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1.
J Enzyme Inhib Med Chem ; 25(1): 126-31, 2010 Feb.
Artigo em Inglês | MEDLINE | ID: mdl-20030516

RESUMO

Novel 1-[[4-(4-bromophenyl)-5-(2-furyl)-4H-1,2,4-triazole-3-yl]mercaptoacetyl]-4-alkyl/aryl-3-thiosemicarbazides (5-12) were synthesized by the reaction of 4-(4-bromophenyl)-5-(2-furyl)-4H-1,2,4-triazole-3-ylmercaptoacetylhydrazide (4) with substituted isothiocyanates. Cyclodehydration of thiosemicarbazides with concentrated sulfuric acid yielded 2-[4-(4-bromophenyl)-5-(2-furyl)-4H-1,2,4-triazole-3-yl]mercaptomethyl-5-alkyl/arylamino-1,3, 4-thiadiazoles (13-17). The new compounds were evaluated for in vitro antifungal activity using the microdilution method. The tested compounds showed varying degrees of activity against Microsporum gypseum NCPF-580, Microsporum canis, Trichophyton mentagrophytes, Trichophyton rubrum, and Candida albicans ATCC 10231 (MIC 8-4 microg/mL).


Assuntos
Antifúngicos/síntese química , Antifúngicos/farmacologia , Carbazóis/síntese química , Carbazóis/farmacologia , Fungos/efeitos dos fármacos , Tiadiazóis/síntese química , Tiadiazóis/farmacologia , Triazóis/síntese química , Triazóis/farmacologia , Antifúngicos/química , Carbazóis/química , Fungos/classificação , Espectroscopia de Ressonância Magnética , Testes de Sensibilidade Microbiana , Especificidade da Espécie , Espectrofotometria Ultravioleta , Tiadiazóis/química , Triazóis/química
2.
Acta Crystallogr Sect E Struct Rep Online ; 64(Pt 10): o1939-40, 2008 Sep 13.
Artigo em Inglês | MEDLINE | ID: mdl-21201146

RESUMO

Mol-ecules of the title spiro-[4.5]decane derivative, C(17)H(30)N(2)O(3)S, are linked by paired O-H⋯N hydrogen bonds into centrosymmetric R(2) (2)(16) dimers and these dimers are linked into a three-dimensional framework structure by C-H⋯O interactions.

3.
Acta Crystallogr Sect E Struct Rep Online ; 64(Pt 8): o1572-3, 2008 Jul 23.
Artigo em Inglês | MEDLINE | ID: mdl-21203273

RESUMO

In the title compound, C(15)H(26)N(2)O(2)S, the cyclo-hexane and morpholine rings adopt chair conformations, while the thia-zole ring has a twist conformation. An intra-molecular C-H⋯S hydrogen-bond inter-action forms a five-membered ring. The crystal packing involves C-H⋯O=C inter-molecular inter-actions where carbonyl O atoms act as double acceptors to two symmetrically related H atoms.

4.
Acta Crystallogr Sect E Struct Rep Online ; 64(Pt 8): o1574-5, 2008 Jul 23.
Artigo em Inglês | MEDLINE | ID: mdl-21203274

RESUMO

The title compound, C(16)H(28)N(2)O(3)S, is dimerized by inversion symmetry-related inter-molecular O-H⋯N hydrogen bonding, forming an R(2) (2)(16) motif. The dimers are also linked through inter-molecular C-H⋯O hydrogen bonding. The compound is chiral with a stereogenic centre located in the thia-zole ring, but in the crystal structure it forms a racemate. The thia-zole ring has an envelope conformation, while the cyclo-hexane and morpholine rings adopt chair conformations.

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