Chemical modification of the bicyclo[3.1.0]hexane ring C-3 position led to the discovery of 3-alkoxy-2-aminobicyclo[3.1.0]hexane-2,6-dicarboxylic acid, 3-benzylthio-, and 3-benzylamino-2-amino-6-fluorobicyclo[3.1.0]hexane-2,6-dicarboxylic acid derivatives, metabotropic glutamate receptor 2 (mGlu...

A series of 2-acylated and 2-alkylated amino-5-(4-(benzyloxy)phenyl)thiophene-3-carboxylic acid derivatives were synthesized and evaluated for anti-tubercular activity. Among these compounds, 10d, 15, 12h and 12k inhibited Mycobacterium tuberculosis (Mtb) growth with MIC values between 1.9 and 7...

3-(3,4-Dichlorobenzyloxy)-2-amino-6-fluorobicyclo[3.1.0]hexane-2,6-dicarboxylic acid 5 (MGS0039) is a highly selective and potent group II metabotropic glutamate receptor (mGluR) antagonist (antagonist activities for mGluR2; IC50 = 20.0 nM, mGluR3; IC50 = 24.0 nM) and is detected in both plasma ...

Octa-substituted zinc(II) phthalocyanines with nonfluorinated (ZnPc1) and fluorinated (ZnPc2) n-propanol in peripheral positions have been prepared as thin films by spin coating and examined for their potential as an optical membrane to detect trimethylamine. In this work, the method of spectros...

Room temperature Cl2 sensing characteristics of highly selective spin coated Zn (II) 1,4,8,11,15,18,22,25-octabutoxy-29H,31H-phthalocyanine (ZnPc(OBu)8) film and self-assembled nanobelts (NBs) have been studied in the concentration range of 5–1500 ppb. UV–Visible absorption spectroscopic studi...

Nanowires of Cu(II) 1,4,8,11,15,18,22,25-octabutoxy-29H,31H-phthalocyanine (CuPcOC4) have been fabricated onto the glass substrate by using low cost self-assembly technique. It has been demonstrated that these nanowires were highly sensitive and selective towards Cl2 at room temperature with min...

The photo-physical aspects of non-covalently linked assemblies of a series of fullerenes, namely, C60, C70, tert-butyl-(1,2-methanofullerene)-61-carboxylate (1) and [6,6]-phenyl C70 butyric acid methyl ester (2) with a designed zinc phthalocyanine (ZnPc), viz., zinc-1,4,8,11,15,18,22,25-octabuto...

Thin films of Zinc Phthalocyanine (ZnPc) with a range of different substitutes have been investigated as chemical active layers for sensing selected organic vapour such as (Ethanol, Toluene) by a standard Quartz Crystal Resonator (QCR) based sensor with fundamental resonance 10MHz. Adsorption of...

A biomimetic sensor based on a carbon paste electrode modified with the nickel(II) 1,4,8,11,15,18,22,25-octabutoxy-29H,31H-phthalocyanine complex was developed as a reliable alternative technique for the sensitive and selective analysis of the herbicide diuron in environmental media. The sensor ...

Cevimeline is muscarinic receptor agonist which increases secretion of exocrine glands. Cevimeline base is a liquid (m.p. 20–25 °C) at ambient conditions, therefore its pharmaceutical formulation as a solid hydrochloride hemihydrate has been developed. The synthesis of cevimeline yields its ci...

Pelleted feeds (PF) are popular in horse nutrition because of high palatability and improved feeding hygiene, but ingestion is faster for PF than for cereals or muesli feed. The aim of the study was to evaluate whether variable amounts of two PFs produced with different physical properties from ...

A new material—poly{methyl[3-(2-hydroxy-3,4-difluoro)phenyl]propyl siloxane}(PMDFPS) sensitive to toxic organophosphate vapor was synthesized with 2,3-difluorophenol, allyl bromide and poly (methyl hydrosiloxane) as raw materials, via O-alkylation, Claisen rearrange reaction and hydrosilylation...

Novel sulfonated poly(arylene ether sulfone) polymers with 3,4-difluoro-phenyl group (2F-SPAES-xx) were successfully synthesized via the direct copolymerization of 3,3′-disulfonate-4,4′-dichlorodiphenylsulfone, 4,4-dichlorodiphenylsulfone and 3,4-difluoro-phenyl hydroquinone. The polymers with...

A new strategy to 6-hydroxy-2-naphthoic acid (HNPA) and 4-hydroxybenzoic acid from 2,6-diisopropylnaphthalene and p-cymene, respectively, was developed using the NHPI-catalyzed aerobic oxidation as a principal reaction. 2,6-Diisopropylnaphthalene was oxidized by the oxidation with O2 (1 atm) by ...

The discovery of dipeptide, H-Asp(Gly)-OH, having an inhibition activity of PHA-induced lymphocyte transformation is reported. The seven analogs of H-Asp(Gly)-OH are described in which H-β-aspartyl, H-D-β-aspartyl, and Z-β-aspartyl respectively. The H-Gly-OH residue of H-Asp(Gly)-OH is also s...

A methodology directed toward the stereoselective synthesis of novel quinolyl glycines is presented. This strategy is based on the cyclocondensation reaction between 2-amino thiophenol 4 and chiral acetylenic ketones of the type 3 containing a latent α-amino acid functionality. The initially fo...

The enzymatic reduction of N-Boc-4S-amino-3-oxo-5-phenylpentanoic acid methylester, the key intermediate in the stereoselective synthesis of a statinanalogue, was studied with Hansenula anomala and Hansenula silvicola. Using whole cells of H. anomala gives complete conversion and a diastereomeri...

A concise enantioselective synthesis of (3S,6S,9S)-2-oxo-3-(N-Boc-amino)-1-azabicyclo[4.3.0]nonane-9-carboxylic acid methyl ester from N-protected glutamic acid is described.

(2S,3S)-N-Boc-3-amino-1,2-epoxy-4-phenylbutane is prepared in four steps from commercially available N,N-dibenzyl-L-phenylalaninol. The synthesis is amenable to the preparation of kilogram quantities of enantiomerically pure material.

BackgroundInflammatory serine proteases (ISPs) play an important role in cardiac repair after injury through hydrolysis of dead cells and extracellular matrix (ECM) debris. Evidence also suggests an important role of ISPs in the coordination of the inflammatory response. However, the effect of I...