Synthesis, characterization and in vitro biological evaluation of some new 1,3,5-triazine-chalcone hybrid molecules as Mycobacterium tuberculosis H37Rv inhibitors

A novel series of 1,3,5-triazine-chalcone hybrid molecules (4a-ii) have been synthesized and evaluated in vitro for Mycobacterium tuberculosis H37Rv inhibitory potency using Alamar blue assay and the activity expressed as the minimum inhibitory concentration (MIC) in µg/mL. The antitubercular activity screening data revealed that the compound 4z demonstrated comparatively the most potent inhibitory activity, with MIC value 3.125 µg/mL. It is noteworthy that the compounds 4e, 4p and 4bb also showed appreciable inhibitory activity with MIC value 6.25 µg/mL. Most of the compounds displayed significantly promising activity and their structure-activity relationships were also discussed. This could be the remarkable starting point to develop new lead molecules with potential antitubercular activity

Synthesis, characterization and in vitro evaluation of some new 5-benzylidene-1,3-thiazolidine-2,4-dione analogs as new class of α-glucosidase inhibitors

A series of 5-benzylidene-1,3-thiazolidine-2,4-dione derivatives (5a-u) were synthesized and tested against α-glucosidase. Preparation of the titled compounds was achieved by reaction of (Z)-4-((2,4-dioxo-1,3-thiazolidin-5-ylidene)methyl)benzaldehyde (4) and aromatic/hetero aromatic ketone. Among the compounds tested, (5p) and (5o) were identified as the most active in vitro with minimum inhibitory concentration (MIC) of 6.56±0.81 and 8.92±0.21 µg/mL against α-glucosidase, respectively. Evaluation of the structure activity relationship of substituents within these series has followed the discovery of a variety of compounds

Synthesis, characterization and in vitro biological evaluation of some new diarylsulfonylurea-chalcone hybrids as potential 5-lipoxygenase inhibitors

A series of some new diarylsulfonylurea-chalcone hybrids (4a-4y) have been synthesized via Claisen-Schmidt condensation reaction by treating 1-(3-acetylphenyl)-3-tosylurea with various aromatic/heteroaromatic aldehydes in the presence of alkali and characterized by FT-IR, 1H NMR, 13C NMR and LC mass spectral analysis. All the synthesized compounds were evaluated for their in vitro 5-Lipoxygenase inhibitory activity using potato 5-lipoxygenase enzyme. Among the tested compounds 4r and 4o exhibited significant inhibitory activity at IC50 values 7.88±0.14 and 11.77±0.21 µg/mL, respectively. This level of activity was found comparable to that of the reference drug Abietic acid (LI01020) with IC50 value 4.34±0.37 µg/mL and it could be a remarkable starting point to develop new lead molecules