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Items from 1 to 20 out of 282 results

article

Synthesis and evaluation of pharmacological properties of some new xanthone derivatives with piperazine moiety

A.M. Waszkielewicz, A. Gunia, N. Szkaradek, K. Pytka, more

Bioorganic & Medicinal Chemistry Letters > 2013 > 23 > 15 > 4419-4423

A series of new xanthone derivatives with piperazine moiety [1–7] was synthesized and evaluated for their pharmacological properties. They were subject to binding assays for α ₁ and β ₁ adrenergic as well as 5-HT _1A , 5-HT ₆ and 5-HT _7b serotoninergic receptors. Five of the tested compounds were also evaluated for their anticonvulsant properties. The compound...

article

Evaluation of thiopyrano[2,3‐d]thiazole derivatives as potential anticonvulsant agents

Eduard Davydov, Mykhailo Hoidyk, Sergiy Shtrygol', Andriy Karkhut, more

Archiv der Pharmazie > 357 > 10 > n/a - n/a

Anticonvulsant drug discovery has achieved significant progress; however, pharmacotherapy of epilepsy continues to be a challenge for modern medicine and pharmacy. To expand the chemical space of heterocycles as potential antiepileptic agents, herein we report on the synthesis and evaluation of anticonvulsant properties of a series of thiopyrano[2,3‐d]thiazoles. The studied heterocycles are characterized...

article

Synthesis, characterization, and biological study of new synthetic opioid hemorphin‐4 peptides containing sterically restricted nonnatural amino acids

Petar Todorov, Stela Georgieva, Claudio Trapella, Kalin Chakarov, more

Archiv der Pharmazie > 357 > 7 > n/a - n/a

Some new hemorphin‐4 analogs with structures of Xxx‐Pro‐Trp‐Thr‐NH₂ and Tyr‐Yyy‐Trp‐Thr‐NH₂, where Xxx is 2‐amino‐3‐(4−hydroxy‐2,6‐dimethylphenyl)propanoic acid or 2‐amino‐3‐(4‐dibenzylamino‐2,6‐dimethylphenyl)propanoic acid, and Yyy is (2S,4S)‐4‐amino‐pyrrolidine‐2‐carboxylic acid, were synthesized and characterized by electrochemical and spectral analyses. In vivo anticonvulsant and antinociceptive...

article

Promising anticonvulsant and/or analgesic compounds among 5‐chloro‐2‐ or 5‐chloro‐4‐methyl derivatives of xanthone coupled to aminoalkanol moieties—Design, synthesis and pharmacological evaluation

Gabriela Mazur, Katarzyna Pańczyk‐Straszak, Anna Rapacz, Jan Kiszela, more

Chemical Biology & Drug Design > 101 > 2 > 278 - 325

A series of 10 aminoalkanol derivatives of 5‐chloro‐2‐ or 5‐chloro‐4‐methylxanthone was synthetized and evaluated for anticonvulsant properties (MES test, mice, intraperitoneal) and compared with neurotoxicity rotarod test (NT, mice, i.p.). The best results both in terms of anticonvulsant activity and protective index value were obtained for 3: 5‐chloro‐2‐([4‐hydroxypiperidin‐1‐yl]methyl)‐9H‐xanthen‐9‐one...

article

Polymeric nanoencapsulation of zaleplon into PLGA nanoparticles for enhanced pharmacokinetics and pharmacological activity

Yusuf A. Haggag, Ahmed Kh. Abosalha, Murtaza M. Tambuwala, Enass Y. Osman, more

Biopharmaceutics & Drug Disposition > 42 > 1 > 12 - 23

Zaleplon (ZP) is a sedative and hypnotic drug used for the treatment of insomnia. Despite its potent anticonvulsant activity, ZP is not commonly used for the treatment of convulsion since ZP is characterized by its low oral bioavailability as a result of poor solubility and extensive liver metabolism. The following study aimed to formulate specifically controlled release nano‐vehicles for oral and...

article

Synthesis, anticonvulsant, and antinociceptive activity of new 3‐(3‐methyl‐2,5‐dioxo‐3‐phenylpyrrolidin‐1‐yl)propanamides and 3‐phenyl‐butanamides

Jolanta Obniska, Małgorzata Góra, Anna Rapacz, Kinga Sałat, more

Archiv der Pharmazie > 354 > 1 > n/a - n/a

A focused library of new 3‐(3‐methyl‐2,5‐dioxo‐3‐phenylpyrrolidin‐1‐yl)propanamides and their nonimide analogs were synthesized and tested for anticonvulsant activity. These compounds were obtained through the coupling reaction of the starting carboxylic acids with appropriate amines. The initial anticonvulsant screening was performed in mice (intraperitoneal administration) using the maximal electroshock...

