01369nas a2200193   4500008004100000022001400041245012600055210006900181260011000250300001400360490000600374520053000380100002800910700002700938700002600965700002900991700002601020856012901046       2011                        eng d  a1477-052000aEfficient synthesis of benzodiazepinyl phosphonates as clostripain inhibitors via FeCl3 catalyzed four-component reaction0 aEfficient synthesis of benzodiazepinyl phosphonates as clostripa  aTHOMAS GRAHAM HOUSE, SCIENCE PARK, MILTON RD, CAMBRIDGE CB4 0WF, CAMBS, ENGLANDbROYAL SOC CHEMISTRYcOCT  a5407-54130 v93 a<p>A novel one-pot route for the synthesis of benzodiazepinyl phosphonates (BDPs) has been achieved. FeCl3 efficiently catalyzed four-component condensation of diamines, acetone and phosphites in the presence of molecular sieves to furnish BDPs as novel chemical entities with good yield. The synthesized BDPs have shown significant protease inhibition activity against clostripain, a disease model for gas gangrene, suggesting that these novel chemical entities could be further explored as cysteine protease inhibitors.</p>1 aBhattacharya, Asish, K.1 aRana, Kalpeshkumar, C.1 aRaut, Dnyaneshwar, S.1 aMhaindarkar, Vaibhav, P.1 aKhan, Mohammad, Islam  uhttps://library.ncl.res.in/content/efficient-synthesis-benzodiazepinyl-phosphonates-clostripain-inhibitors-fecl3-catalyzed-002197nas a2200241   4500008004100000022001400041245015400055210006900209260007700278300001400355490000600369520123800375653002401613653002101637653003201658653002101690653001401711100002801725700002701753700002801780700002001808856012701828       2012                        eng d  a1860-717900aEfficient synthesis of a hydroxyethylamine (HEA) isostere and its alpha-aminophosphonate and phosphoramidate derivatives as potential anti-HIV agents0 aEfficient synthesis of a hydroxyethylamine HEA isostere and its   aBOSCHSTRASSE 12, D-69469 WEINHEIM, GERMANYbWILEY-V C H VERLAG GMBHcSEP  a1601-16110 v73 a<p>HIV protease is a promising drug target for AIDS therapy, and several potent HIV-1 protease inhibitors have been reported to date. Although existing inhibitors exhibit high selectivity, they have also been associated with severe side effects and the possible emergence of therapeutic resistance. As HIV protease cleaves the peptide bond via a tetrahedral intermediate, various transition-state models such as hydroxyethylamine (HEA) have been designed. We therefore pursued an efficient synthesis of an HEA isostere; this was performed with a novel one-pot reductiontransiminationreduction reaction sequence as a key step. a-Aminophosphonate and phosphoramidate derivatives of the HEA isostere were designed and synthesized, and all of the synthesized derivatives were assayed for their anti-HIV activities against wild-type and mutant HIV strains. Phosphoramidate derivative 15?a was found to be the most active of all synthesized compounds against the IIIB and RES056 strains. As phosphonates are known to exhibit physiological stability, good cell permeability, and other promising pharmacokinetic characteristics, our newly synthesized compounds have the potential as alternatives to existing therapeutics and diagnostics.</p>10aa-aminophosphonates10aantiviral agents10ahydroxyethylamine isosteres10aphosphoramidates10asynthesis1 aBhattacharya, Asish, K.1 aRana, Kalpeshkumar, C.1 aPannecouque, Christophe1 aDe Clercq, Eric  uhttps://library.ncl.res.in/content/efficient-synthesis-hydroxyethylamine-hea-isostere-and-its-alpha-aminophosphonate-and-0