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The monoamine oxidase inhibition properties of C6- and N1-substituted 3-methyl-3,4-dihydroquinazolin-2(1H)-one derivatives
(Springer, 2020)
Quinazolinone compounds are of interest in medicinal chemistry since they display a wide range of biological properties. In the present study, a series of C6- and N1-substituted 3-methyl-3,4-dihydroquinazolin-2(1H)-one ...
Synthesis and evaluation of C3 substituted chalcone-based derivatives of 7-azaindole as protein kinase inhibitors
(Wiley, 2020)
Chalcones are a group of naturally occurring or synthetic compounds which possess a wide range of biological activities. In this paper, a series of twenty‐three 7‐azaindole‐chalcone hybrids (5a–w) were synthesized and ...
Metronidazole-conjugates: a comprehensive review of recent developments towards synthesis and medicinal perspective
(Elsevier, 2020)
Nitroimidazoles based compounds remain a hot topic of research in medicinal chemistry due to their numerous biological activities. Moreover, many clinical candidates based on this chemical core have been reported to be ...
C3 amino-substituted chalcone derivative with selective adenosine rA1 receptor affinity in the micromolar range
(Springer, 2020)
To identify novel adenosine receptor (AR) ligands based on the chalcone scaffold, herein the synthesis, characterization and in vitro and in silico evaluation of 33 chalcones (15–36 and 37–41) and structurally related ...
Synthesis and evaluation of methoxy substituted 2-benzoyl-1-benzofuran derivatives as lead compounds for the development adenosine A1 and/or A2A receptor antagonists
(Elsevier, 2020)
A series of fourteen methoxy substituted 2-benzoyl-1-benzofuran derivatives were synthesised and their affinities determined for adenosine A1 and A2A receptors via radioligand binding assays to establish the structure ...
Synthesis and evaluation of 7-azaindole derivatives bearing benzocycloalkanone motifs as protein kinase inhibitors
(Elsevier, 2020)
Protein kinases are important drug targets, especially in the area of oncology. This paper reports the synthesis and biological evaluation of new 7-azaindole derivatives bearing benzocycloalkanone motifs as potential protein ...
The evaluation of 1-tetralone and 4-chromanone derivatives as inhibitors of monoamine oxidase
(Springer, 2020)
Monoamine oxidase (MAO) is of much clinical relevance, and inhibitors of this enzyme are used in the treatment for neuropsychiatric and neurodegenerative disorders such as depression and Parkinson’s disease. The present ...
6-Nitro-1-benzylquinolones exhibiting specific antitubercular activity
(Wiley, 2020)
In this study, we synthesized novel nitro quinolone‐based compounds and tested them in vitro against a panel of Gram‐positive and Gram‐negative pathogens including Mycobacterium tuberculosis (MTB), Pseudomonas aeruginosa ...
Recent advances in radical C-H bond functionalization of imidazoheterocycles
(Wiley, 2020)
Direct C−H bond functionalization through radical pathway has emerged as a powerful and ideal strategy for the synthesis of organic compounds. This review provides an overview of recent developments in radical C−H ...
Synthesis and structure activity relationships of chalcone based benzocycloalkanone derivatives as adenosine a 1 and/or a 2a receptor antagonists
(Thieme, 2020)
Adenosine A1 and/or A2A receptor antagonists hold promise for the potential treatment of neurological conditions, such as Parkinson’s disease. Herein, a total of seventeen benzocycloalkanone derivatives were synthesised ...