
doi：10.1016/j.bioorg.2019.103160
更新日期：2019-10-01 00:00:00
abstract：:A phytochemical study to obtain new nitric oxide (NO) inhibitors resulted in the isolation of five new withanolides from the whole plants of Physalis peruviana. The structures were determined on the basis of extensive NMR spectroscopic data analysis as well as the time-dependent density functional theory (TDDFT) elect...
journal_title：Bioorganic chemistry
pub_type： 杂志文章
doi：10.1016/j.bioorg.2019.03.051
更新日期：2019-06-01 00:00:00
abstract：:Based on current treatment of Alzheimer's disease, where the carbamate inhibitor Rivastigmine is used, two series of carbamate derivatives were prepared: (i) N-phenylcarbamates with additional carbamate group (1-12) and (ii) N-phenylcarbamates with monosaccharide moiety (13-24). All compounds were tested for the inhib...
journal_title：Bioorganic chemistry
pub_type： 杂志文章
doi：10.1016/j.bioorg.2018.03.012
更新日期：2018-08-01 00:00:00
abstract：:The marine environment remains a rich source for the discovery and development of novel bioactive compounds. The present paper describes the design, synthesis and biological evaluation of a library of small molecule heterocyclic mimetics of the marine 2,5-diketopiperazine barettin which is a powerful natural antioxida...
journal_title：Bioorganic chemistry
pub_type： 杂志文章
doi：10.1016/j.bioorg.2018.11.024
更新日期：2019-03-01 00:00:00
abstract：:In order to develop multitarget-directed ligands as potential treatments for Alzheimer's disease, twenty-eight new tacrine-hydroxamate derivatives were designed, synthesized, and biologically evaluated. As expected, most of the compounds exhibited inhibitory activities against cholinesterases (ChEs) and histone deacet...
journal_title：Bioorganic chemistry
pub_type： 杂志文章
doi：10.1016/j.bioorg.2020.103721
更新日期：2020-05-01 00:00:00
abstract：:Cervical cancer is a leading cause of cancer-related deaths among women in developing countries. Therefore, development of new chemotherapeutic agents is required. Unlike normal cells, cancer cells contain elevated copper levels which play an integral role in angiogenesis. Thus, targeting copper via copper-specific ch...
journal_title：Bioorganic chemistry
pub_type： 杂志文章
doi：10.1016/j.bioorg.2019.03.031
更新日期：2019-06-01 00:00:00
abstract：:As an effective strategy of the drug discovery for peptide-binding GPCRs based on the natural ligands, beta-turn peptidomimetic compound library with benzodiazepine skeleton was constructed using solid and solution phase parallel synthesis with four different scaffolds containing Phe, Lys, Ser and Glu, respectively. T...
journal_title：Bioorganic chemistry
pub_type： 杂志文章
doi：10.1016/j.bioorg.2009.04.001
更新日期：2009-06-01 00:00:00
abstract：:In an approach to develop potent cytotoxic compounds with targeted action, a systematic methodology was employed to design and initially synthesize parent compounds A1, A8, A13 and A14 followed by synthesis of further analogs of A1 (A2-A7) and A8 (A9-A12) with characterization by IR, NMR, mass and elemental techniques...
journal_title：Bioorganic chemistry
pub_type： 杂志文章
doi：10.1016/j.bioorg.2019.103539
更新日期：2020-01-01 00:00:00
abstract：:A series of kojic acid-derived compounds 6a-p bearing aryloxymethyl-1H-1,2,3-triazol-1-yl moiety were designed by modifying primary alcoholic group of kojic acid as tyrosinase inhibitors. The target compounds 6a-p were synthesized via click reaction. All compounds showed very potent anti-tyrosinase activity (IC50s = 0...
journal_title：Bioorganic chemistry
pub_type： 杂志文章
doi：10.1016/j.bioorg.2018.10.069
更新日期：2019-02-01 00:00:00
abstract：:The dimeric Mycobacterium tuberculosis FabH (mtFabH) catalyses a Claisen-type condensation between an acyl-CoA and malonyl-acyl carrier protein (ACP) to initiate the Type II fatty acid synthase cycle. To analyze the initial covalent acylation of mtFabH with acyl-CoA, we challenged it with mixture of C6-C20 acyl-CoAs a...
journal_title：Bioorganic chemistry
pub_type： 杂志文章
doi：10.1016/j.bioorg.2007.11.001
更新日期：2008-04-01 00:00:00
abstract：:Glycyrrhetinic acid has been usually studied for their anti-tumor activities. However, the low bioavailability and poor aqueous solubility as well as limited intracellular accumulation have limited their utility. In this present study, a series of new glycyrrhetinic acid conjugates with a triphenylphosphonium cation (...
