37865-26-2Relevant academic research and scientific papers
Synthesis, characterization and biological evaluation of new 3,5-disubstituted-pyrazoline derivatives as potential anti-Mycobacterium tuberculosis H37Ra compounds
Azmi, Mohamad Nurul,Che Omar, Mohammad Tasyriq,Osman, Hasnah,Parumasivam, Thaigarajan,Supratman, Unang,Wong, Kok Tong
, (2021/05/29)
A total of fourteen pyrazoline derivatives were synthesized through cyclo-condensation reactions by chalcone derivatives with different types of semicarbazide. These compounds were characterized by IR, 1D-NMR (1H, 13C and Distortionless Enhancement by Polarization Transfer-DEPT-135) and 2D-NMR (COSY, HSQC and HMBC) as well as mass spectroscopy analysis (HRMS). The synthesized compounds were tested for their antituberculosis activity against Mycobacterium tuberculosis H37Ra in vitro. Based on this activity, compound 4a showed the most potent inhibitory activity, with a minimum inhibitory concentration (MIC) value of 17 μM. In addition, six other synthesized compounds, 5a and 5c–5g, exhibited moderate activity, with MIC ranges between 60 μM to 140 μM. Compound 4a showed good bactericidal activity with a minimum bactericidal concentration (MBC) value of 34 μM against Mycobacterium tuberculosis H37Ra. Molecular docking studies for compound 4a on alpha-sterol demethylase was done to understand and explore ligand– receptor interactions, and to hypothesize potential refinements for the compound.
Substituted pyrazolines and their cardiovascular activity
Malhotra, Vineet,Pathak, Seema,Nath, Rajendra,Mukerjee, Devashis,Shanker, Kirpa
, p. 1310 - 1313 (2007/10/03)
1-Thiocarbamoyl-3, 5-diphenyl-2-pyrazolines 4 and 5 have been prepared by cyclization of 1,3-diphenyl-2-propene-1 ones (chalcones) 3 with thiosemicarbazide in the presence of sodium hydroxide. Reaction of 3 with hydrazine hydrate followed by condensation with aryl isothiocyanates yields 1-N-substituted thiocarbamoyl-3, 5-diphenyl-2-pyrazolines 5. These compounds have been characterized on the basis of elemental analysis, IR, 1H NMR and MS. Compounds have been evaluated for their cardio-vascular activity and toxicity.
