New pyrrole derivatives as DNA gyrase and 14α-demethylase inhibitors: Design, synthesis, antimicrobial evaluation, and molecular docking.
Sign Up to like & getrecommendations! Published in 2023 at "Drug development research"
DOI: 10.1002/ddr.22080
Abstract: An efficient one-pot reaction utilizing readily available chemical reagents was used to prepare novel 2-amino-1,5-diaryl-1H-pyrrole-3-carbonitrile derivatives and the structures of these compounds were validated by spectroscopic data and elemental analyses. All the synthetic compounds were… read more here.
Keywords: demethylase; dna gyrase; ic50; gyrase demethylase ... See more keywords
Tetra-substituted pyrrole derivatives act as potent activators of p53 in melanoma cells
Sign Up to like & getrecommendations! Published in 2019 at "Investigational New Drugs"
DOI: 10.1007/s10637-019-00813-4
Abstract: Cutaneous melanoma, the most aggressive form of skin cancer, is characterized by activating BRAF mutations. Despite the initial success of selective BRAF inhibitors, only few patients exhibited complete responses, whereas many showed disease progression. Melanoma… read more here.
Keywords: tetra substituted; pyrrole derivatives; substituted pyrrole; p53 ... See more keywords
Switching on the activity of 1,5-diaryl-pyrrole derivatives against drug-resistant ESKAPE bacteria: Structure-activity relationships and mode of action studies.
Sign Up to like & getrecommendations! Published in 2019 at "European journal of medicinal chemistry"
DOI: 10.1016/j.ejmech.2019.05.087
Abstract: Antibiotic resistance represents a major threat worldwide. Gram-positive and Gram-negative opportunistic pathogens are becoming resistant to all known drugs mainly because of the overuse and misuse of these medications and the lack of new antibiotic… read more here.
Keywords: pyrrole derivatives; drug resistant; activity; eskape bacteria ... See more keywords
Facile one-pot synthesis of novel highly functionalized dihydro-1H-pyrrole derivatives catalyzed by molecular iodine
Sign Up to like & getrecommendations! Published in 2019 at "Tetrahedron Letters"
DOI: 10.1016/j.tetlet.2019.150996
Abstract: Abstract An efficient, environmentally benign and molecular iodine promoted protocol was described for cascade synthesis of two kinds of novel dihydro-1H-pyrrole derivatives, 5 and 7. Compounds 5 were prepared via four-component reaction between diethyl acetylenedicarboxylate… read more here.
Keywords: iodine; synthesis; molecular iodine; dihydro pyrrole ... See more keywords
Functional 4H-Dithieno[3,2-b:2′,3′-d]pyrrole Derivatives in Base-Dopable Conjugated Polymers and Oligomers
Sign Up to like & getrecommendations! Published in 2020 at "Macromolecules"
DOI: 10.1021/acs.macromol.0c01071
Abstract: A novel derivative of dithieno[3,2-b:2′,3′-d]pyrrole containing solubilizing side chains in the β-positions is reported and incorporated into a conjugated oligomer by a Pd-catalyzed direct arylatio... read more here.
Keywords: pyrrole; pyrrole derivatives; functional dithieno; derivatives base ... See more keywords
Solid-Phase Synthesis of Pyrrole Derivatives through a Multicomponent Reaction Involving Lys-Containing Peptides.
Sign Up to like & getrecommendations! Published in 2018 at "ACS combinatorial science"
DOI: 10.1021/acscombsci.8b00006
Abstract: The synthesis of pyrroles has received considerable attention because of their biological and pharmaceutical activities. Herein we describe a solid-phase multicomponent reaction that utilizes Lys as a N donor, β-nitrostyrenes, 1,3-dicarbonyl compounds, and FeCl3 as… read more here.
