| Revue: | Brazilian Journal of Pharmaceutical Sciences |
| Base de datos: | PERIÓDICA |
| Número de sistema: | 000451296 |
| ISSN: | 1984-8250 |
| Autores: | Iqbal, Javed1 Rehman, Aziz ur1 Abbasi, Muhammad Athar1 Siddiqui, Sabahat Zahra1 Rasool, Shahid1 Ashraf, Muhammad2 Iqbal, Ambar2 Hamid, Sujhla2 Chohan, Tahir Ali3 Khalid, Hira4 Laulloo, Sabina Jhaumeer5 Shah, Syed Adnan Ali6 |
| Instituciones: | 1Government College University, Department of Chemistry, Lahore, Punjab. Pakistán 2The Islamia University of Bahawalpur, Department of Chemistry, Bahawalpur, Punjab. Pakistán 3University of Veterinary and Animal Science, Institute of Pharmaceutical Science, Lahore, Punjab. Pakistán 4Forman Christian College University, Department of Chemistry, Lahore, Punjab. Pakistán 5University of Mauritius, Department of Chemistry, Reduit. Mauricio 6Universiti Teknologi MARA, Faculty of Pharmacy, Bandar Puncak Alam, Selangor Darul Ehsan. Malasia |
| Año: | 2020 |
| Volumen: | 56 |
| País: | Brasil |
| Idioma: | Inglés |
| Tipo de documento: | Artículo |
| Enfoque: | Experimental, aplicado |
| Resumen en inglés | We synthesized a series of compounds bearing pharmacologically important 1,3,4-oxadiazole and piperidine moieties. Spectral data analysis by 1H-NMR, 13C-NMR, IR and EI-MS was used to elucidate the structures of the synthesized molecules. Docking studies explained the different types of interaction of the compounds with amino acids, while bovine serum albumin (BSA) binding interactions showed their pharmacological effectiveness. Antibacterial screening of these compounds demonstrated moderate to strong activity against Salmonella typhi and Bacillus subtilis but only weak to moderate activity against the other three bacterial strains tested. Seven compounds were the most active members as acetyl cholinesterase inhibitors. All the compounds presented displayed strong inhibitory activity against urease. Compounds 7l, 7m, 7n, 7o, 7p, 7r, 7u, 7v, 7x and 7v were highly active, with respective IC50 values of 2.14±0.003, 0.63±0.001, 2.17±0.006, 1.13±0.003, 1.21±0.005, 6.28±0.003, 2.39±0.005, 2.15±0.002, 2.26±0.003 and 2.14±0.002 µM, compared to thiourea, used as the reference standard (IC50 = 21.25±0.15 µM). These new urease inhibitors could replace existing drugs after their evaluation in comprehensive in vivo studies |
| Disciplinas: | Química |
| Palabras clave: | Química farmacéutica, 1,3,4-Oxadiazol, Inhibición enzimática, Acetilcolinesterasa, Actividad antibacteriana, Piperidina, Sulfonamidas |
| Keyword: | Medicinal chemistry, 1,3,4-Oxadiazole, Enzymatic inhibition, Acetylcholinesterase, Antibacterial activity, Piperidine, Sulfonamides |
| Texte intégral: | Texto completo (Ver HTML) Texto completo (Ver PDF) |
