Abstract：
:Herein, substituted imidazole-pyrazole hybrids (2a-2n) were prepared via a multi component reaction employing pyrazole-4-carbaldehydes (1a-1d), ammonium acetate, benzil and arylamines as reactants. All the new compounds were characterized through their spectral and elemental analyses. Further these compounds were tested against α-glucosidase enzyme. The compounds 2k, 2l and 2n possessed good inhibition potencies, however, compounds 2f (IC50 value: 25.19 ± 0.004 μM) and 2m (IC50 value: 33.62 ± 0.03 μM) were the most effective compounds of the series. Furthermore, molecular docking helped to understand the binding interactions of 2f and 2m with the understudy yeast's α-glucosidase enzyme.
journal_name
Bioorg Chemjournal_title
Bioorganic chemistryauthors
Chaudhry F,Naureen S,Ashraf M,Al-Rashida M,Jahan B,Munawar MA,Khan MAdoi
10.1016/j.bioorg.2018.10.047subject
Has Abstractpub_date
2019-02-01 00:00:00pages
267-273eissn
0045-2068issn
1090-2120pii
S0045-2068(18)30679-5journal_volume
82pub_type
杂志文章abstract：:Inhibition of α-glucosidase is one of the important approaches in designing antidiabetic drugs for its role in decrease of the carbohydrates digestion to avoid post-prandial increase in blood sugar levels in diabetic patients. In the present study we designed a novel series of 2-acetylbenzofuran hydrazones (L1-L7) and...
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更新日期：2020-09-01 00:00:00
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journal_title：Bioorganic chemistry
pub_type： 杂志文章
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更新日期：2019-12-01 00:00:00
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journal_title：Bioorganic chemistry
pub_type： 杂志文章
doi：10.1016/j.bioorg.2008.11.001
更新日期：2009-02-01 00:00:00
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journal_title：Bioorganic chemistry
pub_type： 杂志文章
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journal_title：Bioorganic chemistry
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journal_title：Bioorganic chemistry
pub_type： 杂志文章
doi：10.1016/j.bioorg.2019.103548
更新日期：2020-03-01 00:00:00
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journal_title：Bioorganic chemistry
pub_type： 杂志文章
doi：10.1016/j.bioorg.2018.04.024
更新日期：2018-09-01 00:00:00
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journal_title：Bioorganic chemistry
pub_type： 杂志文章
doi：10.1016/j.bioorg.2019.103183
更新日期：2019-11-01 00:00:00
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journal_title：Bioorganic chemistry
pub_type： 杂志文章
doi：10.1016/j.bioorg.2019.03.067
更新日期：2019-07-01 00:00:00
abstract：:In addition to its catalytic domain, phosphoinsositide-dependent protein kinase-1 (PDK1) contains a C-terminal pleckstrin homology (PH) domain, which binds the membrane-bound phosphatidylinositol (3,4,5)-triphosphate [PI(3,4,5)P3] second messenger. Here, we report in vitro kinetic, phosphopeptide mapping, and oligomer...
journal_title：Bioorganic chemistry
pub_type： 杂志文章
doi：10.1016/j.bioorg.2006.05.002
更新日期：2006-08-01 00:00:00
abstract：:Chondrocyte based therapy is promising to treat symptomatic chondral and osteochondral lesions. Growth factors to accelerate the proliferation and retain the phenotype of chondrocytes in vitro are imperative. However, the high cost and rapid degradation of growth factors limited their further application. Therefore, i...
journal_title：Bioorganic chemistry
pub_type： 杂志文章
doi：10.1016/j.bioorg.2014.09.005
更新日期：2014-12-01 00:00:00
abstract：:A novel series of tacrine derivatives containing sulfonamide group were synthesized and their inhibitory effects on acetylcholinesterase (AChE) and butyrylcholinesterase (BuChE) were evaluated. The result showed that all the synthesized tacrine-sulfonamides (VIIIa-o) exhibited inhibitory activity on both cholinesteras...
