Synthesis of barbituric acid derivatives using microwave irradiation method and in vitro evaluation of antimicrobial and cytotoxic activity.

The research work was involved in rapid and efficient procedure for the attachment of barbituric acid with arylidene acetophenone under microwave irradiation (MWI) and conventional heating. The result showed that the time was reduced from the conventional 24 hours to 5-10 minutes. In conventional heating, the yield of the compounds 2a-2e were very poor (75-81%), but in MW methods the yields were observed 96.48-98% which was comparatively too high. The structures of the compounds were characterized by FT-IR, 1H-NMR spectral data. The antimicrobial and cytotoxic activities of the synthesized compounds were also investigated. Staphylococcus aureus, Bacillus megaterium, Escherichia coli and Pseudomonas aeruginosa revealed the zone of inhibition were 6-12 mm where sample concentration was 100 μg/disc. However, cytotoxic analysis, the mortality 47-95% were appeared when sample concentration were 0.78-25 (μg/ml) and more than 50 (μg/ml) concentration showed 100% mortality. The presence of a reactive and unsaturated ketone function in synthesized compounds was found to be responsible for their potential antimicrobial and cytotoxic activity.

Role of norepinephrine & angiotensin II in the neural control of renal sodium & water handling in spontaneously hypertensive rats.

Background & objectives: A wealth of information concerning the essential role of renal sympathetic nerve activity (RSNA) in the regulation of renal function and mean arterial blood pressure homeostasis has been established. However, many important parameters with which RSNA interacts are yet to be explicitly characterized. Therefore, the present study aimed to investigate the impact of acute renal denervation (ARD) on sodium and water excretory responses to intravenous (iv) infusions of either norepinephrine (NE) or angiotensin II (Ang II) in anaesthetized spontaneously hypertensive rats (SHR). Methods: Anaesthetized SHR were acutely denervated and a continuous iv infusion of NE (200 ng/min/kg) or Ang II (50 ng/min/kg) was instigated for 1 h. Three 20-min urine clearances were subsequently collected to measure urine flow rate (UV) and absolute sodium excretion (UNaV). Results: Higher UV and UNaV (P<0.05) were observed in denervated control SHR as compared to innervated counterparts. The administration of NE or Ang II to innervated SHR produced lower UV and UNaV (P<0.05 vs. innervated control SHR). Lower diuresis/natriuresis response to ARD was observed in NE-treated SHR compared to denervated control SHR (P<0.05). Salt and water excretions in denervated NE-treated SHR, however, were significantly higher (P<0.05) relative to the excretion levels in control denervated SHR. Conversely, there was a higher (all P<0.05) diuresis/natriuresis response to ARD when Ang II was administered to SHR compared to denervated control or innervated Ang II-treated SHR. Interpretation & conclusions: NE retains its characteristic antidiuretic/antinatriuretic action following ARD in SHR. Typical action of Ang II on salt and water excretions necessitates the presence of an intact renal innervation. Ang II is likely to facilitate the release of NE from renal sympathetic nerve terminals through a presynaptic site of action. Moreover, there is a lack of an immediate enhancement in the renal sensitivity to the actions of NE and Ang II following ARD in a rat model of essential hypertension.