Novel domino reactions for the efficient synthesis of 5,6-dihydro-1,4,2-oxathiazines

A facile efficient synthesis of novel 3-aryl-5,6-dihydro-1,4,2-oxathiazin-6-ols from the reaction of (E)-N-hydroxyarylimidoyl chlorides and 1,4-dithiane-2,5-diol in the presence of triethylamine is described. This transformation presumably proceeds via in situ generation of 2-mercaptoacetaldehyde and nitrile oxide and their concomitant [3+3] annulation.     

An unusual conformation of gabapentin (Gpn) in Pyr‐Gpn‐NH‐NH‐Pyr stabilized by weak interactions

The crystal structure of N‐[(1‐{2‐oxo‐2‐[2‐(pyrazin‐2‐ylcarbonyl)hydrazin‐1‐yl]ethyl}cyclohexyl)methyl]pyrazine‐2‐carboxamide monohydrate (Pyr‐Gpn‐NN‐NH‐Pyr·H₂O), C₁₉H₂₃N₇O₃·H₂O, reveals an unusual trans–gauche (tg⁻) conformation for the gabapentin (Gpn) residue around the C^γ—C^β (θ₁) and C^β—C^α (θ₂) bonds. The molecular conformation is stabilized by intramolecular N—H...N hydrogen bonds and weak C—H...O interactions. The packing of the molecules in the crystal lattice shows a network of strong N—H...O and O—H...O hydrogen bonds together with weak C—H...O and π–π inteactions.     

Synthesis and biological evaluation of novel 4-(6-substituted quinolin-4-yl)-N-aryl thiazol-2-amine derivatives as potential antimicrobial agents

Cyclocondensation reaction of 4-(2-bromoacetyl)quinolin-1-ium bromide ( 4a–d ) with substituted arylthiourea, ( 5a–g ) afforded 4-(6-substituted quinolin-4-yl)-N-aryl/pyridyl thiazol-2-amine ( 6a-ab ). These newly synthesized derivatives were evaluated for in vitro antibacterial activity against Escherichia coli (NCIM 2574), Proteus mirabilis (NCIM 2388) (Gram-negative strains), Bacillus subtilis (NCIM 2063), Staphylococcus albus (NCIM 2178) (Gram-positive strains) and in vitro antifungal activity against Aspergillus niger (ATCC 504) and Candida albicans (NCIM 3100). Compounds 6a , 6b , 6d , 6f , 6k , and 6l showed moderate to good antibacterial activity against S. albus. Ten derivatives 6c , 6q , 6r , 6s , 6t , 6v , 6w , 6x , 6y , and 6aa , showed moderate to good activity against A. niger. N-[4-(Quinolin-4-yl)-1,3-thiazol-2-yl]pyridin-2-amine presented comparable activity against A. niger with respect to standard drug Rouconazole.     

Biofortification—A Frontier Novel Approach to Enrich Micronutrients in Field Crops to Encounter the Nutritional Security

Globally, many developing countries are facing silent epidemics of nutritional deficiencies in human beings and animals. The lack of diversity in diet, i.e., cereal-based crops deficient in mineral nutrients is an additional threat to nutritional quality. The present review accounts for the significance of biofortification as a process to enhance the productivity of crops and also an agricultural solution to address the issues of nutritional security. In this endeavor, different innovative and specific biofortification approaches have been discussed for nutrient enrichment of field crops including cereals, pulses, oilseeds and fodder crops. The agronomic approach increases the micronutrient density in crops with soil and foliar application of fertilizers including amendments. The biofortification through conventional breeding approach includes the selection of efficient genotypes, practicing crossing of plants with desirable nutritional traits without sacrificing agricultural and economic productivity. However, the transgenic/biotechnological approach involves the synthesis of transgenes for micronutrient re-translocation between tissues to enhance their bioavailability. Soil microorganisms enhance nutrient content in the rhizosphere through diverse mechanisms such as synthesis, mobilization, transformations and siderophore production which accumulate more minerals in plants. Different sources of micronutrients viz. mineral solutions, chelates and nanoparticles play a pivotal role in the process of biofortification as it regulates the absorption rates and mechanisms in plants. Apart from the quality parameters, biofortification also improved the crop yield to alleviate hidden hunger thus proving to be a sustainable and cost-effective approach. Thus, this review article conveys a message for researchers about the adequate potential of biofortification to increase crop productivity and nourish the crop with additional nutrient content to provide food security and nutritional quality to humans and livestock.     

