65results about How to "Broad spectrum antifungal" patented technology

The invention discloses a water soluble triazole compound and a synthesis method thereof. The water soluble triazole compound has a structure as shown in Formula Ia, Formula Ib, Formula Ic or Formula Id, wherein R1 is a group in Formula II. The compound of the invention is formed by adding a new group on the structural basis of a broad-spectrum, high-efficiency antifungal compound discovered in the present clinical application and new drug development process to increase the water solubility and reduce the toxicity, is a derivate of the triazole antifungal drug, and has the characteristics of broad antifungal spectrum, high antifungal activity, good safety and the like.

The invention relates to the technical field of medicines. Present antifungal medicines which have problems of large side effect, narrow antimicrobial spectrum, easy generation of the drug resistance and the like cannot satisfy clinical treatment needs. The invention provides novel triazole alcohol antifungal compounds with high efficiency, low toxicity and wide spectrum and pharmaceutically acceptable salts thereof. The compounds are 1-(1H-1,2,4-triazol-1-yl)-2-(2,4-difluorophenyl)-3-(nitrogen-containing side chain substituted)-2-propanol compounds, and the general structure of the compounds is shown in the specification. The invention also provides a preparation method of the compounds and an application of the compounds in the preparation of antifungal medicines.

The invention relates to the medical technical field, in particular to a new triazole alcohols antifungal compound and salts thereof with the following chemical structure formula and a preparation method and the application thereof; R1 is selected from n-propyl, isopropyl or butyl; R2 is selected from alkyl or halogen; the salts include hydrochloride, hydrobromide and methane sulphonate. The compound has strong antifungal activity on various fungi in shallow parts and deep parts. Compared with the antifungal medicines used in the existing clinical applications, the compound has the advantages of high efficiency, low toxicity, broad antifungal spectrum, and the like, and can be used for preparing new antifungal medicines.

The invention relates to a substituted triazolone benzyl amine triazole antifungal compound, i.e. 1-(1H-1,2,4-triazol-1-yl)-2-(2,4-difluorophenyl)-3-[N-methyl-N-(2-substituted-2H-1,2,4-triazol-3-one-4-yl) benzylaminoformyl]-2-propanols compounds, their salts and their preparation process. The compounds has very strong antimycotic effect.

The invention discloses a tricyclic isoxazole derivative, belongs to the technical field of medicines, and provides a compound with a general formula (1) as shown in the specification, a geometrical isomer of the compound or pharmaceutically acceptable salt, hydrates, solvates and prodrugs of the compound and preparation methods of the salt, the hydrates, the solvates and the prodrugs. The compound has good antifungal activity for various superficial and deep fungi and the advantages of high efficiency, low toxicity, wide antifungal spectrum and the like as compared with existing clinically-applied antifungal drugs, and the compound can be used for preparing antifungal drugs.

The invention provides a novel azole antifungal compound. According to the azole antifungal compound, a structural general formula is shown in the specification, wherein X is hydroxyl, Ar is 2,4-difluoro phenyl, and R is selected from hydrogen, alkyl, halogen, cyano-group, nitryl, amino or alkoxy and can be positioned at the ortho-position, meta-position or para-position of a benzene ring and can be mono-substituted or multi-substituted; the alkyl has 1 to 4 carbon atoms; the halogen is selected from F, Cl, Br and I; the amino is selected from -NH2, one or two aminos substituted by the alkyl and cyclic amino; and the alkoxy is selected from methoxyl, ethyoxyl and tert-butyl oxygroup. The invention also provides a method for preparing the compound and application of the compound to preparation of antifungal medicines. Compared with the conventional antifungal medicines which are applied clinically, the azole antifungal compound has the advantages of high antifungal activity on invasive fungi, high efficiency, low toxicity, broad spectrum and the like; and the method is simple and high in yield, and the prepared compound has a good antifungal effect.

The invention belongs to the technical field of drug synthesis, and relates to 2, 4, 4-trisubstituted dihydrooxazole derivatives, pharmaceutically acceptable salts, hydrates, solvates or prodrugs thereof, preparation methods of the 2, 4, 4-trisubstituted dihydrooxazole derivatives and the pharmaceutically acceptable salts, hydrates, solvates or prodrugs thereof, and an application of the 2, 4, 4-trisubstituted dihydrooxazole derivatives and the prodrugs thereof as drugs for treating various diseases caused by fungal infection. The general formula of the 2, 4, 4-trisubstituted dihydrooxazole derivative and the stereoisomer or the pharmaceutically acceptable salt, hydrate, solvate or prodrug thereof is shown as (I), wherein MBG, X, Y, M and R1 are shown in the claims and the specification. .

