A series of morpholine substituted amino acids (phenylalanine, leucine, lysine and glutamic acid) was synthesized. A fragment-based screening approach was then used to evaluate a series of small heterocycles, including morpholine, oxazoline, dihydro-1,3-oxazine, tetrahydro-1,3-oxazepine, thiazoline, tetrahydro-1,3-pyrimidine, tetrahydro-1,3-diazepine and hexahydro-1H-benzimidazole, as potential...

a quantitative structure-activity relationship (qsar) study was conducted for the prediction of inhibitory activity of 1-phenyl[2h]-tetrahydro-triazine-3-one analogues as inhibitors of 5-lipoxygenase. the inhibitory activities of the 1-phenyl[2h]-tetrahydro-triazine-3-one analogues modeled as a function of molecular structures using chemometrics methods such as multiple linear regression (mlr) ...

The cyclization of b-anilino propionic acids in the presence of polyphosphoric acid (PPA) afforded the 2,3-Dihydroquinoline-4-(1H)-ones in good yields. N,N'-bis(2-carboxyethyl)-4-methyl-1,2-diaminobenzene (7) is cyclized under this condition to produce the 1,5-diaza-2,3,6,7-tetrahydro-4-methyl-pheranthrene-4,8-dione(bis-quinolone) (8).

Leishmaniasis is a neglected disease responsible for about 56,000 deaths every year. Despite its importance, there are no effective, safe and proper treatments for leishmaniasis due to strain resistance and/or drug side-effects. In this work we report the synthesis, molecular modeling, cytotoxicity and the antileishmanial profile of a series of 4-(1H-pyrazol-1-yl)benzenesulfonamides. Our exper...

Tetrahydrocarbazoles are important class of heterocycles that exhibit numerous biological properties. They also found in several natural products. In the present study, Fischer indolization L-menthone was investigated for diastereoselectivity using different reaction conditions. No appreciable observed acids used except CuBr and boric acid at varying temperatures, where satisfactory results wer...

SKF83959 (3-methyl-6-chloro-7,8-hydroxy-1-[3-methylphenyl]-2,3,4,5-tetrahydro-1H-3-benzazepine), an atypical dopamine receptor-1 (D(1) receptor) agonist, has shown many D(1) receptor-independent effects, such as neuroprotection, blockade of Na(+) channel, and promotion of spontaneous glutamate release, which resemble the effects of the sigma-1 receptor activation. In the present work, we explor...

R-(+)-7-chloro-8-hydroxy-3-methyl-1-phenyl-2,3,4,5-tetrahydro-1H-3-benzazepine hydrochloride (SCH23390) is a widely used, highly selective antagonist of D1 dopamine receptors. While investigating the crosstalk between D1 and D3 dopamine receptor signaling pathways, we discovered that in addition to being a D1 receptor antagonist, SCH23390 and related compounds inhibit G protein-coupled inwardly...

In 1-cyclohexyl-6,6,8a-trimethyl-3a,6,7,8a-tetrahydro-1H-1-benzofuro[2,3-b]pyrrole-2,4(3H,5H)-dione, C19H27NO3, (I), and the isomorphous compounds 6,6,8a-trimethyl-1-phenyl-3a,6,7,8a-tetrahydro-1H-1-benzofuro[2,3-b]pyrrole-2,4(3H,5H)-dione, C19H21NO3, (II), and 6,6,8a-trimethyl-1-(3-pyridyl)-3a,6,7,8a-tetrahydro-1H-1-benzofuro[2,3-b]pyrrole-2,4(3H,5H)-dione, C18H20N2O3, (III), the tetrahydroben...

Although anion-binding processes are well-known for their crucial role in molecular recognition, they have only recently been utilized catalysis. Herein, a new class of chiral, enantiopure C2-symmetrical thioureas that, combination with 4-methoxybenzoic acid, promotes the enantioselective protio-Pictet-Spengler reaction to provide unprotected tetrahydro-?-carbolines good yields (40–93 %) and mo...

Structurally dissimilar dopamine D(1) receptor agonists were compared with dopamine in their ability to activate adenylate cyclase and to internalize hemagglutinin-tagged human D(1) receptors in a stably transfected human embryonic kidney cell line. Thirteen dopamine D(1) receptor agonists were selected rationally from three different structural classes: rigid fused ring compounds [dihydrexidin...