Anti-fungal agents

A cyclocondensation involving the carbonyl of a benzoquinone was used for the synthesis of a cinnoline 15 of interest as a potential anti-fungal agent <06BMCL1850>. 

Anti-diabetic agents Anti-epileptics Anti-fungal agents Anti-gout agents Anti-hypertensive agents... 

The 5-fluorocytosine (flucytosine) is an inhibitor of sterol C-14 demethylase, an enzyme involved in the biosynthesis of ergosterol, an element of fungal wall. It is marketed as an anti-fungal agent, whereas nucleoside derivatives of the... 

Certain APIs are administered topically, e.g., topical anti-inflammatory steroids and topical anti-fungal agents. The release of these APIs from their formulation was thought to be maximized when the solution of the drug in the vehicle is just saturated (27). However, Davis and Hadgraft (28) have shown that supersaturation can increase the penetration even further. The interaction of the moisture present in the skin with the topical formulation can be used to change the degree of saturation of the formulation and thereby enhance the release of the API from the formulation into the skin. 

Malik lA, Mold 1, Aziz Z, Khan S, Suleman M. A randomized comparison of fluconazole with amphotericin B as empiric anti-fungal agents in cancer patients with prolonged fever and neutropenia. Am J Med 1998 105(6) 478-83. 

MVP shows some interesting applications such as that from C. albicans MVP, which appears to be an attractive candidate for the development of anti-fungal agents [296]. As far as we could search, not literature records exist on the genetic manipulation of this key enzyme in plant species although fast progress in this research field would likely produce these expected results in the near future. 

Itraconazole, a widely used broad-spectrum anti-fungal agent has been used as an example (De Beule and Van Gestel, 2001 Peeters et al., 2002). As indicated in Figure 3, the compound is predicted to have extremely low water solubility but useful intestinal permeability. The parameter sensitivity analysis indicated that fraction absorbed could be substantially increased if the apparent solubility of the drug could be increased to 100 pg/mL or greater. Such manipulation is possible through the use of hydrophilic cyclodextrins such as 2-hydroxypropyl-... 

Scheme 11. Chemo-enzymatic synthesis of the anti-fungal agent lysofungin [173]...

Chiral racemic vinylepoxides react with phthalimide at the more substituted end of the 7t-allyl intermediate to give the chiral allylamine in up to 98% ee. Scheme 34 [ 116]. Some modification of the standard DPPBA-type ligand was required in order to achieve this level of selectivity. In particular, increased steric bulk in the form of a naphthyl moiety was claimed to restrict the number of ro-tamers and thereby increase the selectivity. This sequence was used to prepare vinylglycinol and a related reaction was used to synthesize a key intermediate for the synthesis of some anti-fungal agents [117]. 

Amphotericin B is an extremely potent anti-fungal agent used in the treatment of systemic fungal infections. However, delivery of amphotericin B is very difficult due to its insolubility in the water as well as commonly used oils. Furthermore, it shows several adverse effects such as nephrotoxicity. Brime et al. [109] successfully entrapped amphotericin B in the lecithin-based microemulsions and evaluated their acute toxicity in the mice in comparison to the marketed formulation. Acute toxicity studies indicated that... 

Metronidazole (Flagyl) is used for both bacterial (commonly for dental infections) and some protozoan infections, such as amoebic dysentery. Benzimidazoles, such as mebendazole (Pripsen), are an important group of anthelmintics. The most common anti-fungal agents are triazoles such as fluconazole (Diflucan). 

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