Organic and Medicinal Chemistry Letters

BACKGROUND: Aryl sulfides have significant importance from biological and pharmaceutical aspects. Transition metal-catalyzed carbon-sulfur cross-coupling reaction represents an important tool for the synthesis of sulfides. Among various transition metals, copper salts or oxides have found vast applicability. RESULTS: A simple procedure for the preparation of poly-ionic amberlite resins embedded with copper oxide nanoparticles (CuO NPs) (denoted as CuO@ARF) has been developed, characterized, and employed for the first time as a heterogeneous ligand-free catalyst for 'on-water' C-S cross-coupling reaction...

BACKGROUND: 1,8-Naphthyridine derivatives have attracted considerable attention because the 1,8-naphthyridine skeleton is present in many compounds that have been isolated from natural substances, with various biological activities. FINDINGS: N,N-dimethoxy-N-methyl-1,8-naphthyridine-3-carboxamide (1) on reaction with Grignard reagent forms 2-methoxy-1,8-naphthyridine-3-carbaldehyde (2). Compound 2 on reaction with different aromatic aldehydes provided 1-(2-cyclopropyl-1,8-naphthyridin-3-yl)-3-arylprop-2-en-1-ones (3a-e) and these compounds on cyclisation with hydrazine hydrate 99% yielded 2-cyclopropyl-3-(5-aryl-1H-pyrazol-3-yl)-1,8-naphthyridines (4-a-e)...

BACKGROUND: A rapid and sensitive ultraviolet-visible (UV-VIS) spectroscopic method was developed for the estimation of pyrimidine derivative 6-Bromo-3-(6-(2,6-dichlorophenyl)-2-(morpolinomethylamino) pyrimidine4-yl) -2H-chromen-2-one (BT10M) in bulk form. RESULTS: Pyrimidine derivative was monitored at 275 nm with UV detection, and there is no interference of diluents at 275 nm. The method was found to be linear in the range of 50 to 150 μg/ml. The accuracy and precision were determined and validated statistically...

BACKGROUND: Benzimidazoles and triazoles are useful structures for research and development of new pharmaceutical molecules and have received much attention in the last decade because of their highly potent medicinal activities. FINDINGS: A simple and efficient synthesis of triazole was carried out by treatment of 2-(4-azidophenyl)-1H-benzo[d]imidazole (6) with different types of terminal alkynes in t-BuOH/H2O, sodium ascorbate, and Zn(OTf)2, screened for cytotoxicity assay and achieved good results...

BACKGROUND: Macrotyloma uniflorum Linn (Fabaceae) is a herbaceous plant with annual branches. It is used in kidney stones, inflamed joints, fever, musculoskeletal disorders, sinus wounds and localized abdominal tumors. It is reported as an antioxidant and nutraceutical (forage and food). GC-MS analysis of ethanol extract has led to identification of twenty-eight compounds from M. uniflorum by comparison of their retention indices and mass spectra fragmentation patterns with those stored on the GC-MS computer library...

BACKGROUND: Leishmaniasis is a neglected tropical parasitic diseases affecting millions of people around the globe. Quinazolines are a group of compounds with diverse pharmacological activities. Owing to their promising antileishmanial activities, some 3-aryl-2-(substitutedstyryl)-4(3H)-quinazolinones were synthesized in good yields (65.2% to 86.4%). RESULTS: The target compounds were synthesized by using cyclization, condensation, and hydrolysis reactions. The structures of the synthesized compounds were determined using elemental microanalysis, infrared (IR), and proton nuclear magnetic resonance ((1)H NMR)...

BACKGROUND: Azaheterocycles are an important class of compounds because of their highly potent medicinal activities, and the imidazole subcategory is of special interest in regard to drug discovery research. FINDINGS: An expeditious synthetic protocol of 2-aryl-4-phenyl-1H-imidazoles has been accomplished by reacting phenylglyoxal monohydrate, ammonium acetate, and aldehyde under sonication. Following this green approach a series of 2-aryl-4-phenyl-1H-imidazoles has been synthesized using diversely substituted aldehydes...

BACKGROUND: The current investigation sought to explore the nature of the secondary metabolites in the algae, Laurencia pacifica. RESULTS: This report details the first isolation of the sesquiterpenes isoaplysin (1), isolaurenisol (2), debromoisolaurinterol (3), debromoaplysinol (4), laur-11-en-10-ol (5), 10α-hydroxyldebromoepiaplysin (6), and the previously unknown 10-bromo-3,7,11,11-tetramethylspiro[5.5]undeca-1,7-dien-3-ol (7) from the algae, Laurencia pacifica...

BACKGROUND: Malaria is an endemic disease affecting many countries in Tropical regions. In the search for compound hits for the design and/or development of new drugs against the disease, many research teams have resorted to African medicinal plants in order to identify lead compounds. Three-dimensional molecular models were generated for anti-malarial compounds of African origin (from 'weakly' active to 'highly' active), which were identified from literature sources. Selected computed molecular descriptors related to absorption, distribution, metabolism, excretion and toxicity (ADMET) of the phytochemicals have been analysed and compared with those of known drugs in order to access the 'drug-likeness' of these compounds...

