Design, synthesis and biological evaluation of AT1 receptor blockers derived from 6-substituted aminocarbonyl benzimidazoles.

A series of new 6-substituted aminocarbonyl benzimidazole derivatives with 1, 4-disubsituted or 1, 5-disubsituted indole moiety and benzoic acid moiety were designed, synthesized and pharmacologically evaluated. Most of the synthesized compounds could bind to the AT1 receptor and decrease blood pressure significantly. Notably, 2e and 1h could obviously decrease MBP in a dose dependent manner. The maximal response lowered 57.9 ±â€¯2.3 mmHg (2e) and 57.6 ±â€¯1.9 mmHg (1h) of MBP at 10 mg/kg after oral administration, and the antihypertensive effect lasted beyond 24 h, which performed better than Losartan (Fig. 1). These results indicate that 2e and 1h are effective and long-lasting anti-hypertension drug candidates and deserve further investigation for therapeutic application.

Outcomes of Bone Marrow Mononuclear Cell Transplantation for Neurological Sequelae Due to Intracranial Hemorrhage Incidence in the Neonatal Period: Report of Four Cases.

Aim: The aim of this study was to present primary outcomes of autologous bone marrow mononuclear cell (BMMNC) transplantation to improve neurological sequelae in four children with intracranial hemorrhage (ICH) incidence during the neonatal period. Methods: GMFM88 and modified Ashworth score were used to assess motor function and muscle spasticity before BMMNC transplantation and after transplantation. Brain MRI was performed to evaluate brain morphology before and after BMMNC transplantation. Bone marrow were harvested from anterior iliac crest puncture and BMMNCs were isolated using Ficoll gradient centrifugation. The microbiological testing, cell counting, and hematopoietic stem cell (hHSC CD34+ cell) analysis were performed, following which BMMNCs were infused intrathecally. Results: Improvement in motor function was observed in all patients after transplantation. In addition, muscle spasticity was reduced in all four patients. Conclusion: Autologous BMMNC transplantation may improve motor function and reduce muscle spasticity in children with ICH incidence during the neonatal period.