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A number of new 5'-phosphonate derivatives of 4'-thio-5-ethyl-2'-deoxyuridine (TEDU) were synthesized. These compounds displayed a low cytotoxicity and, except for TEDU 5'-fluorophosphate, antiherpes activity similar to that of 9-[(2-hydroxyethoxy)methyl]guanine (acyclovir) and 9-(4-hydroxy-3-hydroxymethylbut-1-yl)guanine (pencyclovir). 5'-Ethoxycarbonylphosphonate and 5'-aminocarbonylphosphonate of TEDU were also found to suppress the reproduction of herpes simplex type 1 virus, which is resistant to acyclovir.

online pharmacy ref source: www.ncbi.nlm.nih.gov/entrez/query.fcgi?cmd=Retrieve&db=PubMed&list_uids=12408030&dopt=Abstract




J Med Chem. 2002 Nov 7;45(23):5052-7.
Synthesis and biological activity of strongly fluorescent tricyclic analogues of acyclovir and ganciclovir.

Goslinski T, Golankiewicz B, De Clercq E, Balzarini J.

Institute of Bioorganic Chemistry, Polish Academy of Sciences, Noskowskiego 12/14, 61-704 Poznan, Poland.

In search of strongly fluorescent tricyclic analogues of acyclovir (ACV, 1) and ganciclovir (GCV, 2), derivatives of the 3,9-dihydro-9-oxo-5H-imidazo[1,2-a]purine system, several 6-[4-(acyloxy)phenyl], 6-[4-(acylamino)phenyl], and 6-[4-(phenoxycarbonyloxy)phenyl]-substituted TACV and TGCV analogues were synthesized and evaluated for their activity against herpes simplex virus types 1 and 2 in cell culture. All TACV and TGCV analogues showed strong fluorescence (quantum yield of 30-65% vs 2-aminopurine 100%). The 6-[4-(phenoxycarbonyloxy)phenyl]-substituted compounds 11 and 19 displayed the best combination of the fluorescence and antiviral potency.

online pharmacy ref source: www.ncbi.nlm.nih.gov/entrez/query.fcgi?cmd=Retrieve&db=PubMed&list_uids=12408716&dopt=Abstract




Ann Otolaryngol Chir Cervicofac. 2002 Sep;119(4):209-15.
[Treatment of Bell's palsy with acyclovir and methylprednisolone]

[Article in French]

Lejeune D, Bernat I, Vitte E, Lamas G, Willer JC, Soudant J, Tankere F.

Service d'ORL et de Chirurgie Cervico-Faciale, France.

OBJECTIVE: An open therapeutic trial was conducted in patients with Bell's palsy. Results were compared with data in the literature.MATERIALS AND METHODS: Between 1997 and 2000, 76 patients with Bell's palsy were treated with intravenous methylprednisolone (2 mg/kg/day) and acyclovir (5-10 mg/kg/8 hours) for 7 days. Treatment was initiated in all patients before the 14th day of illness. Severity of the palsy was scored on the first day of treatment and again one year later using the House and Brackman scale.RESULTS: Grade II or III palsy were observed in 38% of the patients at initial presentation, grades IV to VI in 62%. After treatment, 92% of the patients had reverted to grades I and II (good outcome) and only 8% had sequelae at 1-year follow-up. All patients with initial grade I or II recovered completely. For patients with grade IV, V, or VI complete recovery at 1 year was observed in 94, 86 and 50% respectively.CONCLUSION: Data in the literature suggest that corticosteroids should improve recovery in Bell's plasy. In our study, adjunction of acyclovir did not demonstrate any clear improvement in the cure rate. Benefit could depend on early prescription.

online pharmacy ref source: www.ncbi.nlm.nih.gov/entrez/query.fcgi?cmd=Retrieve&db=PubMed&list_uids=12410117&dopt=Abstract













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