212143-40-3Relevant academic research and scientific papers
Solution-phase parallel synthesis of acyclic nucleoside libraries of purine, pyrimidine, and triazole acetamides
Pathak, Ashish K.,Pathak, Vibha,Reynolds, Robert C.
, p. 485 - 493 (2014/12/10)
Molecular diversity plays a pivotal role in modern drug discovery against phenotypic or enzyme-based targets using high throughput screening technology. Under the auspices of the Pilot Scale Library Program of the NIH Roadmap Initiative, we produced and report herein a diverse library of 181 purine, pyrimidine, and 1,2,4-triazole-N-acetamide analogues which were prepared in a parallel high throughput solution-phase reaction format. A set of assorted amines were reacted with several nucleic acid N-acetic acids utilizing HATU as the coupling reagent to produce diverse acyclic nucleoside N-acetamide analogues. These reactions were performed using 24 well reaction blocks and an automatic reagent-dispensing platform under inert atmosphere. The targeted compounds were purified on an automated purification system using solid sample loading prepacked cartridges and prepacked silica gel columns. All compounds were characterized by NMR and HRMS, and were analyzed for purity by HPLC before submission to the Molecular Libraries Small Molecule Repository (MLSMR) at NIH. Initial screening through the Molecular Libraries Probe Production Centers Network (MLPCN) program, indicates that several analogues showed diverse and interesting biological activities.
Chiral peptide nucleic acid monomers (PNAM) with modified backbones
Katritzky, Alan Roy,Narindoshvili, Tamari
experimental part, p. 3171 - 3176 (2009/02/03)
Convenient high yielding syntheses of optically pure PNAMs comprising l- or d-serine, l-lysine and l-arginine units linked to thymine or Cbz-cytosine are described. Simple workup and inexpensive reagents are employed and free amino acids are used as coupl
Cyclic PNA hexamer-based compound: Modelling, synthesis and inhibition of the HIV-1 RNA dimerization process
Schwergold, Caroline,Depecker, Geoffrey,Giorgio, Christophe Di,Patino, Nadia,Jossinet, Fabrice,Ehresmann, Bernard,Terreux, Raphael,Cabrol-Bass, Daniel,Condom, Roger
, p. 5675 - 5687 (2007/10/03)
A cyclic molecule constituted by (i) a hexameric PNA moiety complementary to six among the nine residues of the dimerization initiation site loop of HIV-1 and (ii) a spacer tethering the N- to the C-extremities of the PNA, has been elaborated to inhibit the dimerization process of HIV-1 genome. This compound has been synthesized following a liquid-phase procedure (fully protected backbone approach). Preliminary agarose gel electrophoresis analyses have shown that the cyclic PNA conjugate is able to inhibit the HIV-1 dimerization.
Synthesis of Peptide Nucleic Acid Monomers Containing the Four Natural Nucleobases: Thymine, Cytosine, Adenine, and Guanine and Their Oligomerization
Dueholm, Kim L.,Egholm, Michael,Behrens, Carsten,Christensen, Leif,Hansen, Henrik F.,et al.
, p. 5767 - 5773 (2007/10/02)
The preparation of mixed-sequence PNAs (PNAs containing the four natural nucleobases; thymine, cytosine, adenine, and guanine) is described.The PNA monomers containing thymine, Cbz-protected cytosine, or adenine or benzyl-protected guanine were prepared v
