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Featured researches published by Rodolfo do Couto Maia.


British Journal of Pharmacology | 2013

Beneficial effects of a novel agonist of the adenosine A2A receptor on monocrotaline-induced pulmonary hypertension in rats.

Allan K Alencar; Sharlene L Pereira; Tadeu L Montagnoli; Rodolfo do Couto Maia; Arthur E. Kümmerle; Sharon S. Landgraf; Celso Caruso-Neves; Emanuelle Baptista Ferraz; Roberta Tesch; José Nascimento; Carlos Mauricio R. Sant'Anna; Carlos Alberto Manssour Fraga; Eliezer J. Barreiro; Roberto T. Sudo; Gisele Zapata-Sudo

Pulmonary arterial hypertension (PAH) is characterized by enhanced pulmonary vascular resistance, right ventricular hypertrophy and increased right ventricular systolic pressure. Here, we investigated the effects of a N‐acylhydrazone derivative, 3,4‐dimethoxyphenyl‐N‐methyl‐benzoylhydrazide (LASSBio‐1359), on monocrotaline (MCT)‐induced pulmonary hypertension in rats.


Expert Opinion on Therapeutic Patents | 2014

Acylhydrazone derivatives: a patent review

Rodolfo do Couto Maia; Roberta Tesch; Carlos Alberto Manssour Fraga

Introduction: The N-acylhydrazone (NAH) moiety has been characterized as a privileged structure, capable of providing ligands points for more than one type of bioreceptor. Modifications of the subunits bonded to its acyl and imine functions resulted in several derivatives, which modulate a great diversity of molecular targets. In this context, this patent review reflects the use of the NAH moiety in different compounds. Areas covered: In this review, the authors perform an analysis of the therapeutic profile of NAH compounds together with their perspective of its usability. The Espacenet and Delphion databases were used as main sources of search, and ‘N-acylhydrazone,’, ‘Acylhydrazone’ and ‘hydrazone’ were used as keywords. From a total of 117 patents retrieved, 22 presented pharmacological activities described in the document, thus being chosen for this review. Expert opinion: In the last century, only six patents disclosing NAH derivatives for therapeutic purposes were published, and only in 2010, this subunit started receiving some real attention regarding its therapeutic potential. In this review, the Brazilian and Chinese Universities were identified as the major patent applicants, especially for drug candidates for the treatment of chronic pain, inflammatory disorders and cancer. The NAH subunit is very versatile both from synthetic and medicinal chemistry point of view. This feature is a direct result from the conformational diversity that this framework presents, achievable by subtle and simple chemical changes. Therefore, our opinion is that this moiety suits a lot more drug discovery projects than it seems to at first glance. In conclusion, we strongly support and encourage a raise in the use of this unique subunit.


Bioorganic & Medicinal Chemistry | 2009

Synthesis and analgesic profile of conformationally constrained N-acylhydrazone analogues: Discovery of novel N-arylideneamino quinazolin-4(3H)-one compounds derived from natural safrole

Rodolfo do Couto Maia; Leandro L. da Silva; Eduardo F. Mazzeu; Milla Machado Fumian; Claudia M. Rezende; Antonio C. Doriguetto; Rodrigo S. Corrêa; Ana Luisa P. Miranda; Eliezer J. Barreiro; Carlos Alberto Manssour Fraga

In this work we reported the synthesis and evaluation of the analgesic, anti-inflammatory, and platelet anti-aggregating properties of new 3-(arylideneamino)-2-methyl-6,7-methylenedioxy-quinazolin-4(3H)-one derivatives (3a-j), designed as conformationally constrained analogues of analgesic 1,3-benzodioxolyl-N-acylhydrazones (1) previously developed at LASSBio. Target compounds were synthesized in very good yields exploiting abundant Brazilian natural product safrole (2) as starting material. The pharmacological assays lead us to identify compounds LASSBio-1240 (3b) and LASSBio-1272 (3d) as new analgesic prototypes, presenting an antinociceptive profile more potent and effective than dipyrone and indomethacin used, respectively, as standards in AcOH-induced abdominal constrictions assay and in the formalin test. These results confirmed the success in the exploitation of conformation restriction strategy for identification of novel cyclic N-acylhydrazone analogues with optimized analgesic profile.


