Design and Synthesis of 5‐Substituted Benzo[d][1,3]dioxole Derivatives as Potent Anticonvulsant Agents
Sign Up to like & getrecommendations! Published in 2017 at "Archiv der Pharmazie"
DOI: 10.1002/ardp.201600274
Abstract: A series of 5‐substituted benzo[d][1,3]dioxole derivatives was designed, synthesized, and tested for anticonvulsant activity using the maximal electroshock (MES) and subcutaneous pentylenetetrazole (scPTZ) screens. Neurotoxicity was determined by rotarod test. In the preliminary screening, six… read more here.
Keywords: design synthesis; derivatives potent; synthesis substituted; dioxole derivatives ... See more keywords
Some pyrazoles derivatives: Potent carbonic anhydrase, α‐glycosidase, and cholinesterase enzymes inhibitors
Sign Up to like & getrecommendations! Published in 2018 at "Archiv der Pharmazie"
DOI: 10.1002/ardp.201800200
Abstract: A series of substituteed pyrazol‐4‐yl‐diazene derivatives were found to be effective inhibitors against α‐glycosidase, cytosolic carbonic anhydrase I and II isoforms (hCA I and II), butyrylcholinesterase (BChE), and acetylcholinesterase (AChE) with Ki values in the… read more here.
Keywords: carbonic anhydrase; glycosidase; derivatives potent; pyrazoles derivatives ... See more keywords
Design and synthesis of novel quinazolin‐4(1H)‐one derivatives as potent and selective inhibitors targeting AKR1B1
Sign Up to like & getrecommendations! Published in 2023 at "Archiv der Pharmazie"
DOI: 10.1002/ardp.202200577
Abstract: Inhibition of aldose reductase (AKR1B1) is a promising option for the treatment of diabetic complications. However, most of the developed small molecule inhibitors lack selectivity or suffer from low bioactivity. To address this limitation, a… read more here.
Keywords: design synthesis; derivatives potent; quinazolin one; selective inhibitors ... See more keywords
Semisynthetic Vitamin E Derivatives as Potent Antibacterial Agents against Resistant Gram‐Positive Pathogens
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DOI: 10.1002/cmdc.202000792
Abstract: New 5‐substituted vitamin E derivatives were semisynthesized, and their antibacterial activity against human Gram‐positive and Gram‐negative pathogens was evaluated. Several vitamin E analogues were active against methicillin‐resistant Staphylococcus aureus (MRSA) and/or methicillin‐resistant Staphylococcus epidermidis (MRSE);… read more here.
Keywords: gram positive; gram; derivatives potent; vitamin ... See more keywords
Assessment of novel azaanthraquinone derivatives as potent multi-target inhibitors of inflammation and amyloid-β aggregation in Alzheimer's disease.
Sign Up to like & getrecommendations! Published in 2019 at "Bioorganic chemistry"
DOI: 10.1016/j.bioorg.2018.10.073
Abstract: A series of 6-substituted azaanthraquinone derivatives have been designed, synthesized, and their anti-inflammatory activities, antiaggregation effects on β-amyloid proteins, anticholinesterase and neuroprotective activity were tested. The new derivatives strongly suppressed NO and iNOS production and… read more here.
Keywords: novel azaanthraquinone; aggregation; derivatives potent; potent multi ... See more keywords
Synthesis of benzothiazole derivatives as a potent α-glucosidase inhibitor.
Sign Up to like & getrecommendations! Published in 2019 at "Bioorganic chemistry"
DOI: 10.1016/j.bioorg.2018.12.021
Abstract: Diabetes is one of the pre-dominant metabolic disorders all over the world. It is the prime reason of mortality and morbidity due to hyperglycemia which is link with numerus obstacles. Delaying absorption and digestion of… read more here.
Keywords: benzothiazole; potent glucosidase; synthesis benzothiazole; derivatives potent ... See more keywords
Identification of novel quinazoline derivatives as potent antiplasmodial agents.
Sign Up to like & getrecommendations! Published in 2019 at "European journal of medicinal chemistry"
DOI: 10.1016/j.ejmech.2018.10.041
Abstract: Despite the recent reductions in the global burden of malaria, this disease remains a devastating cause of death in tropical and subtropical regions. As there is no broadly effective vaccine for malaria, prevention and treatment… read more here.
Keywords: derivatives potent; antiplasmodial agents; quinazoline derivatives; potent antiplasmodial ... See more keywords
Design, synthesis, and structure activity relationship analysis of new betulinic acid derivatives as potent HIV inhibitors.
Sign Up to like & getrecommendations! Published in 2021 at "European journal of medicinal chemistry"
DOI: 10.1016/j.ejmech.2021.113287
Abstract: Prior modification of betulinic acid (1), a natural product lead with promising anti-HIV activity, produced 3-O-(3',3'-dimethylsuccinyl)betulinic acid (bevirimat, 3), the first-in-class HIV maturation inhibitor. After 3-resistant variants were found during Phase I and IIa clinical… read more here.
Keywords: derivatives potent; betulinic acid; activity relationship; structure activity ... See more keywords
Discovery of novel thiophene derivatives as potent neuraminidase inhibitors.
Sign Up to like & getrecommendations! Published in 2021 at "European journal of medicinal chemistry"
DOI: 10.1016/j.ejmech.2021.113762
Abstract: Neuraminidase (NA) is an important target for the treatment of influenza. In this study, a new lead NA inhibitor, 4 (ZINC01121127), was discovered by pharmacophore-based virtual screening and molecular dynamic (MD) simulation. Some novel NA… read more here.
Keywords: derivatives potent; thiophene derivatives; potent neuraminidase; thiophene ... See more keywords
Novel 2-phenyl-3-(Pyridin-2-yl) thiazolidin-4-one derivatives as potent inhibitors for proliferation of osteosarcoma cells in vitro and in vivo.
Sign Up to like & getrecommendations! Published in 2021 at "European journal of medicinal chemistry"
DOI: 10.1016/j.ejmech.2021.114010
Abstract: Due to unknown pathogenesis and unidentified drug target, no drug for the treatment of osteosarcoma (OS) has been launched to the market. Herein, thiazolidinone 1a was discovered as a hit compound by phenotypic screening with… read more here.
Keywords: derivatives potent; one derivatives; phenyl pyridin; thiazolidin one ... See more keywords
Clofazimine derivatives as potent broad-spectrum antiviral agents with dual-target mechanism
Sign Up to like & getrecommendations! Published in 2022 at "European Journal of Medicinal Chemistry"
DOI: 10.1016/j.ejmech.2022.114209
Abstract: Thirty-two clofazimine derivatives, of which twenty-two were new, were synthesized and evaluated for their antiviral effects against both rabies virus and pseudo-typed SARS-CoV-2, taking clofazimine (1) as the lead. Among them, compound 15f bearing 4-methoxy-2-pyridyl… read more here.
Keywords: spectrum antiviral; broad spectrum; clofazimine derivatives; derivatives potent ... See more keywords