Time domain measurement of dispersion in optical fibres

A time domain dispersion measurement apparatus was successfully built and tested at the Indian Institute of Technology, Madras. This instrument can measure directly the pulse broadening in a multimode optical fibre. The basic dispersion mechanisms in optical fibres and the design details of the system are discussed.     

Modified sub-population teaching-learning-based optimization for design of truss structures with natural frequency constraints

In this paper, a modified sub-population teaching-learning-based optimization (MS-TLBO) algorithm is proposed to improve the exploration and exploitation capacities by including the concept of number of teachers, adaptive teaching factor, learning through tutorial, and self-motivated learning in the basic TLBO algorithm. The multiple frequency responses to the structural optimization problems are challenging due to its search space, which is implicit, nonconvex, nonlinear, and often leading to divergence. The viability and efficiency of the proposed method are tested by five structural benchmark problems of shape and size optimization with multiple natural frequency constraints on the planar and space trusses. The results reveal that MS-TLBO is more effective as compared to the original TLBO and other state-of-the-art algorithms.     

Lewis acids catalyze the addition of allylboronates to aldehydes by electrophilic activation of the dioxaborolane in a closed transition structure

This study addressed the mechanism of the recently reported Lewis acid-catalyzed manifold for additions of allylboronates to aldehydes. A series of control experiments using various reagents and conditions, and kinetic studies by low-temperature NMR spectroscopy, were performed to investigate the origin of the activation provided by the best catalyst, Sc(OTf)3. The results obtained are strongly supportive of a mechanism involving electrophilic boron activation by coordination of the metal ion to one of the boronate oxygens in a closed bimolecular transition state.     

A solid-phase synthetic strategy for labeled peptides: synthesis of a biotinylated derivative of the delta opioid receptor antagonist TIPP (Tyr-Tic-Phe-Phe-OH)

A general solid-phase synthetic strategy for labeled peptides was developed and used to prepare a biotinylated derivative of the delta opioid receptor antagonist TIPP (Tyr-Tic-Phe-Phe-OH). A monoprotected hydrophilic diamine linker was attached to an aldehyde-containing solid-phase resin by reductive amination, followed by introduction of biotin and peptide synthesis to yield Tyr-Tic-Phe-Phe-Asp-NH(CH(2)CH(2)O)(2)CH(2)CH(2)NH-biotin (2). The high delta receptor affinity and selectivity of 2 demonstrate the applicability of this design approach for labeled peptide derivatives.     

Investigations on Pd:SnO2/porous silicon structures for sensing LPG and NO2 gas

P-type porous silicon (PS) structure has been prepared by anodic electrochemical etching process under optimized conditions. Photoluminescence studies of the PS structure show emission at longer wavelengths (red) for the excitation at 365 nm. Scanning electron microscope investigations of the PS surface confirm the formation of uniform porous structure, and the pore diameter have been estimated as 25 μm. Pd:SnO₂/PS/p-Si heterojunction with top gold ohmic contact developed by conventional methods has been used as the sensor device. Sensing properties of the device towards liquefied petroleum gas (LPG) and NO₂ gas have been investigated in an indigenously developed sensor test rig. The response and recovery characteristics of the sensor device at different operating temperatures show short response time for LPG. From the studies, maximum sensitivity and optimum operating temperature of the device towards LPG and NO₂ gas sensing has been estimated as 69% at 180 °C and 52% at 220 °C, respectively. The developed sensor device shows a short response time of 25 and 57 s for sensing LPG and NO₂ gases, respectively. Paper presented at the Third International Conference on Ionic Devices (ICID 2006), Chennai, Tamilnadu, India, Dec. 7–9, 2006.