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Jee Hee Suh et al.
Chemical & pharmaceutical bulletin, 63(8), 573-578 (2015-06-05)
We describe the synthesis and biological evaluation of N-aryl-5-aryloxazol-2-amine derivatives that are able to inhibit 5-lipoxygenase (5-LOX), a key enzyme of leukotriene synthesis, for the treatment of inflammation-related diseases including asthma and rheumatoid arthritis. A novel structural moiety containing oxazole...
Kuruva Chandra Sekhar et al.
Daru : journal of Faculty of Pharmacy, Tehran University of Medical Sciences, 22, 76-76 (2014-12-30)
Chronic and oral administration of benzylamine improves glucose tolerance. Picolylamine is a selective functional antagonist of the human adenosine A2B receptor. Phosphonic diamide derivatives enhance the cellular permeability and in turn their biological activities. A series of heteroaryl phosphonicdiamide derivatives...
Benjamin J Pages et al.
Dalton transactions (Cambridge, England : 2003), 43(41), 15566-15575 (2014-09-10)
Eight platinum(II) complexes with anticancer potential have been synthesised and characterised. These complexes are of the type [Pt(I(L))(A(L))](2+), where I(L) is either dipyrido[3,2-f:2',3'-h]quinoxaline (dpq) or 2,3-dimethyl-dpq (23Me2dpq) and A(L) is one of the R,R or S,S isomers of either 1,2-diaminocyclohexane...
Xiu-Mei Li et al.
European journal of medicinal chemistry, 96, 436-444 (2015-04-29)
Hypericum ascyron L. has been used as a traditional medicine for the treatment of wounds, swelling, headache, nausea and abscesses in China for thousands of years. However, modern pharmacological studies are still necessary to provide a scientific basis to substantiate...
Aditya Kapil Valiveti et al.
Chemico-biological interactions, 237, 125-132 (2015-06-14)
A series of mono pyridinium oximes linked with arenylacetamides as side chains were synthesized and their in vitro reactivation potential was evaluated against human acetylcholinesterase (hAChE) inhibited by organophosphorus inhibitors (OP) such as sarin, VX and tabun. The reactivation data...
Virsinha Reddy et al.
Organic & biomolecular chemistry, 13(12), 3732-3741 (2015-02-18)
An efficient and mild protocol for the direct construction of aryl- and alkyl-substituted isoquinolines has been realized through silver nitrate catalyzed aromatic annulation of o-(1-alkynyl)arylaldehydes and ketones with ammonium acetate. The salient feature of this methodology is that this annulation...
Phuong Hoang Tran et al.
Molecules (Basel, Switzerland), 20(10), 19605-19619 (2015-10-31)
A fast and green method is developed for regioselective acylation of indoles in the 3-position without the need for protection of the NH position. The method is based on Friedel-Crafts acylation using acid anhydrides. The method has been optimized, and...
Wieland Peschel et al.
Talanta, 140, 150-165 (2015-06-07)
The medicinal use of different chemovars and extracts of Cannabis sativa L. requires standardization beyond ∆9-tetrahydrocannabinol (THC) with complementing methods. We investigated the suitability of (1)H NMR key signals for distinction of four chemotypes measured in deuterated dimethylsulfoxide together with...
Ahmed M Younis et al.
International journal of medicinal mushrooms, 17(6), 579-590 (2015-09-10)
Pleurotus ostreatus is an edible mushroom that also has high medicinal values. In this study, P. ostreatus was tested for its ability to inhibit the growth of fungi and bacteria. The freeze-dried fruiting body, broth from submerged culture, and mycelial...
Yingli Yang et al.
Oncology reports, 34(3), 1311-1318 (2015-07-03)
In the present study, 2-pyridinecarboxaldehyde 2-pyridinecarboxylic acid hydrazone (PPAH) was prepared and its antitumor activity was evaluated. The inhibition of proliferation of PPAH against the HepG2 and HCT-116 cell lines was less effective, yet in the presence of copper ions...
