HOE 140 is a second-generation B-2 bradykinin receptor antagonist that is resistant to degradation by carboxypeptidase N and endopeptidase 24.11 …
This paper reports the synthesis and insecticidal activity of a series of novel 4-hydroxy-3-mesityl-1-methoxymethoxy-1,5-dihydro-2H-pyrrol-2-one derivatives, in which the substituents at the 5-position were varied with a number of alkyl and spirocycloalkyl groups. Investigation of the structure–...
A novel vinyl monomer, (S)-3-vinyl-2,2′-bis(methoxymethoxy)-1,1′-binaphthyl 2, was synthesized and underwent helix-sense-selective anionic polymerization to obtain helical polymers with an excess screw sense. The polymer ([α]36525 = −1610.0°) exhibited optical rotation as large as fourfold t...
Enantiospecific total synthesis of the crinipellin mentioned in the title was accomplished. In the present synthesis cyclopentane ring in campholenaldehyde was identified as the B-ring, two intramolecular rhodium carbenoid CH insertion reactions were employed for the construction of the A and C ...
Chalcone (1,3-diphenyl-2-propen-1-one) derivatives exert anti-cancer activity by targeting key molecules that can lead to carcinogenesis. We synthesized the chalcone derivative 3-phenyl-1-(2,4,6-tris(methoxymethoxy)phenyl)prop-2-yn-1-one (KB-34) and previously reported its anti-inflammatory acti...
Liquid–liquid equilibria data for the ternary mixture of 1-Butanol + methoxy(methoxymethoxy)methane + water were measured at atmospheric pressure and temperatures of 303.15, 323.15 and 343.15 K. The ternary system forms a type Ⅱ phase diagram with two partially miscible region. The distributio...
5-Methoxymethoxy-6-nitrohex-1-ene on treatment with sodium methoxide undergoes three cascade reactions to afford diastereomeric 3-methoxy-2-nitrohept-6-en-1-ols.
Isobaric vapour-liquid equilibria (VLE) experimental results for binary systems of 1-(methoxymethoxy)-2-methyl-propane with 1-butanol and isobutanol at 101.33 kPa were determined. Each binary mixture shows a minimum boiling azeotrope at 101.33 kPa, in which the azeotropic temperature and composi...
Isobaric vapor–liquid equilibrium (VLE) data for 1-propanol + 1-(methoxymethoxy)-butane and 1-butanol + 1-(methoxymethoxy)-butane systems were measured at 101.3 kPa with a modified Rose still. The results indicated that two minimum temperature binary azeotropes were formed in two systems above....
Isobaric vapor–liquid equilibrium (VLE) data have been measured for methanol + 1-(methoxymethoxy)-propane and 1-propanol + 1-(methoxymethoxy)-propane systems at 101.33 kPa. The two binary systems present two minimum temperature azeotropes at 101.33 kPa. Saturated vapor pressure data for the pur...
The reaction of Re(CO)5Cl with 2-thienyl-N,N-bis(2-thienylmethylene)methanediamine (tbtmma) has been examined and a novel Re(CO)3+ tricarbonyl – fac-[Re(CO)3(tbtmma)Cl] – has been obtained. The compound has been studied by IR, UV–Vis spectroscopy and X-ray crystallography. The molecular orbit...
Two new copolymers were synthesized by electrochemical polymerization of 2-[3-thienylmethylene]aminophenol (2,3-TMAP) and poly-2-[3-thienylmethylene]aminophenol (P-2,3-TMAP) with thiophene (Th) and the obtained thiophene copolymers were examined as electrochromic materials. Electro copolymerizat...
The molecular geometry and vibrational frequencies of N-phenyl-N′-(2-thienylmethylene)hydrazine (C11H10N2S) have been calculated using Hartree–Fock and density functional method (B3LYP) with 6-31G(d) basis set. The optimized geometric bond lengths and angles obtained using HF and DFT (B3LYP) a...
A new electron withdrawing monomer, cyano substituted (Z)-(thienylmethylene)-2-indolone (TEI(CN)) has been synthesized and polymerized with different donors to give three alternating donor/acceptor conjugated polymers. The cyano substituted polymers showed significantly reduced LUMO energy level...
HIV develops drug resistance at a high rate under drug selection pressure. Resistance tests are recommended to help physicians optimize antiretroviral drug therapies. For this purpose, genotypic and phenotypic tests have been developed. In order to propose a new phenotypic test that will be less...
ABSTRACTA colloidal gold-based immunochromatographic (IC) strip test was developed and validated for the detection of HIV-1 protease (HIV-PR) activity and inhibitory effect of HIV-PR inhibitors (PIs). It is a unique ‘two-step’ process requiring the combination of proteolysis of HIV-PR and an i...
Combination antiretroviral therapy (cART) is currently the most effective treatment for HIV-1 infection. HIV-1 protease inhibitors (PIs) are an important component of some regimens of cART. However, PIs are known for sub-optimal ADME properties, resulting in poor oral bioavailability. This often...
Pre-steady state kinetic analysis of mechanistic features of substrate binding and processing is crucial for insight into the evolution of inhibitor-resistant forms of HIV-1 protease. These data may provide a correct vector for rational drug design assuming possible intrinsic dynamic effects. Th...
The success of highly active antiretroviral therapy (HAART) in anti-HIV therapy is severely compromised by the rapidly developing drug resistance. HIV-1 protease inhibitors, part of HAART, are losing their potency and efficacy in inhibiting the target. Multi-drug resistant (MDR) 769 HIV-1 protea...
In connection with the intensive investigation of proteases, several methods have been developed for analysis of the substrate specificity. Due to the great number of proteases and the expected target molecules to be analyzed, time- and cost-efficient high-throughput screening (HTS) methods are ...
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