Academic Journal
Design, Synthesis, and Pharmacological Evaluation of Novel Hybrid Compounds To Treat Sickle Cell Disease Symptoms
| العنوان: | Design, Synthesis, and Pharmacological Evaluation of Novel Hybrid Compounds To Treat Sickle Cell Disease Symptoms |
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| المؤلفون: | dos Santos, Jean Leandro, Lanaro, Carolina, Lima, Lidia Moreira, Gambero, Sheley, Franco-Penteado, Carla Fernanda, Aexandre-Moreira, Magna Suzana, Wade, Marlene, Yerigenahally, Shobha, Kutlar, Abdullah, Meiler, Steffen E., Costa, Fernando Ferreira, Chung, ManChin |
| المساهمون: | Universidade Estadual Paulista (UNESP) |
| بيانات النشر: | Amer Chemical Soc |
| سنة النشر: | 2011 |
| المجموعة: | Universidade Estadual Paulista São Paulo: Repositório Institucional UNESP |
| الوصف: | Fundação de Amparo à Pesquisa do Estado de São Paulo (FAPESP) ; Processo FAPESP: 10/12495-6 ; Processo FAPESP: 07/56115-0 ; A novel series of thalidomide derivatives (4a-f) designed by molecular hybridization were synthesized and evaluated in vitro and in vivo for their potential use in the oral treatment of sickle cell disease symptoms. Compounds 4a-f demonstrated analgesic, anti-inflammatory, and NO-donor properties. Compounds 4c and 4d were considered promising candidate drugs and were further evaluated in transgenic sickle cell mice to determine their capacity to reduce the levels of the proinflammatory cytokine tumor necrosis factor alpha (TNF alpha). Unlike hydroxyurea, the compounds reduced the concentrations of TNF alpha to levels similar to those induced with the control dexamethasone (300 mu mol/kg). These compounds are novel lead drug candidates with multiple beneficial actions in the treatment of sickle cell disease symptoms and offer an alternative to hydroxyurea treatment. |
| نوع الوثيقة: | article in journal/newspaper |
| وصف الملف: | 5811-5819 |
| اللغة: | English |
| ردمك: | 978-973-43-3360-8 973-43-3360-7 |
| تدمد: | 0022-2623 |
| Relation: | Journal of Medicinal Chemistry; 6.253; 2,567; http://dx.doi.org/10.1021/jm200531f; Journal of Medicinal Chemistry. Washington: Amer Chemical Soc, v. 54, n. 16, p. 5811-5819, 2011.; http://hdl.handle.net/11449/7800; WOS:000294077300014; 9734333607975413; orcid:0000-0003-4141-0455 |
| DOI: | 10.1021/jm200531f |
| الاتاحة: | http://hdl.handle.net/11449/7800 https://doi.org/10.1021/jm200531f |
| Rights: | closedAccess |
| رقم الانضمام: | edsbas.A4CB41E8 |
| قاعدة البيانات: | BASE |
| ردمك: | 9789734333608 9734333607 |
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| تدمد: | 00222623 |
| DOI: | 10.1021/jm200531f |