Anja Balk et al.
Pharmaceutical research, 32(6), 2154-2167 (2014-12-24)
A poorly water soluble acidic active pharmaceutical ingredient (API) was transformed into an ionic liquid (IL) aiming at faster and higher oral availability in comparison to a prodrug. API preparations were characterized in solid state by single crystal and powder...
Pavla Simerska et al.
Drug delivery and translational research, 4(3), 246-255 (2015-03-20)
Peptide-based vaccine delivery can be hampered by rapid peptidase activity and poor inherent immunogenicity. The self-adjuvanting lipid core peptide system (LCP) has been shown to confer improved stability and immunogenicity on peptide epitopes of group A Streptococcus, Chlamydia, hookworm, and...
Chi-Yuan Cheng et al.
Biophysical journal, 109(2), 330-339 (2015-07-23)
Dimethyl sulfoxide (DMSO) has been broadly used in biology as a cosolvent, a cryoprotectant, and an enhancer of membrane permeability, leading to the general assumption that DMSO-induced structural changes in cell membranes and their hydration water play important functional roles....
Denis A Babkov et al.
Bioorganic & medicinal chemistry, 23(21), 7035-7044 (2015-10-08)
The need for novel therapeutic options to fight herpesvirus infections still persists. Herein we report the design, synthesis and antiviral evaluation of a new family of non-nucleoside antivirals, derived from 1-[ω-(4-bromophenoxy)alkyl]uracil derivatives--previously reported inhibitors of human cytomegalovirus (HCMV). Introduction of...
Chung Ying Chan et al.
Dalton transactions (Cambridge, England : 2003), 44(44), 19126-19140 (2015-10-20)
A series of eight Rhenium(I)-N-heterocyclic carbene (NHC) complexes of the general form [ReCl(CO)3(C^C)] (where C^C is a bis(NHC) bidentate ligand), [ReCl(CO)3(C^C)]2 (where C^C is a bis-bidentate tetra-NHC ligand) and [Re(CO)3(C^N^C)](+)[X](-) (where C^N^C is a bis(NHC)-amine ligand and the counter ion...
Unraveling the dissociation of dimethyl sulfoxide following absorption at 193 nm.
Blank DA, et al.
J. Chem. Phys. , 106(2), 539-550 (1997)
Jinyun Dong et al.
Bioorganic & medicinal chemistry, 22(24), 6876-6884 (2014-12-04)
Bcr-Abl plays an essential role in the pathogenesis and development of chronic myeloid leukaemia (CML). Inhibition of Bcr-Abl has great potential for therapeutic intervention in CML. In order to obtain novel and potent Bcr-Abl inhibitors, twenty seven 4,6-disubstituted pyrimidines were...
Amir Mahboubi et al.
Plant physiology, 168(2), 478-489 (2015-05-02)
Wood of trees is formed from carbon assimilated in the photosynthetic tissues. Determining the temporal dynamics of carbon assimilation, subsequent transport into developing wood, and incorporation to cell walls would further our understanding of wood formation in particular and tree...
Daishun Ling et al.
ACS nano, 8(8), 8027-8039 (2014-08-06)
Hepatocellular carcinoma (HCC) has one of the worst prognoses for survival as it is poorly responsive to both conventional chemotherapy and mechanism-directed therapy. This results from a lack of therapeutic concentration in the tumor tissue coupled with the highly toxic...
Iwona Kowalska et al.
Journal of agricultural and food chemistry, 62(46), 11200-11208 (2014-10-31)
Fourteen phenolic compounds (flavonoids and phenolic acids) were isolated and 19 were identified in the aerial parts of Triticum aestivum L. The structures of these compounds were established on the basis of the data obtained by electrospray ionization-mass spectrometry (ESI-MS)...
Navneet Chandak et al.
