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.

Brain Injury Lesion Imaging Using Preconditioned Quantitative Susceptibility Mapping without Skull Stripping.

BACKGROUND AND PURPOSE: Identifying cerebral microhemorrhage burden can aid in the diagnosis and management of traumatic brain injury, stroke, hypertension, and cerebral amyloid angiopathy. MR imaging susceptibility-based methods are more sensitive than CT for detecting cerebral microhemorrhage, but methods other than quantitative susceptibility mapping provide results that vary with field strength and TE, require additional phase maps to distinguish blood from calcification, and depict cerebral microhemorrhages as bloom artifacts. Quantitative susceptibility mapping provides universal quantification of tissue magnetic property without these constraints but traditionally requires a mask generated by skull-stripping, which can pose challenges at tissue interphases. We evaluated the preconditioned quantitative susceptibility mapping MR imaging method, which does not require skull-stripping, for improved depiction of brain parenchyma and pathology. MATERIALS AND METHODS: Fifty-six subjects underwent brain MR imaging with a 3D multiecho gradient recalled echo acquisition. Mask-based quantitative susceptibility mapping images were created using a commonly used mask-based quantitative susceptibility mapping method, and preconditioned quantitative susceptibility images were made using precondition-based total field inversion. All images were reviewed by a neuroradiologist and a radiology resident. RESULTS: Ten subjects (18%), all with traumatic brain injury, demonstrated blood products on 3D gradient recalled echo imaging. All lesions were visible on preconditioned quantitative susceptibility mapping, while 6 were not visible on mask-based quantitative susceptibility mapping. Thirty-one subjects (55%) demonstrated brain parenchyma and/or lesions that were visible on preconditioned quantitative susceptibility mapping but not on mask-based quantitative susceptibility mapping. Six subjects (11%) demonstrated pons artifacts on preconditioned quantitative susceptibility mapping and mask-based quantitative susceptibility mapping; they were worse on preconditioned quantitative susceptibility mapping. CONCLUSIONS: Preconditioned quantitative susceptibility mapping MR imaging can bring the benefits of quantitative susceptibility mapping imaging to clinical practice without the limitations of mask-based quantitative susceptibility mapping, especially for evaluating cerebral microhemorrhage-associated pathologies, such as traumatic brain injury.

Gender Differences in Perceived Social Support and Stressful Life Events in Depressed Patients.

OBJECTIVE: To study the gender differences in perceived social support and life events in patients with depression. METHODS: A total of 118 patients aged 18 to 60 years, with depressive disorder according to the DSM-IV-TR, were evaluated using the Multidimensional Scale of Perceived Social Support and Presumptive Stressful Life Events Scale. RESULTS: The perceived social support score was significantly higher in males than females (p < 0.001). Males perceived significantly higher social support from friends than females (p < 0.001), whereas support from significant others was higher in females. There was a higher mean number of total life events as well as specific type of life events in males that became apparent after controlling for education (p < 0.05). Financial loss or problems was the most commonly reported life event in both males and females. Work-related problems were more commonly reported by males, whereas family and marital conflict were more frequently reported by females. CONCLUSION: Perceived social support and stressful life events were higher in males with depression than females.

Improved T2* imaging without increase in scan time: SWI processing of 2D gradient echo.

BACKGROUND AND PURPOSE: 2D gradient-echo imaging is sensitive to T2* lesions (hemorrhages, mineralization, and vascular lesions), and susceptibility-weighted imaging is even more sensitive, but at the cost of additional scan time (SWI: 5-10 minutes; 2D gradient-echo: 2 minutes). The long acquisition time of SWI may pose challenges in motion-prone patients. We hypothesized that 2D SWI/phase unwrapped images processed from 2D gradient-echo imaging could improve T2* lesion detection. MATERIALS AND METHODS: 2D gradient-echo brain images of 50 consecutive pediatric patients (mean age, 8 years) acquired at 3T were retrospectively processed to generate 2D SWI/phase unwrapped images. The 2D gradient-echo and 2D SWI/phase unwrapped images were compared for various imaging parameters and were scored in a blinded fashion. RESULTS: Of 50 patients, 2D gradient-echo imaging detected T2* lesions in 29 patients and had normal findings in 21 patients. 2D SWI was more sensitive than standard 2D gradient-echo imaging in detecting T2* lesions (P < .0001). 2D SWI/phase unwrapped imaging also improved delineation of normal venous structures and nonpathologic calcifications and helped distinguish calcifications from hemorrhage. A few pitfalls of 2D SWI/phase unwrapped imaging were noted, including worsened motion and dental artifacts and challenges in detecting T2* lesions adjacent to calvaria or robust deoxygenated veins. CONCLUSIONS: 2D SWI and associated phase unwrapped images processed from standard 2D gradient-echo images were more sensitive in detecting T2* lesions and delineating normal venous structures and nonpathologic mineralization, and they also helped distinguish calcification at no additional scan time. SWI processing of 2D gradient-echo images may be a useful adjunct in cases in which longer scan times of 3D SWI are difficult to implement.

