A group of alkyl 7,7-dihalo-3-methyl-5-(2- or 3-nitrophenyl)-2-azabicyclo[4.1.0]hept-3-ene-4-carboxylates were prepared by reaction of dihalocarbenes (:CX2, X = Br, Cl) with alkyl 2-methyl-4-(2- or 3-nitrophenyl)-1,4-dihydropyridine-3-carboxylates. In vitro calcium channel antagonist activities ...

The synthesis and characterization of several new dimethylgold(III) complexes are reported along with the X-ray crystal structure of [(CH32AuSC2H5]2. The latter compound crystallizes in a triclinic space group P1, a = 6.193(1) Å, b = 7.852(1) Å, c = 14.614(3) Å, α = 92.36(1)°, β = 93.99(2)°,...

Zafirlukast is an oral leukotriene receptor antagonist (LTRA) for the treatment of pulmonary disorders such as asthma. During the process development of zafirlukast, eight process related impurities were observed at a level of 0.1–0.15 area percent. Synthesis and characterization of these impur...

The West Nile virus (WNV) has spread throughout the world causing neuroinvasive diseases with no treatments available. The viral NS2B-NS3 protease is essential for WNV survival and replication in host cells and is a promising drug target. Through an enzymatic screen of the National Institute of ...

Zafirlukast, a leukotriene receptor antagonist, has been shown to exert a wide range of effects including anti-asthmatic, anti-inflammatory and oral anti-bacterial. Osteoarthritis is one of the most prevalent age-related public health burdens in the modern world. In the present study, we applied...

Endothelial dysfunction induced by chronic inflammation has been considered one of the most important mechanisms behind a variety of cardiovascular diseases. Extensive efforts have been made in past decades to explore the underlying mechanisms of endothelial dysfunction and to develop new therap...

An efficient and multifunctional three component synthetic protocol was developed to synthesize ethyl 6-amino-4-aryl-5-cyano-2-propyl-4H-pyran-3-carboxylates from ethyl 3-oxohexanoate, malononitrile and corresponding aldehydes (1a–11a) using K2CO3 as a catalyst under water solvent in good yield...

In the present study, we report the discovery of a novel class of substituted 4-amino-2-thiopyrimidines as antiangiogenic and antiproliferative agents. Structural hybridization between 4-substituted aminopyrimidines (VEGFR-2 inhibitors) and 2-thioxopyrimidines (BRAF inhibitors) was carried out t...

The crystal structure of 2-amino-N′-[(1Z)-1-(4-chlorophenyl)ethylidene]benzohydrazide (I) is determined by X-ray diffraction at room temperature. The structure of I also was characterized by elemental analysis, mass, FT-IR and NMR spectroscopic techniques. The compound crystallizes in triclinic...

Copper (II) complexes are promising in the development of new synthetic models for cancer treatment. In this context, we synthesized a new copper complex containing the pharmacophore group 1,4-dioxo-2-butenyl, the Bis(((Z)-4-((4-chlorophenyl) amino)-4-oxobut-2-enoyl)oxy) copper compound and we e...

A simple and efficient one-pot synthesis of tetrahydrobenzo[b]pyrans from the three-component reaction between dimedone, aldehydes, and active methylene compounds using NH4Al(SO4)2·12H2O (Alum) as a catalyst at 80 °C is described. The catalyst exhibits remarkable reactivity and is reusable.

A novel quinazoline Schiff base ligand, 3-((5-bromo-2-hydroxy-3-methoxybenzylidene)amino)-2-methylquinazolin-4(3H)-one [HL] and its mixed-ligand Cu(II) complex [Cu(L′)(Imi)], [L′] = 2-acetamido-N-(5-bromo-2-oxidobenzylidene) benzohydrazonate, [Imi] = imidazole, were synthesized and characteriz...

The methanolysis of aldgamycin E yields, in addition to methyl mycinoside, two anomeric carbonate containing methyl glycosides, A and B. The structures of the two carbonate sugars have been elucidated and found to belong to the D series.

The broad spectrum antibiotic sorangicin A (1) has been isolated from Sorangium cellulosum, and its structure was determined spectroscopically as a 31-membered macrocyclic hydroxy-lactone carboxylic acid, containing four ether rings.

A carbohydrate derived synthesis of C16–C29 fragment of sorangicin A is described utilizing regioselective epoxide opening, segment-coupled Prins cyclization reaction and cross metathesis as the key steps.

In normal rats treated with the inhibitor of cerebral decarboxylase, NSD-1015 (100 mg kg−1 i.p.), umespirone (1.9–30.0 μmol kg−1 s.c.) produced an increase in neostriatal DOPA (dihydroxyphenylalanine) accumulation, whereas decreased DOPA accumulation was obtained in reserpine-pretreated (5 mg ...

Umespirone was compared to buspirone, diazepam and clozapine as a potential anxiolytic and antipsychotic agent. In the mouse black and white test box, umespirone was considerably more potent than diazepam or buspirone to reduce aversive responding, tolerance to its effects was not observed and s...

We present the study of synthetic pathways to prepare carboxylic acid substituted phthalocyanines from glycolic and lactic acids. Hydroquinone was used as an alternative catalyst for cyclotetramerization reaction of metal free and zinc phthalocyanines, which were characterized by 1H MR spectrosc...

All the synthesized compounds have been characterized by 1H, 13C, 2D NMR and mass spectral studies. The spectral data suggest that compounds 2, 3, 5 and 6 exist in chair conformation with axial orientation of the hydroxyl group and equatorial orientations of all the other substituent. Long-range...

The effect of addition of gramine on mild steel dissolution in deaerated 1.0 M hydrochloric acid was studied through potentiodynamic polarisation curves, electrochemical impedance spectroscopy and gravimetric measurements in the temperature range from 25 °C to 55 °C. Gramine was found to shift...