Asunto(s)
Angioedema , Trasplante de Células Madre de Sangre del Cordón Umbilical , Enfermedad Injerto contra Huésped , Humanos , Enfermedad Injerto contra Huésped/etiología , Trasplante de Células Madre de Sangre del Cordón Umbilical/efectos adversos , Angioedema/etiología , Enfermedad Crónica , Masculino , Femenino , Adulto , Síndrome de Bronquiolitis ObliteranteRESUMEN
A novel microbial method for the production of 2',3'-dideoxynucleosides by transdideoxyribosylation has been developed. By screening microorganisms producing 2',3'-dideoxyadenosine (DDA) from 2',3'-dideoxyuridine (DDU) and adenine, Escherichia coli AJ 2595 was selected as the best producer. Optimal pH and temperature for the DDA-producing reaction were ca. 6.5 and 50 degrees C, respectively. Pi seemed to be an essential factor for the reaction, and its optimal concentration was ca. 25 mM. Moreover, polyethylene glycol had a notable effect on DDA production. Under the best conditions established, 52 mM DDA was obtained from 100 mM DDU and 100 mM adenine after 48 h of incubation from resting cells of E. coli AJ 2595. This strain could also produce 2',3'-dideoxynucleosides, such as 2',3'-dideoxyinosine (DDI), 2',3'-dideoxyguanosine, and 2',3'-dideoxythymidine, from DDU and the corresponding bases. In particular, this strain could produce DDI in high yield (ca. 32 mM from 100 mM DDU and 100 mM hypoxanthine) after 24 h of incubation. However, 2',3'-dideoxycytidine was not produced from DDU and cytosine by resting cells of E. coli AJ 2595.
Asunto(s)
Antivirales/síntesis química , Didesoxinucleósidos/metabolismo , Escherichia coli/metabolismo , Bacterias/metabolismo , Didanosina , Didesoxiadenosina , Escherichia coli/crecimiento & desarrollo , Concentración de Iones de Hidrógeno , Cinética , TemperaturaRESUMEN
An economical synthesis of famciclovir from N-2-acetyl-7-benzylguanine by a novel regioselective alkylation with the diester cyclopropane compound was developed.