摘要 :
<abstract_text><p>Flavonoids are a large group of polyphenolic compounds that are present in almost all higher plants. Recent research demonstrated a wide range of biological effects of these compounds under both normal and variou...
展开
<abstract_text><p>Flavonoids are a large group of polyphenolic compounds that are present in almost all higher plants. Recent research demonstrated a wide range of biological effects of these compounds under both normal and various pathological conditions. Apparently, the biological activity of most flavonoids is due mainly to their ability to penetrate into cells and block enzymes of signaling pathways and transcription factors, including those involved in the activation, proliferation, and realization of effector functions of immune system cells. Moreover, it should be noted that flavonoids were highly efficacious in several instances in experimental therapy of model immune pathologies, suggesting that they were promising as platforms for creating new pharmacological agents that suppress or "normalize" the immune response.</p></abstract_text>
收起
摘要 :
<abstract_text><p>Two benzimidazole derivatives and one nitroimidazole derivative were designed using molecular hybridization approach. The designed compounds were synthesized and their in vitro antifungal activities were tested a...
展开
<abstract_text><p>Two benzimidazole derivatives and one nitroimidazole derivative were designed using molecular hybridization approach. The designed compounds were synthesized and their in vitro antifungal activities were tested against Candida albicans and Saccharomyces cerevisiae strains. Based on the antifungal activity data, compound 9 containing 2-methyl-5-nitroimidazole moiety proved to be the most potent compound. It was more active than the reference drugs fluconazole and ketoconazole against S. cerevisiae.</p></abstract_text>
收起
摘要 :
<abstract_text><p>The cerebrovascular and anti-ischemic effects of dopamine and synthetic docosahexaenoyldopamine (DHA-DA) and the GABA-DHA-DA conjugate (OXL1220) were compared and found to differ. Dopamine and DHA-DA increased bl...
展开
<abstract_text><p>The cerebrovascular and anti-ischemic effects of dopamine and synthetic docosahexaenoyldopamine (DHA-DA) and the GABA-DHA-DA conjugate (OXL1220) were compared and found to differ. Dopamine and DHA-DA increased blood flow in intact and ischemic brain that was associated with pronounced hypertensive reactions. The latter inhibited dopamine transporter with IC50 - 29 mu M but was practically inactive as a ligand for dopamine receptors. OXL1220 produced a selective vasodilating effect on blood flow in brain subjected to transient global ischemia. Only OXL1220 competed in vitro for specific binding sites of [H-3]-gabazine in rat-brain GABA(A)-receptors. Therefore, conjugation of a neuromediator (GABA) to the DHA-DA changed the dopaminergic activity of the compound to GABA-ergic with respect to vascular tone in ischemic brain.</p></abstract_text>
收起
摘要 :
<abstract_text><p>Despite advances in anticancer drug development and discovery, the survival of patients is so poor. A deep need for discovery of novel anticancer drugs is among priority issues in medicinal chemistry now. A new s...
展开
<abstract_text><p>Despite advances in anticancer drug development and discovery, the survival of patients is so poor. A deep need for discovery of novel anticancer drugs is among priority issues in medicinal chemistry now. A new series of 1,2,4-triazole derivatives were designed and synthesized by means of bioisosteric replacement. In vitro cytotoxicity evaluation was carried out with respect to PC3 (prostate carcinoma), HT29 (colorectal cancer) and SKNMC (neuroblastoma) cell lines using MTT assay, and the obtained results were compared to imatinib as a reference drug. Spectroscopic methods including H-1 NMR, IR, and MS were used for characterization of the synthesized compounds. Generally, none of the tested compounds showed superior activity in comparison to imatinib against PC3 and SKNMC cell lines. However, compound 3b (IC50 = 3.69 +/- 0.9 mu M) and 3e (IC50 = 15.31 +/- 2.1 mu M) exhibited higher activity than imatinib (18.1 +/- 2.6) against HT29 cells. Some of the obtained 1,2,4-triazole derivatives can be proposed as potential anticancer agents - in particular, against colorectal cancer - but further structural modifications and experimental tests are needed to increase the anticancer activity.</p></abstract_text>
收起
摘要 :
<abstract_text><p>The key intermediates 3H-imidazo[4 ',5 ':3,4]benzo[c] isoxazoles were synthesized by the reaction of N-alkyl-5-nitrobenzimidazoles with aryl acetonitriles under basic conditions. These compounds were converted to...
展开
<abstract_text><p>The key intermediates 3H-imidazo[4 ',5 ':3,4]benzo[c] isoxazoles were synthesized by the reaction of N-alkyl-5-nitrobenzimidazoles with aryl acetonitriles under basic conditions. These compounds were converted to 3H-imidazo[4,5-a]acridin-11(6H)-ones by the Tanasescu reaction in excellent yields. The structures of all newly synthesized compounds were confirmed by IR, H-1 NMR, and mass spectroscopic data. The interactions of 3H-imidazo[4,5-a] acridin-11-ones with human serum albumin (HSA) have been studied by fluorescence spectroscopy. The binding of 3H-imidazo[4,5-a] acridin-11(6H)-ones quenches the HSA fluorescence, revealing a 1 : 1 interaction with a binding constant of about 4.50 x 10(4) - 1.25 x 10(5) M-1. A decrease in the fluorescence intensity at 339.41 nm, when excited at 280 nm, is attributed to changes in the environment of protein fluorophores caused by the presence of the ligands. Differences in the interactions of 3H-imidazo[4,5-a] acridin-11(6H)-one derivatives with HSA were observed using the spectrofluorimetry technique. Thermodynamic characteristics and the parameters of HSA binding with these compounds are in accordance with the antibacterial activity of various derivatives of 3H-imidazo[4,5-a] acridin-11(6H)-one.</p></abstract_text>
收起
摘要 :
<abstract_text><p>The reaction in aqueous medium of phytic acid (myo-inositol hexakisphosphate) and glucosamine hydrochloride (2-amino-2-deoxy-beta-D-glucopyranose hydrochloride) formed phytic acid-glucosamine complexes of formula...
