Hitherto unknown unsymmetrical squaraines containing 2,3-dihydro-1H-perimidine terminal groups that are linked through the 4-position and the 6-positions of the 2,3-dihydro-1H-perimidine terminal groups to the four membered squaraine ring, were obtained as minor products in the reaction of squar...

Inhibition of MAO-B has been an effective strategy for the treatment of Parkinson’s disease. To find more potent and selective MAO-B inhibitors with novel chemical scaffold, we designed and synthesized a series of new 2,3-dihydro-1H-inden-1-amine derivatives on basis of our previous study. Furt...

The first greenest methodology for the synthesis of 2,3-dihydro-1H-perimidines on water is described. 1,8-Diamino naphthalene was reacted with different types of aldehydes at room temperature to furnish the product in moderate to excellent yields in 30 min. A multi-gram scale reaction is also pe...

Borage oil (BO) reverses a disrupted epidermal lipid barrier and hyperproliferation in essential fatty acid deficiency (EFAD). However, little is known about its effect on skin pH, which is maintained by epidermal lactate, free fatty acids (FFAs), and free amino acids (FAAs) which is generated b...

A metal-free cross coupling between common CH2Cl2 and carboxylic acids has been achieved with K2CO3 as the sole additive. This simple protocol is a convenient and cost-effective route to synthesize methylene diesters from a wide scope of carboxylic acids substrates with good functional group tol...

The Culex quinquefasciatus mosquito is a vector of several diseases, and its control has been performed with synthetic insecticides, which may have human and environmental side effects. Thus, the use of new and safe molecules are important, and this study evaluated the toxicity of active substan...

Caffeic acid (CA) is a plant metabolite acting as a carcinogenic inhibitor, and exhibits a high antioxidant effect and some antimicrobial activity. Besides, this compound can be useful in the prevention of heart diseases and atherosclerosis, among others. The present study aims to determine the ...

Reaction of 2-iodo-3-nitrobenzoic acid with arylalkynyl copper(I) reagent gave 3-aryl-5-nitroisocoumarins. Castro–Stephens coupling was followed by in situ Cu-catalysed ring-closure. 1H NMR and X-ray crystallography showed the cyclisations to be 6-endo, contrasting with reports of 5-exo cyclisa...

1-Palmitoyl-2-thiopalmitoyl phosphatidylcholine (2-thioPC), a structurally modified phospholipid analog is specifically hydrolyzed by phospholipase A2 to liberate 2-thiolysophosphatidylcholine and palmitic acid. The sulfhydryl group of the product is readily trapped by 5,5′-dithiobis (2-nitrobe...

The nonlinear optical properties of hydrazones substituted with different donor groups were studied using single beam Z-scan technique with nanosecond laser pulses at 532 nm. The nonlinear response in these molecules was found to increase with increase in the donor strength of the substituted gr...

A series of 4-(2-fluorophenoxy)quinoline derivatives containing an acylhydrazone moiety were designed, synthesized and evaluated for their in vitro biological activities against c-Met kinase and five cancer cell lines (A549, H460, HT-29, MKN-45, and U87MG). Most compounds showed weak to excellen...

ABSTRACTMethionine is considered one of the most important essential AA for milk protein synthesis in dairy cows. Supplementation of unprotected, free Met is nearly 100% degraded by ruminal microorganisms, which complicates supplementation. 2-Hydroxy-4-methylthio-butanoic acid (HMTBa) can be con...

ABSTRACT2-Hydroxy-4-(methylthio)butanoate (HMTBa) is a methionine analog that has been observed to attenuate biohydrogenation (BH)-induced milk fat depression (MFD), possibly through reducing the shift to altered BH pathways. It has also been suggested that HMTBa increases microbial protein synt...

Aimed at the chemotherapy of chronic pain two kinds of analgesic pharmacophores, substituted purine and Gly-AA-OBzl, were coupled via a five-step-reaction procedure and 19 novel conjugates N-[2-chloro-9-(tetrahydropyran-2-yl)-9H-purin-6-yl]-N-cyclopropylglycylamino acid benzylesters were provide...

From the anti-tumor active N-tryptophanyl-β-carboline-3-carboxylic acid benzyl ester and β-carboline-3-carbonyltryptophan benzyl ester, a pharmacophore, Trp-Trp-OBzl, was drawn. Based on the DOCK scores amino acid residue was inserted into the C-terminus of Trp-Trp-OBzl and twenty Trp-Trp-AA-O...

Among the CCK derivatives, the tetrapeptide Boc-Trp-Phg-Asp-Nal-NH2 (1) behaves as a short potent CCK-B agonist which led to the development of an efficient peptidase-resistant CCK-B antagonist by bismethylation of its terminal CONH2 group. Further modifications of the N- and C-terminal moieties...

The oligopeptide transporter, which is responsible for the absorption of various di/tripeptides and several peptidomimetic drugs across the intestinal epithelia, is expressed in mature Caco-2 monolayers. Using certain enzymatically stable dipeptides containing either l- or d-aspartic acid at the...

Synthetic caspase inhibitors and particularly broad-spectrum caspase inhibitors can prevent cells from death or at least slow down cell death process and abrogate some apoptotic hallmarks [Kitanaka, C., Kuchino, Y., 1999. Caspase-independent programmed cell death with necrotic morphology. Cell D...

Treatment of [(η5-C5Me5)Ir(H2O)3](CF3SO3)2 with adenine (AH) and 9-ethyladenine (9-EtA) affords the respective tetra- and trinuclear complexes [{(η5-C5Me5)Ir(A)}4](CF3SO3)4 (1) and [{(η5-C5Me5)Ir(9-EtAH−1)}3](CF3SO3)3 (2), whose structures were established by X-ray analysis. The former compou...

Treatment of [Cp*RuCl2]2 (1a) (Cp* = η5-C5Me5) with NaBr KI leads to the complexes [Cp*RuBr2]2 (1b) and [Cp*RuI2]2 1c). Reduction of these RuIII halides with cobaltocene gives pentane-soluble, paramagnetic, molecular mixed valence RuIII/II complexes [Cp*Ru(μ-X)3RuCp*] (3a, 3b, 3c) and on furth...