Design and Synthesis of Novel Fluorescent 2-(aryloxy)-3-(4,5-diaryl)-1H-imidazol-2-yl)quinolines: Solvatochromic, DFT, TD-DFT Studies, COX-1 and COX-2 Inhibition and Antioxidant Properties.

The present work focuses on the synthesis of novel heterocycles 2-(aryloxy)-3-(4,5-diaryl-1H-imidazol-2-yl)quinolines (6k-v) by an effective condensation reaction. These molecules exhibited fluorescent properties and hence for the proper understanding of their optical behavior and quantum yields, solvatochromic studies have been carried out. Further, frontier molecular orbitals, molecular electrostatic potential (MEP), and geometrical structure optimization have been investigated using the B3LYP/6-311G ++ (d, p) method. The energy gap between the HOMO, LUMO of the optical and energy band gap is determined by DFT and UV-visible spectra for TD-DFT studies are done. The screening of these compounds for in vitro COX-1 and COX-2 inhibition and DPPH free radical scavenging ability assays produced promising results. The binding interactions of these molecules against the COX-2 enzyme (PDB: 5IKR) were validated by docking studies.

Exploration of Coumarin Derivative: Experimental and Computational Modeling for Dipole Moment Estimation and Thermal Sensing Application.

The Optical properties of the FBTC (1-((4-((5-chlorobenzo[d]oxazol-2-ylthio)methyl)-1H-1,2,3-triazol-1-yl)methyl)-3H-benzo[f]chromen-3-one) molecule were studied experimentally and theoretically. The spectra of absorption and fluorescence were recorded in various solvents to explore their Solvatochromic behavior and dipole moment at room temperature. To determine the ground and excited state of dipole moment experimentally and theoretically, we employed different Solvatochromic techniques, including microscopic solvent polarity functions developed by Lippert, Bakhshiev, Kawaski-Chamma-Viallet, and Reichardt's, as well as density functional theory (DFT) and time-dependent density functional theory (TD-DFT) methods. The stability of the excited state dipole moment in FBTC is higher. Using prime functional, FBTC was optimized in its ground state, and its HOMO (Highest Occupied Molecular Orbital) and LUMO (Lowest Unoccupied Molecular Orbital), energies were estimated. These values were then compared with those obtained through cyclic voltammetry. Based on the HOMO and LUMO values given, we calculated the global reactivity parameter and energy gap, which was found to be low at 3.77 eV. This study also includes an estimation of electron absorption energies and oscillator strength. Natural population analysis (NPA), Milliken atomic charge, and molecular electrostatic potential (MESP) map are correlated. In addition, FBTC exhibited exceptional physiological temperature sensing behaviour from 20 °C -65 °C with high relative sensitivity and firm stability. Hence these results confirm that FBTC is a potential candidate for photonic devices and it's also applicable in optical temperature sensing.

Experimental and Theoretical Spectroscopic Investigation on Coumarin Based Derivatives for Non-Linear Optoelectronics Application.

The spectral properties of MBTC (4-((4-((Benzo[d]oxazol-2-ylthio)methyl)-1H-1,2,3-triazol-1-yl)methyl)-7-methoxy-2H-chromen-2-one), CBTC (4-((4(((5Chlorobenzo[d]oxazol-2-yl)thio)methyl)-1H-1,2,3-triazol-1-yl)methyl)-2H-benzo[h]chromen-2-one) and TBTC (4-((4-((Benzo[d]oxazol-2-ylthio)methyl)-1H-1,2,3-triazol-1-yl)methyl)6(tertbutyl)2Hchromen-2-one) were studied in series of solvents with different polarity at room temperature to explore their solvatochromic effect and dipole moment. Stokes shift revealed a bathochromic shift with varying solvent polarity for all molecules which implies π-π*transition. The ground state and excited state dipole moment of the molecules are calculated experimentally using salvatochromic methods like Lippert-Mataga, Bakhshiev, Kawaski-chamma-viallet, and Reichardt's microscopic solvent polarity functions and computationally by density functional theory (DFT) method. It is observed that the excited state dipole moment is higher than the ground state so synthesized molecules are more polar in the excited state than in the ground state. Using the DFT method HOMO and LUMO energy values were obtained and compared with values obtained by the cyclic voltammetry. Using the values of HOMO (highest occupied molecular orbital) and LUMO (lowest unoccupied molecular orbital) we have estimated energy gap, chemical hardness (ɳ), chemical softness (s), ionization potential (IP), electron affinity (EA), electronegativity (χ), electrophilicity (ω), and chemical potential (µ) of the molecules were estimated. The energy gap of MBTC, CBTC, and TBTC were found to be low, that is 3.861 eV, 3.822 eV, and 3.801 eV respectively, this indicates molecules are more reactive and it has the easiest π-π* transition. Further electrophilic and nucleophilic sites were figured out using molecular electrostatic potential (MESP) which is useful in photochemical reactions. Hence the quantum chemical calculation and spectroscopic properties of the molecules can give a better understanding of their use in an optoelectronic device.

