Prodrugs for the Treatment of Neglected Diseases
Abstract
:Introduction
Chagas’disease
Sleeping sickness
Leishmaniasis
Malaria
Schistosomiasis
Tuberculosis
Sickle cell disease
Antichagasic prodrugs
Prodrugs of primaquine and nitrofurazone
Prodrugs of N-isopropyl oxamate
Prodrugs for Sleeping Sickness
ADEPT approach and mAb-drug conjugate for treatment of African trypanosomiasis
Prodrugs of aromatic diamines
Prodrugs for Leishmaniasis
Glutathione prodrugs
Thermolytically activated oligonucleotide prodrugs
Pyrimethamine polymer prodrugs
Prodrugs of buparvaquone
Antimalarial prodrugs
Polymeric antimalarial prodrugs
Prodrugs of bisthiazolium salts
Prodrugs of fosmidomycin and FR900098
Prodrugs of trioxane and dioxane derivatives (endoperoxidic agents)
Prodrugs of 4-aminoquinoline
Prodrugs of 8-aminoquinoline
Prodrugs of protein farnesyltransferase inhibitors
CH3 (FTI-2153) | 4.44 | >1000 | 3300 |
C2H5 | 4.88 | 750 | 1900 |
| 5.19 | >1000 | 1800 |
| 5.19 | >1000 | 800 |
| 7.09 | >1000 | 700 |
| 4.94 | >1000 | 350 |
| 6.09 | 1000 | 150 |
H (FTI-2148) | 1.77 | 15 | >66,000 |
Prodrugs of pyrroloquinazolinediamine
Prodrugs of aromatic amidine
CD-CS approach
Prodrugs for Schistosomiasis
Prodrugs of oxamniquine
Prodrugs of dihydroartemisinin
Tuberculostatic prodrugs
Bioprecursors for tuberculosis chemotherapy
Mutual prodrug of isoniazid, para-aminosalicylic acid, and ethambutol
Prodrugs of nitroimidazoles
Nucleoside analogues prodrugs
Polymeric prodrugs of norfloxacin
Polymeric prodrug of isoniazid and pyrazinamide
DA-7218 prodrugs
Prodrugs for Sickle Cell Disease
Butyric acid prodrugs
Vanillin prodrugs
Hydroxyurea and nitrate derivatives
Nitrate derivatives
Conclusions
Acknowledgements
List of abbreviations used
5-FC | 5-fluorocytosine |
5-FU | 5-fluorouracil |
ADEPT | antibody-directed enzyme prodrug therapy |
AN-10 | butylidene dibutyrate |
apoL-I | apolopoprotein L1 |
BA | butyric acid |
CD-CS | recombinant fusion protein consisting of CS protein as a ligand and bacterial CD: cytosine deaminase |
CL | cutaneous leishmaniasis |
CMD-P | carboxymethyldextran-thiomannopyranoside-pyrimethamine |
CpG ODN | CpG oligodeoxynucleotides |
CpG | a dinucleotide constituted by a cytosine followed by guanine separated by a phosphate |
CQ | chloroquine |
CS | malaria circunsporozoite |
DFMO | eflornithine |
DHA | dihydroartemisinin |
DHFR | dihydrofolate reductase |
DHFR-TS | dihydrofolate reductase thymidilate synthase |
dNTPs | deoxyribonucleotides |
DOXP | 1-deoxy-D-xylulose 5-phosphate |
EB | ethambutol |
ETA | ethionamide |
EthA | a flavin monooxygenase found to catalyze the Baeyer-Villiger reaction |
Et-NIPOx | ethyl ester of N-isopropyl oxamate |
fma | 2-(N-formyl-N-methyl)aminoethyl |
GI | gastrointestinal |
GR | glutathione reductase |
GSH | glutatione |
HADH-isozyme | α-hydroxyacid dehydrogenase-isozyme |
HAT | Human African Trypanosomiasis |
Hb | hemoglobin |
Hb F | fetal hemoglobin |
Hb S | hemoglobin S |
HU | hydroxyurea |
INH | isoniazid |
InhA | enoyl-acyl carrier protein reductase |
KatG | catalase/peroxidase |
LDH-C4 | lactate dehydrogenase isozyme-x |
mAb | monoclonal-antiboby |
mAb-drug | monoclonal-antiboby drug conjugate |
MBCs | minimal bactericidal concentrations |
NbAn33 | a mAB specific for the conserved carbohydrate epitope of VSGs |
NF | nitrofurazone |
NFOH | nitrofurazone hydroxymethyl derivative |
NHS | normal human serum |
NIPOx | N-isopropyl oxamate |
NMPC | N-methylene phosphonic chitosan |
OEC | oxygen equilibrium curve |
PAS | 4-aminosalicylic acid |
PEG-PAS | polyethyleneglycol-poly(aspartic acid) |
PEG-PASP-PZA | poly(ethyleneglycol)-poly(aspartic acid) block copolymer by substituting pyrazinamide on the aspartate free carboxylic groups |
pfDHFR-TS | P. falciparum dihydrofolate reductase thymidilate synthase |
PFT | protein farnesyltransferase |
PLMII | plasmepsinII |
PncA | mycobacterial pyrazinamidase |
PQ | primaquine |
PQD | pyrroloquinazolinediamine |
PQD-A4 | tetra-acetamido pyrroloquinazolinediamine |
PQD-BE | bis-ethylcarbamyl pyrroloquinazolinediamine |
Pro-D ODN | a prodrug form of CpG ODN type D |
Pro-D35 | D-35 prodrug |
PTR1 | pteridine reductase enzyme |
PZA | pyrazinamide |
SCD | sickle cell disease |
SD-P | succinyldextran-thiomannopyranoside-pyrimethamine |
SRA | serum resistance-associated |
SS cells | sickle erythrocytes |
TAZ | thiacetazone |
TB | tuberculosis |
TLR-9 | Toll-like receptor 9 |
Tr-apoL-I | truncated apoL-I |
VL | visceral leishmaniasis |
VSG | variant surface glycoprotein |
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Chung, M.C.; Ferreira, E.I.; Santos, J.L.; Giarolla, J.; Rando, D.G.; Almeida, A.E.; Bosquesi, P.L.; Menegon, R.F.; Blau, L. Prodrugs for the Treatment of Neglected Diseases. Molecules 2008, 13, 616-677. https://doi.org/10.3390/molecules13030616
Chung MC, Ferreira EI, Santos JL, Giarolla J, Rando DG, Almeida AE, Bosquesi PL, Menegon RF, Blau L. Prodrugs for the Treatment of Neglected Diseases. Molecules. 2008; 13(3):616-677. https://doi.org/10.3390/molecules13030616
Chicago/Turabian StyleChung, Man Chin, Elizabeth Igne Ferreira, Jean Leandro Santos, Jeanine Giarolla, Daniela Gonçales Rando, Adélia Emília Almeida, Priscila Longhin Bosquesi, Renato Farina Menegon, and Lorena Blau. 2008. "Prodrugs for the Treatment of Neglected Diseases" Molecules 13, no. 3: 616-677. https://doi.org/10.3390/molecules13030616