New drug development in India

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Schiff’s base Fufural Phenylhydrazone as a Potential Corrosion Inhibitor for Mild Steel in Hydrochloric Acid Solution

Heterocyclic Schiff base furfural phenylhydrazone [FPH] was prepared and formulated as a corrosion inhibitor for mild steel in 2M hydrochloric acid solution. Mass change measurement and electrochemical methods adapted to study the effectiveness of the FPH during the corrosion process. FPH inhibitor protected 94.53 % corrosion of mild steel at optimum inhibitor strength of 0.0007 M at 303 ±1 K. Route of corrosion protection was interpreted through adsorption of FPH molecules on specimen surfaces in acid solution. Nature of the adsorption was established via Langmuir adsorption isotherm. Stability of the inhibitor was investigated with higher temperatures. Tafel polarization curves revealed, FPH molecules exhibit mixed nature of inhibitor. SEM and AFM images suggested that corroded specimen surface was severely affected in free acid comparatively in presence of FPH inhibitor. FT-IR analysis proved that, chemical interaction takes place between specimen surface atoms with FPH molecules and established chemical bond between them

Investigation of Laurus Tamala leaves extract as an environmentally acceptable corrosion inhibitor for soft steel in 1M HCl: Electrochemical, DFT, and surface characterization techniques

Laurus Tamala leaves extract (LTLE) has been employed as a soft steel corrosion inhibitor in a 1M Hydrochloric acid media. Chemical (weight loss) and electrochemical investigations were carried out to assess the corrosion rate and percentage inhibition efficiency of the extract. The electrochemical polarization results have demonstrated that plant leaves extract functions as a mixed type inhibitor. The stability of the inhibitor is tested at elevated temperatures by weight loss method. The corrosion inhibition mechanism is interpreted through adsorption mechanism, and the LTLE components has obeyed the Langmuir adsorption isotherm for soft steel. The interaction of the components of the extract is assessed through FT-IR technique. The surface morphology, roughness and hydrophobicity in presence and absence of the extract have been characterized through SEM, AFM and water contact angle techniques respectively. The highest inhibitory efficiency is 96.21% for 24 h as recorded by weight loss method. Additionally, the DFT computations has revealed the inhibitor’s adsorption through electron donor-acceptor interactions

Basic science232. Certolizumab pegol prevents pro-inflammatory alterations in endothelial cell function

Background: Cardiovascular disease is a major comorbidity of rheumatoid arthritis (RA) and a leading cause of death. Chronic systemic inflammation involving tumour necrosis factor alpha (TNF) could contribute to endothelial activation and atherogenesis. A number of anti-TNF therapies are in current use for the treatment of RA, including certolizumab pegol (CZP), (Cimzia ®; UCB, Belgium). Anti-TNF therapy has been associated with reduced clinical cardiovascular disease risk and ameliorated vascular function in RA patients. However, the specific effects of TNF inhibitors on endothelial cell function are largely unknown. Our aim was to investigate the mechanisms underpinning CZP effects on TNF-activated human endothelial cells. Methods: Human aortic endothelial cells (HAoECs) were cultured in vitro and exposed to a) TNF alone, b) TNF plus CZP, or c) neither agent. Microarray analysis was used to examine the transcriptional profile of cells treated for 6 hrs and quantitative polymerase chain reaction (qPCR) analysed gene expression at 1, 3, 6 and 24 hrs. NF-κB localization and IκB degradation were investigated using immunocytochemistry, high content analysis and western blotting. Flow cytometry was conducted to detect microparticle release from HAoECs. Results: Transcriptional profiling revealed that while TNF alone had strong effects on endothelial gene expression, TNF and CZP in combination produced a global gene expression pattern similar to untreated control. The two most highly up-regulated genes in response to TNF treatment were adhesion molecules E-selectin and VCAM-1 (q 0.2 compared to control; p > 0.05 compared to TNF alone). The NF-κB pathway was confirmed as a downstream target of TNF-induced HAoEC activation, via nuclear translocation of NF-κB and degradation of IκB, effects which were abolished by treatment with CZP. In addition, flow cytometry detected an increased production of endothelial microparticles in TNF-activated HAoECs, which was prevented by treatment with CZP. Conclusions: We have found at a cellular level that a clinically available TNF inhibitor, CZP reduces the expression of adhesion molecule expression, and prevents TNF-induced activation of the NF-κB pathway. Furthermore, CZP prevents the production of microparticles by activated endothelial cells. This could be central to the prevention of inflammatory environments underlying these conditions and measurement of microparticles has potential as a novel prognostic marker for future cardiovascular events in this patient group. Disclosure statement: Y.A. received a research grant from UCB. I.B. received a research grant from UCB. S.H. received a research grant from UCB. All other authors have declared no conflicts of interes

Structure of (6S,13bR)-1,2,3,5,6,13b-hexahydro-6-isopropyl-8H-pyrrolo[1',2':1,2]pyrazino[3,4,-b]quinazoline-5,8-dione

C17H19N302, monoclinic, P21, a = 5.382 (1), b = 17.534(4), c = 8.198(1)/L ,8 = 100.46(1) °, Z= 2, d,, = 1.323, dc= 1.299 Mg m-3, F(000) = 316, /~(Cu .Ka) = 0.618 mm -1. R = 0.052 for 1284 significant reflections. The proline-containing cispeptide unit which forms part of a six-membered ring deviates from perfect planarity. The torsion angle about the peptide bond is 3.0 (5) ° and the peptide bond length is 1.313 (5)A. The conformation of the proline ring is Cs-Cf~-endo. The crystal structure is stabilized by C-H... O interactions

Hydroxamic acids and their derivatives. III. Preparation of esters of pivalohydroxamic acid and their use in peptide synthesis

Reaction of N-protected amino acids with pivalonitrile oxide affords "active esters" which are useful in peptide syntheses

Hydroxamic acids and their derivatives. II. Reaction of hydroxamic acids with dicyclohexyl carbodiimide

The reaction of hydroxamic acids with DCCI leads to O-carbamoylhydroxamic acids

A note on auroral electrons

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Structure of (4S)-2,4-dimethyl-1,2-dihydropyrazino[2,1-b]quinazoline-3(4H),6-dione

C13HI3N302, orthorhombic, P2~2121, a = 17.443 (5), b = 11.650 (4), c = 5.784 (1)/~, Z = 4, d m = 1.456, d c = 1.429 Mg m -3, F(000) = 512, g(Cu Ka) = 0.843 mm-L The R index is 0.040 for 1358 significant reflections. The structure is stabilized by C-H...O interactions. The N-methylated eis peptide group which forms part of a six-membered ring is non-planar. The torsion angle about the peptide bond is -6.1 (4) ° and the peptide bond length is 1.337 (3) A