Staying Safe from Radiation Exposure in Cath Lab: A Review.

A successful cardiac catheterization Laboratory radiation safety program must manage patient and staff safety by reducing exposure to ionizing radiation to a level that is as low as reasonably achievable (ALARA). The first step in radiation safety is to avoid unnecessary use of ionizing radiation by justification of exposure, one of the basic principles of radiation protection. All individuals involved in fluoroscopic imaging procedures should familiarize themselves to the measures to protect themselves from exposure to unsafe doses of ionizing radiation.

Study of Angiographic Relationship between Peripheral Arterial Diseases with the Involvement of Specific Coronary Artery Lesion.

The purpose of this study was to investigate magnitude, pattern and involvement of previously unheralded coronary artery disease in patients suffering from clinically significant peripheral artery disease of lower limbs. This cross sectional study was carried out in National Institute of Cardiovascular Diseases, Dhaka, Bangladesh from January 2014 to February 2015. Total 58 patients with clinically diagnosed peripheral arterial disease of lower limb undergoing angiographic evaluation. Selective CAG in addition to peripheral arteriography was performed in all the study population as per ACC/AHA guidelines for CAG (class IIa recommendation).In this study, it was documented that the proportion of coronary arterial disease was highest in LAD (63.9%) followed by LCX (55.6%), RCA (52.8%), and lowest LM (11.1%) in lesion with aorto-iliac segment. But the proportion of coronary arterial disease was highest in LCX (41.9%) followed by LAD (38.7%), RCA (35.5%), and lowest LM (12.9%) in lesion with femero-popliteal blood vessels. Similarly, the proportion of coronary arterial disease was highest in LCX (36.4%) followed by RCA (27.3%) and equal percentage in LAD and lowest in LM (9.1%) in tibioperoneal segment. Patients of peripheral arterial disease (PAD) having no symptoms of coronary artery disease (CAD) are more likely to have severe coronary artery involvement. Coronary angiogram should be done in patient with PAD to detect previously undetected CAD and pattern of PAD reflects the severity and involvement of coronary arteries.

Granulomatosis with Polyangiitis (Wegener Granulomatosis) with Unusual Presentation.

We came across a 32 years old male admitted in our hospital with prolonged low-grade fever, haemoptysis, leg swelling, weight loss, purpuric rashes and malaena. He received anti-TB treatment at another hospital without any improvement. He was pale with bullous and purpuric lesions over legs and feet. He also had features of consolidation over both lung fields. His CRP was 312mg/L, Urine R/M/E showed 40-50 RBC/HPF, Chest X-ray showed features of bilateral consolidation, c-ANCA-10U/L (positive); Tracheal aspirate for AFB was found to be negative. We diagnosed the case as Granulomatosis with Polyangitis (WG) and started treatment with steroid and cyclophosphamide. But the patient could not be saved probably due to delay in starting management.

Longitudinal Stent-Shortening during Percutaneous Transluminal Angioplasty with Stenting of Right Superficial Femoral Artery: A Case Report.

Longitudinal stent deformation (LSD) involving coronary arteries during PCI have been reported in several literatures. But, LSD occurring during PTA (Percutaneous Transluminal Angioplasty) involving peripheral arteries is rare. We had such a case who presented with coronary and peripheral artery disease. Longitudinal stent deformation occurred during PTA with stenting of right superficial femoral artery (SFA). For CAD, PCI to RCA and LAD was done beforehand and the peripheral procedure was done 4 days later to avoid increased contrast load. Due to LSD occurring during PTA to Rt. SFA, we had to deploy another stent to cover the lesion over that artery. There was no technical fault or difficulty during negotiating the stent and positioning it covering the lesion. So, we did not find any obvious reason for this complication. Since longitudinal stent deformation is uncommon during PCI of coronary arteries and probably rare during PTA of peripheral arteries and we did not find any literature regarding this, we decided to report this case.

