Synthesis of Potential Biologically Active Compounds Based on Aryloxy- and Arylaminopropanehydrazides
摘要:
New derivatives of a number of aryloxy and arylaminopropanehydrazides were synthesized. Their heterocyclization under the action of carbon disulfide and potassium hydroxide and subsequent alkylation of the resulting 2-thioxo-1,3,4-oxadiazole ring, the corresponding S-substituted products were obtained. The reaction of the starting hydrazides with arylaldehydes and pentane-2,4-dione afforded theirN '-arylidene and N '-(4-oxopentan-2-ylidene) derivatives. In preliminary laboratory tests, the synthesized compounds showed a pronounced stimulating effect on plant growth. Their activity was 44-95% compared with heteroauxin.
A Facile One-Pot Synthesis of 2-Arylamino-5-Aryloxylalkyl-1,3,4-Oxadiazoles and Their Urease Inhibition Studies
作者:Tashfeen Akhtar、Muhammad A. Khan、Jamshed Iqbal、Peter G. Jones、Shahid Hameed
DOI:10.1111/cbdd.12297
日期:2014.7
A one‐pot method for the synthesis of structural type urease inhibitors, 2‐amino‐1,3,4‐oxadiazoles, was developed. The structures of the compounds were established using spectroanalytical techniques and unambiguously confirmed by single‐crystal X‐ray analysis of compound 3o. The synthesized compounds were tested against jack beans urease, and most of the compounds (3c, 3g, 3j, 3k, 3n, 3r–3v) were found more active than the standard. The most potent compound (3u) had an IC50 value of 6.03 ± 0.02 μm as compared to the IC50 value of the standard (thiourea; 22.0 ± 1.2 μm). The prominent urease inhibition activity of these compounds may serve as an important finding in the development of less toxic and more potent antiulcer drugs. The compounds were also investigated against four bacterial strains, and some of the compounds (3g and 3r) were found more potent than the standard drug (ciprofloxacin) against all the tested strains. The MIC value for compound 3g was 0.156 μmol/mL against the tested bacterial strains.
Synthesis of Potential Biologically Active Compounds Based on Aryloxy- and Arylaminopropanehydrazides
作者:T. A. Gomktsyan、R. S. Shainova、A. V. Karapetyan、A. P. Yengoyan
DOI:10.1134/s1070363220070014
日期:2020.7
New derivatives of a number of aryloxy and arylaminopropanehydrazides were synthesized. Their heterocyclization under the action of carbon disulfide and potassium hydroxide and subsequent alkylation of the resulting 2-thioxo-1,3,4-oxadiazole ring, the corresponding S-substituted products were obtained. The reaction of the starting hydrazides with arylaldehydes and pentane-2,4-dione afforded theirN '-arylidene and N '-(4-oxopentan-2-ylidene) derivatives. In preliminary laboratory tests, the synthesized compounds showed a pronounced stimulating effect on plant growth. Their activity was 44-95% compared with heteroauxin.