Reinvestigating 2,5-di(pyridin-2-yl)pyrazine ruthenium complexes: selective deuteration and Raman spectroscopy as tools to probe ground and excited-state electronic structure in homo- and heterobimetallic complexes.

The mono- (1) and dinuclear (2) ruthenium(II) bis(2,2'-bipyridine) complexes of 2,5-di(pyridin-2-yl)pyrazine (2,5-dpp), for which the UV/Vis absorption and emission as well as electrochemical properties have been described earlier, are reinvestigated here by resonance, surface enhanced and transient resonance Raman spectroscopy together with selective deuteration to determine the location of the lowest lying excited metal to ligand charge transfer ((3)MLCT) states. The ground state absorption spectrum of both the mono- and dinuclear complexes are characterised by resonance Raman spectroscopy. The effect of deuteration on emission lifetimes together with the absence of characteristic bipy anion radical modes in the transient Raman spectra for both the mono- and dinuclear complexes bridged by the 2,5-dpp ligand confirms that the excited state is 2,5-dpp based; however DFT calculations and the effect of deuteration on emission lifetimes indicate that the bipy based MLCT states contribute to excited state deactivation. Resonance Raman and surface enhanced Raman spectroscopic (SERS) data for 1 and 2 are compared with that of the heterobimetallic complexes [Ru(bipy)(2)(2,5-dpp)PdCl(2)](2+)3 and [Ru(bipy)(2)(2,5-dpp)PtCl(2)](2+)4. The SERS data for 1 indicates that a heterobimetallic Ru-Au complex forms in situ upon addition of 1 to a gold colloid.

Drug resistance in Mycobacterium tuberculosis isolates from tuberculosis patients in Kerala, India.

OBJECTIVE: To analyse the extent of drug resistance in clinical isolates of Mycobacterium tuberculosis from patients attending various tuberculosis (TB) clinics in Kerala, India. DESIGN: Mycobacteria were isolated from sputum samples of TB patients. Isolates from 92 new and 104 retreatment cases were tested for resistance to four first-line drugs (isoniazid, rifampicin, ethambutol and streptomycin). RESULTS: Twenty-three per cent of the isolates from new cases and 14% from retreatment cases were pan-susceptible, and the rest were resistant to at least one of the drugs. Multidrug-resistant isolates accounted for 5.4% among new cases and 16.4% among retreatment cases. It should be noted that 18.5% of the isolates were mycobacteria other than tuberculosis. CONCLUSION: There is an urgent need for statewide surveys to assess the level of drug resistance using quality-assured culture and drug susceptibility services. Considering that the Revised National TB Control Programme in India has been made operational nationwide, this kind of screening should be made mandatory under the programme to effectively control the spread of TB.

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.

The Dynamic Aviation Data System (DADS).

This paper proposes The Dynamic Aviation Data System (DADS), which integrates a variety of existing information sources regarding flight to serve as a tool to pilots in dealing with the challenges of flight. The system is composed of three main parts: a pilot's history on disk; a system that can read proposed flight plans and make suggestions based upon Geographical Information Systems, weather, aircraft, and case report databases that exist throughout North America; and a small hand-held computer that interfaces with the aircraft's instruments and that can be brought into the cockpit to aid the pilot before and during flight. The system is based upon technology that currently exists and information that is already regularly collected. While many issues regarding implementation and cost efficiency of the system need to be addressed, the system shows promise in its ability to make useful flight safety information available to all pilots in order to save lives.

MECKEL'S DIVERTICULUM - REVISITED.