article

Development of novel indole‐linked pyrazoles as anticonvulsant agents: A molecular hybridization approach

Deweshri R. Kerzare, Sunil S. Menghani, Nilesh R. Rarokar, Pramod B. Khedekar

Archiv der Pharmazie > 354 > 1 > n/a - n/a

A series of 3‐{2‐[1‐acetyl‐5‐(substitutedphenyl)‐4,5‐dihydropyrazol‐3‐yl]hydrazinylidene}‐1,3‐dihydro‐2H‐indol‐2‐ones 24–43 was synthesized using an appropriate synthetic route and evaluated experimentally by the maximal electroshock test. These compounds were evaluated for antidepressant and antianxiety activities. The most active compound, 3‐{2‐[1‐acetyl‐5‐(4‐chlorophenyl)‐4,5‐dihydropyrazol‐3‐yl]hydrazinylidene}‐1,3‐dihydro‐2...

article

Synthesis, characterization and anticonvulsant activity of new series of N-modified analogues of VV-hemorphin-5 with aminophosphonate moiety

Petar Todorov, Petia Peneva, Jana Tchekalarova, Miroslav Rangelov, more

Amino Acids > 2019 > 51 > 10-12 > 1527-1545

A new series of N-modified analogues of the VV-hemorphin-5 with aminophosphonate moiety have been synthesized, characterized and investigated for anticonvulsant activity. The novel peptide analogues were prepared by solid-phase peptide synthesis–Fmoc-strategy and were evaluated in the timed intravenous pentylenetetrazole infusion test (ivPTZ) and 6-Hz psychomotor seizure test in mice. The acute neurological...

article

Synthesis of 4-Phenylpyrrolidone Derivatives with Anticonvulsant and Nootropic Activity

L. A. Zhmurenko, S. A. Litvinova, G. V. Mokrov, I. G. Kovalev, more

Pharmaceutical Chemistry Journal > 2019 > 53 > 5 > 429-435

New 4-phenylpyrrolidone derivatives were designed from racetam structures that combine nootropic and anticonvulsant activity. The proposed compounds were synthesized using 4-phenylpyrrolidone and aromatic amines. The anticonvulsant activity of the new compounds was studied. The structure–activity relationship was analyzed. The most active compound was the 2,6-dimethylanilide of (2-oxo-4-phenylpyrrolidin-1-yl)acetic...

article

Synthesis and Anticonvulsant Activity of 4-Amino-3-Nitro-1-Thiocoumarins and 4-Amino-3-Nitroquinolin-2-Ones

G. V. Mokrov, T. A. Voronina, S. A. Litvinova, I. G. Kovalev, more

Pharmaceutical Chemistry Journal > 2019 > 53 > 3 > 194-200

Novel thiocoumarins and quinolin-2-ones were synthesized and screened for anticonvulsant activity. The structure–activity relationship of a series of synthesized compounds and previously prepared coumarin derivatives was analyzed. The methyl ester of N-(3-nitro-2-oxo-1,2-dihydroquinolin-4-yl)-4-aminobutyric acid (3a) at a dose of 12.5 mg/kg (i.p.) had the greatest anticonvulsant activity in mouse...

article

Anticonvulsant evaluation and docking analysis of VV‐Hemorphin‐5 analogues

Petar Todorov, Miroslav Rangelov, Petia Peneva, Nadezhda Todorova, more

Drug Development Research > 80 > 4 > 425 - 437

VV‐Hemorphin‐5 is an endogenous opioid peptide of the Hemorphin family with affinity at opioid receptors. A series of C‐amide analogues have been synthesized, based on the structure of VV‐Hemorphin‐5, modified at position 1 and 7 by the un/natural amino acids (Aa8‐Val‐Val‐Tyr‐Pro‐Trp‐Thr‐Gln‐NH₂ and Val‐Val‐Tyr‐Pro‐Trp‐Thr‐Aa1‐NH₂) using SPPS, Fmoc‐chemistry. The peptide derivatives were evaluated...

article

Synthesis and Anticonvulsant Activity of N-Substituted 4-Amino-3-Nitrocoumarins

G. V. Mokrov, V. L. Savel’ev, T. A. Voronina, S. A. Litvinova, more

Pharmaceutical Chemistry Journal > 2019 > 53 > 2 > 118-124

The synthesis and anticonvulsant activity of new coumarin derivatives are reported. N-(3-Nitrocoumarin-4-yl)-4-aminobutyric acid (1a) at doses of 60 and 80 mg/kg (in the MES test) and methyl N-(3,6-dinitrocoumarin-4-yl)-4-aminobutyrate (1e) at doses of 20 and 40 mg/kg (in the corazole antagonism test) possessed the greatest anticonvulsant activity of the synthesized compounds. The results indicated...

