Identification of a novel series of potent HCV NS5B Site I inhibitors |
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| Affiliation: | 1. Department of Medicinal Chemistry, Boehringer Ingelheim Pharmaceuticals Inc., 900 Ridgebury Road, PO Box 368, Ridgefield, CT 06877-0368, USA;2. Department of Immunology & Inflammation, Boehringer Ingelheim Pharmaceuticals Inc., 900 Ridgebury Road, PO Box 368, Ridgefield, CT 06877-0368, USA;1. Dipartimento di Farmacia-Scienze del Farmaco, Università degli Studi ‘Aldo Moro’ di Bari, Via Orabona 4, 70126 Bari, Italy;2. Università degli Studi di Firenze, Via della Lastruccia 3, I-50019 Sesto Fiorentino (Firenze), Italy;3. Università degli Studi di Firenze, Polo Scientifico, Dipartimento NEIROFABA, Sezione di Scienze Farmaceutiche e Nutraceutiche, Via Ugo Schiff 6, 50019 Sesto Fiorentino (Firenze), Italy;2. Coordinación Regional de Trasplantes, Consejería de Sanidad y Consumo de la Región de Murcia, Murcia, España;3. Unidad de Trasplantes, Servicio de Cirugía, Hospital Universitario Virgen de la Arrixaca, Murcia, España;4. Departamento de Cirugía, Universidad de Murcia, Murcia, España;5. Departamento de Psicología, Universidad Católica San Antonio, UCAM, Murcia, España;6. Hospital Regional de Alta Especialidad del Bajío, León, Guanajuato, México;7. HGSZ No, 10 del Instituto Mexicano del Seguro Social Delegación Guanajuato, Guanajuato, León, México;8. Centro de Coordinación de Trasplantes, UMAE Hospital de Especialidades n.° 25 IMSS, Monterrey, México;9. Centro de Investigación Médico-Quirúrgica, La Habana, Cuba;10. Unidad de Intensivos, Coordinación de Trasplantes, Hospital Hermanos Ameijeiras, La Habana, Cuba;11. Facultad de Medicina, Universidad de Guanajuato, Guanajuato, León, México;12. CMN Siglo XXI del Instituto Mexicano del Seguro Social, México DF, México;13. Instituto de Salud Pública del Estado de Guanajuato, Guanajuato, León, México |
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| Abstract: | Efforts investigating spatially comparative alternates of the ethylene-bridged piperazine in BMS-791325 that would offer a maintained or improved virologic and pharmacokinetic profile have been multifaceted. One foray involved the utilization of various octahydropyrrolo[3,4-c]pyrrole propellanes. Many of the propellane analogs described in this work exhibited better than targeted potency (less than 20 nM). Additionally, improved exposure in rats was achieved through the employment of two newly invented and now readily accessible carbon bridged propellanes as compared to their heteroatom bridged analogs. |
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| Keywords: | Hepatitis HCV Propellane NS5B Site I |
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