Enantiopure Nβ-Fmoc-amino alkyl isonitriles and amino acid esters have been employed as building blocks in Ugi four-component reaction (U-4CR) to yield 1,1′-iminodicarboxylated peptidomimetics. By employing trifluoroacetic acid as one of the components, a different outcome has been observed an...

Amino acid appended azobenzene hybrid was synthesized and characterized using Spectroscopic techniques like 1H NMR, 13C NMR, FT-IR and Mass spectrometry analysis and its optical properties were investigated using UV–vis absorption and fluorescence spectroscopy in solvents of different polarity....

AimTo synthesize the baicalein amino acid derivatives and evaluate their cytotoxicity activities in vitro.

Matriptase-2, a type II transmembrane serine protease (TTSP), is expressed in the liver and regulates iron homeostasis via the cleavage of hemojuvelin. Matriptase-2 emerges as an attractive target for the treatment of conditions associated with iron overload, such as hemochromatosis or beta-thal...

We describe here the synthesis and biological activity study of a pair of diastereomeric analogues of Gramicidin S using β,γ-diamino acids as β-turn mimic. The synthesis of the orthogonally protected β,γ-diamino acids was achieved in 6 steps starting from d-alanine. The analogues were then ...

Amino acid appended azobenzene hybrid has been synthesized (Fmoc-al-az) and its electronic absorbance and fluorescence spectra were recorded at room temperature in a series of polar and non-polar solvents. The ground state and excited state dipole moments were calculated using solvatochromic shi...

Four organic dyes with asymmetric double donor-π-acceptor system were designed, synthesized and utilized in dye-sensitized solar cells (DSSCs), where phenothiazine and carbazole were introduced as double donors, butyl or octyl chain as the linker and cyanoacetic acid or rhodanine acetic acid as...

By using chiral auxiliaries and hydrogen bonding interactions, we have developed diastereoselective photocycloaddition of 2-naphthalenecarboxylates and 2,3-naphthalenedicarboxylates with furan derivatives. In photoreactions of (ℓ)-menthyl 2-naphthalenecarboxylate with furan and 3-furanmethanol, ...

A short synthesis of zamifenacin is described by using a ring enlargement of a l-prolinol derivative. © 1997 Elsevier Science Ltd.

The interaction of zamifenacin ((3R)-(+)-diphenylmethoxy-1-(3,4)-methylenedioxyphenethyl)piperidine) at muscarinic receptor subtypes was studied using radioligand binding and functional techniques, in vitro. In radioligand binding studies, zamifenacin acted as a competitive antagonist, with the ...

Synthesis, adsorption and corrosion inhibiting effect of three surfactants consist of Schiff bases as hydrophobic part and poly ethylene glylcol (poly ethylene oxide) as hydrophilic part on steel in 1.0 M HCl was investigated using weight loss, Electrochemical Impedance, potentiodynamic polariza...

The inhibiting action of a Schiff base 4-[(4-hydroxy-3-hydroxymethyl-benzylidene)-amino]-1,5-dimethyl-2-phenyl-1,2-dihydro-pyrazol-3-one (phv), derived from 4-amino-1,5-dimethyl-2-phenyl-1,2-dihydro-pyrazol-3-one (phz) and 4-hydroxy-3-methoxy-benzaldehyde (vn), towards the corrosion behavior of ...

A series of enantiopure 1,4-amino alcohols with a [3]ferrocenophane backbone have been synthesized. Candida rugosa lipases were used in a key step allowing the resolution of amino alcohol (1S,Rp)-1. Two other amino alcohols (1S,2S,Rp)-2 and (1S,2S,Rp)-3 were prepared starting from (1S,Rp)-1. The...

To characterize the role of cAMP-dependent protein kinase (PKA) in regulating vascular Ca2+ current through Cav1.2 channels [ICa1.2], we have documented a marked capacity of the isoquinoline H-89, widely used as a PKA inhibitor, to reduce current amplitude. We hypothesized that the ICa1.2 inhibi...

Herbal pharmaceutical companies are dependent on plant parts which are used as raw materials in their products. The naturally available herbal raw material does not meet the demand of industries. This can lead to exploitation of nature and affect the biodiversity in various ways. In vitro plant ...

SummaryHydrolyzable tannins showed higher cytotoxic activity against human oral squamous cell carcinoma and salivary gland tumor cell lines than against normal human gingival fibroblasts, whereas gallic acid, a component unit of tannins, showed much weaker selective cytotoxicity. The cytotoxic a...

Woodfruticosin (woodfordin C) (WFC), a new inhibitor of DNA topoisomerase II (topo-II), was isolated from methanol extract of Woodfordia fruticosa Kurz (Lythraceae) and studied for in vitro and in vivo antitumor activities in comparison with Adriamycin® (ADR) and etoposide (ETP), well known inhi...

Tannins are a group of widely distributed plant polyphenols, some of which are beneficial to health because of their chemopreventive activities. In the present study, we investigated the effects and action mechanisms of woodfordin I, a macrocyclic ellagitannin dimer, on human chronic myelogenous...

A new organic stilbazolium derivative, 1-Ethyl-2-(2-p-tolyl-vinyl)-pyridinium iodide (TASI), was grown from methanol:acetonitrile (1:3) mixed solvent by slow evaporation technique. Single crystal X-ray diffraction analysis revealed that TASI crystallizes in triclinic system with a centrosymmetri...

The total syntheses of the first examples of diarylheptanoid natural products (5S)-5-acetoxy-1,7-bis(4-hydroxy-3-methoxyphenyl)-3-heptanone 1, and (3S,5S)-3,5-diacetoxy-1,7-bis(4-hydroxy-3-methoxyphenyl)heptane 2 isolated from the rhizomes of Zingiber officinale were accomplished using Sharpless...