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Biosynthesis of human diazepam and clonazepam metabolites.
Bioorg Med Chem Lett. 2015 Mar 01; 25(5):1026-9.BM

Abstract

A screening of fungal and microbial strains allowed to select the best microorganisms to produce in high yields some of the human metabolites of two benzodiazepine drugs, diazepam and clonazepam, in order to study new pharmacological activities and for chemical standard proposes. Among the microorganisms tested, Cunninghamella echinulata ATCC 9244 and Rhizopus arrhizus ATCC 11145 strains, were the most active producers of the mains metabolites of diazepam which included demethylated, hydroxylated derivatives. Beauveria bassiana ATCC 7159 and Chaetomium indicum LCP 984200 produced the 7 amino-clonazepam metabolite and a product of acid hydrolysis of this benzodiazepine.

Authors+Show Affiliations

Laboratório de Bioconversão, Faculdade de Farmácia-Universidade Federal de Goiás, Rua 240 esquina com 5(ª) Avenida S/N., Praça Universitária, CP 131, Setor Universitário, CEP: 74.605-220 Goiânia, GO, Brazil; Laboratório de Saúde Pública Dr. Giovanni Cysneiros, Secretaria Estadual do Estado de Goiás, Goiânia, GO, Brazil.Laboratório de Bioconversão, Faculdade de Farmácia-Universidade Federal de Goiás, Rua 240 esquina com 5(ª) Avenida S/N., Praça Universitária, CP 131, Setor Universitário, CEP: 74.605-220 Goiânia, GO, Brazil.Laboratório de Bioconversão, Faculdade de Farmácia-Universidade Federal de Goiás, Rua 240 esquina com 5(ª) Avenida S/N., Praça Universitária, CP 131, Setor Universitário, CEP: 74.605-220 Goiânia, GO, Brazil.Laboratório de Bioconversão, Faculdade de Farmácia-Universidade Federal de Goiás, Rua 240 esquina com 5(ª) Avenida S/N., Praça Universitária, CP 131, Setor Universitário, CEP: 74.605-220 Goiânia, GO, Brazil.Laboratório de Bioconversão, Faculdade de Farmácia-Universidade Federal de Goiás, Rua 240 esquina com 5(ª) Avenida S/N., Praça Universitária, CP 131, Setor Universitário, CEP: 74.605-220 Goiânia, GO, Brazil.Laboratório de Bioconversão, Faculdade de Farmácia-Universidade Federal de Goiás, Rua 240 esquina com 5(ª) Avenida S/N., Praça Universitária, CP 131, Setor Universitário, CEP: 74.605-220 Goiânia, GO, Brazil.Laboratório de Farmacologia Bioquímica e Molecular, Departamento de Farmacologia Básica e Clínica da Universidade Federal do Rio de Janeiro, RJ, Brazil.Laboratório de Bioconversão, Faculdade de Farmácia-Universidade Federal de Goiás, Rua 240 esquina com 5(ª) Avenida S/N., Praça Universitária, CP 131, Setor Universitário, CEP: 74.605-220 Goiânia, GO, Brazil. Electronic address: valeriaoliveira@ufg.br.

Pub Type(s)

Journal Article

Language

eng

PubMed ID

25655722

Citation

de Paula, Núbia C., et al. "Biosynthesis of Human Diazepam and Clonazepam Metabolites." Bioorganic & Medicinal Chemistry Letters, vol. 25, no. 5, 2015, pp. 1026-9.
de Paula NC, Araujo Cordeiro KC, de Melo Souza PL, et al. Biosynthesis of human diazepam and clonazepam metabolites. Bioorg Med Chem Lett. 2015;25(5):1026-9.
de Paula, N. C., Araujo Cordeiro, K. C., de Melo Souza, P. L., Nogueira, D. F., da Silva e Sousa, D. B., Costa, M. B., Noël, F., & de Oliveira, V. (2015). Biosynthesis of human diazepam and clonazepam metabolites. Bioorganic & Medicinal Chemistry Letters, 25(5), 1026-9. https://doi.org/10.1016/j.bmcl.2015.01.025
de Paula NC, et al. Biosynthesis of Human Diazepam and Clonazepam Metabolites. Bioorg Med Chem Lett. 2015 Mar 1;25(5):1026-9. PubMed PMID: 25655722.
* Article titles in AMA citation format should be in sentence-case
TY - JOUR T1 - Biosynthesis of human diazepam and clonazepam metabolites. AU - de Paula,Núbia C, AU - Araujo Cordeiro,Kelly C F, AU - de Melo Souza,Paula L, AU - Nogueira,Diogo F, AU - da Silva e Sousa,Diego B, AU - Costa,Maísa B, AU - Noël,François, AU - de Oliveira,Valéria, Y1 - 2015/01/20/ PY - 2014/11/13/received PY - 2015/01/12/revised PY - 2015/01/14/accepted PY - 2015/2/7/entrez PY - 2015/2/7/pubmed PY - 2015/12/17/medline KW - Benzodiazepines KW - Demethylation KW - Filamentous fungi KW - Hydroxylation KW - Metabolites KW - Nitroreduction SP - 1026 EP - 9 JF - Bioorganic & medicinal chemistry letters JO - Bioorg. Med. Chem. Lett. VL - 25 IS - 5 N2 - A screening of fungal and microbial strains allowed to select the best microorganisms to produce in high yields some of the human metabolites of two benzodiazepine drugs, diazepam and clonazepam, in order to study new pharmacological activities and for chemical standard proposes. Among the microorganisms tested, Cunninghamella echinulata ATCC 9244 and Rhizopus arrhizus ATCC 11145 strains, were the most active producers of the mains metabolites of diazepam which included demethylated, hydroxylated derivatives. Beauveria bassiana ATCC 7159 and Chaetomium indicum LCP 984200 produced the 7 amino-clonazepam metabolite and a product of acid hydrolysis of this benzodiazepine. SN - 1464-3405 UR - https://www.unboundmedicine.com/medline/citation/25655722/Biosynthesis_of_human_diazepam_and_clonazepam_metabolites_ L2 - https://linkinghub.elsevier.com/retrieve/pii/S0960-894X(15)00037-2 DB - PRIME DP - Unbound Medicine ER -