@article { ISI:000292983400015,
	title = {Efficient synthesis of benzodiazepinyl phosphonates as clostripain inhibitors via FeCl3 catalyzed four-component reaction},
	journal = {Organic \& Biomolecular Chemistry},
	volume = {9},
	number = {15},
	year = {2011},
	month = {OCT},
	pages = {5407-5413},
	publisher = {ROYAL SOC CHEMISTRY},
	address = {THOMAS GRAHAM HOUSE, SCIENCE PARK, MILTON RD, CAMBRIDGE CB4 0WF, CAMBS, ENGLAND},
	abstract = {<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>},
	issn = {1477-0520},
	doi = {10.1039/c0ob01102a},
	author = {Bhattacharya, Asish K. and Rana, Kalpeshkumar C. and Raut, Dnyaneshwar S. and Mhaindarkar, Vaibhav P. and Khan, Mohammad Islam}
}
@article { ISI:000308042000010,
	title = {Efficient synthesis of a hydroxyethylamine (HEA) isostere and its alpha-aminophosphonate and phosphoramidate derivatives as potential anti-HIV agents},
	journal = {Chemmedchem},
	volume = {7},
	number = {9},
	year = {2012},
	month = {SEP},
	pages = {1601-1611},
	publisher = {WILEY-V C H VERLAG GMBH},
	address = {BOSCHSTRASSE 12, D-69469 WEINHEIM, GERMANY},
	abstract = {<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>},
	keywords = {a-aminophosphonates, antiviral agents, hydroxyethylamine isosteres, phosphoramidates, synthesis},
	issn = {1860-7179},
	doi = {10.1002/cmdc.201200271},
	author = {Bhattacharya, Asish K. and Rana, Kalpeshkumar C. and Pannecouque, Christophe and De Clercq, Eric}
}
