220481-70-9

Upstream product

• 295-37-4 1,4,8,11-Tetraazacyclotetradecane 
• 24424-99-5 di-tert-butyl dicarbonate 
• 623-24-5 1,4-bis(bromomethyl)benzene 
• 170161-27-0 1,4,8-tris(tert-butoxycarbonyl)-1,4,8,11-tetraazacyclotetradecane 
• 203568-06-3 5-<4,8-bis(tert-butoxycarbonyl)-1,4,8,11-tetraazacyclotetradecanyl>pentanoic ethyl ester 

Downstream Products

• 220481-72-1 3'-azido-3'-deoxy-5'-O-<5-<4,8-bis(tert-butyloxycarbonyl)-11-(4-<<4,8,11-tris(tert-butoxycarbonyl)-1,4,8,11-tetraazacyclotetradecanyl>methyl>benzyl)-1,4,8,11-tetraazacyclotetradecanyl>pentanoyl>thymidine 

Relevant academic research and scientific papers

New bicyclam-GalCer analogue conjugates: Synthesis and in vitro anti-HIV activity

The synthesis of bipharmacophore anti-HIV compounds which, in a single molecule, combine two ligands, that is, the bicyclam AMD3100 and a GalCer analogue, that might inhibit several steps of the complex virus/cell cascade interactions has been performed. The 'double-drug' Gal-AMD3100 conjugates elicited inhibitory effects on T (or X4)-tropic HIV-1 replication in all CXCR4 expressing cell lines with EC50 values ranging from 0.25 to 6.0 μM which were however ～40- to 125-fold lower than that of AMD3100. Concerning the mechanism of inhibition of the Gal-AMD3100 conjugates, experiments performed with X4 or R5HIV-1 strains and GHOST cells genetically modified to express CD4 and CXCR4 or CCR5 indicated clearly that the conjugates interact with CXCR4 and not with CCR5.

Anti-HIV drug and preparation method therefor

The invention discloses an anti-HIV drug and a preparation method therefor. According to the anti-HIV drug and the preparation method therefor disclosed by the invention, the anti-HIV drug is a Raltegravir derivative ester, the chemical name of which is as follows: N-(2'-(4'-(4'-fluorobenzyl carbamoyl)-1'-methyl-6'-oxo-1',6'-dihydropyrimidine-2'-yl)-5'-methyl-1',3',4'-oxadiazole-2'-formamide-5'-oxy-{5-[1,4,8,11-teraazamacrocycle myristyl]methyl}phenyl)-1,4,8,11-teraazamacrocycle myristyl}-R-carboxylic ester. Compared to Raltegravir, the anti-HIV drug shows obvious and relatively higher activity (EC50) and selectivity index (SI=EC50/CC50), and solubility of the anti-HIV drug is remarkably improved.

New bicyclam-AZT conjugates: Design, synthesis, anti-HIV evaluation, and their interaction with CXCR-4 coreceptor

We report the synthesis of mono- and bis-tetraazamacrocycle-AZT conjugates. All new compounds were screened for their ability to inhibit HIV- 1 replication in MT4 cell line and were compared to AZT alone. It appears that N-protected covalent prodrugs are