journal_title：Bioorganic chemistry
pub_type： 杂志文章
doi：10.1016/j.bioorg.2018.12.036
更新日期：2019-04-01 00:00:00
abstract：:Two new series of ethyl benzoate bearing pyrrolizine and indolizine moieties 8-11 were synthesized and evaluated for their anti-inflammatory and anticancer activities. Among these derivatives, compounds 9a, 10b and 11b displayed in vivo anti-inflammatory and analgesic activity comparable to ibuprofen. The acute ulcero...
journal_title：Bioorganic chemistry
pub_type： 杂志文章
doi：10.1016/j.bioorg.2019.103371
更新日期：2020-01-01 00:00:00
abstract：:Colchicine site antimitotic agents typically suffer from low aqueous solubilities and are formulated as phosphate prodrugs of phenolic groups. These hydroxyl groups are the aim of metabolic transformations leading to resistance. There is an urgent need for more intrinsically soluble analogues lacking these hydroxyl gr...
journal_title：Bioorganic chemistry
pub_type： 杂志文章
doi：10.1016/j.bioorg.2020.103755
更新日期：2020-05-01 00:00:00
abstract：:Monoamine oxidase inhibitors (MAOIs) are potential drug candidates for the treatment of various neurological disorders like Parkinson's disease, Alzheimer's disease and depression. In the present study, two series of 4-substituted phenylpiperazine and 1-benzhydrylpiperazine (1-21) derivatives were synthesized and scre...
journal_title：Bioorganic chemistry
pub_type： 杂志文章
doi：10.1016/j.bioorg.2018.01.020
更新日期：2018-04-01 00:00:00
abstract：:Alzheimer's Disease (AD) is a progressive neurodegenerative disorder that effects 50 million people worldwide. In this review, AD pathology and the development of novel therapeutic agents targeting AD were fully discussed. In particular, common approaches to prevent Aβ production and/or accumulation in the brain inclu...
journal_title：Bioorganic chemistry
pub_type： 杂志文章,评审
doi：10.1016/j.bioorg.2020.103649
更新日期：2020-04-01 00:00:00
abstract：:A series of novel β-pinene-based thiazole derivatives were synthesized and characterized by HRMS, 1H NMR, and 13C NMR analyses as potential antineoplastic agents. Derivatives were evaluated for their anticancer activities in vitro, and the data manifested that most target compounds showed potent anti-proliferative act...
journal_title：Bioorganic chemistry
pub_type： 杂志文章
doi：10.1016/j.bioorg.2018.12.010
更新日期：2019-03-01 00:00:00
abstract：:With the aim of finding new anti-inflammatory drugs, a series of new Glycyrrhetinic acid derivatives (1-34) have been designed and synthesized by structural modification, and their anti-inflammatory activities in vitro have been evaluated. The anti-inflammatory activities assay demonstrated that compound 5b suppressed...
journal_title：Bioorganic chemistry
pub_type： 杂志文章
doi：10.1016/j.bioorg.2020.104598
更新日期：2020-12-29 00:00:00
abstract：:Several new 5,6-dihydropyrimidine-2(1H)-thione derivatives have been prepared and investigated for their potencies for anticonvulsant activity against maximal electroshock (MES) and subcutaneous pentylenetetrazole (scPTZ) test in mice. The acute neurotoxicity was measured by rotarod test. Compounds 3c and 3l were foun...
journal_title：Bioorganic chemistry
pub_type： 杂志文章
doi：10.1016/j.bioorg.2017.07.017
更新日期：2017-10-01 00:00:00
abstract：:Synthesis of C-5-substituted 1,3-dioxoisoindoline-4-aminoquinolines having amide group as a spacer was developed with an intent to evaluate their antiplasmodial activities. The synthesized dioxoisoindoline-aminoquinolines tethered with β-alanine as a spacer and secondary amine as substituent displayed good anti-plasmo...
journal_title：Bioorganic chemistry
pub_type： 杂志文章
doi：10.1016/j.bioorg.2019.04.006
更新日期：2019-07-01 00:00:00
abstract：:In cardiac ischemic disorder, pyroglutamate helix B surface peptide (pHBSP) which derived from erythropoietin causes to increase cell stability. To improve the serum stability of pHBSP, two lipophilic amino acids Arg6, Ala7 were replaced with Fmoc-(Dabcyle)-Lys-OH and Fmoc-Phe-OH during the peptide synthesis. This pep...
journal_title：Bioorganic chemistry
pub_type： 杂志文章
doi：10.1016/j.bioorg.2020.103731
更新日期：2020-05-01 00:00:00
abstract：:A new series of derivatives characterized by the presence of the 3,4,5-trimethoxylbenzamide substituted benzofurans were synthesized and evaluated for antiproliferative activity against four cancer cell lines and one normal human cell line. Among them, derivative 6g with greatest cytotoxicity significantly inhibited t...