Expert Opinion on Therapeutic Patents | 2012

Phenylpiperazine derivatives: a patent review (2006 – present)

Rodolfo do Couto Maia; Roberta Tesch; Carlos Alberto Manssour Fraga

Introduction: The N-phenylpiperazine subunit represents one of the most versatile scaffolds used in the medicinal chemistry field. Recently, some N-phenylpiperazine derivatives have reached late stage clinical trials for the treatment of CNS disorders, thus, this is clearly a molecular template that already has proven its “druglikeness,” However, this scaffold is still strictly seen as a “CNS structure” by great part of the scientific community. The aim of this review is to draw a contemporary profile of the patents regarding N-phenylpiperazine derivatives and, them, suggest new research fields to be explored. Areas covered: The site of the World Intellectual Property Organization (WIPO) was used as the main source in order to perform the research of the patents containing N-phenylpiperazine compounds with therapeutic uses. This review highlights some examples to show that this heterocyclic moiety can successfully yield new classes of hits and prototypes for many other therapeutic fields through appropriate substitution of the molecular skeleton. Expert opinion: The patent research concerning N-phenylpiperazine derivatives indicated for therapeutic uses from 2006 to present date resulted in thirty three documents. It is a low number if one considers the several compounds bearing the N-phenylpiperazine nucleus that reached the market and/or clinical trials. Therefore, this subunit seems to be much underrated at the moment. The adequate use of the N-phenylpiperazine moiety, through modulation of its basicity and substitution pattern of the aromatic ring, can yield pharmacokinetic and pharmacodynamic improvements that are certainly useful in several therapeutic areas, thus, being able to diversify the application and utility of this scaffold. We expect and strongly suggest the growth of this diversification.


British Journal of Pharmacology | 2010

LASSBio-881: an N-acylhydrazone transient receptor potential vanilloid subfamily type 1 antagonist orally effective against the hypernociception induced by capsaicin or partial sciatic ligation

J. L. M. Tributino; M. L. H. Santos; C. M. Mesquita; Cleverton Kleiton Freitas de Lima; L. L. Silva; Rodolfo do Couto Maia; C. D. Duarte; Eliezer J. Barreiro; Carlos Alberto Manssour Fraga; Newton G. Castro; Ana Luisa P. Miranda; M. Z. P. Guimaraes

Background and purpose:  Compound LASSBio‐881 is an orally effective antinociceptive that binds to cannabinoid receptors and is active mainly on the neurogenic component of pain models. We investigated whether transient receptor potential vanilloid subfamily type 1 (TRPV1) channels are involved in the effects of LASSBio‐881.


International Journal of Cardiology | 2016

LASSBio-1425, an analog of thalidomide, decreases triglyceride and increases HDL cholesterol levels by inhibition of TNF-α production

Milla Machado Fumian; Nadia Alice Vieira da Motta; Rodolfo do Couto Maia; Carlos Alberto Manssour Fraga; Eliezer J. Barreiro; Fernanda Carla Ferreira de Brito

a Laboratory of Experimental Pharmacology (LAFE), Department of Physiology and Pharmacology, Biomedical Institute, Fluminense Federal University (UFF), Room 204-A, 24210-130 Niteroi, RJ, Brazil b Laboratory of Evaluation and Synthesis of Bioactive Substances (LASSBio®), Federal University of Rio de Janeiro (UFRJ), Center for Health Sciences (CCS), P.O. Box 68024, 21944-971 Rio de Janeiro, RJ, Brazil


Life Sciences | 2014

N-acylhydrazone improves exercise intolerance in rats submitted to myocardial infarction by the recovery of calcium homeostasis in skeletal muscle.

Jaqueline da Silva; Sharlene L Pereira; Rodolfo do Couto Maia; Sharon S. Landgraf; Celso Caruso-Neves; Arthur E. Kümmerle; Carlos Alberto Manssour Fraga; Eliezer J. Barreiro; Roberto T. Sudo; Gisele Zapata-Sudo

AIMS This work investigated the effects of 3,4-methylenedioxybenzoyl-2-thienylhydrazone (LASSBio-294) treatment on the contractile response of soleus (SOL) muscle from rats submitted to myocardial infarction (MI). MAIN METHODS Following coronary artery ligation, LASSBio-294 (2mg/kg, i.p.) or vehicle was administrated once daily for 4 weeks. KEY FINDINGS The run time to fatigue for sham rats was 17.9 ±2.6 min, and it was reduced to 3.3 ± 0.8 min (P<0.05) in MI rats. In MI rats treated with LASSBio-294, the time to fatigue was 15.1 ± 3.6 min. During the contractile test, SOL muscles from sham rats showed a response of 7.12 ± 0.54N/cm(2) at 60 Hz, which was decreased to 5.45 ± 0.49 N/cm(2) (P<0.05) in MI rats. The contractility of SOL muscles from the MI-LASSBio-294 group was increased to 9.01 ± 0.65N/cm(2). At 16 mM caffeine, the contractility was reduced from 2.31 ± 0.33 to 1.60 ± 0.21 N/cm(2) (P<0.05) in the MI group. In SOL muscles from MI-LASSBio-294 rats, the caffeine response was increased to 2.62 ± 0.33 N/cm(2). Moreover, SERCA2a expression in SOL muscles was decreased by 0.31-fold (31%) in the MI group compared to the Sham group (P<0.05). In the MI-LASSBio-294 group, it was increased by 1.53-fold (153%) compared to the MI group (P<0.05). Meanwhile, the nuclear density in SOL muscles was increased in the MI group compared to the Sham group. Treatment with LASSBio-294 prevented this enhancement of cellular infiltrate. SIGNIFICANCE LASSBio-294 treatment prevented the development of muscular fatigue and improved exercise intolerance in rats submitted to MI.


