Development of New MDR-Tuberculosis Drugs (Pharmacology - Research, Safety Testing and Regulation)

DEVELOPMENT OF NEW  MDR-TUBERCULOSIS DRUGS......Page 5
CONTENTS......Page 7
PREFACE......Page 9
INTRODUCTION......Page 11
ISONIAZID, ETHIONAMIDE......Page 15
PYRAZINAMIDE......Page 18
ETHAMBUTOL......Page 19
FLUOROQUINOLONES......Page 21
RESEARCH OF NOVEL MDR-POTENTIAL DRUGS......Page 23
1. STRUCTURE MODIFICATION OF KNOWN COMPOUNDS (INH, ETH, RIF AND RIFAMYCIN DERIVATIVES, PZA, EMB, AND QUINOLONES)......Page 24
2. NEW LEADS WITH NOVEL MECHANISM OF THE ACTION [74] (LINEZOLID, TMC207, PA-824, OPC-67683, BM212, SQ109, FAS20013, LL-3858)......Page 36
3.1. Cell Wall Biosynthesis......Page 41
3.1.1. Mycolic Acid Synthesis Inhibitors......Page 44
3.1.2. Protein Synthesis Inhibitors [119]......Page 48
3.1.3. Polysaccharide Biosynthesis Inhibitors [137]......Page 51
3.2. Targeting P450 Enzymes [148]......Page 55
3.3. Targeting Isocitrate Lyases......Page 56
3.4. FtsZ-Targeting Compounds......Page 57
3.5. Other Targets......Page 60
4. INVESTIGATION OF “NON-ANTI-TUBERCULOUS” DRUGS AND THEIR DERIVATIVES......Page 66
5. OTHER ACTIVE SYNTHETIC COMPOUNDS......Page 74
6. OTHER ACTIVE, NATURALLY-OCCURRING COMPOUNDS......Page 80
ACKNOWLEDGMENTS......Page 83
REFERENCES......Page 85
INDEX......Page 107