01479nas a2200229 4500008004100000022001400041245009600055210006900151260010600220300001400326490000700340520059400347653001400941653002000955653002900975653001101004653002301015653002901038100002801067700002701095856012701122 2008 eng d a0040-403900aAmberlite-IR 120 catalyzed three-component synthesis of alpha-amino phosphonates in one-pot0 aAmberliteIR 120 catalyzed threecomponent synthesis of alphaamino aTHE BOULEVARD, LANGFORD LANE, KIDLINGTON, OXFORD OX5 1GB, ENGLANDbPERGAMON-ELSEVIER SCIENCE LTDcAPR a2598-26010 v493 a

A simple, efficient, and environmentally benign method for a three-component reaction of an amine, an aldehyde or a ketone, and diethyl phosphite catalyzed by Amberlite-IR 120 resin has been developed to afford alpha-amino phosphonates in high yields and short reaction times under solvent-free reaction conditions. The major advantages of the present method are good yields, inexpensive, ecofriendly and reusable catalyst, mild and solvent-free reaction conditions and tolerance towards various functionalities present in the substrates. (c) 2008 Elsevier Ltd. All rights reserved.

10aaldehydes10aalkyl phosphite10aalpha-amino phosphonates10aamines10aion-exchange resin10amulti-component reaction1 aBhattacharya, Asish, K.1 aRana, Kalpeshkumar, C. uhttps://library.ncl.res.in/content/amberlite-ir-120-catalyzed-three-component-synthesis-alpha-amino-phosphonates-one-pot-001728nas a2200289 4500008004100000022001400041245009000055210006900145260010600214300001400320490000700334520072600341653001301067653001801080653001701098653001701115653002101132653001701153653002501170653001401195100002801209700002701237700002201264700001601286700002101302856011501323 2009 eng d a0960-894X00aSynthesis and in vitro study of 14-aryl-14H-dibenzo[a.j]xanthenes as cytotoxic agents0 aSynthesis and in vitro study of 14aryl14Hdibenzoajxanthenes as c aTHE BOULEVARD, LANGFORD LANE, KIDLINGTON, OXFORD OX5 1GB, ENGLANDbPERGAMON-ELSEVIER SCIENCE LTDcOCT a5590-55930 v193 a

A simple and expedient method for the synthesis of a series of 14-aryl-14H-dibenzo[a.j]xanthenes is described through a one-pot condensation of beta-naphthol with aryl aldehydes catalysed by TaCl(5) under solvent-free conventional heating. The major advantages of the present method are: high yields, less reaction time, solvent-free condition and easy purification of the products. The synthesized 14-aryl-14H-dibenzo[a.j]xanthenes were evaluated against a panel of six human cancer lines of different tissues. Synthesized compound 30 showed IC(50) of 37.9 and 41.3 mu M against Colo-205 and 502713, respectively, whereas 3g showed IC(50) of 41.9 mu M against Colo-205. (C) 2009 Elsevier Ltd. All rights reserved.

10aAldehyde10abeta-Naphthol10acondensation10aCytotoxicity10aOne-pot reaction10aSolvent-free10aTantalum(V) chloride10aXanthenes1 aBhattacharya, Asish, K.1 aRana, Kalpeshkumar, C.1 aMujahid, Mohammad1 aSehar, Irum1 aSaxena, Ajit, K. uhttps://library.ncl.res.in/content/synthesis-and-vitro-study-14-aryl-14h-dibenzoajxanthenes-cytotoxic-agents-001524nas a2200229 4500008004100000022001400041245012100055210006900176260010600245300001400351490000700365520061200372653001300984653002100997653002401018653001401042653002501056653002701081100002801108700002701136856013101163 2011 eng d a0968-089600aDesign, synthesis and biological evaluation of peptidyl-vinylaminophosphonates as novel cysteine protease inhibitors0 aDesign synthesis and biological evaluation of peptidylvinylamino aTHE BOULEVARD, LANGFORD LANE, KIDLINGTON, OXFORD OX5 1GB, ENGLANDbPERGAMON-ELSEVIER SCIENCE LTDcDEC a7129-71350 v193 a

We report herein, design and synthesis of vinylaminophosphonates, a novel class of compounds as possible cysteine protease inhibitors. The synthesis of vinylaminophosphonates has been accomplished employing Tsuji-Trost reaction as a key step. The synthesized compounds were assayed against papain, a model cysteine protease and some of our synthesized compounds showed IC50 values in the range of 30-54 mu M thereby suggesting that these chemical entities thus could constitute an interesting template for the design of potential novel protease inhibitors. (C) 2011 Elsevier Ltd. All rights reserved.

