5-[Aryloxypyridyl (or nitrophenyl)]-4H-1,2,4-triazoles as novel flexible benzodiazepine analogues: Synthesis, receptor binding affinity and lipophilicity-dependent anti-seizure onset of action.

Navidpour, Latifeh; Shabani, Shabnam; Heidari, Alireza; Bashiri, Manouchehr; Ebrahim-Habibi, Azadeh; Shahhosseini, Soraya; Shafaroodi, Hamed; Abbas Tabatabai, Sayyed; Toolabi, Mahsa

Navidpour, Latifeh; Shabani, Shabnam; Heidari, Alireza; Bashiri, Manouchehr; Ebrahim-Habibi, Azadeh; Shahhosseini, Soraya; Shafaroodi, Hamed; Abbas Tabatabai, Sayyed; Toolabi, Mahsa.

Afiliação

Navidpour L; Department of Medicinal Chemistry, Faculty of Pharmacy, Tehran University of Medical Sciences, Tehran 14176, Iran. Electronic address: navidpur@sina.tums.ac.ir.
Shabani S; Department of Medicinal Chemistry, Faculty of Pharmacy, Tehran University of Medical Sciences, Tehran 14176, Iran.
Heidari A; Department of Medicinal Chemistry, School of Pharmacy, Tehran Azad University of Medical Sciences, Tehran, Iran.
Bashiri M; Department of Pharmaceutical Chemistry, School of Pharmacy, Shahid Beheshti University of Medical Sciences, Tehran, Iran.
Ebrahim-Habibi A; Biosensor Research Center, Endocrinology and Metabolism Molecular-Cellular Sciences Institute, Tehran University of Medical Sciences, Tehran, Iran; Endocrinology and Metabolism Research Center, Endocrinology and Metabolism Clinical Sciences Institute, Tehran University of Medical Sciences, Tehran, I
Shahhosseini S; Department of Pharmaceutical Chemistry, School of Pharmacy, Shahid Beheshti University of Medical Sciences, Tehran, Iran.
Shafaroodi H; Department of Pharmacology, Faculty of Medicine, Tehran University of Medical Sciences, Tehran 14174, Iran.
Abbas Tabatabai S; Department of Pharmaceutical Chemistry, School of Pharmacy, Shahid Beheshti University of Medical Sciences, Tehran, Iran.
Toolabi M; Department of Medicinal Chemistry, Faculty of Pharmacy, Tehran University of Medical Sciences, Tehran 14176, Iran.

Bioorg Chem ; 106: 104504, 2021 01.

Article em En | MEDLINE | ID: mdl-33279247

Assuntos

Anticonvulsivantes/farmacologia; Benzodiazepinas/farmacologia; Receptores de GABA-A/química; Convulsões/tratamento farmacológico; Triazóis/farmacologia; Animais; Anticonvulsivantes/síntese química; Anticonvulsivantes/química; Benzodiazepinas/síntese química; Benzodiazepinas/química; Ligação Competitiva/efeitos dos fármacos; Relação Dose-Resposta a Droga; Interações Hidrofóbicas e Hidrofílicas; Masculino; Estrutura Molecular; Ratos; Ratos Sprague-Dawley; Relação Estrutura-Atividade; Triazóis/síntese química; Triazóis/química

Palavras-chave

1,2,4-triazole; Flexible benzodiazepines; GABAA/benzodiazepine receptor complex; Onset of action; PTZ induced seizure threshold

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Texto completo: 1 Base de dados: MEDLINE Assunto principal: Convulsões / Triazóis / Benzodiazepinas / Receptores de GABA-A / Anticonvulsivantes Idioma: En Ano de publicação: 2021 Tipo de documento: Article

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