191859-34-4Relevant academic research and scientific papers
Anti-viral compounds
-
, (2008/06/13)
Nucleotide analogues having the general formula (I) and pharmaceutically acceptable derivatives: STR1 wherein n is 0 or an integer; X is O or S, CH2, CH-halogen, CH--N3, or C=CH2 ; Q and U are independently selected from: O, S, and CH(Ra) wherein Ra is hydrogen, OH, halogen, N3, NH2, SH, carboxyl, C1-6 alkyl or Ra is CH2 (Rb) wherein Rb is hydrogen, OH, SH, NH2, C1-6 alkyl or carboxyl; or both Q and U are CH when Q and U are linked by a double bond; Z is selected from: O, a C1-6 alkoxy, a C1-6 thioalkyl, a C1-6 aminoalkyl, (CH2)m wherein m is 0 or an integer, and N(Rc)2 wherein both Rc are independently hydrogen or a C1-6, alkyl; and R2 is a purine or pyrimidine base or an analogue or derivative thereof are disclosed. Members of this series of analogues possess anti-viral activity.
Syntheses and antiviral activities of 1,3-dioxolanyl-, 1,3-oxathiolanyl- and 1,3-dithiolanylnucleosides with 2-hydroxymethyl substituents
Chun, Moon Woo,Shin, Dae Hong,Moon, Hyung Ryong,Lee, Jeewoo,Park, Hokoon,Jeong, Lak Shin
, p. 1475 - 1480 (2007/10/03)
Novel 1,3-dioxolanyl-, 1,3-oxathiolanyl- and 1,3-dithiolanylnucleosides with 2-hydroxymethyl substituents (1a-4b) were each synthesized with good yields through the condensation of dinucleophiles (oxygen and/or sulfur) with 1,3-dibenzoxy-2-propanone methyl ketal as a key step.
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.
