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Contents for Unit 04 of Medicinal Chemistry 03
Antifungal agents:
Antifungal antibiotics: Amphotericin-B, Nystatin, Natamycin, Griseofulvin.
Synthetic Antifungal agents: Clotrimazole, Econazole, Butoconazole, Oxiconazole Tioconozole, Miconazole*, Ketoconazole, Terconazole, Itraconazole, Fluconazole, Naftifine hydrochloride,
Tolnaftate*.
Anti-protozoal Agents: Metronidazole*, Tinidazole, Ornidazole, Diloxanide,Iodoquinol, Pentamidine Isethionate, Atovaquone, Eflornithine.
Anthelmintics: Diethylcarbamazine citrate*, Thiabendazole, Mebendazole*, Albendazole, Niclosamide, Oxamniquine, Praziquantel, Ivermectin.
Sulphonamides and Sulfones
Historical development, chemistry, classification and SAR of Sulfonamides: Sulphamethizole, Sulfisoxazole, Sulphamethizine, Sulfacetamide*, Sulphapyridine, Sulfamethoxazole*, Sulphadiazine, Mefenide acetate, Sulfasalazine.
Folate reductase inhibitors: Trimethoprim*, Cotrimoxazole.
Sulfones: Dapsone*.
Anti Fungal Agents
These are drugs used for superficial and deep (systemic) fungal infections.
Many topical antifungals have been available since the antiseptic era. Two important antibiotics: amphotericin B to deal with systemic mycosis, and griseofulvin—to supplement attack on dermatophytes were introduced around 1960. Antifungal property of flucytosine was noted in 1970, but it could serve only as a companion drug to amphotericin.
CLASSIFICATION
Classification Based on the Chemical Structure, Action, and Source
The antifungal agents can be divided into the following classes, based on their chemical structure, mechanism of action, and source:
I. Antibiotics: Amphotericin B, Nystatin, Griseofulvin
II. Azoles (imidazole, triazole derivates)
Triazoles—Fluconazole, Itraconzole, Terconazole
Imidazoles—Clotrimazole, Ketoconazole, Miconazole, Bifonazole, Butoconazole, and Zinoconazole
III. Fluorinated pyrimidines: Flucytosine
IV. Chitin synthetase inhibitors: Nikomycin Z
V. Peptides/proteins: Cispentacin
VI. Miscellaneous: Ciclopirox, Tolnaftate, Naftifine, and Terbinafine
Classification Based on the Route of Administration
I. Drugs for subcutaneous and systemic mycoses: Amphotericin B, Fluconazole, Flucytosine, Itraconazole, Ketoconazole.
II. Drugs for superficial mycoses: Clotrimazole, Econazole, Griseofluvin, Miconazole, Nystatin.
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