article

Anticonvulsant Activity of Dimephosphonum

T. R. Abakumova, A. I. Karpenko, V. N. Khaziakhmetova, L. E. Ziganshina

BioNanoScience > 2019 > 9 > 2 > 235-237

A novel Russian medicine dimephosphonum at its therapeutic doses of 50 mg/kg and 100 mg/kg showed anti-seizure activity on models of primary generalized seizures caused by corazolum or by maximal electroshock in rats and mice. Dimephosphonum prevented death of rats and mice in both seizure models like reference preparations phenazepam, valproic acid, and levetiracetam. The effects of dimephosphonum...

article

Synthesis, characterization and anticonvulsant activity of new azobenzene-containing VV-hemorphin-5 bio photoswitch

Petar T. Todorov, Petia N. Peneva, Stela I. Georgieva, Jana Tchekalarova, more

Amino Acids > 2019 > 51 > 3 > 549-563

A novel analog of VV-hemorphin-5 containing azobenzene moiety has been synthesized and investigated for anticonvulsant activity in relation to its E → Z photophysical properties activated by long wavelength light at 365 nm. The synthesis was achieved by a modified SPPS by Fmoc-dimerization strategy. The electrochemical behavior before and after UV illumination was investigated using different voltammetric...

article

Design, graph theoretical analysis, density functionality theories, Insilico modeling, synthesis, characterization and biological activities of novel thiazole fused quinazolinone derivatives

Govindaraj Saravanan, Theivendren Panneerselvam, Veerachamy Alagarsamy, Selvaraj Kunjiappan, more

Drug Development Research > 79 > 6 > 260 - 274

A series of 2‐(2‐substituted benzylidenehydrazinyl‐2‐oxopropyl)‐3‐(4‐[4‐oxo‐2‐phenylthiazolo din‐3‐yl]phenyl)quinazolin‐4(3H)‐one 7a‐7l were synthesized and characterized by IR, ¹H‐NMR, ¹³C‐NMR, mass spectroscopy and elemental analyses. In this present study, the density functionality theory was performed to identify drug stability. Further we introduced graph theoretical analysis by utilised Kyoto...

article

Molecular docking, synthesis and anticonvulsant activity of some novel 3-(2-substituted)-4-oxothiazolidine-3-yl)-2-phenylquinazoline-4(3H)-ones

Sampada S. Jangam, Sagar B. Wankhede, Sohan S. Chitlange

Research on Chemical Intermediates > 2019 > 45 > 2 > 471-486

As the therapeutic potential of quinazolinone and thiazolidinone is well mentioned in literature for their versatile biological activities, their related toxicological profiles cannot be ignored. So, the purpose of this study is to synthesize 3-(2-substituted)-4-oxothiazolidine-3-yl)-2-phenylquinazoline-4(3H)-ones (3a–3k) and evaluate them as anticonvulsant agents. Novel series of 3a–3k were synthesized...

article

Synthesis, anticonvulsant activity, and molecular modeling studies of novel 1-phenyl/1-(4-chlorophenyl)-2-(1H-triazol-1-yl)ethanol ester derivatives

İnci Selin Doğan, Zeynep Özdemir, Suat Sari, İrem Bozbey, more

Medicinal Chemistry Research > 2018 > 27 > 9 > 2171-2186

A series of new ester derivatives were synthesized by the reaction of various acids with 1-phenyl/1-(4-chlorophenyl)-2-(1H-triazol-1-yl)ethanol and in vivo screened for their anticonvulsant activity. The title compounds were screened against MES and ScM seizure tests according to a modified version of the Epilepsy Therapy Screening Program (ETSP) protocol of the National Institutes of Health (NIH)...

article

Thiazoles with cyclopropyl fragment as antifungal, anticonvulsant, and anti-Toxoplasma gondii agents: synthesis, toxicity evaluation, and molecular docking study

Krzysztof Z. Łączkowski, Natalia Konklewska, Anna Biernasiuk, Anna Malm, more

Medicinal Chemistry Research > 2018 > 27 > 9 > 2125-2140

Synthesis and investigation of antifungal, anticonvulsant and anti-Toxoplasma gondii activities of ten novel (2-(cyclopropylmethylidene)hydrazinyl)thiazole 3a–3j are presented. Among the derivatives, compounds 3a–3d and 3f–3j possess very high activity against Candida spp. ATCC with MIC = 0.015–7.81 µg/ml. Compounds 3a–3d and 3f–3j possess also very high activity towards most of strains of Candida...