Transient Loss of Vision after Coronary Angiogram - A Case Report.

A 50-year old, diabetic, hypertensive patient with post-CABG status developed complete loss of vision about one hour after coronary angiogram (CAG). Thorough ophthalmological and neurological examination as well as magnetic resonance imaging of brain especially of the occipital region revealed no abnormality. The patient had complete recovery of vision about 48 hours later. We could not document any specific cause or mechanism for the visual loss, although the selective vulnerability of occipital lobes to contrast agent toxicity (Cortical blindness) was the most likely underlying mechanism.

Resistant hypertension - an update.

Patients with hypertension are increasing in Bangladesh. Among these patients a growing number of patients are having resistant hypertension faced by both primary care physicians and specialists. There is no data regarding prevalence of resistant hypertension in Bangladesh, but clinical trials abroad suggests that it is not rare, involving perhaps 20% to 30% of study participants. Cardiovascular risk is undoubtedly increased in such patients and the condition is often complicated by multiple other cardiovascular risk factors such as obesity, sleep apnea, diabetes, and chronic kidney disease. Resistant hypertension is almost always multifactorial in etiology. Successful treatment requires identification and reversal of lifestyle factors contributing to treatment resistance; diagnosis and appropriate treatment of secondary causes of hypertension; and use of effective multi drug regimens. Studies of resistant hypertension are limited by the high cardiovascular risk of patients within this subgroup, which generally precludes safe withdrawal of medications; presence of multiple disease processes and their associated medical therapies, which confound interpretation of study results. Therefore we should concentrate on expanding our knowledge of the causes of resistant hypertension which will allow for more effective prevention and/or treatment which is essential to improve long-term clinical management of this condition.

Testicular tumour - a review article.

Painless scrotal masses must be investigated with ultrasound imaging and tumour marker assay before being treated with radical inguinal orchidectomy. For unknown reasons, the incidence of this cancer increased in Caucasian population. The incidence of testicular germ cell tumour has doubled in past 40 years. An annual increase of 3-6% is reported in Caucasian population. But the mortality rate has been stable or decreasing due to improvement in treatment. In the past, metastatic testicular cancer was usually fatal, but recent advances in treatment, including high-dose chemotherapy and stem cell rescue, have considerably improved the prognosis. Indeed, testicular cancer is a bright spot in the oncological landscape and is now considered the model for the treatment of solid tumors. We looked into the epidemiology, presentation, classification, work up, staging, various treatment modalities and prognosis of testicular tumour in this article.

In-hospital outcome of patients with acute STEMI with impaired renal function.

Effective risk stratification is integral to the management of patients with acute coronary syndromes. This prospective study was done to evaluate the association between on-admission renal function and in-hospital outcome of patients with acute ST segment elevation myocardial infarction (STEMI). This study was carried out in the department of cardiology, NICVD, Dhaka, Bangladesh during the period from January 2004 to December 2004. Total 90 patients with first episode of acute STEMI were grouped according to renal function. Group I patients had normal renal function and Group II patients had renal impairment. Among group I patients, only 3.7% had Killip class IV heart failure, whereas among group II patients, 19% had Killip class II and 6.3% had Killip class IV heart failure (p<0.001). Mean percent of LVEF was significantly higher in Group I patients (52.0±5.2 vs. 47.9±6.3, p<0.01). Ventricular tachycardia occurred in significantly higher proportion in group II patients (7.4% vs. 63.5%, p<0.001). It was concluded that some in-hospital complications of acute STEMI were significantly higher and others were more prevalent in patients who had associated renal impairment compared to those who had normal renal function. This study can develop a clinical prognostic tool, which is simple, cheap and easily be applied at bedside. Concentrating on aggressive management of such patients may reduce their morbidity and mortality.

Congenital aneurysm of the left atrium.