Journal of Enzyme Inhibition and Medicinal Chemistry | 2012

Novel furfurylidene N-acylhydrazones derived from natural safrole: discovery of LASSBio-1215, a new potent antiplatelet prototype

Ana Cabral Rodrigues; Luciana M.M. Costa; Bruna L. R. Santos; Rodolfo do Couto Maia; Ana Luisa P. Miranda; Eliezer J. Barreiro; Carlos Alberto Manssour Fraga

We describe herein the discovery of (E)-N-methyl-N’-((5-nitrofuran-2-yl)methylene)benzo[d]13 dioxole-5-carbohydrazide (9e), named LASSBio-1215, as a novel antiplatelet agent belonging to the N-methyl-N-acylhydrazone class, which exert their antiaggregating actions on human and rabbit platelets induced by different agonists, through cyclooxygenase-1 (COX-1) or thromboxane synthase inhibition. This compound was elected after screening of a series of functionalized furyl N-acylhydrazone derivatives, synthesized from natural safrole 10. In vitro assays showed that compound 9e presents platelet-aggregating activity in rabbit platelet-rich plasma (PRP) induced by arachidonic acid (IC50 = 0.7 µM) and collagen (IC50 = 4.5 µM). Moreover, LASSBio-1215 also inhibited almost completely the second wave of adenosine diphosphate-induced platelet aggregation in human PRP, and this effect was correlated with their ability to block the production of pro-aggregating autacoid thromboxane A2.


MedChemComm | 2018

Sodium–glucose cotransporter 2 (SGLT-2) inhibitors: a new antidiabetic drug class

Paula Nogueira da Silva; Raissa Alves da Conceição; Rodolfo do Couto Maia; Maria Letícia de Castro Barbosa

Diabetes mellitus is a chronic, complex and multifactorial disease associated characteristically with hyperglycemia. One of the most recently approved antidiabetic drug classes for clinical use are sodium–glucose cotransporter type 2 (SGLT-2) inhibitors. SGLT-2 is a protein expressed in the kidneys, responsible for glucose reabsorption from the glomerular filtrate to the plasma. It is known, nowadays, that diabetic patients show an increased glucose renal reabsorption capacity, caused by the overexpression of the SGLT-2 transporter, thus contributing to hyperglycemia. From establishing this correlation, the SGLT-2 transporter started to be considered as a therapeutic target of interest, culminating in the approval of the first antidiabetic SGLT-2 inhibitor, dapagliflozin (Forxiga® or Farxiga®, Bristol-Myers Squibb & AstraZeneca), in 2012 in Europe. On the other hand, canagliflozin (Invokana®, Janssen Pharmaceutical) was the first drug in this class to be approved by the FDA, the U.S. Food and Drug Administration, in 2013. This review concerns the discovery and development of the first representatives of this class of antidiabetic drugs, and the description of new optimized analogues that are currently in the clinical and preclinical stages of development.


Archive | 2016

Compostos fenil-pirazóis ftalimídicos bioativos, processo para preparação dos compostos, seu uso e composições farmacêuticas

Carlos Alberto Manssour Fraga; Ana Luisa P. Miranda; Rodolfo do Couto Maia; Milla Machado Fumian; Eliezer Jesus de Lacerda Barreiros; Uros Laban; Cleverton Kleiton Freitas de Lima

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Carlos Alberto Manssour Fraga

Federal University of Rio de Janeiro

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Eliezer J. Barreiro

Federal University of Rio de Janeiro

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Roberta Tesch

Federal University of Rio de Janeiro

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Ana Luisa P. Miranda

Federal University of Rio de Janeiro

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Gisele Zapata-Sudo

Federal University of Rio de Janeiro

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Roberto T. Sudo

Federal University of Rio de Janeiro

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Sharlene L Pereira

Federal University of Rio de Janeiro

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Milla Machado Fumian

Federal University of Rio de Janeiro

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Allan K Alencar

Federal University of Rio de Janeiro

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Arthur E. Kümmerle

Universidade Federal Rural do Rio de Janeiro

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