Biosynthesis of human diazepam and clonazepam metabolites. 2015

Núbia C de Paula, and Kelly C F Araujo Cordeiro, and Paula L de Melo Souza, and Diogo F Nogueira, and Diego B da Silva e Sousa, and Maísa B Costa, and François Noël, and Valéria de Oliveira
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.

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.

UI MeSH Term Description Entries
D007218 Industrial Microbiology The study, utilization, and manipulation of those microorganisms capable of economically producing desirable substances or changes in substances, and the control of undesirable microorganisms. Microbiology, Industrial
D008745 Methylation Addition of methyl groups. In histo-chemistry methylation is used to esterify carboxyl groups and remove sulfate groups by treating tissue sections with hot methanol in the presence of hydrochloric acid. (From Stedman, 25th ed) Methylations
D002597 Chaetomium A genus of ascomycetous fungi of the family Chaetomiaceae, order SORDARIALES. Many members are cellulolytic and some mycotoxic. They occur naturally on paper and cotton fabric. Chaetomiums
D002998 Clonazepam An anticonvulsant used for several types of seizures, including myotonic or atonic seizures, photosensitive epilepsy, and absence seizures, although tolerance may develop. It is seldom effective in generalized tonic-clonic or partial seizures. The mechanism of action appears to involve the enhancement of GAMMA-AMINOBUTYRIC ACID receptor responses. 2H-1,4-Benzodiazepin-2-one, 5-(2-chlorophenyl)-1,3-dihydro-7-nitro-,Klonopin,Antelepsin,Rivotril,Ro 5-4023,Ro 54023
D003975 Diazepam A benzodiazepine with anticonvulsant, anxiolytic, sedative, muscle relaxant, and amnesic properties and a long duration of action. Its actions are mediated by enhancement of GAMMA-AMINOBUTYRIC ACID activity. 7-Chloro-1,3-dihydro-1-methyl-5-phenyl-2H-1,4-benzodiazepin-2-one,Apaurin,Diazemuls,Faustan,Relanium,Seduxen,Sibazon,Stesolid,Valium
D005658 Fungi A kingdom of eukaryotic, heterotrophic organisms that live parasitically as saprobes, including MUSHROOMS; YEASTS; smuts, molds, etc. They reproduce either sexually or asexually, and have life cycles that range from simple to complex. Filamentous fungi, commonly known as molds, refer to those that grow as multicellular colonies. Fungi, Filamentous,Molds,Filamentous Fungi,Filamentous Fungus,Fungus,Fungus, Filamentous,Mold
D006801 Humans Members of the species Homo sapiens. Homo sapiens,Man (Taxonomy),Human,Man, Modern,Modern Man
D006868 Hydrolysis The process of cleaving a chemical compound by the addition of a molecule of water.
D006900 Hydroxylation Placing of a hydroxyl group on a compound in a position where one did not exist before. (Stedman, 26th ed) Hydroxylations
D000927 Anticonvulsants Drugs used to prevent SEIZURES or reduce their severity. Anticonvulsant,Anticonvulsant Drug,Anticonvulsive Agent,Anticonvulsive Drug,Antiepileptic,Antiepileptic Agent,Antiepileptic Agents,Antiepileptic Drug,Anticonvulsant Drugs,Anticonvulsive Agents,Anticonvulsive Drugs,Antiepileptic Drugs,Antiepileptics,Agent, Anticonvulsive,Agent, Antiepileptic,Agents, Anticonvulsive,Agents, Antiepileptic,Drug, Anticonvulsant,Drug, Anticonvulsive,Drug, Antiepileptic,Drugs, Anticonvulsant,Drugs, Anticonvulsive,Drugs, Antiepileptic

Related Publications

Núbia C de Paula, and Kelly C F Araujo Cordeiro, and Paula L de Melo Souza, and Diogo F Nogueira, and Diego B da Silva e Sousa, and Maísa B Costa, and François Noël, and Valéria de Oliveira
February 1995, Nihon rinsho. Japanese journal of clinical medicine,
Núbia C de Paula, and Kelly C F Araujo Cordeiro, and Paula L de Melo Souza, and Diogo F Nogueira, and Diego B da Silva e Sousa, and Maísa B Costa, and François Noël, and Valéria de Oliveira
September 1999, Nihon rinsho. Japanese journal of clinical medicine,
Núbia C de Paula, and Kelly C F Araujo Cordeiro, and Paula L de Melo Souza, and Diogo F Nogueira, and Diego B da Silva e Sousa, and Maísa B Costa, and François Noël, and Valéria de Oliveira
December 2004, Nihon rinsho. Japanese journal of clinical medicine,
Núbia C de Paula, and Kelly C F Araujo Cordeiro, and Paula L de Melo Souza, and Diogo F Nogueira, and Diego B da Silva e Sousa, and Maísa B Costa, and François Noël, and Valéria de Oliveira
January 1980, Farmakologiia i toksikologiia,
Núbia C de Paula, and Kelly C F Araujo Cordeiro, and Paula L de Melo Souza, and Diogo F Nogueira, and Diego B da Silva e Sousa, and Maísa B Costa, and François Noël, and Valéria de Oliveira
February 1990, Nihon rinsho. Japanese journal of clinical medicine,
Núbia C de Paula, and Kelly C F Araujo Cordeiro, and Paula L de Melo Souza, and Diogo F Nogueira, and Diego B da Silva e Sousa, and Maísa B Costa, and François Noël, and Valéria de Oliveira
March 1977, Journal of chromatography,
Núbia C de Paula, and Kelly C F Araujo Cordeiro, and Paula L de Melo Souza, and Diogo F Nogueira, and Diego B da Silva e Sousa, and Maísa B Costa, and François Noël, and Valéria de Oliveira
June 1973, Epilepsia,
Núbia C de Paula, and Kelly C F Araujo Cordeiro, and Paula L de Melo Souza, and Diogo F Nogueira, and Diego B da Silva e Sousa, and Maísa B Costa, and François Noël, and Valéria de Oliveira
September 1975, The Journal of pharmacy and pharmacology,
Núbia C de Paula, and Kelly C F Araujo Cordeiro, and Paula L de Melo Souza, and Diogo F Nogueira, and Diego B da Silva e Sousa, and Maísa B Costa, and François Noël, and Valéria de Oliveira
June 1974, Journal of chromatography,
Núbia C de Paula, and Kelly C F Araujo Cordeiro, and Paula L de Melo Souza, and Diogo F Nogueira, and Diego B da Silva e Sousa, and Maísa B Costa, and François Noël, and Valéria de Oliveira
December 1989, Canadian journal of psychiatry. Revue canadienne de psychiatrie,
Copied contents to your clipboard!