Search Results - "Pflégr, Václav"
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Synthesis and Antimycobacterial Activity of Isoniazid Derivatives Tethered with Aliphatic Amines
Published in Current topics in medicinal chemistry (01-01-2022)“…There is an urgent need for new antitubercular compounds. Modification of antimycobacterial isonicotinohydrazide at hydrazide N2 provided antimycobacterial…”
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Design and synthesis of 2-(2-isonicotinoylhydrazineylidene)propanamides as InhA inhibitors with high antitubercular activity
Published in European journal of medicinal chemistry (05-11-2021)“…Based on successful antitubercular isoniazid scaffold we have designed its “mee-too” analogues by a combination of this drug linked with substituted anilines…”
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Iodinated 1,2-diacylhydrazines, benzohydrazide-hydrazones and their analogues as dual antimicrobial and cytotoxic agents
Published in Bioorganic & medicinal chemistry (01-07-2021)“…[Display omitted] •Iodinated hydrazide-hydrazones and diacylhydrazines were obtained via condensation.•Activity against Gram-positive bacteria including MRSA…”
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Novel pyrimidine-1,3,4-oxadiazole hybrids and their precursors as potential antimycobacterial agents
Published in Future medicinal chemistry (01-06-2023)“…Molecular hybridization and isostery are proven approaches in medicinal chemistry, and as such we used them to design novel compounds that we investigated as…”
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N-[3,5-Bis(trifluoromethyl)phenyl]-5-bromo-2-hydroxybenzamide Analogues: Novel Acetyl- and Butyrylcholinesterase Inhibitors
Published in Current topics in medicinal chemistry (01-01-2020)“…Development of acetyl- (AChE) and butyrylcholinesterase (BuChE) inhibitors belongs to viable strategies for the treatment of dementia and other diseases…”
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5-Aryl-1,3,4-oxadiazol-2-amines Decorated with Long Alkyl and Their Analogues: Synthesis, Acetyl- and Butyrylcholinesterase Inhibition and Docking Study
Published in Pharmaceuticals (Basel, Switzerland) (25-03-2022)“…2,5-Disubstituted 1,3,4-oxadiazoles are privileged versatile scaffolds in medicinal chemistry that have exhibited diverse biological activities. Acetyl- (AChE)…”
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Host cell targeting of novel antimycobacterial 4-aminosalicylic acid derivatives with tuftsin carrier peptides
Published in European journal of pharmaceutics and biopharmaceutics (01-05-2022)“…[Display omitted] •Design, synthesis, and characterization of new antimycobacterial 4-aminosalicylic acid derivatives.•New tuftsin bioconjugates targeting cell…”
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Novel Inhibitors of Acetyl- and Butyrylcholinesterase Derived from Benzohydrazides: Synthesis, Evaluation and Docking Study
Published in Pharmaceuticals (Basel, Switzerland) (24-01-2023)“…On the basis of previous reports, novel 2-benzoylhydrazine-1-carboxamides were designed as potential inhibitors of acetylcholinesterase (AChE) and…”
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Novel propargylamine-based inhibitors of cholinesterases and monoamine oxidases: Synthesis, biological evaluation and docking study
Published in Bioorganic chemistry (01-11-2021)“…[Display omitted] •New compounds combine propargylamine and salicylic/cinnamic scaffolds.•The compounds exhibited dual inhibition of AChE, BuChE and…”
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Design and Synthesis of Highly Active Antimycobacterial Mutual Esters of 2-(2-Isonicotinoylhydrazineylidene)propanoic Acid
Published in Pharmaceuticals (Basel, Switzerland) (14-12-2021)“…The combination of two active scaffolds into one molecule represents a proven approach in drug design to overcome microbial drug resistance. We designed and…”
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