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Outstanding effect of the conformational restriction of isoquinolines: hints for the development of optimized antimicrobial agents |
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| Authors: | Berrin Ozcelik Javed Sheikh Ilkay E. Orhan Harjeet Juneja Brahim Bennani Abdelali Kerbal S. M. T. Cavalcanti Ana C. L. Leite Taibi Ben Hadda |
| Affiliation: | 1. Department of Pharmaceutical Microbiology, Gazi University, Ankara, Turkey 2. Department of Chemistry, Dhote Bandu Science College, Gondia, 441614, India 3. Department of Pharmacognosy and Pharmaceutical Botany, Faculty of Pharmacy, Eastern Mediterranean University, Gazimagosa, Famagusta, The Northern Cyprus 4. Department of Chemistry, RTM Nagpur University, Nagpur, 440033, India 5. Laboratoire Chimie Organique, Faculté des Sciences Dhar El Mehraz, Fès, Morocco 6. Centre for Health Science, Federal University of Pernambuco, Recife, Brazil 7. Laboratoire Chimie Matériaux, FSO, Université Med. Premier, Oujda, Morocco |
| Abstract: | Conformational restriction constitutes a useful strategy of molecular modification for the design of new potential drug candidates. Herein we present the planning, antimicrobial evaluation, and establishment of structure–activity relationship (SAR) data for some isoxazole (3a–k, 8a–c, and 9a–c) and pyrazole (5a–h) derivatives. These derivatives were structurally designed by conformational restriction followed by bioisosteric exchange of previously described antimicrobial isoquinolines (1a–c). Some of these more conformationally restricted derivatives present improved properties as new antibacterial drug candidates. |
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