Journal of enzyme inhibition and medicinal chemistry, 29(4), 476-484 (2013-06-20)
Synthesis of total eighteen 2-amino-substituted 4-coumarinylthiazoles including sixteen new compounds (3a-o and 5b) bearing the benzenesulfonamide moiety is described in the present report. All the synthesized target compounds were examined for their in vivo anti-inflammatory (AI) activity and in vitro...
Vincenzo Taresco et al.
The journal of physical chemistry. B, 119(26), 8369-8379 (2015-06-16)
Amphiphilic polyelectrolytes (APEs), exhibiting particular self-association properties in aqueous media, can be used in different industrial applications, including drug delivery systems. Their typical core-shell structure (micelle) depends on the balance of interactions between hydrophobic and ionizable monomer units. In this...
Hannu Elo et al.
European journal of medicinal chemistry, 92, 750-753 (2015-01-27)
Certain substituted salicylaldehydes are potent antibacterial and antifungal agents and some of them merit consideration as potential chemotherapeutic agents against Candida infections, but their mechanism of action has remained obscure. We report here a distinct correlation between broadening of the...
Yan Tan et al.
Biomaterials, 56, 219-228 (2015-05-03)
Serious challenges remain in immunotherapy, such as to effectively deliver antigens and non-invasively monitor biological processes. Therefore, we aim to design a useful nanocarrier for enhancing antigen-specific immune response and performing functional molecular imaging guided immunotherapy. To achieve this goal...
Lenka Roubalová et al.
Bioorganic & medicinal chemistry, 23(17), 5402-5409 (2015-08-12)
Quercetin 3'-O-sulfate is one of the main metabolites of the natural flavonoid quercetin in humans. This study was designed to prepare quercetin 3'-O-sulfate (1), isoquercitrin 4'-O-sulfate (2) and taxifolin 4'-O-sulfate (3) by the sulfation of quercetin, isoquercitrin (quercetin 3-O-glucoside) and...
Nicola Parisi et al.
International journal of pharmaceutics, 493(1-2), 404-411 (2015-08-04)
Hexamidine diisethionate (HEX D) has been used in the personal care industry and in a number of over-the-counter (OTC) drug products as an antimicrobial agent since the 1950's. Recently, the compound has also been investigated for its beneficial effects on...
Yasemin Sahbaz et al.
Molecular pharmaceutics, 12(6), 1980-1991 (2015-04-24)
Absorption after oral administration is a requirement for almost all drug products but is a challenge for drugs with intrinsically low water solubility. Here, the weakly basic, poorly water-soluble drugs (PWSDs) itraconazole, cinnarizine, and halofantrine were converted into lipophilic ionic...
Zongwang Ma et al.
Applied biochemistry and biotechnology, 177(7), 1520-1529 (2015-09-17)
Bacillus mojavensis B0621A was isolated from the mantle of a pearl oyster Pinctada martensii collected from South China Sea. Semi-purified surfactins (225 mg L(-1)) were obtained by acid precipitation and vacuum flash chromatography. The component of the semi-purified surfactins was preliminarily analyzed...
Tristan Gollnest et al.
Nature communications, 6, 8716-8716 (2015-10-28)
The antiviral activity of nucleoside reverse transcriptase inhibitors is often limited by ineffective phosphorylation. We report on a nucleoside triphosphate (NTP) prodrug approach in which the γ-phosphate of NTPs is bioreversibly modified. A series of TriPPPro-compounds bearing two lipophilic masking...
Ting-Ting You et al.
Bioresource technology, 199, 271-274 (2015-09-14)
Acid enhanced ionic liquid (IL) 1-n-butyl-3-methylimidazolium chloride ([C4 mim]Cl) pretreatment has shown great potential for boosting the yield of sugars from biomass cost-effectively and environmental-friendly. Pretreatment with shorter processing time will promote the commercial viability. In this work, pretreatment of...
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