BACKGROUND: The aim of this study was to evaluate the effects of nitroxin biofertilizer and chemical fertilizer on the growth, yield, and essential oil composition of dill. The experiment was conducted under field condition in randomized complete block design with three replications and two factors. RESULTS: The first factor was the concentrations of nitroxin biofertilizer (0%, 50%, and 100%) of the recommended amount (1 l of biological fertilizer for 30 kg of seed)...

BACKGROUND: A series of 6-(substituted aldehyde)-3,4-dihydro-1-(tetrahydro-3,4-dihydroxy-5-(hydroxymethyl) furan-2-yl)-4-phenylpyrimidine-2(1H)-one derivative (6A-6P) was synthesized from the 6-(substituted aldehyde)-4-phenylpyrimidine-2(1H)-one derivative (5A-5P) through following reaction mechanisms Claisen-Schmidt, Cyclization, and Satos fusion. The structures of the synthesized compounds were elucidated by I.R.,(1)H-NMR, elemental analysis, and mass spectroscopic techniques. RESULT: The synthesized compounds were screened for in vitro antifungal activity at 25, 50, 100, and 200 μg/ml concentrations...

BACKGROUND: Nanotechnology is now regarded as a distinct field of research in modern science and technology with multifaceted areas including biomedical applications. Among the various approaches currently available for the generation of metallic nanoparticles, biogenic synthesis is of increasing demand for the purpose of green nanotechnology. Among various natural sources, plant materials are the most readily available template-directing matrix offering cost-effectiveness, eco-friendliness, and easy handling...

BACKGROUND: Schiff's bases are excellent ligands which are synthesized from the condensation of primary amines with carbonyl groups. FINDINGS: The classical reaction for the synthesis of Schiff's bases in an ethanolic solution and glacial acetic acid as a catalyst was followed in the synthesis of substituted sulfamethoxazole compounds. CONCLUSIONS: Some Schiff's bases containing sulfamethoxazole nucleus have been synthesized and characterized...

BACKGROUND: The aim of this study was to evaluate the effect of nano silver and silver nitrate on yield of seed in basil plant. The study was carried out in a randomized block design with three replications. RESULTS: Four levels of either silver nitrate (0, 100, 200 and 300 ppm) or nano silver (0, 20, 40, and 60 ppm) were sprayed on basil plant at seed growth stage. The results showed that there was no significant difference between 100 ppm of silver nitrate and 60 ppm concentration of nano silver on the shoot silver concentration...

BACKGROUND: The aim of the current investigation was to identify bioactive secondary metabolites including phenols, tannins, flavonoids, terpinedes, and steroids and compare the phytochemical analysis and antioxidant profile of the juice extracted from the fruits of Citrus sinensis, Citrus anrantifolia, and Citrus limonum. RESULTS: Phytochemical screening is important for the isolation of new, novel, and rare secondary metabolites before bulk extraction. Phytochemical analysis of the desired plant fruits of family Rutaceae revealed the presence of phenols, flavonoids, reducing sugars, steroids, terpinedes and tannins...

BACKGROUND: Phenylazonaphtol-β-D-O-glycosides are alternative substrates for the detection of enzymatic activity of β-glycosidases which are involved in various important processes. These azoic compounds are currently exploited as prodrugs for colonic disease due the presence of β-glycosidase activity in the gut flora and therefore allowing the release of the drug at the specific site. RESULTS: Phenylazonaphtol-β-D-O-glucoside 3a and galactoside 3b were prepared via diazonium salt conditions under weak acidic conditions which do not compromise the O-glycosidic bond stability, by coupling reaction between 2-naphtol sodium salt with aminoglycosides 1a and 1b...

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BACKGROUND: The level of expression of cannabinoid receptor type 2 (CB2R) in healthy and diseased brain has not been fully elucidated. Therefore, there is a growing interest to assess the regional expression of CB2R in the brain. Positron emission tomography (PET) is an imaging technique, which allows quantitative monitoring of very low amounts of radiolabelled compounds in living organisms at high temporal and spatial resolution and, thus, has been widely used as a diagnostic tool in nuclear medicine...

BACKGROUND: Drug metabolism and pharmacokinetic (DMPK) assessment has come to occupy a place of interest during the early stages of drug discovery today. Computer-based methods are slowly gaining ground in this area and are often used as initial tools to eliminate compounds likely to present uninteresting pharmacokinetic profiles and unacceptable levels of toxicity from the list of potential drug candidates, hence cutting down the cost of the discovery of a drug. RESULTS: In the present study, we present an in silico assessment of the DMPK profile of our recently published natural products database of 1,859 unique compounds derived from 224 species of medicinal plants from the Cameroonian forest...

BACKGROUND: Pyrazole and pyrazolone motifs are well known for their wide range of biological activities such as antimicrobial, anti-inflammatory, and antitumor activities. The incorporation of more than one pharmacophore in a single scaffold is a well known approach for the development of more potent drugs. In the present investigation, a series of differently substituted 4-arylidene pyrazole derivatives bearing pyrazole and pyrazolone pharmacophores in a single scaffold was synthesized...