252669-41-3Relevant academic research and scientific papers
Rotameric properties of novel N-acyl and N-acyloxy dimeric 4-phenyl-1,4- dihydropridines derived from developed solid-state synthesis
Hilgeroth, Andreas,Baumeister, Ute,Heinemann, Frank
, p. 2367 - 2376 (2007/10/03)
Novel N-acyl and N-acyloxy dimeric 4-phenyl-1,4-dihydropyridines are given by solid-state photodimerization of their monomeric educts in excellent yields. The existence of rotamers was demonstrated by 1H NMR spectroscopical measurement at certa
Cage dimeric N-acyl- and N-acyloxy-4-aryl-1,4-dihydropyridines as first representatives of a novel class of HIV-1 protease inhibitors
Hilgeroth, Andreas,Billich, Andreas
, p. 380 - 384 (2007/10/03)
The synthesis of a series of novel cage dimeric N-acyl and N-acyl-oxy-4- aryl-1,4-dihydropyridines starting either from solid-state synthetic ester dimers or from monomeric 4-aryl-1,4-dihydropyridines is presented. Their biological evaluation as novel HIV-1 protease inhibitors showed the most active compounds to be 5c and 5i with inhibitory activities of 52% (50 μM) and 49% (25 μM), respectively. Within each series of N-acyl- and N-acyloxy derivatives NCOBz and NBoc groups were found to be the best substituents. Although they exhibiting only moderate activities these cage dimers hold promise as a class of novel non-peptidic HIV-1 protease inhibitors.
