Design, synthesis, biological evaluation, and molecular dynamics of novel cholinesterase inhibitors as anti‐Alzheimer's agents
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DOI: 10.1002/ardp.201800352
Abstract: A series of novel chroman‐4‐one derivatives were designed and synthesized successfully with good to excellent yield (3a–l). In addition, the obtained products were evaluated for their cholinesterase (ChE) inhibitory activities. The results show that among… read more here.
Keywords: design synthesis; cholinesterase; biological evaluation; molecular dynamics ... See more keywords
Design, synthesis and biological evaluation of 6‐substituted quinolines derived from cabozantinib as c‐Met inhibitors
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DOI: 10.1002/ardp.201900101
Abstract: Based on the cabozantinib scaffold, novel c‐Met inhibitors were rationalized from the limited knowledge of structure‐activity relationships for the quinoline 6‐position. Emphasis was given to modifications capable of engaging in additional polar interactions with the… read more here.
Keywords: design synthesis; biological evaluation; met inhibitors; substituted quinolines ... See more keywords
Synthesis and biological evaluation of Val–Val dipeptide–sulfonamide conjugates
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DOI: 10.1002/ardp.202000074
Abstract: Novel Val–Val dipeptide–benzenesulfonamide conjugates were reported in this study. These were achieved by a condensation reaction of p‐substituted benzenesulfonamoyl alkanamides with 2‐amino‐4‐methyl‐N‐substituted phenyl butanamide using classical peptide‐coupling reagents. The compounds were characterized using Fourier transform… read more here.
Keywords: val dipeptide; biological evaluation; val; synthesis biological ... See more keywords
Synthesis and biological evaluation of new coumarin derivatives as cytotoxic agents
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DOI: 10.1002/ardp.202100029
Abstract: New coumarin derivatives 9a–f, 10a–e, and 11a–f were synthesized and evaluated for their cytotoxic activity against a human breast cancer cell line (MCF‐7). All compounds exhibited good activity in the nanomolar range, using doxorubicin and… read more here.
Keywords: new coumarin; biological evaluation; evaluation new; coumarin derivatives ... See more keywords
Synthesis and preliminary biological evaluation of antibacterial and antifungal 5-arylidene tetramic acid-cadmium(II) complexes.
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DOI: 10.1002/ardp.202100305
Abstract: The synthesis and biological evaluation of 5-arylidene-N-acetyl-tetramic acids cadmium(II) complexes are reported. Eleven novel compounds were prepared, characterized by nuclear magnetic resonance experiments and screened for their antimicrobial activity against five bacterial species (Escherichia coli,… read more here.
Keywords: antibacterial antifungal; biological evaluation; cadmium complexes; arylidene ... See more keywords
Synthesis, characterization, and biological evaluation of some novel Schiff bases as potential metabolic enzyme inhibitors
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DOI: 10.1002/ardp.202100430
Abstract: In this study, a series of novel Schiff base derivatives containing a pyrazolone ring (2a–e) were designed, successfully synthesized for the first time, and characterized by elemental analysis and some spectroscopic methods. These compounds were… read more here.
Keywords: schiff bases; evaluation novel; biological evaluation; novel schiff ... See more keywords
Synthesis of cinnamils and quinoxalines and their biological evaluation as anticancer agents
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DOI: 10.1002/ardp.202100448
Abstract: We synthesized multiple cinnamils and quinoxalines to evaluate their anticancer activity. Cinnamils were used as precursors for quinoxalines via condensation with 1,2‐diaminobenzene. Among the 26 synthesized compounds reported in this article, we found that cinnamil… read more here.
Keywords: cinnamils quinoxalines; quinoxalines biological; biological evaluation; synthesis cinnamils ... See more keywords
Synthesis and biological evaluation of sulfonamide‐based compounds as inhibitors of carbonic anhydrase from Vibrio cholerae
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DOI: 10.1002/ardp.202200070
Abstract: This study reports our continued efforts to identify inhibitors capable of targeting carbonic anhydrases (CAs) expressed in bacteria. Based on previously identified chemotypes, we designed and synthesized new analogs that were screened toward the α,… read more here.
Keywords: synthesis biological; evaluation sulfonamide; biological evaluation; vibrio cholerae ... See more keywords
Design, Synthesis, Biological Evaluation, and X‐ray Studies of HIV‐1 Protease Inhibitors with Modified P2′ Ligands of Darunavir
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DOI: 10.1002/cmdc.201700614
Abstract: The structure‐based design, synthesis, and biological evaluation of a series of nonpeptidic HIV‐1 protease inhibitors with rationally designed P2′ ligands are described. The inhibitors are designed to enhance backbone binding interactions, particularly at the S2′… read more here.
Keywords: design synthesis; biological evaluation; protease inhibitors; hiv protease ... See more keywords
Design and Biological Evaluation of Manganese‐ and Ruthenium‐Based Hybrid CO‐RMs (HYCOs)
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DOI: 10.1002/cmdc.201900426
Abstract: Interest in the therapeutic effects of carbon monoxide (CO), a product of heme degradation catalyzed by the enzyme heme oxygenase‐1 (HO‐1), has led to the development of CO‐releasing molecules (CO‐RMs) for the controlled delivery of… read more here.
Keywords: biological evaluation; ruthenium based; manganese ruthenium; design biological ... See more keywords
Design, Synthesis and Biological Evaluation of Highly Potent Simplified Archazolids
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DOI: 10.1002/cmdc.202000154
Abstract: The archazolids are potent antiproliferative compounds that have recently emerged as a novel class of promising anticancer agents. Their complex macrolide structures and scarce natural supply make the development of more readily available analogues highly… read more here.
Keywords: design synthesis; synthesis biological; biological evaluation;