Scaffold hopping and structure-based drug design were employed to identify substituted 4-aminoquinolines and 4-aminonaphthyridines as potent, small molecule inhibitors of tumor necrosis factor alpha (TNFα). Structure-activity relationships in both the quinoline and naphthyridine series leading to the identification of compound with excellent potency and pharmacokinetic profile are discussed. X-ray co-crystal structure analysis and ultracentrifugation experiments clearly demonstrate that these inhibitors distort the TNFα trimer upon binding, leading to aberrant signaling when the trimer binds to TNF receptor 1 (TNFR1).
View Article and Find Full Text PDFBackground: Hypertension is a challenging public health problem with a huge burden in the developing countries. Non-adherence to antihypertensive treatment is a big obstacle in blood pressure (BP) control and favours disease progression to complications. Our objectives were to determine the rate of non-adherence to antihypertensive pharmacotherapy, investigate factors associated with non-adherence, and to assess the association between non-adherence and BP control in the Buea Health District (BHD), Cameroon.
View Article and Find Full Text PDFBackground: Pulmonary hypertension (PH) is a potent cause of heart failure and has been little investigated in the African setting.
Objective: To investigate the effects of gender on the clinical presentation, echocardiographic features and outcomes of patients with PH in Douala, Cameroon.
Methods: A prospective cohort study was conducted from March 2012 to December 2013 as part of the Pan African Pulmonary Hypertension Cohort study.
Introduction: The prevalence of hypertension has continued to increase and is now a great burden for health care providers. Obtaining information on the factors affecting compliance to antihypertensive drugs is thus important. The aim of this study was to assess knowledge of hypertension and to determine factors affecting the compliance of hypertensive patients to their antihypertensive drugs.
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