158478-16-1Relevant academic research and scientific papers
FUSED TRICYCLIC HETEROCYCLIC COMPOUNDS USEFUL FOR TREATING HIV INFECTION
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, (2016/12/16)
Fused tricyclic heterocycle derivatives of formula (I) and pharmaceutically acceptable salts thereof, compositions comprising at least one fused tricyclic heterocycle derivative, and methods of using the fused tricyclic heterocycle derivatives for treatin
SUBSTITUTED QUINOLIZINE DERIVATIVES USEFUL AS HIV INTEGRASE INHIBITORS
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, (2015/04/15)
The present invention relates to Substituted Quinolizine Derivatives of Formula (I): and pharmaceutically acceptable salts or prodrug thereof, wherein X, Y, R1, R2, R3, R4, R5, R9 and R10 are as defined herein. The present invention also relates to compositions comprising at least one Substituted Quinolizine Derivative, and methods of using the Substituted Quinolizine Derivatives for treating or preventing HIV infection in a subject.
Synthesis of the trans-fusarinine scaffold
Bertrand, Samuel,Duval, Olivier,Hélesbeux, Jean-Jacques,Larcher, Gérald,Richomme, Pascal
scheme or table, p. 2119 - 2122 (2010/06/14)
The trans-fusarinine backbone is a common feature encountered in many fungal siderophores. This monomer is notably the structural base of Nα-methyl coprogen B and dimerumic acid. Both siderophores are known to be secreted by Scedosporium apiosp
Synthesis and activity of 6-substituted purine linker amino acid immunostimulants
Zacharie, Boulos,Gagnon, Lyne,Attardo, Giorgio,Connolly, Timothy P.,St-Denis, Yves,Penney, Christopher L.
, p. 2883 - 2894 (2007/10/03)
A series of 6-substituted purinyl alkoxycarbonyl amino acids were synthesized and evaluated for their ability to stimulate cytotoxic T lymphocytes (CTLs) and the mixed lymphocyte reaction (MLR). A few of these compounds, in particular [[5-[6-(N,V-dimethylamino)purin-9- yl]pentoxy]carbonyl]D-arginine (BCH-1393, 4a), displayed an in vitro stimulation of CTLs comparable to interleukin 2 (IL 2). BCH-1393 increased the CTL response between 10-9 M and 10-5 M. Further, this potent in vitroactivity was reflected as a significant increase in CTL cell number in vivo. However, immunophenotyping of some of the other equipotent compounds did not reveal a parallel relative increase in CTLs in vivo. It was difficult to formulate a rigorous structure-activity relationship based on in vitro CTL activity. Nevertheless, the activity was dependent upon the nature of the 6- substituent on the purine, the type and stereochemistry of the amino acid, and the distance and spatial freedom between the purine and amino acid as defined by the length and rigidity of the linker. These compounds were generally nontoxic, as exemplified by BCH-1393. BCH-1393 is a promising immunostimulant which may be targeted for those disease states which require an increased CTL or TH1 type response.
