Asymmetric synthesis of (+)-stagonolide C and (−)-aspinolide A via organocatalysis

A new enantioselective synthesis of two important fungal metabolites, (+)-stagonolide C and (?)-aspinolide A, has been described from readily available raw materials. Proline catalyzed asymmetric α-aminooxylation and Jorgensen’s epoxidation of aldehydes are the key reactions employed in the introduction of chirality. The formation of the 10-membered lactone core structure was finally accomplished via Steglich esterification and ring closing metathesis reactions.     

Modified Pyridine-Substituted Coumarins: A New Class of Antimicrobial and Antitubercular Agents

Some new biologically potent coumarin derivatives 7a–f, 8a–f, and 9a–f bearing modified pyridine moieties (indeno[1,2-b]pyridine, 4-azaphenanthrene and benzofuro [3,2-b]pyridine) at the sixth position were designed and synthesized. All the synthesized compounds were assayed for their antimicrobial efficiency against Staphylococcus aureus, Bacillus subtilis, Escherichia coli, Salmonella typhi, Candida albicans, and Aspergillus niger. Most of the compounds showed appreciable antimicrobial activity against the tested strains. Compounds 8b, 8c, 9b, 9d, and 9f emerged as most proficient members of the series. The antitubercular activity for all the synthesized compounds was performed against Mycobacterium tuberculosis H37R_v. Compounds 8f, 9b, and 9f exhibited promising antitubercular activity. Consequently, synthesized derivatives were found to be worthy of further investigation.     

High pressure studies using two-stage diamond micro-anvils grown by chemical vapor deposition

Ultra-high static pressures have been achieved in the laboratory using a two-stage micro-ball nanodiamond anvils as well as a two-stage micro-paired diamond anvils machined using a focused ion-beam system. The two-stage diamond anvils’ designs implemented thus far suffer from a limitation of one diamond anvil sliding past another anvil at extreme conditions. We describe a new method of fabricating two-stage diamond micro-anvils using a tungsten mask on a standard diamond anvil followed by microwave plasma chemical vapor deposition (CVD) homoepitaxial diamond growth. A prototype two-stage diamond anvil with 300?µm culet and with a CVD diamond second stage of 50?µm in diameter was fabricated. We have carried out preliminary high pressure X-ray diffraction studies on a sample of rare-earth metal lutetium sample with a copper pressure standard to 86?GPa. The micro-anvil grown by CVD remained intact during indentation of gasket as well as on decompression from the highest pressure of 86?GPa.     

Molecular modeling studies, synthesis, and biological evaluation of Plasmodium falciparum enoyl-acyl carrier protein reductase (PfENR) inhibitors

The search for new antimalarial agents is necessary as current drugs in the market become vulnerable due to the emergence of resistance strains of Plasmodium falciparum (P. falciparum). The biosynthetic pathway for fatty acids has been recognized and validated as an important drug target in P.falciparum. One of the important enzymes in this pathway that has a determinant role in completing the cycles of chain elongation is Enoyl-ACP reductase (ENR) also popularly known as FabI. In this paper we report the design, synthesis, and microbial evaluation of inhibitors of Plasmodium enoyl reductase (PfENR). The search for inhibitors involved a virtual screening of the iResearch database with docking simulations. One of the hits was selected and modified to optimize its binding to PfENR; this resulted in the development of analogues of N-benzylidene-4-phenyl-1,3-thiazol-2-amine. The activity of these analogues was predicted from comparative molecular field analysis (CoMFA) and comparative molecular similarity indices analysis (CoMSIA) models constructed from a dataset of 43 known inhibitors of PfENR. The most promising molecules were synthesized and their structures characterized by spectroscopic techniques. The molecules were screened for in vitro antimalarial activity by whole-cell assay method. Two molecules, viz. VRC-007 and VRC-009, were found to be active at 4.67 and 7.01 μM concentrations, respectively.     

Relation of coordination number to memory and threshold switching in chalcogenides

The paper reports a structural study of some memory and threshold chalcogenides in terms of coordination numberC, defined byC=8−N, and is the average coordination number for covalently bonded materials. The average number of nearest neighbours surrounding a central atom, obtained for As-Ge-Te (memory) and Se-Ge-Te (threshold) systems have been used to estimate the cohesive energies, assuming simple additivity of bond energies. The bonding pattern so obtained, explains certain properties of these glasses.     

Polarography: A classical method with a new lease of life

Classical DC polarography was introduced by Heyrovsky in 1922. Since then substantial advances have been made in the technique, its instrumentation and methodology. These, coupled with the brilliant and innovative thinking of several workers, especially Barker, have transformed polarographic analysis into a powerful analytical tool.     

Nature and properties of ultrathin nanocrystalline gold films formed at the organic-aqueous interface

Ultrathin nanocrystalline films of gold formed at different temperatures at the organic-aqueous interface have been investigated by X-ray diffraction, electron microscopy, atomic force microscopy, and electronic spectroscopy. The films are smooth and continuous over relatively large length scales and are generally approximately 100 nm thick. The size of the nanocrystals is sensitive to the reaction temperature, which also determines whether the film is metallic or an activated conductor. The surface plasmon band of gold is highly red-shifted in the films. Alkanethiols perturb the structure of the films, with the magnitude of the effect depending on the chain length. Accordingly, the position of the plasmon band and the electrical resistance of the films are affected by interaction with alkanethiols; the plasmon band approaches that of isolated nanocrystals in the presence of long-chain thiols.     

A Novel Synthesis and Characterization of Titanium Superoxide and its Application in Organic Oxidative Processes

A novel, exceptionally stable titanium superoxide radical ion was prepared and its structure determined by FTIR, ESR, Raman spectroscopy, X-ray diffraction, thermogravimetric/differential thermal analysis and elemental analysis. This heterogeneous catalyst has been found to be effective for the selective oxidation of aromatic amines and phenols to the corresponding nitro aromatics and p-quinones, respectively. In addition, this non-toxic, inexpensive and reusable catalyst has also been used in aminobromination of olefins, which proceed to give the 1, 2-bromoaminated anti-Markovnikov product. A brief account of these results is summarized in this review.