141829-04-1Relevant articles and documents
Investigation of a novel series of 2-hydroxyisoquinoline-1,3(2 H,4 H)-diones as human immunodeficiency virus type 1 integrase inhibitors
Suchaud, Virginie,Bailly, Fabrice,Lion, Cedric,Calmels, Christina,Andreola, Marie-Line,Christ, Frauke,Debyser, Zeger,Cotelle, Philippe
, p. 4640 - 4660 (2014/07/07)
We report herein further insight into the biological activities displayed by a series of 2-hydroxyisoquinoline-1,3(2H,4H)-diones (HIDs). Substitution of the N-hydroxyimide two-metal binding pharmacophore at position 4 by carboxamido side chains was previously shown by us to be fruitful for this scaffold, since strong human immunodeficiency virus type 1 integrase (HIV-1 IN) inhibitors in the low nanomolar range associated with low micromolar anti-HIV activities were obtained. We investigated the influence of substitution at position 7 on biological activity. Introduction of electron-withdrawing functional groups such as the nitro moiety at position 7 led to a noticeable improvement of antiviral activity, down to low nanomolar anti-HIV potencies, with advantageous therapeutic indexes going close to those of the clinically used raltegravir and retained potencies against a panel of IN mutants.
Chemically-enabled synthesis of 1,2,3,4-tetrahydroisoquinolin-1-ones
Humphries, Paul S.,Balan, Gayatri,Bechle, Bruce M.,Conn, Edward L.,Dirico, Kenneth J.,Hui, Yu,Oliver, Robert M.,Southers, James A.,Yang, Xiaojing
scheme or table, p. 2140 - 2143 (2009/07/26)
We have developed a number of efficient protocols for the facile synthesis of 1,2,3,4-tetrahydroisoquinolin-1-ones. This synthetic methodology allowed concise and efficient exploration of the SAR in all areas of the molecule. A number of these methods pro
Alkylidene analogs of 1'-amino-2-[(benzothiazolyl)-methyl]spiro [isoquinoline-4(1H),3'-pyrrolidine]-1,2',3,5'(2H)-tetrones useful as aldose reductase inhibitors
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, (2008/06/13)
This invention relates to alkylidene analogs of 1'-amino-2-[(benzothiazolyl)-methyl]spiro[isoquinoline-4(1H),3'-pyrrolidone]-1,2',3,5'(2H)-tetrones represented by formula (I): STR1 wherein: R1, R2 and R3 are independently