414861-65-7Relevant academic research and scientific papers
Investigation of the alkenyldiarylmethane non-nucleoside reverse transcriptase inhibitors as potential cAMP phosphodiesterase-4B2 inhibitors
Cullen, Matthew D.,Cheung, York-Fong,Houslay, Miles D.,Hartman, Tracy L.,Watson, Karen M.,Buckheit Jr., Robert W.,Pannecouque, Christophe,De Clercq, Erik,Cushman, Mark
, p. 1530 - 1533 (2008/09/19)
The alkenyldiarylmethanes (ADAMs) are currently being investigated as non-nucleoside HIV-1 reverse transcriptase inhibitors (NNRTIs) of potential value in the treatment of HIV infection and AIDS. During the course of these studies, a number of ADAM analog
Alkenyldiarylmethanes, Fused Analogs And Syntheses Thereof
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Page/Page column 23-24; 10, (2009/01/20)
Non-nucleoside inhibitors of HIV-1 reverse transcriptase are described. Such inhibitors may be used as part of a combination therapy to treat HIV infection. Compounds described herein exhibit antiviral potency. In addition, compounds described herein exhibit metabolic stability. Also described herein are processes for preparing Non-nucleoside inhibitors of HIV-1 reverse transcriptase.
Synthesis and biological evaluation of alkenyldiarylmethane HIV-I non-nucleoside reverse transcriptase inhibitors that possess increased hydrolytic stability
Cullen, Matthew D.,Deng, Bo-Liang,Hartman, Tracy L.,Watson, Karen M.,Buckheit Jr., Robert W.,Pannecouque, Christophe,De Clercq, Erik,Cushman, Mark
, p. 4854 - 4867 (2008/03/12)
Non-nucleoside inhibitors of HIV reverse transcriptase (NNRTIs), albeit not the mainstays of HIV/AIDS treatment, have become increasingly important in highly active antiretroviral therapy (HAART) due to their unique mechanism of action. Several years ago
Synthesis, anti-HIV activity, and metabolic stability of new alkenyldiarylmethane HIV-1 non-nucleoside reverse transcriptase inhibitors
Deng, Bo-Liang,Hartman, Tracy L.,Buckheit Jr., Robert W.,Pannecouque, Christophe,De Clercq, Erik,Fanwick, Phillip E.,Cushman, Mark
, p. 6140 - 6155 (2007/10/03)
Non-nucleoside inhibitors of HIV-1 reverse transcriptase (NNRTIs) are part of the combination therapy currently used to treat HIV infection. Based on analogy with known HIV-1 NNRT inhibitors, 18 novel alkenyldiarylmethanes (ADAMs) containing 5-chloro-2-methoxyphenyl, 3-cyanophenyl, or 3-fluoro-5- trifluoromethylphenyl groups were synthesized and evaluated as HIV inhibitors. Their stabilities in rat plasma have also been investigated. Although introducing 5-chloro-2-methoxyphenyl or 3-fluoro-5-trifluoromethylphenyl groups into alkenyldiarylmethanes does not maintain the antiviral potency, the structural modification of alkenyldiarylmethanes with a 3-cyanophenyl substituent can be made without a large decrease in activity. The oxazolidinonyl group was introduced into the alkenyldiarylmethane framework and found to confer enhanced metabolic stability in rat plasma.
Design, synthesis, anti-HIV activities, and metabolic stabilities of alkenyldiarylmethane (ADAM) non-nucleoside reverse transcriptase inhibitors
Silvestri, Maximilian A.,Nagarajan, Muthukaman,De Clercq, Erik,Pannecouque, Christophe,Cushman, Mark
, p. 3149 - 3162 (2007/10/03)
The alkenyldiarylmethane (ADAM) HIV-1 non-nucleoside reverse transcriptase inhibitors (NNRTIs) are effective anti-HIV agents in cell culture. However, the potential clinical utility of the ADAMs is expected to be limited by the presence of methyl ester mo
Synthesis of alkenyldiarylmethane (ADAM) non-nucleoside HIV-1 reverse transcriptase inhibitors with non-Identical aromatic rings
Xu, Guozhang,Hartman, Tracy L.,Wargo, Heather,Turpin, Jim A.,Buckheit Jr., Robert W.,Cushman, Mark
, p. 283 - 290 (2007/10/03)
The existing methods for the synthesis of alkenyldiarylmethane (ADAM) non-nucleoside reverse transcriptase inhibitors proceed from symmetrical benzophenones and therefore result in products with identical aromatic rings. New methods have therefore been de
