Synthesis and evaluation of anticonvulsant activities of 7‐phenyl‐4,5,6,7‐tetrahydrothieno[3,2‐b ]pyridine derivatives
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DOI: 10.1002/ardp.201900106
Abstract: A series of 7‐phenyl‐4,5,6,7‐tetrahydrothieno[3,2‐b]pyridine derivatives containing triazole and other heterocycle substituents (methyltriazole, tetrazole, and triazolone) is described. Two experimental methods, maximal electroshock (MES) and subcutaneous pentylenetetrazole (scPTZ), were used to evaluate the anticonvulsant activity of… read more here.
Keywords: pyridine; tetrahydrothieno pyridine; evaluation anticonvulsant; synthesis evaluation ... See more keywords
Synthesis and evaluation of novel xanthene‐based thiazoles as potential antidiabetic agents
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DOI: 10.1002/ardp.202200356
Abstract: A series of xanthene‐based thiazoles was synthesized and characterized by different scpectroscopic methods, i.e. Proton nuclear magnetic resonance (1H NMR), carbon nuclear magnetic resonance (13C NMR), infrared spectroscopy, carbon hydrogen nitrogen analysis, and X‐ray crystallography.… read more here.
Keywords: evaluation novel; xanthene based; novel xanthene; based thiazoles ... See more keywords
Building siRNAs with Cubes: Synthesis and Evaluation of Cubane‐Modified siRNAs
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DOI: 10.1002/cbic.202100334
Abstract: Cubane molecules hold great potential for medicinal chemistry applications due to their inherent stability and low toxicity. In this study, we report the synthesis of a cubane derivative phosphoramidite for the incorporation of cubane into… read more here.
Keywords: building sirnas; cubes synthesis; cubane; sirnas cubes ... See more keywords
Design, Synthesis and Evaluation of AdSS Bisubstrate Inhibitors
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DOI: 10.1002/cmdc.202000498
Abstract: Many cancers lack the expression of methylthioadenosine phosphorylase (MTAP). These cancers require adenylosuccinate synthetase (AdSS) for nucleic acid synthesis. By inhibiting adenylosuccinate synthetase, we potentially have a new therapeutic agent. Bisubstrate inhibitors were synthesized and… read more here.
Keywords: evaluation adss; design synthesis; bisubstrate inhibitors; adss ... See more keywords
Synthesis and Evaluation of Voltage‐Gated Sodium Channel Blocking Pyrroline Derivatives Endowed with Both Antiarrhythmic and Antioxidant Activities
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DOI: 10.1002/cmdc.202000692
Abstract: Under the hypothesis that cardioprotective agents might benefit from synergism between antiarrhythmic activity and antioxidant properties, a small series of mexiletine analogues were coupled with the 2,2,5,5‐tetramethylpyrroline moiety, known for its antioxidant effect, in order… read more here.
Keywords: sodium channel; pyrroline derivatives; synthesis evaluation; evaluation voltage ... See more keywords
Synthesis and Evaluation of Functionalized Aryl and Biaryl Isothiocyanates against Human MCF‐7 Cells
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DOI: 10.1002/cmdc.202200250
Abstract: Organic isothiocyanates (ITCs) are a class of anticancer agents which naturally result from the enzymatic degradation of glucosinolates produced by Brassica vegetables. Previous studies have demonstrated that the structure of an ITC impacts its potency… read more here.
Keywords: evaluation; human mcf; itc; mcf cells ... See more keywords
Synthesis and Evaluation of Novel Spiro[oxindole-isoxazolidine] Derivatives as Potent Antioxidants
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DOI: 10.1002/jhet.2712
Abstract: The antioxidant activity of isatin derivatives can be described with the presence of enolic hydroxyl group at the second position of the ring because of the keto-enol tautomerism between NH and CO groups of indolone… read more here.
Keywords: novel spiro; isoxazolidine derivatives; oxindole isoxazolidine; synthesis evaluation ... See more keywords
Synthesis and Evaluation of Novel [1,2,4]Triazolo[1,5‐c]quinazoline Derivatives as Antibacterial Agents
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DOI: 10.1002/jhet.2979
Abstract: A series of new 2-aryl-5-methyl-[1,2,4]triazolo[1,5-c]quinazoline derivatives (5a–5g) have been synthesized by the reaction of 3-amino-2-methylquinazolin-4-(3H)-one (3) with aromatic nitriles in potassium tert-butoxide under reflux conditions. 3-Amino-2-methylquinazolin-4-(3H)-one (3) was synthesized by the reaction 2-methyl-4H-benzo[d][1,3]oxazin-4-one (2) with… read more here.
Keywords: triazolo quinazoline; synthesis evaluation; quinazoline derivatives; evaluation novel ... See more keywords
Design, Synthesis, and Evaluation of Bis‐Benzothiazole Derivatives as DNA Minor Groove Binding Agents
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DOI: 10.1002/jhet.3041
Abstract: A series of novel bis-benzothiazole derivatives with head-to-head orientation were designed, synthesized, and evaluated for their anti-proliferative activities on U937, HL60, and HeLa cells. A significant part of the targets exhibited considerable in vitro anticancer… read more here.
Keywords: design synthesis; bis benzothiazole; minor groove; benzothiazole derivatives ... See more keywords
Synthesis, Evaluation and Proposed Binding Pose of Substituted Spiro‐Oxindole Dihydroquinazolinones as IRAP Inhibitors
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DOI: 10.1002/open.201900344
Abstract: Abstract Insulin‐regulated aminopeptidase (IRAP) is a new potential macromolecular target for drugs aimed for treatment of cognitive disorders. Inhibition of IRAP by angiotensin IV (Ang IV) improves the memory and learning in rats. The majority… read more here.
Keywords: oxindole dihydroquinazolinones; irap inhibitors; evaluation proposed; irap ... See more keywords
Design, synthesis and evaluation of chalcones as H1N1 Neuraminidase inhibitors
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DOI: 10.1007/s00044-017-2124-2
Abstract: A series of chalcone derivatives (1a–2i) were designed based on isoliquiritigenin (the most active natural chalcone non-competitive neuraminidase (NA) inhibitor). Molecular modeling studies revealed that isoliquiritigenin and its designed analogs occupied 430-loop cavity of NA… read more here.
Keywords: h1n1 neuraminidase; design synthesis; chalcones h1n1; inhibition ... See more keywords