- Design, synthesis, and SAR studies of novel and highly active tri-cyclic HIV integrase inhibitors
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A novel class of tri-cyclic HIV integrase inhibitors were designed based on conformational analysis of 1,6-naphthyridine carboxamide compound L-870810 and docking the designed inhibitor into the active site of our integrase enzyme model. The efficient syn
- Jin, Haolun,Cai, Ruby Z.,Schacherer, Laura,Jabri, Salman,Tsiang, Manuel,Fardis, Maria,Chen, Xiaowu,Chen, James M.,Kim, Choung U.
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p. 3989 - 3992
(2007/10/03)
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- PHOSPHONATE ANALOGS OF HIV INTEGRASE INHIBITOR COMPOUNDS
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Novel HIV integrase inhibitor compounds having at least one phosphonate group, protected intermediates thereof, and methods for inhibition of HIV-integrase are disclosed.
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Page/Page column 559
(2010/02/15)
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- PRE-ORGANIZED TRICYCLIC INTEGRASE INHIBITOR COMPOUNDS
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Tricyclic compounds according to the structure below, protected intermediates thereof, and methods for inhibition of HIV-integrase are disclosed. Formula (I). Al and A2 are moieties forming a five, six, or seven membered ring. L is a bond or a linker connecting a ring atom of Ar to N. X is O, S, or substituted nitrogen. Ar is aryl or heteroaryl. Q is N, +NR, or CR4. The aryl carbons may be independently substituted with substituents other than hydrogen. The compounds may include prodrug moieties covalently attached at any site.
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Page 320;321
(2008/06/13)
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