triazole

Efflux inhibition is proven bacterial machinery responsible for removal of bacterial wastage including antibiotics. Recently, efflux inhibitors (EI) have been tested with encouraging results as an adjuvant therapy for treatment of various bacterial invasions especially methicilline-resistant Staphylococcus aureus (MRSA). Although, EI have emerged as innovative approach of treatment for several multi drug resistant bacterial infections including tuberculosis, toxicity profile limits their wider use. To address this issue, we have attempted synthesizing hybrid molecules those results by combining known EI and triazole. This synthesis was aimed to arrive at structure that possesses pharmacophore from known EI. Synthesized molecules were evaluated as growth inhibitors (GI) and Efflux inhibitor of S. aureus. Pharmacologically active compounds were then tested for their cytotoxicity to further narrow down search. Most active compounds 209, 210, 217 & 228 were then tested for their GEI action against MRSA. We arrived at compound 210 as most potent dual inhibitor.

Efflux inhibition is proven bacterial machinery responsible for removal of bacterial wastage including antibiotics. Recently, efflux inhibitors (EI) have been tested with encouraging results as an adjuvant therapy for treatment of various bacterial invasions especially methicilline-resistant Staphylococcus aureus (MRSA). Although, EI have emerged as innovative approach of treatment for several multi drug resistant bacterial infections including tuberculosis, toxicity profile limits their wider use. To address this issue, we have attempted synthesizing hybrid molecules those results by combining known EI and triazole. This synthesis was aimed to arrive at structure that possesses pharmacophore from known EI. Synthesized molecules were evaluated as growth inhibitors (GI) and Efflux inhibitor of S. aureus. Pharmacologically active compounds were then tested for their cytotoxicity to further narrow down search. Most active compounds 177, 178, 187 and 196 were then tested for their GEI action against MRSA. We arrived at compound 145 as most potent dual inhibitor.

  The present study, a series of clubbed triazole generated by microwave organic reaction enhancement (MORE) method and examine for their cyclin dependent kinase-5 (cdk5) inhibitors, potentially useful for treatment of Alzheimer disease. Evaluation of the structure active relationship (SAR) of substitution with-in these series has allowed the identification of a range of compounds which significantly reduce brain cdk5/p25 by scintillation proximate assay method. The cdk5/p25 inhibitor data of the tested compounds indicated that 3E, 4E, 6E, 8E and 8I showed better activity out of which 8E and 8I shows equally selective versus cdk2. Key words: Cyclohexyl thiophene, triazole, cdk5/p25, Alzheimer's disease, MORE.