Isolated left atrial (LA) aneurysm is a rare condition, whereas LA aneurysm secondary to other causes is a fairly common condition. A case of large left atrial aneurysm presented with features of heart failure with cardiac arrhythmia and an abnormal cardiac silhouette on chest X-ray. A 14 years old girl presented with palpitation at rest, shortness of breath, productive cough and bilateral leg swelling for last 8 months. There was no history of chest pain, hemoptysis, syncope, prolonged fever, and rheumatic fever. She was mildly anemic, had raised JVP and mild bilateral pedal edema. There was left parasternal heave, soft S1, loud P2 and a pansystolic murmur of grade 3/6 over mitral area radiating to the left axilla. ECG showed multifocal atrial tachycardia (MAT), chest X-ray showed cardiomegaly with bulging of the left heart border with upper lobe diversion. Echo-Doppler study showed hugely dilated LA (115 mm in diameter), dilated left ventricle, Grade-2+ mitral regurgitation (MR), mild tricuspid regurgitation (TR) and mild pulmonary hypertension with normal appearing mitral, aortic and tricuspid and pulmonary valves. The patient was diagnosed as a case of congenital aneurysm of LA.

Involvement of glutathione in puberty and FSH release.

Administration of glutathione subcutaneously to immature female (age and weight matched) rats brings about a pre-ponement of puberty. A significant increase in pituitary, ovaries and uterine mass was observed in the experimental rats. Further, a considerable increase in pituitary FSH levels was also observed after intraventricular injection of glutathione in ovariectomized-steroid primed rats. Intraventricular administration of L-buthionine SR sulfoxamine produced a significant decrease in plasma FSH levels in intact male rats. These studies demonstrate the neuroendocrine role of glutathione on gonadotropins, specifically in relation to FSH release.

Altered intravenous pharmacokinetics of topotecan in rats with acute renal failure (ARF) induced by uranyl nitrate: do adenosine A1 antagonists (selective/non-selective) normalize the altered topotecan kinetics in ARF?

A series of exploratory investigations with multiple agents was carried out in normal rats and in rats with uranyl nitrate-induced acute renal failure to understand the disposition characteristics of intravenous topotecan (TPT) used as a model substrate. The disposition of TPT was unaltered in normal rats when treated with methotrexate, whereas treatment with probenecid increased the systemic exposure of TPT. In case of uranyl nitrate-induced acute renal failure (UN-ARF) rats, the systemic exposure of TPT was increased when compared with normal rats, whereas in UN-ARF rats treated with probenecid a further reduction in renal clearance of TPT was noted as compared with that of UN-ARF induced rats. Thus, TPT may be involved in the tubular secretory pathway when a passive glomerular filtration pathway for elimination was not possible. The disposition of TPT did not normalize in UN-ARF rats when treated with caffeine, a non-selective adenosine A1 receptor antagonist, whereas the selective adenosine A1 receptor antagonist (1,3-dipropyl-8-phenylxanthine, DPPX) normalized TPT pharmacokinetic disposition by improving renal function. Renal excretion studies demonstrated that CLR improved by almost fivefold following DPPX treatment in ARF rats. In addition, the qualitative stability/metabolism pattern of TPT in liver microsomes prepared from various groups of rats (normal rats, UN-ARF rats, rats treated with DPPX, and UN-ARF rats treated with DPPX) was found to be similar. In summary, using a pharmacokinetic tool as a surrogate, it has been shown that the pharmacokinetic disposition of TPT improved considerably upon treatment with DPPX, a selective adenosine A1 antagonist.

Acute and short-term effects of intraventricular injection of somatostatin and LHRH on glutamate and GABA levels in rat brain.

Glutamate and GABA content in different regions of adult female rat brain were determined at 10 and 30 min following intraventricular injection of LHRH or somatostatin. Cerebral cortex, cerebellar and hypothalamic glutamate levels were significantly elevated at 30 min following injection of 1 micrograms somatostatin, whereas hypothalamic glutamate levels were elevated at 10 min following a 0.5 micrograms dose. LHRH at a dose of 1 micrograms elevated cerebellar and brain stem glutamate levels at 10 and 30 min, whereas a 0.5 micrograms dose significantly elevated cerebral cortex, cerebellar and hypothalamic glutamate levels at 30 min. Third ventricular injection of 1 micrograms somatostatin produced a significant decrease in hypothalamic GABA levels at 10 and 30 min, whereas a 0.5-microgram dose decreased brain stem GABA levels at 10 min. LHRH at a dose of 0.1 microgram significantly increased cerebral cortex and cerebellar GABA levels at 10 min and brain stem GABA levels at 10 and 30 min following injection. Intraventricular injection of LHRH at a dose of 0.5 microgram significantly elevated cerebral cortex, cerebellar and brain stem GABA levels at 30 min. Hypothalamic GABA levels were elevated at 10 and 30 min following 0.5 and 1 microgram intraventricular LHRH injection. The implications of these results are discussed in relation to probable interaction between these neuroactive amino acids and neuropeptides in the rat brain.

