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Tuberculosis
Organic Compounds to Combat Neglected Tropical Diseases 261
Refs.
Class Compounds
MW
Best Compound
MIC IC
50
SI
μg/mL μM μg/mL μM
IC
50
/
MIC
[44]
724.47 Phenoxy linked bisquinoline derivatives 1.10
d
1.52 887.00
e
1224.34 805
(a) REMA; (b) MABA; (c) BACTEC; (d) Agar dilution method (NCCLS); (e) MTT; (f) Neutral Red; (g) Other.
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262 Organic Compounds to Combat Neglected Tropical Diseases Santos et al.
In conclusion, the literature reports a lot of potent and selective new molecules
active against M. tuberculosis, however, the number of new drug candidates in
clinical trials are not in the same proportion. This paradox is due the serious
difficulties to obtain an effective drug that could be able to act not only against
sensible strains but also effective against multiresistant strains. This chapter aims
to indentify new antitubercular prototypes that could be used to further drug
development.
ACKNOWLEDGEMENTS
We thank São Paulo Research Foundation (FAPESP) ref. 2013/14957-5 and
2012/50359-2, CNPq-Glaxo ref. Process: 406827/2012-5.
CONFLICT OF INTEREST
The authors confirm that this chapter contents have no conflict of interest.
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Organic Compounds to Combat Neglected Tropical Diseases, 2014, 267-27 6 267
Subject Index
1,4-Naphthoquinone 7, 8, 102, 220
2-Cyanoacetamide 36
2-Nitroanilines 83, 89
3-Aryl-2-cyanoacrylamide 36, 37
4-Hydroxypanduratin A 34
5-Nitrothiophene 9, 73
6-Methylmercaptopurine 47
A
Acridine 91, 108, 175, 176,177
Acridone 38
Active metallic complexes and ligands 14
Active nitrofurans 9
Active nitrogen heterocycles 23
Active vanadyl complexes 13
Adamantine 53
Adenosine analogs 45, 46
Albendazole 153, 154, 160, 161
Aldehyde coupling 35
Aldolic condensation 35, 99
Alkylphosphocholine 103
American trypanosomiasis 4
Amidines 24, 68, 95
Aminobenzamide 36, 37
Aminobenzoates 36
Aminoquinoline-isatin 179, 180
Amodiaquine analogs 78
Amphotericin 64, 65, 66, 75, 79, 80, 82, 84, 92, 98, 99, 103, 106, 108
Anthraquinones 7, 165, 219
Antichagasic compounds 26
Anti-dengue activity 35, 36
Anti-flaviviral activity 42, 45
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268 Organic Compounds to Combat Neglected Tropical Diseases Beatriz and de Lima
Antifungals 66
Antileishmanial activities 67, 83, 91, 105
Antileishmanial agents 76, 84, 94, 107
Antileishmanial candidates 66
Antileprotic compounds 131, 136
Antimalarial drugs 174, 178, 179
Antitubercular 231, 232, 233, 234, 236, 237, 240, 241, 243, 244, 245, 246, 262
Anti-Wolbachia antibiotics 161
ARDP0006 37, 38
Aromatic diamidine 95
Artemisinin 105, 173
Arylsulfonylchlorides 80, 81
Aryltriazolylhydroxamates 67
Asparagine 49
Asymmetric hydrogenation 53
Asymmetric Mannich conditions 69
Avermectins 155, 158
Azepine 93
Azide moiety 39
Azides 36, 40
Azole derivatives 49, 66
B
Barbier-like reaction 211
Baylis-Hillman adducts 106, 223, 224
Benzimidazole 19, 70, 89
Benznidazole 3, 5, 6, 7, 11, 20, 22
Benzofuroxans 19, 20, 90
Benzothiazole 89
Benzoxazole 89, 90
Bicyclic phloroglucinols 204
Biguanidines 95
Bischler-Napieralski reaction 83
Boesenbergia rotunda 34
Subject Index
Organic Compounds to Combat Neglected Tropical Diseases 269
Borderline forms 130, 131
Bromobenzenesulfonamides 47
Buparvaquone 103
C
Capping process 51, 52
Castanospermine 50
Castanospermum australae 50
Chagas diseases 3, 4, 5, 6, 15, 17, 18, 22, 75, 86
Chalcone 27, 34, 66, 94, 98, 99, 100, 101, 109, 164, 165, 182, 188, 189
Chartaceone D 55
Chelerythrine 209
Chemical modification 95
Chlorosulphonic acid 44
Claisen rearrangement 93
Claisen-Schmidt condensation 101, 188, 189
Click chemistry 36, 40
Clofazimine 131, 132, 135
Coumarine 92
Cryptocarya chartacea 55
Curtius rearrangement 53
Cyanolide 210, 211, 212, 213, 214, 224, 226
Cysteine 17, 25, 26, 27, 172, 179, 181, 182, 183, 185, 190, 192
D
Dacrydium balansae 55
Danuravir 39
Dapsone 127, 131, 134, 135, 140, 141
Dengue fever 32
Deoxynorijimycin 50, 51
D-glucose 49
Dialkyldithiocarbamates 140
Diamidines 24, 95, 96
Diels–Alder cycloaddition 34
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270 Organic Compounds to Combat Neglected Tropical Diseases Beatriz and de Lima
Diethylcarbamazine 149, 153, 154, 159
Dihydropyridine 74, 76
Dithiocarbamate 140
Doxycycline 161, 162
Drug development 33, 56, 154, 155, 173, 262
E
Electron-withdrawing residues 36
Epimastigote 4, 9, 10, 11, 12, 13, 14, 17, 21, 25, 27
Ethylenediammonium diacetate 102
EUDOC docking 37
Evans-Tishenko reduction 211
F
Filaricidal agents 163
Filariosis 3
Flacourtia ramontchi 45, 46
Flavivirus infection 33
G
Galactomannans 44
Gastrodia elata 44
Ginko biloba 221
Glabranine 55
Glucans 44
Glucantime 64, 88
Gould-Jacobs reaction 47
Grignard reagent 44, 45
H
Hematophagous insects 4
Hepatitis C virus 39
High-throughput 41, 48, 166
Human african trypanosomiasis 86, 95
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