journal_title：Bioorganic chemistry
pub_type： 杂志文章
doi：10.1016/j.bioorg.2017.01.005
更新日期：2017-02-01 00:00:00
abstract：:Phosphite dehydrogenase catalyzes the NAD+-dependent oxidation of hydrogen phosphonate (common name phosphite) to phosphate in what amounts to a formal phosphoryl transfer reaction from hydride to hydroxide. This review places the enzyme in the context of phosphorus redox metabolism in nature and discusses the results...
journal_title：Bioorganic chemistry
pub_type： 杂志文章,评审
doi：10.1016/j.bioorg.2005.01.003
更新日期：2005-06-01 00:00:00
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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：: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
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更新日期：2019-06-01 00:00:00
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journal_title：Bioorganic chemistry
pub_type： 杂志文章
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更新日期：2019-05-01 00:00:00
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journal_title：Bioorganic chemistry
pub_type： 杂志文章
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更新日期：2020-01-01 00:00:00
abstract：:Starting from the molecular simplification of (R) 4-(3,4-dibenzylpiperazine-1-carbonyl)benzenesulfonamide 9a, a compound endowed with selectivity for human Carbonic Anhydrase (hCA) IV, a series of piperazines and 4-aminopiperidines carrying a 4-sulfamoylbenzamide moiety as Zn-binding group have been designed and teste...
journal_title：Bioorganic chemistry
pub_type： 杂志文章
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更新日期：2019-10-01 00:00:00
abstract：:In search of better α-glucosidase inhibitors, a series of bis-indolylmethane sulfonohydrazides derivatives (1-14) were synthesized and evaluated for their α-glucosidase inhibitory potential. All derivatives exhibited outstanding α-glucosidase inhibition with IC50 values ranging between 0.10 ± 0.05 to 5.1 ± 0.05 μM whe...
journal_title：Bioorganic chemistry
pub_type： 杂志文章
doi：10.1016/j.bioorg.2018.06.001
更新日期：2018-10-01 00:00:00
abstract：:Twenty known Amaryllidaceae alkaloids of various structural types, and one undescribed alkaloid of narcikachnine-type, named narcieliine (3), have been isolated from fresh bulbs of Zephyranthes citrina. The chemical structures of the isolated alkaloids were elucidated by a combination of MS, HRMS, 1D and 2D NMR, and C...
journal_title：Bioorganic chemistry
pub_type： 杂志文章
doi：10.1016/j.bioorg.2020.104567
更新日期：2020-12-19 00:00:00
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journal_title：Bioorganic chemistry
pub_type： 杂志文章
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更新日期：2018-12-01 00:00:00
abstract：:Plant compounds have been identified as new drug prototypes. In this line, this work aimed to isolate the indole alkaloid affinisine from Tabernaemontana catharinensis and test its antitumor activity. The alkaloid was isolated by silica gel open column chromatography from the ethanolic extract of the stem of T. cathar...
journal_title：Bioorganic chemistry
pub_type： 杂志文章
doi：10.1016/j.bioorg.2019.103079
更新日期：2019-09-01 00:00:00
abstract：:2-Epi-jaspine B is an isomer of the natural product jaspine B and shows certain selectivity for SphK1 and potent antitumor activity. Based on the crystal structure of SphK1, we transformed the structure of 2-epi-jaspine B and modified the hydrophobic side chain to obtain a series of 2-epi-jaspine B analogs. The MTT as...
journal_title：Bioorganic chemistry
pub_type： 杂志文章
doi：10.1016/j.bioorg.2019.103369
更新日期：2020-05-01 00:00:00
abstract：:Interactions of two newly synthesized and six previously reported benzoxanthene lignans (BXLs), analogues of rare natural products, with DNA/RNA, G-quadruplex and HSA were evaluated by a set of spectrophotometric methods. Presence/absence of methoxy and hydroxy groups on the benzoxanthene core and minor modifications ...
journal_title：Bioorganic chemistry
pub_type： 杂志文章
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更新日期：2020-11-01 00:00:00
