Activity, antifungal

For example, Ghorab and coworkers exploited the classical Biginelli reaction to synthesize a variety of potentially active antifungal agents such as 56 from DHPM 55. ... 

ATC D01AE15 D01BA02 J02AX Use orally and topically active antifungal... 

Morgan, B., Dodds, D.R., Zaks, A., Andrews, D.R. and Klesse, R., Enzymatic desymmetrisa-tion of prochiral 2-substituted-l,3-propanediols apracticalchemoenzymatic s3mthesis of akey precursor of SCH51048, a broad-spectrum orally active antifungal agent. J. Org. Chem., 1997, 62, 7736-7743. 

Lee J, Choi Y, Woo ER, Lee DG. (2009) Isocryptomerin, a novel membrane-active antifungal compound from Selaginella tamariscina. Biochem Biophys Res Commun 379 676-680. 

Fluconazole (4) is the first member of a new generation of orally active antifungal agents, highly effective in the treatment of dermal and vaginal infections [6, 7] 5-Fluorocytosine (5) is also used to treat serious systemic fungal infections [5]... 

Total synthesis of an orally active antifungal agent, ambruticin (112), which was isolated from fermentation extracts of Myxobacteria species Polyangium... 

Upadhayaya, R. S., Sinha, N., Jain, S., Kishore, N., Chandra, R., Arora, S.K. Optically active antifungal azoles synthesis and antifungal activity of (2R,3S)-2-(2,4-difluorophenyl)-3-(5-[2-[4-arylpipera-zin-l-yl]ethyl]tetrazol-2-yl/l-yl)-l-[ 1,2,4]-triazol-l-yl-butan-2-ol. Bioorg. Med. Chem. 2004, 12, 2225-2238. 

The 1,3-dioxolane ring is found in a major antifungal drug, ketoconazole (123). Ketoconazole is a broad spectrum, orally active antifungal agent and is used to treat a wide variety of superficial or deep fungal infections. Various workers, especially in Russia, have explored the use of simple oxathiolanes as radioprotectants. For example, the survival rate of mice irradiated with lethal doses of X- or -y-rays was 40% when they were pretreated with 2,2-dimethyl-l,3-oxathiolane. Other oxathiolanes were less active. 1,3-Oxathiolane, administered intravenously to dogs 2 or 3 times daily for 2-4 days before chronic irradiation with polonium-210, increased their life expectancy from 9 months to 3-7 years and alleviated radiation sickness. Some blood indicators were also restored to normal. 

ANTITUMORAL ACTIVITY ANTIPROTOZOAL ACTIVITY ANTIBACTERIAL ACTIVITY ANTIFUNGAL ACTIVITY... 

Undecenoic acid, the active antifungal entity, is liberated from the zinc salt on contact with moisture on the skin. 

Pisatin (42) was shown to be an active antifungal agent, and (—)-pisatin also showed weak bioactivity. In this case, even the unnatural enantiomer (—)-42 was bioactive, as tested by Dr. G. Russell in... 

Compound 13 was used to construct the left half of the orally active antifungal agent ambru-ticin319. For a convergent total synthesis of ambruticin via the Eschenmoser rearrangement see ref 320. 

Ten different fungi were grown in each of the four test media both as still cultures (21 days) and shaken (6 days). The cultures were extracted as described above at time of harvest, and each extract was tested for antibacterial activity, antifungal activity, and brine shrimp toxicity. The Media D cultures were consistent with earlier growth profiles, as should be expected. 

Cabral, K.M., Almeida, M.S., Valente, A.P., Almeida, F.C., and Kurtenbach, E. (2003) Production of the active antifungal Pisum sativum defensin 1 (Psdl) in Pichia pastoris overcoming the inefficiency of the STE13 protease. Protein Expression PuriJ., 31, 115-122. 

Sensitisation to the topical antifungal agent, Mycanodin is difficult to quantitate. The active antifungal is 3-(2-hydroxy-5-chlorophenyl)pyrazole and this can cause contact allergic dermatitis and photoallergic reactions (Fig. 4 Burckhardt et al. 1968). The same authors showed, however, that an antihistamine co-formu-... 

An efficient and highly enantio- and diastereoselective bromocycliza-tion-desymmetrization of olefmic 1,3-diols used a cyclic sulfide as catalyst. Olefmic 1,3-diols as substrates gave substituted THFs with up to three ste-reogenic centers, with two tetra-substituted carbons. This protocol represents the first case of a monofunctional C2-symmetric Lewis basic sulfide-catalyzed enantioselective bromoetherification reaction, which was applicable to the synthesis of a key intermediate to the orally active antifungal drug posaconazole (Noxafil) (14JA5627). 

The relative stereochemistry of the orally active antifungal metabolite ambruticin (3) from Polvanaium cellulosum is known from 2i-ray crystallographic... 

Major Applications Display device,4 sensors,5 6 photochrotnic materials, inks, detergent, cos-metics,io biosensors, i assay for enzyme activity,antifungal agent,i3 antiAlDS agenti Safety/Toxicity No data available... 

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