Drug resistance patterns of herpes simplex virus isolates from patient treated with acyclovir was written by McLaren, Colin; Chen, Ming S.; Ghazzouli, Ismail; Saral, Rein; Burns, William H.. And the article was included in Antimicrobial Agents and Chemotherapy on December 31,1985.Synthetic Route of C10H13FN2O5 The following contents are mentioned in the article:
A decrease in the in vitro sensitivity to acyclovir (ACV) [59277-89-3] was observed in successive isolates of herpes simplex virus type 1 from immunocompromised patients during i.v. therapy with this drug. The ACV-resistant isolate from patient 1 was cross-resistant to 9-(1,3-dihydroxy-2-propoxymethyl)guanine [82410-32-0] and (E)-5-(2-bromovinyl-2′-deoxyuridine [69304-47-8], but still susceptible to 3 fluoro-substituted pyrimidines, 2′-fluoro-5-iodo-1-β-D-arabinofuranosylcytosine (FIAC) [69123-90-6], 2′-fluoro-5-iodo-1-β-D-arabinofuranosyluracil (FIAU) [69123-98-4] and 2′-fluoro-1-β-D-arabinofuranosylthymine (FMAU) [69256-17-3]. Thymidine kinase (TK) [9002-06-6] from the resistant isolate showed a 50-fold or greater reduction in affinity for thymidine, FIAU, FMAU, and ACV, but the total enzyme activity was similar to that of the sensitive isolate. The ACV-resistant isolate from patient 2 was also resistant to the dihydroxypropyoxymethylguanine, the bromovinyldeoxyuridine, and the fluoro-substituted compounds; TK activity for this isolate was <1% of the patient's pretherapy isolate. An isolate obtained during a subsequent recurrence in patient 2 was susceptible to ACV and the other TK-dependent agents. The ACV-resistant isolate from patient 3 was partially resistant to FIAC and FIAU but still susceptible to FMAU; the viral TK had a 10-fold-lower affinity for ACV, FIAU, and FMAU than did the sensitive pretherapy isolate, whereas the level of TK activity detected was reduced to 6%. In none of the isolates studied was a change in sensitivity to phosphonoformic acid observed Compared with the corresponding pretherapy ACV-sensitive isolates, there was a 30-fold decrease in neurovirulence for mice of the 2 drug-resistant isolates with diminished levels of thymidine-phosphorylating activity and no change in virulence for the 3rd isolate. These findings indicate that mixed patterns of drug-resistance to TK-dependent antiviral compounds can occur in clin. isolates, resulting from changes in either the amount or the affinity of viral TK activity. This study involved multiple reactions and reactants, such as 1-((2R,3S,4R,5R)-3-Fluoro-4-hydroxy-5-(hydroxymethyl)tetrahydrofuran-2-yl)-5-methylpyrimidine-2,4(1H,3H)-dione (cas: 69256-17-3Synthetic Route of C10H13FN2O5).
1-((2R,3S,4R,5R)-3-Fluoro-4-hydroxy-5-(hydroxymethyl)tetrahydrofuran-2-yl)-5-methylpyrimidine-2,4(1H,3H)-dione (cas: 69256-17-3) belongs to pyrimidine derivatives. The aromatic compound pyrimidine, and its derivatives, are ubiquitous in nature. They are found in nucleic acids, vitamins, amino acids, antibiotics, alkaloids, and a variety of toxins. Drugs having the pyrimidine motif have manifested to exhibit gratifying biological activity like anticancer, antiviral, anti-inflammatory, antibacterial, and antihypertensive activities.Synthetic Route of C10H13FN2O5
69256-17-3;1-((2R,3S,4R,5R)-3-Fluoro-4-hydroxy-5-(hydroxymethyl)tetrahydrofuran-2-yl)-5-methylpyrimidine-2,4(1H,3H)-dione;The future of 69256-17-3;New trend of C10H13FN2O5;function of 69256-17-3