Design, Synthesis, and SAR Studies of Heteroarylpyrimidines and Heteroaryltriazines as CB2R Ligands
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DOI: 10.1002/cmdc.201800541
Abstract: Herein we describe the design and synthesis of a new series of heteroarylpyrimidine/heteroaryltriazine derivatives on the basis of quinazoline‐2,4(1H,3H)‐diones as CB2R‐selective ligands using a bioisosterism strategy. An acetamide group was explored to displace the enamine… read more here.
Keywords: design synthesis; synthesis sar; activity; sar studies ... See more keywords
Synthesis and SAR studies of novel isoquinoline and tetrahydroisoquinoline derivatives as melatonin receptor ligands.
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DOI: 10.1002/cmdc.202100658
Abstract: In our constant search for new successors of Agomelatine, we report herein another new series of compounds resulting from bio-isosteric modulation of the naphthalene ring. New isoquinoline and tetrahydroisoquinoline derivatives were synthesized and pharmacologically evaluated.… read more here.
Keywords: sar studies; studies novel; synthesis sar; tetrahydroisoquinoline derivatives ... See more keywords
N-monoarylacetothioureas as potent urease inhibitors: synthesis, SAR, and biological evaluation
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DOI: 10.1080/14756366.2019.1706503
Abstract: Abstract A urease inhibitor with good in vivo profile is considered as an alternative agent for treating infections caused by urease-producing bacteria such as Helicobacter pylori. Here, we report a series of N-monosubstituted thioureas, which… read more here.
Keywords: inhibitors synthesis; synthesis sar; sar biological; urease inhibitors ... See more keywords
Design, Synthesis and SAR in 2,4,7-Trisubstituted Pyrido[3,2-d]Pyrimidine Series as Novel PI3K/mTOR Inhibitors
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DOI: 10.3390/molecules26175349
Abstract: This work describes the synthesis, enzymatic activities on PI3K and mTOR, in silico docking and cellular activities of various uncommon 2,4,7 trisubstituted pyrido[3,2-d]pyrimidines. The series synthesized offers a chemical diversity in C-7 whereas C-2 (3-hydroxyphenyl)… read more here.
Keywords: design synthesis; pi3k mtor; synthesis sar; series ... See more keywords
Synthesis and SAR Analysis of Novel 4-Hydroxytamoxifen Analogues Based on Their Cytotoxic Activity and Electron-Donor Character
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DOI: 10.3390/molecules27196758
Abstract: Utilizing McMurry reactions of 4,4′-dihydroxybenzophenone with appropriate carbonyl compounds, a series of 4-Hydroxytamoxifen analogues were synthesized. Their cytotoxic activity was evaluated in vitro on four human malignant cell lines (MCF-7, MDA-MB 231, A2058, HT-29). It… read more here.
Keywords: hydroxytamoxifen analogues; sar analysis; synthesis sar; cytotoxic activity ... See more keywords