Strategies of synthesis of aromatic polyketides using cyclohexa-1,4-and-1,3-dienes in Alder Rickett reactions

Cyclohexa-1, 4-dienes with appropriate substituents, obtained by birch reduction of the substituted benzene, react directly with derivatives of propiolic ester or aldchyde to yield aromatic polyketides. The following compounds have been synthesized; mycophenolic acid, nidulol methyl other, the root growth hormone 3, 5-dihydroxy-2-formyl-4-mythyl-benzoic acid, antibiotic DB 2073, the macrocyclic lactones lasiodiplodin and dihydrozearalenone and the biphenyl derivatives alternario and altenusin. Polyketide anthraquinones can be made from naphthoquinone precursors.

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.

Editorial of "International Journal of Critical Indigenous Studies Volume 4, Number 1, 2011"

This special edition of the International Journal of Critical Indigenous Studies highlights the work of emerging scholars in the field of Indigenous Studies. The five featured authors were all finalists for the prize awarded by the Native American and Indigenous Studies Association (NAISA) to the best post-graduate student paper at the NAISA meeting held in 2010 in Tucson, Arizona. While the breadth of scholarship encompassed by the term ‘Indigenous Studies’ and the global representation of Indigenous peoples at NAISA mean that the topics and approaches vary widely, a common thematic of fraught post-colonial relations can be discerned within all five articles.

Complexes of lanthanide iodides with 3-methylpyridine-1-oxide

Complexes of lanthanide iodides with 3-methylpyridine-1-oxide of the formula Ln(3-MePyO)8I3.xH2O where x = 0 for Ln = La and Tb, x = 1 for Ln = Pr, and x = 2 for Ln = Nd, Sm, Dy, Yb, and Y have been prepared and characterized by chemical analyses, conductance, infrared, proton nmr, and DTA data. Infrared and proton nmr data have been interpreted in terms of the coordination of the ligand to the metal ion through the oxygen of the N—O group. Proton nmr spectrum of the Yb(III) complex is indicative of a restricted rotation of the pyridine ring about the N—O bond.

Pyridine-1-oxide complexes of lanthanide iodides

Pyridine-1-oxide complexes of lanthanide iodides of the formulaLn(PyO)8I3 whereLn=La, Pr, Nd, Tb, Dy, Er, and Yb have been prepared and characterised by analyses, molecular weight, conductance, infrared and proton NMR data. Proton NMR and IR data have shown the coordination of the ligand to the metal through the oxygen atom of the N–O group. NMR data have been interpreted in terms of a distorted square antiprismatic geometry in solution.

Facile synthesis, ex-vivo and in vitro screening of 3-sulfonamide derivative of 5-(4-chlorophenyl)-1-(2,4-dichlorophenyl)-4-methyl-1H-pyrazole-3-carboxylic acid piperidin-1-ylamide (SR141716) a potent CB1 receptor antagonist

Facile synthesis of biaryl pyrazole sulfonamide derivative of 5-(4-chlorophenyl)-1-(2,4-dichlorophenyl)-4-methyl-1H-pyrazole-3-carboxylic acid piperidin-1-ylamide (SR141716, 1) and an investigation of the effect of replacement of the –CO group in the compound 1 by the –SO2 group in the aminopiperidine region is reported. Primary ex-vivo pharmacological testing and in vitro screening of sulfonamide derivative 2 showed the loss of CB1 receptor antagonism.

3D QSAR studies of N-4-arylacryloylpiperazin-1-yl-phenyl-oxazolidinones: A novel class of antibacterial agents

Three-dimensional QSAR studies for N-4-arylacryloylpiperazin-1-yl-phenyl-oxazolidinones were conducted using TSAR 3.3. The in vitro activities (MICs) of the compounds against Staphylococcus aureus ATCC 25923 exhibited a strong correlation with the prediction made by the model developed in the present study.

Stereospecific photodimerization of coumarins in crystalline inclusion complexes. Molecular and crystal structure of 1:2 complex of (S,S)-(-)-1,6-bis(o-chlorophenyl)-1,6-diphenyl-hexa-2,4-diyne-1,6-diol and coumarin

Proximity of molecules is a crucial factor in many solid- state photochemical processes.'S2 The biomolecular photodimerization reactions in the solid state depend on the relative geometry of reactant molecules in the crystal lattice with center-to-center distance of nearest neighbor double bonds of the order of ca. 4 A. This fact emanates from the incisive studies of Schmidt and Cohen.2 One of the two approaches to achieve this distance requirement is the so-called "Crystal-Engineering" of structures, which essentially involves the introduction of certain functional groups that display in-plane interstacking interactions (Cl...Cl, C-He-0, etc.) in the crystal The chloro group is by far the most successful in promoting the /3- packing m ~ d e ,th~o,u~gh recent studies have shown its limitations? Another approach involves the use of constrained media in which the reactants could hopefully be aligned.

