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10 results on '"Monzon, Katina"'

1. Discovery of adamantane ethers as inhibitors of 11β-HSD-1: Synthesis and biological evaluation

Author

Patel, Jyoti R., Shuai, Qi, Dinges, Jurgen, Winn, Marty, Pliushchev, Marina, Fung, Steven, Monzon, Katina, Chiou, William, Wang, Jiahong, Pan, Liping, Wagaw, Seble, Engstrom, Kenneth, Kerdesky, Francis A., Longenecker, Kenton, Judge, Russell, Qin, Wenying, Imade, Hovis M., Stolarik, DeAnne, Beno, David W.A., Brune, Michael, Chovan, Linda E., Sham, Hing L., Jacobson, Peer, and Link, J.T.

Published
2007
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2. Adamantane sulfone and sulfonamide 11-β-HSD1 Inhibitors

Author

Sorensen, Bryan, Winn, Martin, Rohde, Jeff, Shuai, Qi, Wang, Jiahong, Fung, Steven, Monzon, Katina, Chiou, William, Stolarik, DeAnne, Imade, Hovis, Pan, Liping, Deng, Xiaoqing, Chovan, Linda, Longenecker, Kenton, Judge, Russell, Qin, Wenying, Brune, Michael, Camp, Heidi, Frevert, Ernst U., Jacobson, Peer, and Link, J.T.

Published
2007
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3. Discovery and Metabolic Stabilization of Potent and Selective 2-Amino-N-(adamant-2-yl) Acetamide 11β-Hydroxysteroid Dehydrogenase Type 1 Inhibitors

Author

Rohde, Jeffrey J., primary, Pliushchev, Marina A., additional, Sorensen, Bryan K., additional, Wodka, Dariusz, additional, Shuai, Qi, additional, Wang, Jiahong, additional, Fung, Steven, additional, Monzon, Katina M., additional, Chiou, William J., additional, Pan, Liping, additional, Deng, Xiaoqing, additional, Chovan, Linda E., additional, Ramaiya, Atul, additional, Mullally, Mark, additional, Henry, Rodger F., additional, Stolarik, DeAnne F., additional, Imade, Hovis M., additional, Marsh, Kennan C., additional, Beno, David W. A., additional, Fey, Thomas A., additional, Droz, Brian A., additional, Brune, Michael E., additional, Camp, Heidi S., additional, Sham, Hing L., additional, Frevert, Ernst Uli, additional, Jacobson, Peer B., additional, and Link, J. T., additional

Published
2006
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6. Discovery of orally active butyrolactam 11β-HSD1 inhibitors

Author

Yeh, Vince S.C., primary, Kurukulasuriya, Ravi, additional, Fung, Steven, additional, Monzon, Katina, additional, Chiou, William, additional, Wang, Jiahong, additional, Stolarik, Deanne, additional, Imade, Hovis, additional, Shapiro, Robin, additional, Knourek-Segel, Victoria, additional, Bush, Eugene, additional, Wilcox, Denise, additional, Nguyen, Phong T., additional, Brune, Michael, additional, Jacobson, Peer, additional, and Link, J.T., additional

Published
2006
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8. Synthesis and biological evaluation of heterocycle containing adamantane 11β-HSD1 inhibitors

Author

Yeh, Vince S.C., primary, Patel, Jyoti R., additional, Yong, Hong, additional, Kurukulasuriya, Ravi, additional, Fung, Steven, additional, Monzon, Katina, additional, Chiou, William, additional, Wang, Jiahong, additional, Stolarik, Deanne, additional, Imade, Hovis, additional, Beno, David, additional, Brune, Michael, additional, Jacobson, Peer, additional, Sham, Hing, additional, and Link, J.T., additional

Published
2006
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9. Discovery and metabolic stabilization of potent and selective 2-amino-N-(adamant-2-yl) acetamide 11beta-hydroxysteroid dehydrogenase type 1 inhibitors.

Author

Rohde JJ, Pliushchev MA, Sorensen BK, Wodka D, Shuai Q, Wang J, Fung S, Monzon KM, Chiou WJ, Pan L, Deng X, Chovan LE, Ramaiya A, Mullally M, Henry RF, Stolarik DF, Imade HM, Marsh KC, Beno DW, Fey TA, Droz BA, Brune ME, Camp HS, Sham HL, Frevert EU, Jacobson PB, and Link JT

Subjects
11-beta-Hydroxysteroid Dehydrogenase Type 1 genetics, Adamantane pharmacokinetics, Animals, Cell Line, Humans, In Vitro Techniques, Mice, Microsomes, Liver metabolism, Piperazines pharmacokinetics, Rats, Stereoisomerism, Structure-Activity Relationship, Tissue Distribution, 11-beta-Hydroxysteroid Dehydrogenase Type 1 antagonists & inhibitors, Adamantane analogs & derivatives, Adamantane chemical synthesis, Piperazines chemical synthesis
Abstract

Starting from a rapidly metabolized adamantane 11beta-hydroxysteroid dehydrogenase type 1 (11beta-HSD1) inhibitor 22a, a series of E-5-hydroxy-2-adamantamine inhibitors, exemplified by 22d and (+/-)-22f, was discovered. Many of these compounds are potent inhibitors of 11beta-HSD1 and are selective over 11beta-HSD2 for multiple species (human, mouse, and rat), unlike other reported species-selective series. These compounds have good cellular potency and improved microsomal stability. Pharmacokinetic profiling in rodents indicated moderate to large volumes of distribution, short half-lives, and a pharmacokinetic species difference with the greatest exposure measured in rat with 22d. One hour postdose liver, adipose, and brain tissue 11beta-HSD1 inhibition was confirmed with (+/-)-22f in a murine ex vivo assay. Although 5,7-disubstitued-2-adamantamines provided greater stability, a single, E-5-position, polar functional group afforded inhibitors with the best combination of stability, potency, and selectivity. These results indicate that adamantane metabolic stabilization sufficient to obtain short-acting, potent, and selective 11beta-HSD1 inhibitors has been discovered.

Published
2007
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10. Adamantane 11-beta-HSD-1 inhibitors: Application of an isocyanide multicomponent reaction.

Author

Sorensen B, Rohde J, Wang J, Fung S, Monzon K, Chiou W, Pan L, Deng X, Stolarik D, Frevert EU, Jacobson P, and Link JT

Subjects
11-beta-Hydroxysteroid Dehydrogenase Type 1 metabolism, 11-beta-Hydroxysteroid Dehydrogenase Type 2 antagonists & inhibitors, 11-beta-Hydroxysteroid Dehydrogenase Type 2 metabolism, Adamantane chemistry, Adamantane pharmacokinetics, Animals, Enzyme Inhibitors chemistry, Enzyme Inhibitors pharmacokinetics, Humans, Mice, Molecular Structure, Structure-Activity Relationship, 11-beta-Hydroxysteroid Dehydrogenase Type 1 antagonists & inhibitors, Adamantane chemical synthesis, Adamantane pharmacology, Cyanides chemistry, Enzyme Inhibitors chemical synthesis, Enzyme Inhibitors pharmacology
Abstract

A series of potent and selective adamantane aminoamide 11-beta-HSD-1 inhibitors has been optimized. Chemically these studies were expedited by utilizing readily obtained amino acids as starting materials or an isocyanide multicomponent reaction. Structure-activity relationship studies resulted in the discovery of dual human and mouse 11-beta-HSD-1 potent and selective inhibitors like adamantane 11 and related compounds with high metabolic stability and robust pharmacokinetic profiles.

Published
2006
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