An efficient and scalable route for a series of novel substituted 2-anilino-7H-pyrrolopyrimidine compounds as potential inhibitors of PDK1, an important regulator of the PI3K/Akt pathway that is dysregulated in many cancers, was developed and is described. The synthetic strategy was designed aro...

The 2,4-dinitrophenyl group used for histidine side chain protection is not stable during aminolytic removal of Fmoc protecting groups. In the presence

The asymmetric aza-Diels–Alder reaction of the (1R)-8-phenylmenthyl or (1R)-8-phenylisoneomenthyl glyoxylate-derived N-benzylimine with cyclopentadiene resulted in the enantioselective synthesis of the corresponding pure [(1S,3-exo)-2-benzyl-2-azabicyclo[2.2.1]hept-5-ene]-3-carboxylates (80 or ...

Following the recent disclosure of 3-methyl pyrrole-2,4-dicarboxylic acid 2-propyl ester 4-(1,2,2-trimethyl-propyl) ester, a potent and selective mGluR1 non-competitive antagonist, we report here a detailed exploration of the C-2 position of this scaffold with the preparation of differently subs...

Pentacarbonylbromorhenium(I) reacted with 2,6-bis(benzimidazol-2′-yl)pyridine (bbip), 2,6-bis(1′-methylbenzimidazol-2′-yl)pyridine (bmbip), 2,6-bis(5′,6′-dimethylbenzimidazol-2′-yl)pyridine (bdmbip), and 2,6-bis(1′,5′,6′-trimethylbenzimidazol-2′-yl)pyridine (btmbip) to form stable octa...

Two bis-tridentate pincer complexes [Ru(H2bip)(Mebib)](PF6)2 (1(PF6)2) and [Ru(H2bip)(H2bib)](PF6)2 (2(PF6)2) were prepared and studied, where H2bip is 2,6-bis(benzimidazol-2-yl)pyridine, Mebib is the 2-deprotonated 1,3-bis(N-methylbenzimidazol-2-yl)benzene, and H2bib is 2-deprotonated 1,3-bis(b...

Aniba riparia (Nees) Mez. (Lauraceae) is popularly known as “louro”, and is found in Amazonia and in the Guianas, its distribution extends to the Andes. Alkamide alkaloids were isolated from its green fruit; they were denominated riparin I (methyl ether of N-benzoyl tyramine), riparin II (meth...

Riparin II (RipII), an alkamide isolated from the green fruit of Aniba riparia, was tested in the various animal models of inflammation to investigate its anti-inflammatory activity. Male Wistar rats (180–240 g) were treated with RipII by gavage at doses 25 or 50 mg/kg, before initiating the in...

Riparin II (RIP II) is an alkamide isolated from Aniba riparia that has presented antidepressant and anxiolytic effects in acute stress behavioral models. This study aimed to investigate the activity of RIP II in a corticosterone-induced depression mice model. Corticosterone (20 mg/kg, s.c.) was...

Inflammation is a local tissue response to attacks characterized by vascular and cellular events, including intense oxidative stress. Riparin A, a compound obtained from Aniba riparia, has been shown to have antioxidant activity and cytotoxicity in vitro. This study was aimed at evaluating the a...

Riparin II (RipII) has an anti-inflammatory activity potentially due its ability to decrease TNF-α and IL-1β production and its histamine antagonism. The objective of this study was to evaluate the role of RipII in the pain process and the possible antinociceptive mechanisms involved, using cl...

We have reported Riparin A as a promising antiparasitic molecule ​​against Leishmania amazonensis promastigotes. This work evaluated the acute oral toxicity of Riparin A and its anxiolytic effects using in vivo models and computational tools. Mice were submitted to acute oral toxicity tests (Gui...

This study performed a physicochemical characterization of the inclusion complex generated between Riparin A and β-cyclodextrin (Rip A/β-CD) and compared the cytotoxic potential of the incorporated Rip A upon Artemia salina larvae. Samples were analyzed by phase solubility diagram, dissolution...

The green Brazilian bay leaf, a spice much prized in local cuisine (Aniba riparia, Lauraceae), contains chemical compounds presenting benzoyl-derivatives named riparins, which have anti-inflammatory, antimicrobial and anxiolytic properties. However, it is unclear what kind of interaction riparin...

Schistosomiasis, caused by helminth flatworms of the genus Schistosoma, is one of the most important parasitic diseases in the world, affecting over 200 million people in developing countries. Riparins are natural alkamides found in Aniba riparia (Lauraceae) fruits that possess several pharmacol...

Mental disorders have a multifactorial etiology and stress presents as one of the causal factors. In depression, it is suggested that high cortisol concentration contributes directly to the pathology of this disease. Based on that, the study aims to evaluate the potential antidepressant effect o...

A study was undertaken of bone marrow transplant patients receiving parenteral nutrition containing an amino solution and either glucose alone or 25% or 60% of parenteral calories as Liposyn® 20% which compared the nitrogen balance, liver function tests and other biochemical and hematological va...

N-Acetyl-S-(3-coumarinyl)cysteine, a metabolite of coumarin in rodents, has been synthesized as methyl ester. A new synthetic route to prepare N-acetyl-S-(3-coumarinyl)-d,l-cysteine methyl ester (1) comprises reaction of 3-mercaptocoumarin (3) with N-acetyl-3-chloro-d,l-alanine methyl ester (4)....

In situ prepared Cp2(Cl)Zr⊛ catalyzes the formation of ortho eśters from epoxy esters. Acid-sensitive α-amino and α-hydroxy acid derivatives are converted in high yield to 2,7,8-trioxabicyclo[3.2.1]octanes (ABO-esters) using this protocol. This strategy is complementary to the OBO-ester techno...

The major metabolite of a novel non-steroidal anti-inflammatory drug, dl-4-(2′-4′-difluorobiphenyl-4-yl)-4-oxo-2-methylbutonoic acid (flobufen, I), namely 4-(2′,4′-difluorobiphenyl-4-yl)-2-methyl-γ-butyrolactone (4-dihydroflobufen lactone, III), has four stereoisomers consisting of two race...