展开
<abstract_text><p>The reaction in aqueous medium of phytic acid (myo-inositol hexakisphosphate) and glucosamine hydrochloride (2-amino-2-deoxy-beta-D-glucopyranose hydrochloride) formed phytic acid-glucosamine complexes of formula InsP(6) . 5GA. Their compositions were proved by elemental analysis for C, H, N, and P. IR, PMR, C-13 NMR, and P-31 NMR spectroscopy and potentiometric titration showed that the complexes of phytic acid and glucosamine were formed by H-bonds and electrostatic salt interactions. High antioxidant activity against lipid peroxidation and a positive effect on superoxide dismutase activity were found for complexes of InsP(6)H(12) and glucosamine in in vitro studies of human blood plasma under oxidative stress.</p></abstract_text>
收起
摘要 :
<abstract_text><p>New 2-amino-6-ethoxybenzothiazole derivatives were synthesized and tested for their influence on physical work capacity in mice. It was shown that a pyridylidene or furylidene radical on the amine or a formulatio...
展开
<abstract_text><p>New 2-amino-6-ethoxybenzothiazole derivatives were synthesized and tested for their influence on physical work capacity in mice. It was shown that a pyridylidene or furylidene radical on the amine or a formulation with carboxypentanoate were important for producing effective new 2-amino-6-ethoxybenzothiazole derivatives. These compounds were either more effective or comparable with the well-known actoprotectors metaprot and ladasten, which are used at significantly higher doses.</p></abstract_text>
收起
摘要 :
<abstract_text><p>Microcrystals of 6 alpha-methyl-16 alpha,17 alpha-cyclohexapregn-4-ene-3,20-dione(mecigestone) that differed from the starting drug substance by decreased sizes and altered morphologies were produced using a Nano...
展开
<abstract_text><p>Microcrystals of 6 alpha-methyl-16 alpha,17 alpha-cyclohexapregn-4-ene-3,20-dione(mecigestone) that differed from the starting drug substance by decreased sizes and altered morphologies were produced using a Nano Spray Dryer B-90 (Buchi, Switzerland) that allowed operation with organic solvents in a closed cycle. The bioavailability of starting crystalline and micronized mecigestone drug substance was studied by oral administration to laboratory white rats. Mecigestone was extracted from rat blood serum using solvent extraction. The extraction coefficient was 64%. The detection limit of the drug substance was 0.08 ng/mL. The content of unaltered mecigestone in the extracts was determined using HPLC with high-resolution mass spectrometric detection. Micronized mecigestone was 7.5 times more bioavailable than the starting drug substance.</p></abstract_text>
收起
摘要 :
<abstract_text><p>A series of phenyl- and alkylthiocarbamides were synthesized by the reaction of 2,9-disubstituted imidazo-[1,2-a]benzimidazoles with phenyl- and alkylisothiocyanates. The structures of the products were confirmed...
展开
<abstract_text><p>A series of phenyl- and alkylthiocarbamides were synthesized by the reaction of 2,9-disubstituted imidazo-[1,2-a]benzimidazoles with phenyl- and alkylisothiocyanates. The structures of the products were confirmed by elemental analysis and PMR spectroscopy. Some of the synthesized compounds were capable of inhibiting non-enzymatic glycosylation of proteins. The concentration dependences of the antiglycation effect of the most active substances and aminoguanidine were studied.</p></abstract_text>
收起
摘要 :
Ethyl-2-amino-1-benzamido-4-oxo-5-(2-oxo-2-arylethylidene)pyrrolidine-3-carboxylates (IIa-g) were synthesized via recyclization of 3-(2-benzoylhydrazono)-5-arylfuran-2(3H)-ones (I) through the action of ethylcyanoacetate. The synt...
展开
Ethyl-2-amino-1-benzamido-4-oxo-5-(2-oxo-2-arylethylidene)pyrrolidine-3-carboxylates (IIa-g) were synthesized via recyclization of 3-(2-benzoylhydrazono)-5-arylfuran-2(3H)-ones (I) through the action of ethylcyanoacetate. The synthesized compounds were screened for biological activity and were found to have low toxicity. Ethyl-2-amino-1-benzamido-5-[2-(3, 4-dimethoxyphenyl)-2-oxoethylidene]-4-oxopyrrolidine-3-carboxylate exhibited antiradical activity in a diphenylpicrylhydrazyl (DPPH)-binding assay that was greater than that of the reference drug trolox. This same compound showed anti-inflammatory activity in a carrageenan edema model that was greater than that of diclofenac sodium. Assessment of antihypoxic activity in an acute normobaric hypoxia test found that ethyl-2-amino-1-benzamido-5-[2-oxo-2-(4-methylphenyl)ethylidene]-4-oxopyrrolidine-3-carboxylate was comparable with the succinic acid standard.
收起
原文获取