Microwave assisted synthesis and biological evaluation of a series of 1,5-benzothiazepines as potential cytotoxic and antimicrobial agents

A series of 2,3-dihydro-2-(susbtituted)-4-(1-methyl-1H-pyrrol-2-yl)-1,5-benzothiazepines (4a-v) have been synthesized evaluated for their in vitro cytotoxicity and antimicrobial activities. Among the tested compounds for cytotoxicity using Brine shrimp lethality assay, compound 4q exhibited significant cytotoxicity at ED50 values 3.45±0.15 µg/mL. This level of activity was found comparable to that of the reference drug podophyllotoxin with ED50 value 3.61±0.17 µg/mL. Antimicrobial activity was assessed using agar well diffusion assay method against selected Gram-positive, Gram-negative and fungal strains. Among the compounds tested, 4q, 4r and 4l were found to be more active with MIC 16-32 µg/mL against all tested microorganisms

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