Antifungal activities heterocycles

Caballero, J. and Fernandez, M. (2006) Linear and nonlinear modeling of antifungal activity of some heterocyclic ring derivatives using multiple linear regression and Bayesian-regularized neural networks./. Mol. Model., 12, 168-181. 

Ursu, O., Costescu, A., Diudea, M.V. and Parv, B. (2004) QSARs of some novel isosteric heterocyclic with antifungal activity. Carpathian J. Math., 20, 267-274. 

Heterocycles are contained in a large number of agrochemicals . Triazoles, such as cyproconazole, are effective plant fnngicides and have mechanisms of action - inhibition of steroid synthesis - similar to those used medicinally. Other triazoles have limited antifungal activity, bnt are nseful plant-growth regulators, for example paclobutrazol. Another widely used fungicide is davicil. 

The following section illustrates the synthesis of organophosphorus heterocycles with antibacterial and antifungal activities. For most of them, no biological target is mentioned. Therefore, the corresponding compounds are described according to the nature of the heterocycle. 

The condensation of heterocyclic chalcone 64 and hydroxylamine in PEG 400 afforded isoxazolines 65, which demonstrated antibacterial and antifungal activities (Scheme 35) [59]. 

The condensation of o-phenylenediamine with heterocyclic chalcone 150 in PEG 400 provided 1,5-benzodiazepines 151, which demonstrated antibacterial and antifungal activities in vitro (Scheme 86) [119]. The yield of the products significantly decreased when conventional organic solvents were used as a medium for this reaction. 

Rajasekhar et al. also synthesized a new class of diethyl a-aryl/2-thienyl-a-[2-(phenylthio)phenylamino]methylphosphonates (54) via a three-component Kabachnik-Fields reaction of 2-aminodiphenylsulfide (53), substituted phenyl/heterocyclic aldehydes (44), and diethyl-phosphate (2) in the presence of heterogeneous nano-silica-supported nano-BFs SiOa under solvent-free conditions under microwave irradiation (Scheme 25). The procedure has several advantages such as short reaction time, low loading of catalyst, good yields, and reusability of the heterogeneous silica-supported nano-catalyst. The title compounds were found to exhibit considerable in vitro antibacterial and antifungal activity. 

Didemnolines A-D form an original series of P-carbo-line alkaloids in which a thioether-containing imidazole is linked to nitrogen 9 of the heterocyclic system. Isolated from an imdetermined species of Didemnum genus harvested in the Mariana Islands (Rota Island), didemnolines are only moderately cytotoxic, but also have antibacterial and antifungal activities (Schumacher and Davidson, 1995). 

Benzimidazole is an important heterocyclic nucleus in the field of medicinal chemistry. The most prominent benzimidazole compound in nature is N-ribosyldimethylbenzimidazole, which serves as an axial ligand for cobalt in vitamin B12. The versatile nature of benzimidazole makes it a highly explored molecule in medicinal chemistry. A number of pharmacological activities are associated with benzimidazole derivatives such as anthelmintic, antiulcer, antipsychotic, proton pump inhibitor, antianxiety, anti-emetic and sedative, vasodilator, anticancer, analgesic, antihistaminic, antifungal, antiviral and antimicrobial. 

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