Glutathione and gamma-glutamyl transpeptidase in the adult female rat brain after intraventricular injection of LHRH and somatostatin.

Glutathione content and glutamyl transpeptidase activity in different regions of adult female rat brain were determined at 10 and 30 min following intraventricular injection of LHRH and somatostatin. Hypothalamic glutathione levels were significantly elevated at 10 and 30 min after a single injection of a 0.1 micrograms dose of LHRH. On the contrary, glutathione levels significantly decreased in the hypothalamus, cerebral cortex and cerebellum at 10 and 30 min after 0.5 or 1 microgram dose. However, significant decrease in brain stem glutathione was evident at 30 min after 0.5 microgram and 10 min after the 1 microgram dose. Somatostatin at doses of 0.5 microgram and 1 microgram significantly decreased glutathione levels in all four brain regions both at 10 and 30 min following injection into the 3rd ventricle. Gamma-glutamyl transpeptidase activity in the hypothalamus and cerebral cortex was significantly elevated after intraventricular injection of LHRH. However, a significant increase in gamma-glutamyl transpeptidase activity in cerebellum and brain stem was seen only with 0.5 and 1 micrograms doses of LHRH. Somatostatin also significantly increased gamma-glutamyl transpeptidase activity in hypothalamus, cerebral cortex, brain stem and cerebellum. The decrease in glutathione levels with corresponding increase in gamma-glutamyl transpeptidase activity after intraventricular administration of LHRH and somatostatin suggests a possible interaction between glutathione and hypothalamic peptides.

Glutathione distribution in rat brain at different ages and the effect of intraventricular glutathione on gonadotropin levels in ovariectomized steroid-primed rats.

Glutathione levels were estimated in different regions of the brain of 21-, 30-, 40-, 42-, 45-day-old and adult female rats. Glutathione content in the cerebral cortex, cerebellum and the brain stem remained almost the same beginning from day 21 to sexually mature adult rats. There is a significant increase in hypothalamic glutathione content reaching a peak at puberty (42 days) and thereafter decreasing to the adult levels. Plasma gonadotropin levels were evaluated at 5 and 15 min after third ventricular injection of 15 and 30 microgram doses of glutathione in ovariectomized steroid-primed rats. Intraventricular injection of either 15 or 30 micrograms dose of glutathione significantly elevated plasma FSH levels. The 15 micrograms dose of glutathione significantly decreased plasma LH levels whereas 30 micrograms dose had no effect. Lower dose of glutathione inhibits LH release and stimulates FSH release whereas the higher dose of glutathione specifically elevates FSH levels without any change in LH levels suggesting a selective FSH releasing action of glutathione.

Intracellular content of thiol compounds, thiobarbituric acid reactive substances and gamma-glutamyl transpeptidase in rat brain during anoxia.

Intracellular thiol compounds like glutathione play an important role in scavenging free radicals. Free radical reactions occur in the respiratory chain, and free radicals are known to accumulate in hypoxia and ischaemia. The content of thiobarbituric acid (TBA) reactive substances, thiol and non-protein thiol (reduced glutathione) concentrations along with the activity of gamma-glutamyl transpeptidase (GGTP), a membrane enzyme, were estimated in three regions of the brain in rats exposed to anoxia. It was observed that no change occurred in the content of TBA-reactive substances in any one of the three brain regions, although a significant increase in the non-protein thiol concentration occurred uniformly during anoxia. A significant increase in GGTP occurred in all the three brain regions during anoxia. The increase in the activity of GGTP is suggestive of an alteration in the function of blood-brain barrier during anoxia. These results are suggestive of an absence of lipid peroxidative damage during anoxia.