Antifungal agents antibiotic

Nucleoside antibiotics biosynthesis, 1, 88-90 Nucleosides oxa analogues, 3, 1085 as pharmaceuticals, 1, 153 protected, 5, 316 Nucleosidin occurrence, 5, 603 Nupharolutine synthesis, 2, 393 Nybomycin applications, 6, 667 Nybomycin, deoxy-applications, 6, 667 Nystatin antifungal agent veterinary use, 1, 211... 

Certain compounds are known to achieve higher absorption rates from the GI tract if they are taken with food, and this observation has been linked to their solubilization by bile salts [74], Bile salts, especially those of cholic and deoxycholic acids, have been used to solubilize steroid hormones [75], antibiotics [76], and nonsteroidal antiinflammatory drugs [77]. For example, amphotericin B (an antifungal agent) has been solubilized for parenteral use in micelles composed of sodium desoxycholate [78], As illustrated in Fig. 11, the degree of solubilization of carbamazepine by sodium desoxycholate is minimal below the critical micelle concentration but increases rapidly above this value [79]. At sufficiently high concentrations, when the micelles become saturated in carb-amezepine, the apparent solubility reaches a limiting value approximately seven times the true aqueous solubility in the absence of desoxycholate. 

Amphotericin B (AmB) is a broad-spectrum antifungal agent that is the antibiotic of choice for disseminated fungal infections, particularly in immunocompromised patients. AmB is also used for the treatment of Leishmaniasis as a second-line treatment. However, its toxicity toward mammalian cells is often dose limiting, whatever its indication. 

Many natural aromatic compounds are produced from the cyclization of poly- -keto chains by enzymic aldol and Claisen reactions. Examples include simple structures like orsellinic acid and phloracetophenone, and more complex highly modified structures of medicinal interest, such as mycophenolic acid, used as an immunosuppressant drug, the antifungal agent griseofulvin, and antibiotics of the tetracycline group, e.g. tetracycline itself. 

A4 inhibitors - Patients receiving cytochrome P450 3A4 inhibitors, such as macrolide antibiotics (erythromycin and clarithromycin), antifungal agents (ketoconazole, itraconazole, and miconazole), or cyclosporine or vinblastine should not receive doses of tolterodine greater than 1 mg twice/day (greater than 2 mg/day for ER capsules). 

Drugs that may interact with rifabutin include the following Anticoagulants, azole antifungal agents, benzodiazepines, beta blockers, buspirone, corticosteroids, cyclosporine, delavirdine, doxycycline, hydantoins, indinavir, rifamycins, losartan, macrolide antibiotics, methadone, morphine, nelfinavir, quinine, quinidine, theophylline, aminophylline, tricyclic antidepressants, and zolpidem. 

Coval, S.J. Puar, M.S. Phife, D.W. Terracciano, J.S. Patel, M. (1995) SCH57404, an antifungal agent possessing the rare sordaricin skeleton and a tricyclic sugar moiety. J. Antibiot., 48, 1171-2. 

Inhibitors of the CYP3A4 isoenzyme could increase systemic dofetilide exposure. Inhibitors of this isoenzyme (e.g., macrolide antibiotics, azole antifungal agents, protease inhibitors, serotonin reuptake inhibitors, amiodarone, cannabinoids, diltiazem, grapefruit juice, nefazadone, norfloxacin, quinine, and zafirlukast) should be cautiously coadministered with TIKOSYN, because they can potentially increase dofetilide levels... 

The complex polyene macrolide antibiotics are clinically effective as antifungal agents. Scott Rychnovsky of the University of California at Irvine has reported (Angew. Chem. hit. Ed. 2004,43, 2822) the first synthesis of rimocidinolide methyl ester 4, the aglycone of rimocidin 1. The key step in the synthesis is the condensation of the aldehyde 2 with the phosphonate 3, leading to 4. 

Natamycin is another polyene antibiotic effective against dermatophytes. The name originally proposed for the compound was pimaricin, which has been used in some of the earlier literature studies and reports. It has been used as topical therapeutic in animals and humans for over 30 years, and it is also used as an antifungal agent in food processing. 

Griseofulvin (60) is an antifungal agent that becomes concentrated in the skin after oral administration, and it is useful in the treatment of cutaneous fungal infections. Bleomycin and similar antibiotics are discussed as chelating agents (p. 159). 

The antibiotic cycloheximide, isolated from Strepomyces griseus, is used as an antifungal agent and for inhibition of protein synthesis. The biosynthesis of cycloheximide via the polyacetate pathway is easily demonstrated by culturing S. griseus in the presence of [l-l3C]- and [2-13C]-acetate and, after the isolation of the antibiotic, by comparing the natural abundance 13CNMR spectrum with those of labeled cycloheximide [1006]. Table 5.40 demonstrates that six carbons (C-4, C-6, C-8, C-10, C-12 and C-14) are incorporated from the carbonyl carbon and six from the methyl carbon (C-3, C-5, C-7, C-9, C-ll and C-13) of acetate. 

Macrolides. Antibiotics in the macrolide group are macrocyclic lactones that can be further classified into two main subgroups (I) polyene macrolides that are antifungal agents and include compounds like nystatin and amphotericin B and (2) antibacterial antibiotics represented by erythromycin and tylosin. A number of other subfamilies of antibacterial and antifungal antibiotics fall into the broad category of macrolides,... 

Antibiotics are used as antibacterial agents, anticancer agents, antituberculin agents, antifungal agents, antiviral agents, and in veterinary products and animal feed supplements for growth promotion. 

Watanabe S, Hirai H, Kato Y, Nishida H, Saito T, Yoshikawa N, Parkinson T, Kojima Y (2001) CJ-19,784, a New Antifungal Agent from a Fungus, Acanlhosligmella sp. J Antibiot 54 1031... 

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