Flurbiprofen derivatives as novel α-amylase inhibitors: Biology-oriented drug synthesis (BIODS), in vitro, and in silico evaluation.
Sign Up to like & getrecommendations! Published in 2018 at "Bioorganic chemistry"
DOI: 10.1016/j.bioorg.2018.07.038
Abstract: Novel derivatives of flurbiprofen 1-18 including flurbiprofen hydrazide 1, substituted aroyl hydrazides 2-9, 2-mercapto oxadiazole derivative 10, phenacyl substituted 2-mercapto oxadiazole derivatives 11-15, and benzyl substituted 2-mercapto oxadiazole derivatives 16-18 were synthesized and characterized by… read more here.
Keywords: flurbiprofen derivatives; mercapto oxadiazole; flurbiprofen; derivatives novel ... See more keywords
9,9′-bifluorenylidene derivatives as novel hole-transporting materials for potential photovoltaic applications
Sign Up to like & getrecommendations! Published in 2020 at "Dyes and Pigments"
DOI: 10.1016/j.dyepig.2019.108031
Abstract: Abstract Novel 9,9′-bifluorenylidene derivatives were designed to study the effect of alkyl chain length on selected physical properties. The structure of the synthesized compounds was confirmed by using NMR spectroscopy (1H, 13C, H–H COSY, H–C… read more here.
Keywords: hole transporting; derivatives novel; transporting materials; bifluorenylidene derivatives ... See more keywords
Synthesis and antibacterial evaluation of 13-substituted cycloberberine derivatives as a novel class of anti-MRSA agents.
Sign Up to like & getrecommendations! Published in 2018 at "European journal of medicinal chemistry"
DOI: 10.1016/j.ejmech.2018.08.050
Abstract: A series of new 13-substituted cycloberberine (CBBR) derivatives were prepared and evaluated for their antibacterial activities against Gram-positive bacteria taking CBBR as the lead. Structure-activity relationship revealed that the introduction of a suitable electron-donating group… read more here.
Keywords: substituted cycloberberine; anti mrsa; derivatives novel; mrsa agents ... See more keywords
Discovery of imidazopyrrolopyridines derivatives as novel and selective inhibitors of JAK2.
Sign Up to like & getrecommendations! Published in 2021 at "European journal of medicinal chemistry"
DOI: 10.1016/j.ejmech.2021.113394
Abstract: Herein, we describe the design, synthesis, and structure-activity relationships of a series of imidazopyrrolopyridines derivatives that selectively inhibit Janus kinase 2 (JAK2). These screening cascades revealed that 6k was a preferred compound, with IC50 values… read more here.
Keywords: imidazopyrrolopyridines derivatives; derivatives novel; discovery imidazopyrrolopyridines; novel selective ... See more keywords
4- Substituted sampangine derivatives: Novel acetylcholinesterase and β-myloid aggregation inhibitors.
Sign Up to like & getrecommendations! Published in 2018 at "International journal of biological macromolecules"
DOI: 10.1016/j.ijbiomac.2017.10.157
Abstract: A series of 4- substituted sampangine derivatives (4-aminoalkylaminosampangine Ar-NH(CH2)nNR1R2) has been designed, synthesized, and tested for their ability to inhibit acetylcholinesterase (AChE), butyrylcholinesterase (BChE) and β-myloid (Aβ) aggregation. The synthetic compounds exhibited high AChE inhibitory… read more here.
Keywords: aggregation; sampangine derivatives; acetylcholinesterase; myloid aggregation ... See more keywords
Discovery of Aldisine and Its Derivatives as Novel Antiviral, Larvicidal, and Antiphytopathogenic-Fungus Agents.
Sign Up to like & getrecommendations! Published in 2022 at "Journal of agricultural and food chemistry"
DOI: 10.1021/acs.jafc.2c04256
Abstract: Based on the widespread use of hydrogen bonds in drug design, a series of aldisine derivatives containing oxime, oxime ether, and hydrazone moieties were designed and synthesized, and their antiviral, larvicidal, and fungicidal activities were… read more here.
Keywords: novel antiviral; discovery aldisine; derivatives novel; antiviral larvicidal ... See more keywords
Aryl Quinazolinone Derivatives as Novel Therapeutic Agents against Brain-Eating Amoebae.
Sign Up to like & getrecommendations! Published in 2020 at "ACS chemical neuroscience"
DOI: 10.1021/acschemneuro.9b00596
Abstract: Naegleria fowleri and Balamuthia mandrillaris are protist pathogens that infect the central nervous system, causing primary amoebic meningoencephalitis and granulomatous amoebic encephalitis with mortality rates of over 95%. Quinazolinones and their derivatives possess a wide… read more here.
Keywords: quinazolinone derivatives; eating amoebae; derivatives novel; aryl quinazolinone ... See more keywords
Discovery of 9,11-Seco-Cholesterol Derivatives as Novel FXR Antagonists
Sign Up to like & getrecommendations! Published in 2022 at "ACS Omega"
DOI: 10.1021/acsomega.2c01567
Abstract: The farnesoid X receptor (FXR) plays an important role in the regulation of bile acid, lipid, and glucose homeostasis. Recent findings have shown that the inhibition of FXR is beneficial to improvement of related metabolic… read more here.
Keywords: discovery seco; seco cholesterol; derivatives novel; fxr antagonists ... See more keywords
C-Glycosylated cinnamoylfuran derivatives as novel anti-cancer agents
Sign Up to like & getrecommendations! Published in 2017 at "RSC Advances"
DOI: 10.1039/c7ra04207h
Abstract: A series of C-glycosylated cinnamoylfuran derivatives were synthesized in excellent yield from free sugars. The C-glycosylated furan derivatives were prepared under aqueous reaction conditions. The anticancer potentials of the synthesized compounds were evaluated on the… read more here.
Keywords: cytotoxic effects; derivatives novel; glycosylated cinnamoylfuran; novel anti ... See more keywords
Molecular modeling studies of 1,2,4-triazine derivatives as novel h-DAAO inhibitors by 3D-QSAR, docking and dynamics simulations
Sign Up to like & getrecommendations! Published in 2018 at "RSC Advances"
DOI: 10.1039/c8ra00094h
Abstract: Human D-amino acid oxidase (h-DAAO) can effectively act on D-serine, which has been actively explored as a novel therapeutic target for treating schizophrenia. In this study, 37 h-DAAO inhibitors based on a 6-hydroxy-1,2,4-triazine-3,5(2H,4H)-dione scaffold were… read more here.
Keywords: molecular modeling; studies triazine; modeling studies; derivatives novel ... See more keywords
Identification of 3-(piperazinylmethyl)benzofuran derivatives as novel type II CDK2 inhibitors: design, synthesis, biological evaluation, and in silico insights
Sign Up to like & getrecommendations! Published in 2022 at "Journal of Enzyme Inhibition and Medicinal Chemistry"
DOI: 10.1080/14756366.2022.2062337
Abstract: Abstract In the current work, a hybridisation strategy was adopted between the privileged building blocks, benzofuran and piperazine, with the aim of designing novel CDK2 type II inhibitors. The hybrid structures were linked to different… read more here.
Keywords: cell; identification piperazinylmethyl; cdk2; benzofuran derivatives ... See more keywords