A medicinal chemistry program based on the small-molecule HCV NS5A inhibitor daclatasvir has led to the discovery of dimeric phenylthiazole compound 8, a novel and potent HCV NS5A inhibitor. The subsequent SAR studies and optimization revealed that the cycloalkyl amide derivatives 27a-29a exhibi...

The cocrystallization of salicylamide (2-hydroxybenzamide, SMD) and ethenzamide (2-ethoxybenzamide, EMD) with aromatic carboxylic acids was examined both experimentally and theoretically. The supramolecular synthesis taking advantage of the droplet evaporative crystallization (DEC) technique was...

The identification and optimization of a novel series of centrally efficacious gamma secretase modulators (GSMs) offering an alternative to the privileged aryl imidazole motif is described. Chiral bicyclic tetrahydroindazolyl amine substituted triazolopyridines were identified as structurally di...

An alpidem-insensitive benzodiazepine binding site in the rat spinal cord has recently been identified in our laboratory. We report here the binding of 23 1,4-benzodiazepines to this site using [3H]Ro15-4513 (ethyl-8-azido-6-dihydro-5-methyl-4H-imidazo[1,5-a][1,4]benzodiazepine-3-carboxylate) in...

The triazolopyrimidine scaffold represents one of the privileged structure in chemistry, and there has been an increase in number of studies utilizing this scaffold and its derivatives. Optimization of synthetic protocols such as aza-Wittig reaction, [3 + 2] cycloaddition reaction along with pre...

A series of ferrocene-based organosilicon compounds have been prepared via hydrosilylation or double silylation of carbonyl compounds with 1,1′-bis(dimethylsilyl)ferrocene using (C2H4)Pt(PPh3)2 or Ni(PEt3)4 catalysts. In general, while the platinum catalyst (C2H4)Pt(PPh3)2 preferentially produc...

A study has been made of the possibility of increasing the stability of the 1,1′-bis(diphenylphosphino)ferrocenium monocation by introduction of appropriate substituents into the cyclopentadienyl ligands. The electrochemical behaviour of a series of 1,1′-bis(diphenylphosphino)ferrocenes bearin...

The cationic palladium(II) complexes with 1,1′-bis(phosphino)ferrocenes [Fe(η5-C5H4PR2)2Pd(NCMe)n](OTf)2 (n = 0–2) (OTf = CF3SO3; 5, R = o-MeOC6H4, n = 0; 6, R = o-MeC6H4, n = 1; 7, R = o-PriC6H4, n = 1; 8, R = C6F5, n = 1) have been prepared by treatment of the corresponding dichlorides [Fe(...

The oxidative electrochemistry of group VI and group VII metal carbonyl compounds containing 1,1′-bis(phosphino)ferrocene ligands with the general formula [M(CO)4(P∩P)] (M = Cr, Mo, or W, P∩P = 1,1′-bis(diisopropylphosphino)ferrocene (dippf) or 1,1′-bis(dicyclohexylphosphino)ferrocene (dcpf...

The asymmetric synthesis of 1,1′-bis-(methyl-phenyl-phosphino) ferrocene 1 is described using the oxazaphospholidine borane complex 5 as synthon. Two strategies were investigated, based either on PC bond formation by ring opening of complex 5 with the 1,1′-dilithio ferrocene 10, or on homocoup...

The electrochemistry of 1,1′-bis(diphenylphosphino)cobaltocenium hexafluorophosphate ([dppc][PF6]), 1,1′-bis(dicyclohexylphosphino)cobaltocenium hexafluorophosphate ([dcpc][PF6]), 1,1′-bis(di-iso-propylphosphino)cobaltocenium hexafluorophosphate ([dippc][PF6]), and 1-(di-tert-butylphosphino)c...

A 1,1′ bis(diphenyl phosphino ferrocene) dioxide complex of the uranyl dichloride was synthesized and characterized by elemental analysis, 1H, 31P{1H} NMR and X-ray diffraction methods. The structure of the compound shows that the uranium(VI) ion is surrounded by four oxygen and two chlorine at...

E. coli tRNAPhe was modified at its 3-(3-amino-3-carboxypropyl)uridine residue with the N-hydroxysuccinimide ester of N-4-azido-2-nitrophenyl)glycine. Exclusive modification of this base was shown by two-dimensional TLC analysis of the T1 oligonucleotide and nucleoside products of nuclease diges...

A novel enzyme which catalyzes the transfer of the 3-amino-3-carboxypropyl group into tRNA to form 3-(3-amino-3-carboxypropyl)uridine was isolated from Escherichia coli. The enzyme required S-adenosylmethionine as donor molecule.

Alkylation of 3,17β-bis(2-trimethylsilyl)ethoxymethyl-1,3,5(10) estratriene-6-one (2) with 5-bromo-1-pentene using NaHMDS in THF afforded 3,17β-bis(2-trimethylsilyl)ethoxymethyl-7-α-(4′-pentenyl)-1,3,5(10)estratriene-6-one (3) in excellent stereoselectivity (>95% epimeric excess). Functional...

The screening of potential affinity ligands and the development of a two-stage affinity purification of an S-adenosylmethionine-dependent 3-amino-3-carboxypropyl transferase involved in the biosynthesis of the β-lactam antibiotic nocardicin A is described from a cell-free extract of Nocardia un...

N,N-diethyl-N-methyl-N-(2-methoxyethyl) ammonium tetrafluoroborate, [DEME][BF4], and H2O mixtures were investigated in optical properties by UV–visible spectroscopy. The concentration region of H2O in the mixtures was 0–100 mol%. At room temperature, the mixtures of H2O exhibit absorption peak...

We previously reported that amorphization was observed in a room temperature ionic liquid (RTIL)-6.7 mol% H2O mixture by simultaneous X-ray diffraction and differential scanning calorimetry measurements (Y. Imai, H. Abe, T. Goto, Y. Yoshimura, Y. Michishita, H. Matsumoto, Chem. Phys. 352 (2008) ...

The pH oscillations related to the protonation/deprotonation process in a room temperature ionic liquid (RTIL)–water system were observed at fixed temperatures. The RTIL was hydrophilic N, N-diethyl-N-methyl-N-2-methoxyethyl ammonium tetrafluoroborate ([DEME][BF4]). The rhythmic oscillations of...

For a room temperature ionic liquid, N,N-diethyl-N-methyl-N-(2-methoxyethyl) ammonium tetrafluoroborate, [DEME][BF4]–H2O system, we have observed two glass transitions in the region of 16.5–30.0 mol% H2O. The nano-phase separations in [DEME][BF4] enhanced by a small amount of H2O may be the ca...