Ethyl 6-chloro-2-oxo-4-phenyl-1,2-dihydroquinoline-3-carboxylate

In the title compound,C18H14ClNO3,the dihydroquinolin-2-one ring system is almost planar (r.m.s.deviation = 0.033 angstrom).The carboxylate plane and the phenyl group are twisted away from the dihydroquinolin-2-one ring system by 50.3(1) and 64.9(1)degrees,respectively.In the crystal structure, inversion-related molecules form R-2(2)(8)dimers via pairs of N-H center dot center dot center dot O hydrogen bonds.

2-(4-Chloro-3-nitrophenyl)-4-(4-chlorophenyl)-1,3-thiazole

The title compound, C15H8Cl2N2O2S, crystallizes with two molecules in the asymmetric unit. The dihedral angles between the 4-chloro-3-nitrophenyl ring and the thiazole ring are 0.5 (1) and 7.1 (1)° and those between the 4-chlorophenyl ring and the thiazole ring are 7.1 (1) and 7.4 (1)° in the two molecules. The crystal structure is stabilized by intermolecular C-H...Cl and C-H...O hydrogen bonds.

(2E)-3-(4-Bromophenyl)-1-(2-methyl-4phenyl-3-quinolyl)prop-2-en-1-one

The conformation about the ethene bond [1.316 (3) angstrom] in the title compound, C25H18BrNO, is E. The quinoline ring forms dihedral angles of 67.21 (10) and 71.68 (10)degrees with the benzene and bromo-substituted benzene rings, respectively. High-lighting the non-planar arrangement of aromatic rings, the dihedral angle formed between the benzene rings is 58.57 (12)degrees.

Indoleacetaldoxime hydro-lyase (4.2.1.29). III. Further studies on the nature and mode of action of the enzyme

Further purification of indoleacetaldoxime (IAOX) hydro-lyase from Gibberella fujikuroi by DEAE-cellulose chromatography is described. The purified enzyme was activated by dehydroascorbic acid (DHA), ascorbic acid (AA), and pyridoxal phosphate (PALP) and was inhibited by thiol compounds and thiol reagents including phenylthiocyanate. Ferrous ions but not ferric ions activated the purified enzyme. The enzyme was activated by dihydrofolic acid but inhibited by tetrahydrofolic acid. Phenylacetaldoxime, a competitive inhibitor, afforded partial protection of the enzyme from the action of N-ethylmaleimide suggesting the involvement of a thiol function at the active site or substrate-binding site. The inhibition of the enzyme by 2,3-dimercaptopropanol was reversed by DHA, PALP, or frozen storage. KCN inhibition of the enzyme was reversed by PALP. NaBH4 reduction of the purified enzyme in the presence of PALP gave an active enzyme which was further activated by PALP or DHA but not by ferrous ions. These results suggested a "structural" role for PALP in the activity of IAOX hydro-lyase. Dilute solutions of the purified enzyme, obtained during DEAE-cellulose chromatography and concentrated using sucrose, showed enhanced activity upon frozen storage and thawing. The increase in activity of the enzyme during certain culture conditions, the activation and inhibition of the enzyme by several unrelated compounds, and the effect of freezing indicate that IAOX hydro-lyase is probably a metabolically regulated enzyme with a structure composed of subunits.

Bi2−xPbx(Ca, Sr)n+1CunO2n+4+δ (n = 1, 2, 3, and 4) family of superconductors

Superconducting oxides of the Bi1.5Pb0.5(Ca, Sr)n+1CunO2n+4+δ series with n = 1, 2, 3 and 4 have been characterized. The superconducting transition temperature increases markedly with n up to n = 3, but the Tc of the n = 4 member is not much higher than that of the n = 3 member. The Tc does not change significantly in Bi2−xPbxCaSr2Cu2O8+δ with x (0.1 < x ≤ 0.5).

A regio and stereospecific radical annulation route to chiral tricyclo[4.3.1.o3,7]decane (isotwistane) system1 synthesis of (+)-10-α-Naphthyl-5-epi-Pupukean-9-one

Contrary to that of phenyl derivative 1 the radical 4 adds to radicophiles in an inter- followed by intra-molecular radical Michael addition (radical annulation), furnishing a novel route to chiral isotwistanes 5.