New peptide derived antimalaria and antimicrobial agents bearing sulphonamide moiety.

Fourteen novel dipeptide carboxamide derivatives bearing benzensulphonamoyl propanamide were synthesized and characterized using 1H NMR, 13C NMR, FTIR and MS spectroscopic techniques. In vivo antimalarial and in vitro antimicrobial studies were carried out on these synthesized compounds. Molecular docking, haematological analysis, liver and kidney function tests were also evaluated to assess the effect of the compounds on the organs. At 200 mg/kg body weight, 7i inhibited the multiplication of the parasite by 81.38% on day 12 of post-treatment exposure. This was comparable to the 82.34% reduction with artemisinin. The minimum inhibitory concentration (MIC) in µM ranged from 0.03 to 2.34 with 7h having MIC of 0.03 µM against Plasmodium falciparium. The in vitro antibacterial activity of the compounds against some clinically isolated bacteria strains showed varied activities with some of the new compounds showing better activities against the bacteria and the fungi more than the reference drug ciprofloxacin and fluconazole.

Coronary calcification and cardiac events after percutaneous intervention in dialysis patients.

BACKGROUND: Previous studies have described increased vascular calcification in renal dialysis patients. The clinical significance of this finding with respect to outcomes after percutaneous coronary intervention in this population is unknown. METHODS: We analysed a prospective interventional database at a single tertiary center and identified 41 dialysis patients who underwent coronary angioplasty. All studies were reviewed for the presence of coronary calcium in the target and reference vessels and compared with respect to baseline clinical factors and cardiovascular outcomes. RESULTS: The mean ages for those with and without coronary calcification were 63.6 +/- 11.0 and 67.3 +/- 11.0, respectively, P = 0.30. The groups were similar in years on dialysis, diabetes, hypertension, smoking, and measures of calcium and phosphate balance. The total cholesterol, LDL-C, HDL-C, and triglycerides were 162.5 +/- 42.3 and 202.0 +/- 54.5, P = 0.02; 94.9 +/- 39.6 and 121.2 +/- 48.1, P = 0.18; 39.3 +/- 12.4 and 47.3 +/- 12.2, P = 0.15; 157.4 +/- 100.4 and 181.3 +/- 187.4, P = 0.15, for those with and without calcification, respectively. The composite of target vessel revascularization, myocardial infarction, or death was 47.4% and 77.3% for those with and without calcification, respectively, P = 0.06. The Cox proportional hazards model, controlling for years on dialysis, showed a significant, event-free survival in those with coronary calcium seen fluoroscopically, P = 0.05. CONCLUSIONS: In dialysis patients, coronary calcification identified in the target or reference vessels is associated with lower total cholesterol and favourable interventional outcomes.

Determinants of mortality after myocardial infarction in patients with advanced renal dysfunction.

Previous studies using administrative data have shown high mortality in patients with renal failure requiring dialysis after acute myocardial infarction (AMI). There has been little investigation into the mortality after AMI in those with advanced renal disease who are not on dialysis therapy. We analyzed a prospective coronary care unit registry of 1,724 patients with ST segment elevation myocardial infarction admitted over an 8-year period at a single tertiary-care center. Those not on chronic dialysis therapy were stratified into groups based on corrected creatinine clearance, with cutoff values of 46.2, 63.1, and 81.5 mL/min/72 kg. Dialysis patients (n = 47) were considered as a fifth comparison group. Older age, black race, diabetes, hypertension, previous coronary disease, and heart failure were incrementally more common across increasing renal dysfunction strata. There were also graded increases in the relative risk for atrial and ventricular arrhythmias, heart block, asystole, development of pulmonary congestion, acute mitral regurgitation, and cardiogenic shock. Primary angioplasty, thrombolysis, and beta-blockers were used less often across the risk strata (P < 0.0001 for all trends). There was an early mortality hazard (age-adjusted relative risk, 8.76; P < 0.0001) for those with renal dysfunction but not on dialysis therapy for the first 60 months, followed by graded decrements in survival across increasing renal dysfunction strata. The excess mortality in this population appears to be mediated through arrhythmias, adverse hemodynamic events, and the lower use of mortality-reducing therapy.

Risks associated with renal dysfunction in patients in the coronary care unit.

OBJECTIVES: The purpose of this study was to quantify the impact of baseline renal dysfunction on morbidity and mortality in patients in the coronary care unit (CCU). BACKGROUND: The presence of renal dysfunction is an established independent predictor of survival after acute myocardial infarction and revascularization procedures. METHODS: We analyzed a prospective CCU registry of 12,648 admissions by 9,557 patients over eight years at a single, tertiary center. Admission serum creatinine was available in 9,544 patients. Those not on long-term dialysis were classified into quartiles of corrected creatinine clearance, with cut-points of 46.2, 63.1 and 81.5 ml/min per 72 kg. Dialysis patients (n = 527) were considered as a fifth comparison group. RESULTS: Baseline characteristics, including older age, African-American race, diabetes, hypertension, previous coronary disease and heart failure, were incrementally more common across increasing renal dysfunction strata. There were graded increases in the relative risk for atrial and ventricular arrhythmias, heart block, asystole, development of pulmonary congestion, acute mitral regurgitation and cardiogenic shock across the risk strata. Survival analysis demonstrated an early mortality hazard for those with renal dysfunction, but not on dialysis, for the first 60 months, followed by graded decrements in survival across increasing renal dysfunction strata. CONCLUSIONS: Baseline renal function is a powerful predictor of short- and long-term events in the CCU population. There is an early hazard for in-hospital and postdischarge mortality for those with a corrected creatinine clearance <46.2 ml/min per kg, but not on dialysis.