Synthesis, biological evaluation, and docking studies of some 5‐chloro‐2(3H)‐benzoxazolone Mannich bases derivatives as cholinesterase inhibitors
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DOI: 10.1002/ardp.201700273
Abstract: A series of N‐substituted‐5‐chloro‐2(3H)‐benzoxazolone derivatives were synthesized and evaluated for their acetylcholinesterase (AChE), butyrylcholinesterase (BuChE) inhibitory, and antioxidant activities. The structures of the title compounds were confirmed by spectral and elemental analyses. The cholinesterase (ChE)… read more here.
Keywords: ache; chloro benzoxazolone; compound; synthesis biological ... See more keywords
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 screening of some novel 6‐substituted 2‐alkylpyridazin‐3(2H)‐ones as anti‐inflammatory and analgesic agents
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DOI: 10.1002/ardp.201900295
Abstract: Some novel derivatives of 2‐alkyl 6‐substituted pyridazin‐3(2H)‐ones were synthesized by condensation of 3,6‐dichloropyridazine with the sodium salt of benzyl cyanide, followed by hydrolysis and coupling with alkyl halides. The synthesized compounds were screened as cyclooxygenase… read more here.
Keywords: anti inflammatory; biological screening; novel substituted; substituted alkylpyridazin ... 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 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
Myxochelin‐Inspired 5‐Lipoxygenase Inhibitors: Synthesis and Biological Evaluation
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DOI: 10.1002/cmdc.201600536
Abstract: A total of 48 analogues of the natural product myxochelin A were prepared and evaluated for their inhibitory effects on human 5‐lipoxygenase in both cell‐free and cell‐based assays. Structure–activity relationship analysis revealed that the secondary alcohol… read more here.
Keywords: inhibitors synthesis; myxochelin inspired; inspired lipoxygenase; myxochelin ... 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, 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;
Design, Synthesis, and Biological Evaluation of Lysine Demethylase 5 C Degraders
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DOI: 10.1002/cmdc.202000933
Abstract: Lysine demethylase 5 C (KDM5C) controls epigenetic gene expression and is attracting great interest in the field of chemical epigenetics. KDM5C has emerged as a therapeutic target for anti‐prostate cancer agents, and recently we identified triazole… read more here.
Keywords: design synthesis; biological evaluation; kdm5c; synthesis biological ... See more keywords