Twenty five cases of Meckel's diverticulum were studied between 1985-1995. Eight of these were symptomatic and in the remaining 17 it was an incidental finding. The symptomatic patients presented with intestinal obstruction (5 cases), perforated peritonitis (2 cases) and intussusception (1 case). All cases of acute appendicitis were also subjected to a search for Meckel's diverticulum. Of the 25 Meckel's diverticuli encountered, 22 were resected and in 3 patients it was left in situ. Both the patients with perforated Meckel's diverticulum showed ectopic gastric mucosa. Complications occurred only after surgery for symptomatic Meckel's diverticulum. All patients undergoing incidental diverticulectomy had a smooth and uncomplicated recovery.

A study on cancer mortality in Tarapur-based atomic energy community.

Cancer mortality risks for individuals who were employed at nuclear facilities in Tarapur and for their respective family members with whom they lived were examined. Cancer deaths that occurred in this population between 1971 and 1988 were compared with death rates published by the Bombay City Cancer Registry. Risks were expressed as standardized mortality ratios (SMRs), which were computed by dividing the observed number of deaths by the expected number of deaths and multiplying this value times 100. There were 11 deaths from cancer among the employees, and this figure was too small to permit any trend analysis with respect to radiation exposures. The SMRs for all cancers and leukemia for male employees and for middle-aged male family members who were not exposed to any radiation were not statistically significant. A much larger database of person years at risk would be required to reach definite conclusions. The combined cancer risks for employees and families combined were similar to risks experienced by individuals in Bombay.

A cancer mortality study in Bombay-based atomic energy community: 1975-1987.

Cancer deaths recorded by the centralised health services of the Department of Atomic Energy (DAE) among its employees and their families stationed in Bombay during 1975-1987 have been analysed. Expected number of deaths due to cancer in the study group has been estimated by using the age-sex-specific cancer death rates reported for Bombay resident population for the year 1983. The size of the database for the entire DAE community is about 702,000 person years and the number of cancer deaths observed in 154. Analysis has been done separately for employees and their families, individually for important groups of cancer sites such as respiratory organs, digestive organs, breast, genito-urinary organs and lymphatic and haematopoietic systems. The standardised mortality ratios are generally lower than 100, which may partly be due to the 'healthy worker effect' in the DAE community and partly because of its differences in the social class distribution and the concomitant differences in lifestyle with respect to the comparison group of Bombay city.

Non-Hodgkin's lymphoma of prostate: a rare site of primary extranodal presentation (a report of two cases).

We report two cases of primary extranodal lymphoma of the prostate, an unusual site for extranodal presentation. The clinical presentation and treatment is discussed.

A sensitive method for the determination of Th in body fluids.

A method involving neutron activation followed by simple radiochemical separation was developed and applied to determine the concentrations of Th in blood serum and urine. The method is sufficiently sensitive to detect 0.025 ng of 232Th. The average concentration of Th found in the blood serum and urine of subjects from normal environments is 7.9 ng L-1 and 2.7 ng L-1, respectively.

Measurement of 14C emission rates from a pressurised heavy water reactor.

Carbon-14 is produced in pressurised heavy water reactors (PHWR), mainly as an activation product in the fuel. It is also produced in the heavy water used as the primary coolant and moderator, and is produced in the air in the annular space between the pressure tube and calandria tubes as well as in the free space in the calandria vault. The production rates in different systems of a PHWR are calculated on the basis of design parameters. During a period of 3 y, 14C released through the gaseous route has been measured at Rajasthan Atomic Power Station, Kota, India, a PHWR unit. These releases have been found to be mainly 14CO2. This reduced form of 14C is less than 5% of the releases. The normalised releases of 14C have a geometric mean of 5.17 TBq GWe-1 y-1 and a geometric standard deviation of 1.52. The 14C present in the form of carbonates in liquid effluents has also been measured and is 0.14% of the gaseous releases.

Environmental radiation and cancer in India.

The hormesis hypothesis, which suggests that ecologically realistic low levels of ionising radiations may be beneficial to humans, seems to be substantiated significantly by the data available on cancer incidence/mortality rates and environmental radiation levels in various cities and states of India. Where the radiation level is greater, cancer risk is invariably less. The annual cancer incidence rate (per 100,000 population) seems to decrease by 0.03/microSv increase in the external background radiation dose from a hypothetical incidence level of 79 per 100,000 corresponding to "zero environmental radiation".