Chemical images of marine bio-active compounds by surface enhanced Raman spectroscopy and transposed orthogonal partial least squares (T-OPLS)

Surface enhanced Raman spectroscopy combined with transposed Orthogonal Partial Least Squares (T-OPLS) was shown to produce chemical images of the natural antibacterial surface-active compound 1,1,3,3-tetrabromo-2-heptanone (TBH) on Bonnemaisonia hamifera. The use of gold colloids functionalised with the internal standard 4-mercapto-benzonitrile (MBN) made it possible to create images of the relative concentration of TBH over the surfaces. A gradient of TBH could be mapped over and in the close vicinity of the B. hamifera algal vesicles at the attomol/pixel level.     

Few-Nucleon System Dynamics Studied via Deuteron–Deuteron Breakup Reactions at 160 MeV

An experiment, with the deuteron beams at energy of 160 MeV impinging on the liquid deuterium target, was carried out using the BINA detector at KVI, in Groningen, the Netherlands. Data were collected for the purpose of obtaining high precision differential cross-sections for the deuteron break-up reaction. The elastic scattering channel was also measured alongside for the purpose of cross-section normalization.     

A green one-pot multicomponent synthesis of 4H-pyrans and polysubstituted aniline derivatives of biological, pharmacological, and optical applications using silica nanoparticles as reusable catalyst

A one-pot practical, efficient, and environmentally benign multicomponent synthesis of 4H-pyrans and polysubstituted aniline derivatives of biological, pharmacological, and optical applications has been developed using a very mild, neutral, and reusable silica nanoparticles as catalyst. The 4H-pyran derivatives were synthesized by a three component reaction of an aldehyde, malononitrile, and 5,5-dimethyl-1,3-cyclohexanedione or ethyl acetoacetate at room temperature or refluxing in ethanol. Alternatively, polysubstituted anilines were synthesized via a four component reaction of an aldehyde, a ketone, and two equivalents of malononitrile in ethanol.     

Novel N-(benzo[d]oxazol-2-yl)alkanamides; synthesis and carbonic anhydrase II inhibition studies

Carbonic anhydrase (CA II) inhibitors are very important therapeutic targets in drug design for treatment of neuropathic pain and in eradication of glaucoma, cancer, epilepsy, ulcer and obesity. In this study, some two2-substituted benzoxazoles ( 3a-j ) were developed as a new family of carbonic anhydrase II inhibitors by employing acyl thiourea chemistry via a simple and expedient protocol and evaluated for CA II inhibitor activity and radical scavenging ability. Compounds 3f and 3j were found to be the most potent inhibitors, with IC₅₀ values of 0.00564 and 0.00596 μM, respectively which are several times better than that of the standard, acetazolamide (IC₅₀ value 0.997 ± 0.0586 μM). Docking experiments were carried out against the carbonic anhydrase II crystal structure to better rationalize the inhibitory activities of these new structures. Moreover, the results of a DPPH radical scavenging assay showed that the antioxidant profile of compound 3i is superior to those of other derivatives. The results have revealed that derivatives 3f and 3j behave as CA-II inhibitors significantly better than standard and 3i has good anti-oxidation potential.     

Green Synthesis of Some New (Substituted Fluorobenzoylimino)-3-aryl-4-methyl-1,3-thiazolines

A series of 2-, 3-, and 4-substituted (fluorobenzoylimino)-3-aryl-4-methyl-1,3-thiazolines (2a–j) were synthesized in good yields by the base-catalyzed cyclization of corresponding 1-(fluorobenzoyl)-3-(fluorophenyl)thioureas (1a–j) with α-bromoacetone in water. Compared to the reactions in conventional nonaqueous solvents under inert anhydrous conditions, the aqueous medium provides a much cleaner, more efficient, and simpler method for synthesis.     

Synthesis and Crystal Structure of Some Novel 2-Aroylimino-3-aryl-4-phenyl-1,3-thiazolines

An efficient synthesis of some novel 2-aroylimino-3-aryl-4-phenyl-1,3-thiazolines was carried out by base-catalyzed cyclization of 1-aroyl-3-arylthioureas with acetophenone in the presence of bromine. The structures were confirmed by spectroscopic data, elemental analyses, and in one case (2t) by single-crystal X-ray diffraction data.