10aCysteine10aInhibitor design10aProtease inhibitors10asynthesis10aTsuji-Trost reaction10aVinylaminophosphonates1 aBhattacharya, Asish, K.1 aRana, Kalpeshkumar, C. uhttps://library.ncl.res.in/content/design-synthesis-and-biological-evaluation-peptidyl-vinylaminophosphonates-novel-cysteine-001369nas 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

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.

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

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.

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-001350nas a2200217 4500008004100000022001400041245008800055210006900143260010300212300001200315490000700327520053200334653001000866653002800876653001400904653002000918653002600938100002800964700002700992856011301019 2013 eng d a0376-469900aAntimycobacterial agent, (E)-phytol and lauric amide from the plant Lagascea mollis0 aAntimycobacterial agent Ephytol and lauric amide from the plant  aANUSANDHAN BHAWAN, 2 RAFI MARG, NEW DELHI, 110001, INDIAbCOUNCIL SCIENTIFIC & INDUSTRIAL REScJUL a901-9030 v523 a

Chemical examination of aerial parts of the plant, Lagascea mollis has resulted in the isolation of two compounds, an acyclic diterpene alcohol which has been identified as (E)-phytol 1 and lauric amide 3. Their structures have been elucidated by spectral data and chemical transformations. This is the first report of isolation of both these compounds from this plant It is noteworthy that compound 1 has been found to be a potent antimycobacterial agent and thus, L. mollis could be exploited as an alternative source.

10aamide10achemical transformation10aditerpene10aLagascea mollis10astructure elucidation1 aBhattacharya, Asish, K.1 aRana, Kalpeshkumar, C. uhttps://library.ncl.res.in/content/antimycobacterial-agent-e-phytol-and-lauric-amide-plant-lagascea-mollis-003623nas a2200229 4500008004100000245018000041210006900221260000800290300001100298490000800309520275800317100002603075700001903101700002703120700001803147700001503165700002803180700002003208700001803228700002803246856011903274 2021 eng d00aCombating multi-drug resistant malaria parasite by inhibiting falcipain-2 and heme-polymerization: Artemisinin-peptidyl vinyl phosphonate hybrid molecules as new antimalarials0 aCombating multidrug resistant malaria parasite by inhibiting fal cAUG a1134540 v2203 a

Artemisinin-based combination therapies (ACTs) have been able to reduce the clinical and pathological malaria cases in endemic areas around the globe. However, recent reports have shown a progressive decline in malaria parasite clearance in South-east Asia after ACT treatment, thus envisaging a need for new artemisinin (ART) derivatives and combinations. To address the emergence of drug resistance to current antimalarials, here we report the synthesis of artemisinin-peptidyl vinyl phosphonate hybrid molecules that show superior efficacy than artemisinin alone against chloroquine-resistant as well as multidrug-resistant Plasmodium falciparum strains with EC50 in pico-molar ranges. Further, the compounds effectively inhibited the survival of ring-stage parasite for laboratory-adapted artemisinin-resistant parasite lines as compared to artemisinin. These hybrid molecules showed complete parasite clearance in vivo using P. berghei mouse malaria model in comparison to artemisinin alone. Studies on the mode of action of hybrid molecules suggested that these artemisinin-peptidyl vinyl phosphonate hybrid molecules possessed dual activities: inhibited falcipain-2 (FP-2) activity, a P. falciparum cysteine protease involved in hemoglobin degradation, and also blocked the hemozoin formation in the food-vacuole, a step earlier shown to be blocked by artemisinin. Since these hybrid molecules blocked multiple steps of a pathway and showed synergistic efficacies, we believe that these lead compounds can be developed as effective antimalarials to prevent the spread of resistance to current antimalarials.

1 aAratikatla, Eswar, K.1 aKalamuddin, Md1 aRana, Kalpeshkumar, C.1 aDatta, Gaurav1 aAsad, Mohd1 aSundararaman, Srividhya1 aMalhotra, Pawan1 aMohmmed, Asif1 aBhattacharya, Asish, K. uhttps://library.ncl.res.in/content/combating-multi-drug-resistant-malaria-parasite-inhibiting-falcipain-2-and-heme