New 1,2,3‐triazole–(thio)barbituric acid hybrids as urease inhibitors: Design, synthesis, in vitro urease inhibition, docking study, and molecular dynamic simulation
Sign Up to like & getrecommendations! Published in 2020 at "Archiv der Pharmazie"
DOI: 10.1002/ardp.202000023
Abstract: A new series of 1,2,3‐triazole–(thio)barbituric acid hybrids 8a–n was designed and synthesized on the basis of potent pharmacophores with urease inhibitory activity. Therefore, these compounds were evaluated against Helicobacter pylori urease. The obtained result demonstrated… read more here.
Keywords: dynamic simulation; barbituric acid; triazole thio; thio barbituric ... See more keywords
Cinnamic acid hybrids as anticancer agents: A mini‐review
Sign Up to like & getrecommendations! Published in 2022 at "Archiv der Pharmazie"
DOI: 10.1002/ardp.202200052
Abstract: Cancer, as a long‐lasting and dramatic disease, affects almost one‐third of human beings globally. Chemotherapeutics play an important role in cancer treatment, but multidrug resistance and severe adverse effects have already become the main causes… read more here.
Keywords: cancer; hybrids anticancer; acid; cinnamic acid ... See more keywords
Itaconic acid hybrids as potential anticancer agents
Sign Up to like & getrecommendations! Published in 2020 at "Molecular Diversity"
DOI: 10.1007/s11030-020-10147-6
Abstract: Abstract In this paper, we report the synthesis of novel hybrids 2–14 based on itaconic acid and fluoroaniline, pyridine, indole and quinoline scaffolds. Itaconic acid is a naturally occurring compound with a Michael acceptor moiety,… read more here.
Keywords: anticancer agents; itaconic acid; acid hybrids; hybrids potential ... See more keywords
Hydroxamic acid hybrids as the potential anticancer agents: An Overview.
Sign Up to like & getrecommendations! Published in 2020 at "European journal of medicinal chemistry"
DOI: 10.1016/j.ejmech.2020.112679
Abstract: Hydroxamic acid derivatives are potential histone deacetylase inhibitors, and several hydroxamic acid-based histone deacetylase inhibitors have already been used clinically as potent anticancer agents, so hydroxamic acid derivatives are useful scaffolds for the development of… read more here.
Keywords: anticancer agents; hydroxamic acid; acid hybrids; anticancer ... See more keywords
Design, synthesis, in vitro and in vivo evaluation of tacrine–cinnamic acid hybrids as multi-target acetyl- and butyrylcholinesterase inhibitors against Alzheimer's disease
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DOI: 10.1039/c7ra04385f
Abstract: Previously, we have reported tacrine–ferulic acid hybrids as multi-target cholinesterase inhibitors against Alzheimer's disease. However, the detailed structure–activity relationship (SAR), especially regarding the ferulic acid moiety, has yet to be elucidated. Herein we report the… read more here.
Keywords: hybrids multi; alzheimer disease; inhibitors alzheimer; acid hybrids ... See more keywords
Synthesis and bioevaluation of new tacrine-cinnamic acid hybrids as cholinesterase inhibitors against Alzheimer’s disease
Sign Up to like & getrecommendations! Published in 2018 at "Journal of Enzyme Inhibition and Medicinal Chemistry"
DOI: 10.1080/14756366.2017.1412314
Abstract: Abstract Small molecule cholinesterases inhibitor (ChEI) provides an effective therapeutic strategy to treat Alzheimer’s disease (AD). Currently, the discovery of new ChEI with multi-target effect is still of great importance. Herein, we report the synthesis,… read more here.
Keywords: cholinesterase; cinnamic acid; alzheimer disease; acid hybrids ... See more keywords
New Zileuton-Hydroxycinnamic Acid Hybrids: Synthesis and Structure-Activity Relationship towards 5-Lipoxygenase Inhibition
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DOI: 10.3390/molecules25204686
Abstract: A novel series of zileuton-hydroxycinnamic acid hybrids were synthesized and screened as 5-lipoxygenase (5-LO) inhibitors in stimulated HEK293 cells and polymorphonuclear leukocytes (PMNL). Zileuton’s (1) benzo[b]thiophene and hydroxyurea subunits combined with hydroxycinnamic acid esters’ ester… read more here.
Keywords: acid; zileuton hydroxycinnamic; inhibition; hydroxycinnamic acid ... See more keywords
Nucleic Acid Hybrids as Advanced Antibacterial Nanocarriers
Sign Up to like & getrecommendations! Published in 2020 at "Pharmaceutics"
DOI: 10.3390/pharmaceutics12070643
Abstract: Conventional antibiotic therapy is often challenged by poor drug penetration/accumulation at infection sites and poses a significant burden to public health. Effective strategies to enhance the therapeutic efficacy of our existing arsenal include the use… read more here.
Keywords: advanced antibacterial; hybrids advanced; nanocarriers nucleic; acid hybrids ... See more keywords