Design and Synthesis of 5‐Substituted Benzo[d][1,3]dioxole Derivatives as Potent Anticonvulsant Agents
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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
Design, Synthesis, and Screening of Triazolopyrimidine–Pyrazole Hybrids as Potent Apoptotic Inducers
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DOI: 10.1002/ardp.201700137
Abstract: An efficient synthesis of novel 3‐(3‐aryl‐1‐phenyl‐1H‐pyrazol‐4‐yl)‐5,7‐dimethyl‐[1,2,4]triazolo[4,3‐a]‐pyrimidines was accomplished by the oxidation of pyrimidinylhydrazones by using organoiodine(III) reagent. All new triazolopyrimidine derivatives bearing the pyrazole scaffold were screened to evaluate them as a reproductive toxicant in… read more here.
Keywords: design synthesis; screening triazolopyrimidine; testicular germ; germ cells ... See more keywords
Design, synthesis, in silico and antiproliferative evaluation of novel pyrazole derivatives as VEGFR‐2 inhibitors
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DOI: 10.1002/ardp.201700234
Abstract: As the blockade of the VEGFR‐2 signaling pathway is a viable approach in cancer therapy, the present study focuses on a series of pyrazole based VEGFR‐2 inhibitors that were designed on the basis of the… read more here.
Keywords: design synthesis; evaluation novel; synthesis silico; vegfr inhibitors ... See more keywords
Design, synthesis, biological evaluations, molecular docking, and in vivo studies of novel phthalimide analogs
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DOI: 10.1002/ardp.201700363
Abstract: A series of novel phthalimide analogs containing an indole or brominated indole moiety were synthesized and their antimicrobial activity was evaluated. Compound 8 showed a broad spectrum activity, revealing 53–67% of erythromycin activity on the… read more here.
Keywords: design synthesis; novel phthalimide; cell lines; compound ... See more keywords
Design and synthesis of novel annulated thienopyrimidines as phosphodiesterase 5 (PDE5) inhibitors
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DOI: 10.1002/ardp.201800018
Abstract: Novel cycloalkene‐fused thienopyrimidine analogues with enhanced phosphodiesterase 5 (PDE5) inhibitory properties are presented. The structure of the reported scaffold was modulated through variation of the terminal cycloalkene ring size, as well as by varying the… read more here.
Keywords: design synthesis; synthesis novel; phosphodiesterase; phosphodiesterase pde5 ... See more keywords
Design, synthesis, and molecular docking study of benzothiazolotriazine derivatives for anticonvulsant potential
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DOI: 10.1002/ardp.201800154
Abstract: A series of newer benzothiazolotriazine derivatives (4a–k) was designed, synthesized, and characterized as anticonvulsant agents against the two classically used MES and scPTZ animal models. The synthesized derivatives were tested in vivo in both the… read more here.
Keywords: design synthesis; benzothiazolotriazine derivatives; study; animal models ... See more keywords
Design, synthesis, and antitubercular activity of 3‐amidophenols with 5‐heteroatomic substitutions
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DOI: 10.1002/ardp.201800277
Abstract: A series of novel 3‐amidophenols with 5‐heteroatomic substitutions were designed and synthesized. Several compounds showed potent antitubercular activity against Mycobacterium tuberculosis H37Ra (MIC = 0.25–5 μg/mL). Compounds 12j and 14i also displayed good inhibitory activity against M. tuberculosis… read more here.
Keywords: design synthesis; heteroatomic substitutions; activity; synthesis antitubercular ... See more keywords
Design, synthesis, biological evaluation, and molecular dynamics of novel cholinesterase inhibitors as anti‐Alzheimer's agents
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DOI: 10.1002/ardp.201800352
Abstract: A series of novel chroman‐4‐one derivatives were designed and synthesized successfully with good to excellent yield (3a–l). In addition, the obtained products were evaluated for their cholinesterase (ChE) inhibitory activities. The results show that among… read more here.
Keywords: design synthesis; cholinesterase; biological evaluation; molecular dynamics ... See more keywords
Design, synthesis and biological evaluation of 6‐substituted quinolines derived from cabozantinib as c‐Met inhibitors
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DOI: 10.1002/ardp.201900101
Abstract: Based on the cabozantinib scaffold, novel c‐Met inhibitors were rationalized from the limited knowledge of structure‐activity relationships for the quinoline 6‐position. Emphasis was given to modifications capable of engaging in additional polar interactions with the… read more here.
Keywords: design synthesis; biological evaluation; met inhibitors; substituted quinolines ... See more keywords
Design, synthesis, and antiproliferative effect of 2,9‐bis[4‐(pyridinylalkylaminomethyl)phenyl]‐1,10‐phenanthroline derivatives on human leukemic cells by targeting G‐quadruplex
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DOI: 10.1002/ardp.202000450
Abstract: Current multiagent chemotherapy regimens have improved the cure rate in acute leukemia patients, but they are highly toxic and poorly efficient in relapsed patients. To improve the treatment approaches, new specific molecules are needed. The… read more here.
Keywords: phenyl phenanthroline; phenanthroline derivatives; bis; design synthesis ... See more keywords
Design, synthesis, and molecular docking study of novel quinoline‐based bis‐chalcones as potential antitumor agents
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DOI: 10.1002/ardp.202100094
Abstract: A novel series of quinoline‐based symmetrical and unsymmetrical bis‐chalcones was synthesized via a Claisen–Schmidt condensation reaction between 3‐formyl‐quinoline/quinolone derivatives with acetone or arylidene acetones, respectively, by using KOH/MeOH/H2O as a reaction medium. Twelve of the… read more here.
Keywords: design synthesis; bis chalcones; quinoline; bis ... See more keywords