The invention relates to application of formononetin in aspergillus fumigatus prevention. The technical scheme of the invention provides application of the formononetin in preparation of a fungus infectious disease medicament. The fungus is aspergillus fumigatus. The compound in the invention is high in antifungal activity to various funguses on both the superficial part and the deep part. Compared with the conventional clinically applied antifungal medicament, the formononetin has the advantages of high efficiency, low toxicity, large antifungal spectrum and the like and can be used for preparing antifungal medicaments.

The invention relates to a triazole alcohol derivative, and a preparation method and an application thereof. The chemical structure of the triazole alcohol derivative is represented by formula I, A inthe formula I represents a benzene ring or a substituted benzene ring, and the substituent group of the substituted benzene ring can be located at each position of the benzene ring, is monosubstituted or polysubstituted, and is selected from: a) halogen which is F, Cl, Br or I; b) an electron-withdrawing group, wherein the electron withdrawing group is a cyano group, a nitro group or a trifluoromethyl group; c) a C1-4 low alkyl group or a halogen-substituted low alkyl group; and d) a C1-4 low alkoxy group or a halogen-substituted low alkoxy group. The compound has the advantages of high antifungal activity, low toxicity, wide antibacterial spectrum and the like, and can be used for preparing antifungal medicines.

An antifungus compound 1-(1H-1,2,4-triazole-1-yl)-2-(2,4- difluorophenyl)-3-[N-methyl-N-(4-substituted amino) benzylamino]-2-propanol and its salts, and its preparing process are disclosed. Its advantages are high curative effect, low poison and broad spectrum.

The invention relates to the technical field of medicine, and provides a class of 1-(1H-1,2,4-triazole-1-yl)-2-(2,4-difluorophenyl)-3-((piperidine oxadiazole side chain substituted))-2-propanol compound, which comprises cis-trans-isomers of the compound and any mixture of these forms or medical salts thereof. The chemical structure of the compound is as shown in a formula (I) in the Specification. The invention further provides a preparation method of the compound, and an application in the preparation of an antifungal drug. Antifungal experiments show that the compound has excellent antifungal effect for various shallow and deep funguses; compared with an existing antifungal drug such as fluconazole in clinical application, the compound has the advantages of high efficiency, low toxicity and wide antifungal spectrum, and can be used for preparing new antifungal drugs.

The invention relates to application of formononetin in cryptococcus neoformans. The technical scheme of the invention is the application of formononetin in preparing medicaments for treating antifungal infected diseases, wherein the fungus is cryptococcus neoformans. The compound has an excellent antifungal activity on various superficial and deep funguses, has the advantages of high activity, low toxicity, broad antifungal spectrum and the like when being compared with an antifungal medicament in existing clinical application, and can be used for preparing antifungal medicaments.

The invention relates to a triazole aromatic alcohol heterocyclic ether derivative and the preparing method and application thereof, and particularly provides the general structure, crystal form, pharmaceutically acceptable inorganic acid salt or organic acid salt, aquo-complex, and solvate or prodrug of the triazole aromatic alcohol heterocyclic ether derivative. In-vitro and in-vivo bacteriostasis experiments prove that the compound has remarkable activity in inhibiting human body pathomycete candida albicans, candida parapsilosis, cryptococcus neoformans, candida glabrata, aspergillus fumigates, gypseous microsporum and trichophyton rubrum, and the activity is higher than that of fluconazole. Furthermore, the compound has the advantages of being low in toxicity, wide in antifungal spectrum and the like, and therefore the compound can be used for preparing antifungal drugs.

The invention relates to triazole alcohol derivatives, and a preparation method and application thereof. The chemical structures of the derivatives are shown as a formula I shown in the specification,wherein R represents a structure shown in the specification or a structure shown in the specification; R1 and R2 may individually represent a hydrogen atom, alkyl, aryl, aralkyl, or cycloalkyl; substituents may be located at various positions of the benzene ring in a mono- or poly-substituted manner; the substituents and R3 are selected from: a) a halogen which is F or Cl, b) an electron withdrawing group which is cyano or trifluoromethyl, c) C1-C4 lower alkyl or halogen-substituted C1-C4 lower alkyl, and d) C1-C4 lower alkoxy or halogen-substituted C1-C4 lower alkoxy. The compounds of the invention have strong antifungal activity, have the advantages of low toxicity, wide antibacterial spectrum and the like, and can be used for preparing antifungal drugs.