journal_title：Bioorganic chemistry
pub_type： 杂志文章
doi：10.1016/j.bioorg.2020.104076
更新日期：2020-09-01 00:00:00
abstract：:Enantioselective synthesis of functionalized cyclic allylic alcohols via kinetic resolution in transesterifcation with different lipase enzymes has been developed. The influence of the enzymes and temperature activity was studied. By determination of ideal reaction conditions, byproduct formation is minimized; this ma...
journal_title：Bioorganic chemistry
pub_type： 杂志文章
doi：10.1016/j.bioorg.2019.102980
更新日期：2019-07-01 00:00:00
abstract：:In efforts to develop new antitubercular agents, we report here the synthesis of a series of novel pyrrole hydrazine derivatives. The molecules were evaluated against inhibitors of InhA, which is one of the key enzymes involved in type II fatty acid biosynthetic pathway of the mycobacterial cell wall as well as inhibi...
journal_title：Bioorganic chemistry
pub_type： 杂志文章
doi：10.1016/j.bioorg.2017.09.008
更新日期：2017-12-01 00:00:00
abstract：:A series of thirteen novel 2,4-thiazolidinedione derivatives were synthesized through three step reaction procedure. The title compounds were synthesized by Knoevenagel condensation at the 5th position of the 2,4-thiazolidinedione ring. Various physicochemical and spectral studies were conducted to characterize the sy...
journal_title：Bioorganic chemistry
pub_type： 杂志文章
doi：10.1016/j.bioorg.2019.102993
更新日期：2019-08-01 00:00:00
abstract：:The chemical investigation of the fruits of a mangrove Sonneratia apetala collected from the Beibu Gulf led to the isolation of four new compounds, sonneradons A-D (1-4), as well as 18 known compounds (5-22). The structures of the new compounds were elucidated based on extensive spectroscopic analysis, and the structu...
journal_title：Bioorganic chemistry
pub_type： 杂志文章
doi：10.1016/j.bioorg.2020.103813
更新日期：2020-06-01 00:00:00
abstract：:Drug resistance and cancer cells metastasis have been the leading causes of chemotherapy failure and cancer-associated death in breast cancer patients. In present, various active molecules either exhibiting novel mechanism of action such as inducing autophagy or inhibiting metastasis have been developed to address the...
journal_title：Bioorganic chemistry
pub_type： 杂志文章
doi：10.1016/j.bioorg.2018.11.025
更新日期：2019-03-01 00:00:00
abstract：:3-Amino-1-aryl-1H-benzo[f]chromene-2-carbonitrile derivatives were synthesized from three-component reaction of arylaldehyde, malononitrile and 2-naphthol in the presence of 1, 4-bis(4-ferrocenylbutyl)piperazine as a new catalyst. Cytotoxic potencies of the compounds were tested on HT-29 cells. 3-Amino-1-(4-fluorophen...
journal_title：Bioorganic chemistry
pub_type： 杂志文章
doi：10.1016/j.bioorg.2019.103329
更新日期：2019-12-01 00:00:00
abstract：:This study was designed to evaluate the antioxidant, antibacterial and cytotoxicity effects of Satureja hortensis (S. hortensis) essential oil (EO). The GC-MS analysis of S. hortensis EO (SEO) has identified seven compounds, representing 96.84% of the oil. The two main constituents of the oil were; carvacrol (48.51%) ...
journal_title：Bioorganic chemistry
pub_type： 杂志文章
doi：10.1016/j.bioorg.2019.103559
更新日期：2020-01-01 00:00:00
abstract：:HDAC inhibitors and BRD4 inhibitors were considered to be potent anti-cancer agents. Recent studies have demonstrated that HDAC and BRD4 participate in the regulation of some signal paths like PI3K-AKT. In this work, a series of indole derivatives that combine the inhibitory activities of BRD4 and HDAC into one molecu...
journal_title：Bioorganic chemistry
pub_type： 杂志文章
doi：10.1016/j.bioorg.2018.12.011
更新日期：2019-03-01 00:00:00
abstract：:Based on a report that sulfanylphthalimides are highly potent monoamine oxidase (MAO) B selective inhibitors, the present study examines the adenosine receptor affinities and MAO-B inhibitory properties of a series of 4- and 5-sulfanylphthalimide analogues. Since adenosine antagonists (A1 and A2A subtypes) and MAO-B i...
journal_title：Bioorganic chemistry
pub_type： 杂志文章
doi：10.1016/j.bioorg.2015.02.005
更新日期：2015-04-01 00:00:00
