581106-29-8Relevant academic research and scientific papers
Double ester prodrugs of FR900098 display enhanced in-vitro antimalarial activity
Wiesner, Jochen,Ortmann, Regina,Jomaa, Hassan,Schlitzer, Martin
, p. 667 - 669 (2007)
Fosmidomycin and FR900098 are inhibitors of the 1-deoxy-D-xylulose 5-phosphate reductoisomerase (DXR; IspC), a key enzyme of the mevalonate-independent isoprenoid biosynthesis pathway. We have determined the in-vitro antimalarial activity of two double ester prodrugs 2, 3 in direct comparison with the unmodified FR900098 1 against intraerythrocytic forms of Plasmodium falciparum. Temporarily masking the polar properties of the phosphonate moiety of the DXR inhibitor FR900098 1 enhanced not only its oral bioavailability but also the intrinsic activity of this series against the parasites.
Compounds for inhibiting 1-deoxy-D-xylulose-5-phosphate reductoisomerase
-
Page/Page column 48; 49; 50, (2017/04/11)
In particular, the compound is effective to inhibit Dxr in Mycobacterium tuberculosis (Mtb). The present invention relates to compounds having general formula (I) or (II) where X is an acidic group, such as carboxylate, phosphonate, sulfate, and tetrazole; Ar is a substituted or unsubstituted aromatic or heteroaromatic group; and n is 0, 1, 2, 3, or 4, preferably 2, 3, or 4. The compounds inhibits 1-deoxy-D-xylulose-5-phosphate reductoisomerase (Dxr), particularly Dxr in Mycobacterium tuberculosis (Mtb).
COMPOUNDS FOR INHIBITING 1- DEOXY-D-XYLULOSE- 5 - PHOSPHATE REDUCTOISOMERASE
-
, (2013/03/26)
[0082] In particular, the compound is effective to inhibit Dxr in Mycobacterium tuberculosis (Mtb). The present invention relates to compounds having general formula (I) or where X is an acidic group, such as carboxylate, phosphonate, sulfate, and tetrazole; Ar is a substituted or unsubstituted aromatic or heteroaromatic group; and n is 0, 1, 2, 3, or 4, preferably 2, 3, or 4. The compounds inhibits l-deoxy-D-xylulose-5-phosphate reductoisomerase (Dxr), particularly Dxr in Mycobacterium tuberculosis (Mtb).
Growth inhibition of Mycobacterium smegmatis by prodrugs of deoxyxylulose phosphate reducto-isomerase inhibitors, promising anti-mycobacterial agents
Ponaire, Sarah,Zinglé, Catherine,Tritsch, Denis,Grosdemange-Billiard, Catherine,Rohmer, Michel
, p. 277 - 285 (2012/07/14)
Since Mycobacterium tuberculosis sets up several multiple anti-tuberculosis drug resistance mechanisms, development of new drugs with innovative target is urgent. The methylerythritol phosphate pathway (MEP) involved in the biosynthesis of essential metab
Antibacterial and antitubercular activity of fosmidomycin, FR900098, and their lipophilic analogs
Uh, Eugene,Jackson, Emily R.,San Jose, Géraldine,Maddox, Marcus,Lee, Robin E.,Lee, Richard E.,Boshoff, Helena I.,Dowd, Cynthia S.
, p. 6973 - 6976 (2012/01/06)
The nonmevalonate pathway (NMP) of isoprene biosynthesis is an exciting new route toward novel antibiotic development. Inhibitors against several enzymes in this pathway are currently under examination. A significant liability of many of these agents is p
Alkoxycarbonyloxyethyl ester prodrugs of FR900098 with improved in vivo antimalarial activity
Ortmann, Regina,Wiesner, Jochen,Reichenberg, Armin,Henschker, Dajana,Beck, Ewald,Jomaa, Hassan,Schlitzer, Martin
, p. 305 - 314 (2007/10/03)
FR900098 represents a derivative of the new antimalarial drug fosmidomycin with enhanced activity. The mechanism of action is the inhibition of the 1-desoxy-D-xylulose 5-phosphate (DOXP) reductoisomerase, an essential enzyme of the mevalonate independent
Acyloxyalkyl ester prodrugs of FR900098 with improved in vivo anti-malarial activity
Ortmann, Regina,Wiesner, Jochen,Reichenberg, Armin,Henschker, Dajana,Beck, Ewald,Jomaa, Hassan,Schlitzer, Martin
, p. 2163 - 2166 (2007/10/03)
FR900098 represents an improved derivative of the new antimalarial drug fosmidomycin and acts through inhibition of the 1-deoxy-D-xylulose 5-phosphate (DOXP) reductoisomerase, an essential enzyme of the mevalonate independent pathway of isoprenoid biosynt
