A small series of pyrazoles and isoxazoles derived from thiochroman-4-one has been synthesized and characterized. The compounds were examined for their in vitro inhibitory activity against Bacillus subtilis and Pseudomonas fluorescens. Among the tested compounds the pyrazole derivative from thiochroman-4-one was found to be the most effective inhibitor of growth of B. subtilis. Extensive H NMR analysis was recorded for all compounds.
A proton-magnetic-resonance study of the complex formed between actinomycin D and 10,11-dihydro-3H-naphth[1,2-g]indazol-7-ol strongly suggests that the indazole lies above the phenoxazine ring of actinomycin D. The complex can be destroyed by addition of dimethyl sulphoxide or dimethylformamide. The actinomycin D-indazole complex inhibits growth of Pseudomonas fluorescens and raises the thermal denaturation response of DNA. These data support the hypothesis that a molecular complex is formed which readily inhibits cell growth and interacts with DNA.
The structure of 1,4‐rlihydro[1 ]benzothiopyrano[4,3‐c ]pyrazole 5,5‐dioxide was determined by single crystal x‐ray diffraction. The molecule crystallizes in space group P21/c with a = 13.4378(6), b = 5.5938(3), c = 12.9837(6)Å, and β = 103.831°. The final R value is 0.083. Surprisingly, the tautomer with N(2)‐H exists in the crystal with the pyrazole ring being planar. The entire system is not planar as the benzene ring is rotated about C(9a) and C(9b) with respect to the pyrazole ring. In the crystal structure the pyrazole exists as hydrogen‐bonded dimers with two molecules related by a center of symmetry.
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