In the present investigation, we report an efficient, direct, one-pot synthesis of mononuclear, mono(bis(2-(4-butylphenyl)imino)methyl)phenoxy)zinc(II)dichloride complex (C34H38Cl2N2O2)Zn in ethanol. The synthesized coordination compound was subjected to crystal growth by repeated recrystallizat...

Late-phase long-term depression (L-LTD) in middle-aged mice has been difficult to achieve and maintain. Here we report an electrically induced, homosynaptic, input-specific form of LTD that could be stably maintained for at least 4 h in the CA1 area of hippocampal slices of 10–14 months old mic...

Thermolysis in refluxing xylene of 4-(2-azido-3-nitrophenyl)-1,4-dihydropyridines was investigated. β-Carboline derivatives and related compounds were obtained in various yields, according to the nature of the substituents in the 1,4-dihydropyridine ring.

A new, potent vasodilator (YC-93), 2,6-dimethyl-4-(3-nitrophenyl)-1,4-dihydropyridine-3,5-dicarboxylic acid 3-[2-(N-benzyl-N-methyl amino)] ethyl ester 5-methyl ester hydrochloride, competitively inhibited cyclic adenosine 3′,5′-monophosphate (cyclic AMP) phosphodiesterase in the 105,000 g sup...

The synthesis and anticonvulsant properties of new N-diethylmalonyl derivatives of nifedipine and other isosteric analogues (7a–7n) were described. Anticonvulsant screening was performed by subcutaneous pentylenetetrazole (scPTZ) and maximal electroshock (MES) induced seizures tests. Majority o...

An efficient total synthesis of (R) and (S)-3-methyl 5-pentyl 2,6-dimethyl-4-(3-nitrophenyl)-1,4-dihydropyridine-3,5-dicarboxylate in high optical purities is reported. The useful step is the resolution of racemic 2, 6-dimethyl-5-methoxycarbonyl-4-(3-nitrophenyl)-1,4-dihydropyridine-3-carboxylic...

CV-159, 1,4-dihydro-2,6-dimethyl-4-(3-nitrophenyl)-3,5-pyridinedicarboxylic acid methyl 6-(5-phenyl-3-pyrazolyloxy)hexyl ester, is a dihydropyridine derivative that blocks the L-type Ca2+ channel and inhibits the calmodulin (CaM)-dependent pathway. In this study, we examined the effects of CV-15...

Human immunodeficiency virus (HIV) reverse transcriptase (RT)-associated ribonuclease H (RNase H) remains an unvalidated drug target. Reported HIV RNase H inhibitors generally lack significant antiviral activity. We report herein the design, synthesis, biochemical and antiviral evaluations of a ...

Expansion of food industry and international trade in foodstuffs, together with increasing worldwide attention to food safety heightened the need of exploring natural preservatives such as bacteriocins to prevent food contamination and spoilage. In this study, we uncovered a significant diversit...

The solubility of solid compounds and active pharmaceutical ingredient in different solvents is important for its crystallization and purification industry. In this work, by using a laser dynamic method, the solubility of levamisole hydrochloride in methanol (MT), ethanol (ET), isopropanol (IPA)...

The bromodomain and extra-terminal (BET) family of epigenetic proteins has attracted considerable attention in drug discovery given its involvement in regulating gene transcription. Screening a focused small molecule library based on the bromodomain pharmacophore resulted in the identification o...

A series of isoquinolines have been evaluated in a homology model of Plasmodium falciparum Protein Kinase A (PfPKA) using molecular dynamics. Synthesis of these compounds was then undertaken to investigate their structure–activity relationships. One compound was found to inhibit parasite growth...

Treatment of 3-aminoisoquinoline (1) with aryldi-azonium salts gave 2-amino-4-arylazoisoquinolines (2) which reacted with aromatic aldehyde to yield imidazo(4,5-c) iso-quinolines. With 3-amino-4-methylisoquinoline (4), however, the same reaction led to 3-isoquinolyltriazenes (5), and these could...

A new strategy for the synthesis of oxide-containing fragments of morphine has been developed. Thus, the tricyclic (ANO) morphine fragment spiro[7-methoxybenzofuran-3(2H),4′-1′-methylpiperidine] (1) was obtained as the sole product via an intramolecular radical cyclization of 4-[(2′-bromo-6′...

A stereoselective synthesis of the ACNO partial structures of morphine has been developed. Palladium-catalyzed cyclization of carbamate 2 provided the tetracyclic (ACNO) 3-ethoxycarbonyl-9-methoxy-2,3,5,6,7,7a-hexahydro-1H-benzofuro[3,2-e]isoquinoline (14); while treatment of 5-(2-bromo-6-methox...

To strengthen the mechanical properties of a fibrin gel and improve its applicability as a scaffold for tissue engineering (TE) applications, a strategy for the in situ preparation of the interpenetrating network (IPN) of fibrin and hyaluronic acid (HA) was developed on the basis of simultaneous...

Here we describe the design and synthesis of a prodrug developed for pigmented melanoma therapy, consisting of a Melanin-Targeting Probe (MTP) conjugated to 5-iodo-2′-deoxyuridine (IUdR) with a reduction-sensitive pre-determined breaking point. Compared with the non-cleavable conjugate (17b), p...

An easy and mild method has been developed for the synthesis of mixed glycosyl disulfides/selenenylsulfides from glycosyl halides and diaryl/dialkyl dichalcogenides in the presence of benzyltriethylammonium tetrathiomolybdate [(BnEt3N)2MoS4]. The salient feature of this method is the sulfur tran...

4-Formyl- and 4,4′-diformyl-2,2′-bipyridines have been prepared in two steps and in 52–71% overall yields via enamination of the corresponding 4-methyl and 4,4′-dimethyl-2,2′-bipyridine derivatives. The synthesis of two new 4,4′-dialkenyl-2,2′-bipyridyl ligands is also described.

A new Schiff base-bipyridine ligand, [4-(4′-methyl)-2,2′-bipyridyl)imine]-2-hydroxybenzene, was prepared, characterized and its X-ray crystal structure obtained. The rhenium(I) tricarbonylchloro complex of this novel derivative of 2,2′-bipyridine was also prepared and characterized. The photo...