RESUMO
Two amino derivatives of (D3)-Trishomocubanes recently synthesized were evaluated for their in vivo and in vitro activities against selected viruses. Both these derivatives exhibited promising in vivo activity against Herpes simplex Type II and Influenza A2/Taiwan, comparable with aciclovir and amantadine, respectively. No in vitro activity was observed for both compounds against Herpes simplex Types I and II and Rhinovirus 1A.
Assuntos
Antivirais/farmacologia , Hidrocarbonetos Aromáticos com Pontes/farmacologia , Vírus/efeitos dos fármacos , Aciclovir/farmacologia , Amantadina/farmacologia , Animais , Feminino , Herpes Genital/microbiologia , Vírus da Influenza A/efeitos dos fármacos , Camundongos , Rhinovirus/efeitos dos fármacos , Simplexvirus/efeitos dos fármacos , Vidarabina/farmacologiaRESUMO
The D3-trishomocubyl system was prepared from tertiary pentacyclo[5.4.0.0(2,6).0(3,10).0(5,9)]undecan-8-ols 5 in one step by using a modified Ritter reaction yielding only one of the possible two geometrical isomers of 4-amino-3-alkyl (or aryl)-D3-trishomocubane (8). Promising antagonism of reserpine-induced catalepsy was exhibited by these compounds which compared favorable with that of amantadine. Weak to mild anticholinergic properties were observed during the reduction of oxotremorine induced tremor and salivation procedure. Acute toxicities similar to that of amantadine were observed for some of these compounds. D3-Trishomocubyl-4-amines appeared as a promising new class of anti-Parkinson agents.
Assuntos
Antiparkinsonianos/síntese química , Hidrocarbonetos Aromáticos com Pontes/síntese química , Animais , Antiparkinsonianos/uso terapêutico , Antiparkinsonianos/toxicidade , Hidrocarbonetos Aromáticos com Pontes/uso terapêutico , Hidrocarbonetos Aromáticos com Pontes/toxicidade , Catalepsia/tratamento farmacológico , Fenômenos Químicos , Química , Masculino , Camundongos , Estereoisomerismo , Relação Estrutura-AtividadeRESUMO
A new pentacyclic triterpene [1] with anti-inflammatory activity was isolated from the roots of Commiphora merkeri. The structure was established on the basis of spectral data and conversion to its triacetate.
Assuntos
Analgésicos/isolamento & purificação , Anti-Inflamatórios/isolamento & purificação , Compostos Heterocíclicos/farmacologia , Plantas Medicinais/análise , Triterpenos/farmacologia , Compostos Heterocíclicos/isolamento & purificação , Espectroscopia de Ressonância Magnética , Estrutura Molecular , Esteroides , Triterpenos/isolamento & purificaçãoRESUMO
Chemical modification of the naturally occurring phlorophenone antimicrobial agent caespitin is described. These modifications include variations in the phenone side chain, substitution with prenyl, allyl, and benzyl in the 4-position of the phlorophenone nucleus, and ring cyclizations via etherification to give furan and chroman compounds. Several of these derivatives show enhanced in vitro potency over caespitin. Studies on the development of microbial resistance against these compounds show that no or very little resistance developed after several passes of these compounds in representative microbial strains.