article

Water-Soluble Form of 1-Alkyl(Aryl)Imidazole-4,5-Dicarboxylic Acids. Structure and Anticonvulsant Activity of the Triethanolammonium Salt of 1-Propylimidazole-4,5-Dicarboxylic Acid

M. A. Brusina, D. N. Nikolaev, V. S. Fundamenskii, V. V. Gurzhii, more

Pharmaceutical Chemistry Journal > 2018 > 52 > 4 > 299-303

Water-soluble forms of a series of 1-alkyl(aryl)imidazole-4,5-dicarboxylic acids were prepared. Anticonvulsant activity of 1-propylimidazole-4,5-dicarboxylic acid and its triethanolammonium salt was studied using the NMDA-induced convulsion model. The triethanolammonium salt of 1-propylimidazole-4,5-dicarboxylic acid was shown to possess anticonvulsant activity whereas the acid itself was a convulsant...

article

Synthesis and study of substituted amides of some 5-membered isocyclic and heterocyclic acids as potential anticonvulsants

MARZANNA STRUPIŃSKA, BARTŁOMIEJ JAKUBOWICZ, GRAŻYNA ROSTAFIŃSKA-SUCHAR, ELŻBIETA PIRIANOWICZ-CHABER, more

Acta Poloniae Pharmaceutica - Drug Research > 2018 > 75 > 3

A series of substituted amides of isocyclic and heterocyclic acids have been synthesized. All obtained compounds were evaluated qualitatively for their anticonvulsant activity in the maximal electroshock seizure test (MES test) and psychomotor seizure test (6 Hz test) in mice after intraperitoneal administration. The neurological toxicity was determined in the rotorod neurotoxicity test (Tox test)...

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Synthesis and evaluation of pharmacological properties of some new xanthone derivatives with piperazine moiety

Evaluation of thiopyrano[2,3‐d]thiazole derivatives as potential anticonvulsant agents

Synthesis, characterization, and biological study of new synthetic opioid hemorphin‐4 peptides containing sterically restricted nonnatural amino acids

Promising anticonvulsant and/or analgesic compounds among 5‐chloro‐2‐ or 5‐chloro‐4‐methyl derivatives of xanthone coupled to aminoalkanol moieties—Design, synthesis and pharmacological evaluation

Polymeric nanoencapsulation of zaleplon into PLGA nanoparticles for enhanced pharmacokinetics and pharmacological activity

Synthesis, anticonvulsant, and antinociceptive activity of new 3‐(3‐methyl‐2,5‐dioxo‐3‐phenylpyrrolidin‐1‐yl)propanamides and 3‐phenyl‐butanamides

Development of novel indole‐linked pyrazoles as anticonvulsant agents: A molecular hybridization approach

Synthesis, characterization and anticonvulsant activity of new series of N-modified analogues of VV-hemorphin-5 with aminophosphonate moiety

Synthesis of 4-Phenylpyrrolidone Derivatives with Anticonvulsant and Nootropic Activity

Synthesis and Anticonvulsant Activity of 4-Amino-3-Nitro-1-Thiocoumarins and 4-Amino-3-Nitroquinolin-2-Ones

Anticonvulsant evaluation and docking analysis of VV‐Hemorphin‐5 analogues

Synthesis and Anticonvulsant Activity of N-Substituted 4-Amino-3-Nitrocoumarins

Anticonvulsant Activity of Dimephosphonum

Synthesis, characterization and anticonvulsant activity of new azobenzene-containing VV-hemorphin-5 bio photoswitch

Design, graph theoretical analysis, density functionality theories, Insilico modeling, synthesis, characterization and biological activities of novel thiazole fused quinazolinone derivatives

Molecular docking, synthesis and anticonvulsant activity of some novel 3-(2-substituted)-4-oxothiazolidine-3-yl)-2-phenylquinazoline-4(3H)-ones

Synthesis, anticonvulsant activity, and molecular modeling studies of novel 1-phenyl/1-(4-chlorophenyl)-2-(1H-triazol-1-yl)ethanol ester derivatives

Thiazoles with cyclopropyl fragment as antifungal, anticonvulsant, and anti-Toxoplasma gondii agents: synthesis, toxicity evaluation, and molecular docking study

Water-Soluble Form of 1-Alkyl(Aryl)Imidazole-4,5-Dicarboxylic Acids. Structure and Anticonvulsant Activity of the Triethanolammonium Salt of 1-Propylimidazole-4,5-Dicarboxylic Acid

Synthesis and study of substituted amides of some 5-membered isocyclic and heterocyclic acids as potential anticonvulsants

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