Keywords: pyrrole derivatives; synthesis; multicomponent reaction; solid phase ... See more keywords
Synthesis and Toxicological Effect of Some New Pyrrole Derivatives as Prospective Insecticidal Agents against the Cotton Leafworm, Spodoptera littoralis (Boisduval)
Sign Up to like & getrecommendations! Published in 2022 at "ACS Omega"
DOI: 10.1021/acsomega.1c05049
Abstract: Herein, a series of biologically active pyrrole derivatives, namely 2-[(3-cyano-5-aryl-1H-pyrrol-2-yl)thio]acetic acids 2a-c, 2-[(2-hydroxyethyl)-thio]-5-aryl-1H-pyrrole-3-carbonitriles 3a-c, and 2-[(2-amino-ethyl)thio]-5-aryl-1H-pyrrole-3-carbonitriles 4a-c, 2,2′-disulfanediylbis(5-aryl-1H-pyrrole-3-carbonitriles) 5a-c, 2-((3-cyano-5-aryl-1H-pyrrol-2-yl)thio)acetates 6a-c, 2-[(3-cyano-5-phenyl-1H-pyrrol-2-yl)thio]acetohydrazides 7a-c, and 2-{2-[(3-cyano-5-aryl-1H-pyrrol-2-yl)thio]acetyl}-N-phenyl-hydrazinecarbothioamides 8a-c, as insecticidal agents, were synthesized via adaptable, smoothly accessible… read more here.
Keywords: spodoptera littoralis; insecticidal agents; cotton leafworm; pyrrol thio ... See more keywords
Discovery of pyrrole derivatives as acetylcholinesterase-sparing butyrylcholinesterase inhibitor
Sign Up to like & getrecommendations! Published in 2022 at "Frontiers in Pharmacology"
DOI: 10.3389/fphar.2022.1043397
Abstract: Inspired by the crucial roles of (hetero)aryl rings in cholinesterase inhibitors and the pyrrole ring in new drug discovery, we synthesized 19 pyrrole derivatives and investigated their cholinesterase inhibitory activity. As a result, compounds 3o,… read more here.
Keywords: discovery pyrrole; acetylcholinesterase sparing; sparing butyrylcholinesterase; inhibitor ... See more keywords
Microwave-Assisted Synthesis, Biological Activity Evaluation, Molecular Docking, and ADMET Studies of Some Novel Pyrrolo [2,3-b] Pyrrole Derivatives
Sign Up to like & getrecommendations! Published in 2022 at "Molecules"
DOI: 10.3390/molecules27072061
Abstract: Novel pyrrolo [2,3-b] pyrrole derivatives were synthesized and their hypolipidemic activity was assessed in hyperlipidemic rats. The chemical structures of the new derivatives were confirmed through spectral analysis. Compounds 5 and 6 were revealed to… read more here.
Keywords: novel pyrrolo; microwave assisted; activity; pyrrole derivatives ... See more keywords
Heterocyclization of Bis(2-chloroprop-2-en-1-yl)sulfide in Hydrazine Hydrate–KOH: Synthesis of Thiophene and Pyrrole Derivatives
Sign Up to like & getrecommendations! Published in 2022 at "Molecules"
DOI: 10.3390/molecules27206785
Abstract: The article is devoted to heterocyclization of bis(2-chloroprop-2-en-1-yl)sulfide which proceeds in hydrazine hydrate–alkali medium and leads to formation of thiophene and pyrrole derivatives: previously described 4,5,9,10-tetrahydrocycloocta[1,2-c;5,8-c’]dithiophene, as well as unknown hydrazone of 5-methylidene-3-methyldihydrothiophen-2-one and 1-amino-2-(propynylsulfanylpropenylsulfanyl)-3,5-dimethylpyrrole.… read more here.
Keywords: bis chloroprop; hydrazine hydrate; heterocyclization bis; thiophene pyrrole ... See more keywords
Recent advances in the tandem annulation of 1,3-enynes to functionalized pyridine and pyrrole derivatives
Sign Up to like & getrecommendations! Published in 2021 at "Beilstein Journal of Organic Chemistry"
DOI: 10.3762/bjoc.17.163
Abstract: Great progress has been made in the tandem annulation of enynes in the past few years. This review only presents the corresponding reactions of 1,3-enyne structural motifs to provide the functionalized pyridine and pyrrole derivatives.… read more here.
Keywords: pyridine pyrrole; pyrrole derivatives; annulation enynes; functionalized pyridine ... See more keywords