Antimycotic activity

A cytotoxic alkaloid has been isolated from the filamentous species Hapalosi-phon forUinalis strain V-3-1. This isolate was made from soil samples collected in the Marshall Islands in 1981. This strain produces the lipophilic compound hapalindole A, which has a broad range of antialgal and antimycotic activity (9). OscUlatoria acutissima strain B-1, isolated from a freshwater pond in Oahu, was found to produce two novel macrolide compounds termed acutiphycin and 20, 21-didehydroacutiphycin. These macrolides show cytotoxicity (KB and NIH/3T3) and antitumor activity (Murine Lewis lung carcinoma) (10). 

Keywords Antibacterial activity Antimycotic activity Antiprotozoal activity Antiviral activity Cathechins Proanthocyanidins... 

The antimycotic activity of catechins occurring in green tea composition against yeasts and filamentous fungi has been studied. Hirasawa and Takada [66] reported the susceptibility of Candida albicans to EGCG. Anal-... 

Some of the N-alkylated narceine amides and imides were tested for antibacterial effectiveness and showed activity of medium potency against Mycobacterium tuberculosis H37 Rv. Their antimycotic activity was also of medium strength. Coccidiostatic screening showed some effectiveness (100). 

The pharmacologically important tryptanthrine, a quinazoline alkaloid, is known for its antimycotic activity and is used against skin infections. This alkaloid is obtained from isatin (260) and o-azidobenzoyl chloride (261), as shown in Scheme 96. The adduct formed is cyclized via a Staudinger and an aza-Wittig reaction to afford tryptanthrine (262) (92H153). 

New applications of dithioles and dithiolanes include evaluation of compounds such as 69 and 70 as flavour components <98MI177>, 71 for antimycotic activity <99MIP33826>, 72 for antiviral activity <99CC1245>, 73 for antifungal and antibacterial activity <99MI6> and use of 74 in prevention and heatment of asthma complications <99EUP909758>. 

The antimycotic activity of a number of substituted 3-(3,3,3-trichloro-2-hydroxyprop-l-yl)benzofurans has been reported. Diuretic and other activities have been observed in a number of substituted aminobenzofuran-2-carboxylic acid derivatives. a- 2-Benzofuranyl) acrylic acid has exhibited a marked depressive ataratic and hypotensive activity (61MI31200), while 5-cinnamoylbenzofurans, e.g. (499), have been examined for hypertensive, vasodilating and spasmolytic activities (70GEP1933178). 

In similar studies, the reduction potentials of 1,2-benzothiazole derivatives in DMF were correlated to antimycotic activity [166], and those of 1,3,5,7-substituted-1,3-dihydro-2H-l, 4-benzodiazepin-2-ones and benzodiazepine-2-thiones in dimethylformamide (DMF)-water solutions were correlated to inhibition of orientation reactions and to protection from electric shock [167]. 

Normajusculamide C (369), which is closely related to dolastatin 11 (364), was isolated from a deep-water variety of the blue-green alga Lyngbya majuscula collected at Enewetak Atoll in the Marshall Islands (298). Compound 369 exhibits antimycotic activity. From the same alga L. majuscula were isolated the lipopentapeptides majusculamide D (370) and deoxymajusculamide D (371), with both compounds showing moderate cytotoxicity (299). 

Amino-l,2-benzisothiazoles such as 54 have been claimed22 to possess antiinflammatory, analgesic, and hypotensive properties, while 3-dialkylamino-l,2-benzisothiazoles16 and 3-aryloxy- or 3-arylthio-l,2-benzisothiazoles (55)23 have useful antimycotic activity. 

In a recent East German review some biological activities of triazoles (1,2,4- and 1,2,3-) have been described (8iMl4lloo). The virostatic, cytostatic, antimicrobial and antimycotic activities of derivatives of 1,2,3-triazolecarbonamides are discussed. Furthermore, 4- or 5-halomethyl-1,2,3-triazoles, c.g. (420a), can be used as radiomimetica and show cancero-... 

Benzoxonium is a quaternary ammonium compound with antibacterial, antiviral, and antimycotic activity. It can be used in topical disinfection, disinfection of surgical instruments, inhibition of plaque formation, and in veterinary products. 

Ballistreri, A., Bottino, A., Musumarra, G, Fioravanti, R., Biava, M., Porretta, G.C., Simonetti, N. and Villa, A. (1996). Design, Synthesis and Antimycotic Activity of (N-Heteroaryl)Arye-methanamines. J.Phys.Org.Chem., 9, 61-65. 

Trovato et al. [49] reported the antimycotic activity of aqueous, ethanol and petroleum ether extracts of Matricaria recutita L. These extracts inhibited in vitro strains of Candida albicans isolated from clinical samples obtained in the course of acute vaginitis. 

The approach to therapy is to remove or improve any predisposing factors if they can be identified. A pharmacologic agent should have limited local and systemic side effects, a high cure rate, and easy administration. Additionally, it would be advantageous to use a therapy that is able to resolve symptoms within 24 hours, that has broad antimycotic activity (to cover increasing rates on non-albicans Candida), that prevents recurrence, and that can be used over a shortened period of time such as 1 to 3 days. 

Zamilpa A, Tortoriello J, Navarro V, Delgado G, Alvarez L (2002) Five New Steroidal Saponins from Solanum chrysotrichum Leaves and Their Antimycotic Activity. J Nat Prod 65 1815... 

Extensive SAR studies showed that the imidazole ring is crucial for broad-spectrum, high-potency antimycotic activity in vivo. It is ironic that even replacement with benzimidazole, the original lead compound, exhibited very low effectivness. Exchanging one nitrogen with carbon (i.e., pyrazoles and piperazines) also resulted in less active, or even inactive, compounds. 

The importance of deriving a QSAR model on a well-balanced set of structures, even in the presence of a much larger number of available data for the same series, was shown in two studies regarding the antibacterial and antimycotic activity of benzofused heteroaromatic derivatives [42] as well as in the antibacterial activity of quinolones [43,44], working in the PC space of a PCA performed ad hoc on the whole set of available or candidate strictures. 

A monograph on fungal infection in the compromised patient provides timely information on this area of increasing clinical concern. The antifungal action of the intraleukocytlc antibacterial rifan5>in was reviewed and the antimycotic activity and therapeutic effectiveness of 5-bromosalioyl-4 -chloranilide and its derivatives assessed in laboratory animals and man. ... 

Tioxaprofen (10) was synthesised as a non-steroidal antiinflammatory but h been found to have antimycotic activity against T. mentagrophytes. T. mbrum. MLorosporum oanls and C. albicans.51 The compound appears to act by uncoiQ>ling mitochondrial respiration. 

Petranyi G, Stutz A, Ryde NS, et ai. Experimentai antimycotic activity of naftifine and terbinafine. in Fromtiing RA, ed. Recent Trends in the Discovery, Deveiopment, and Evaiuation of Antifungai Agents. Barceiona JR Prous Science, 1987 441-459. 

Caceres, A., et al. "Plants Used in Guatemala for the Treatment of Dermatophytic Infections. 1. Screening for Antimycotic Activity of 44 Plant Extracts." J Ethnopharmacol 31(3) 263276, 1991. Abstract. 

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