15 documents found, page 1 of 2
Synthesis and Antioxidant and Antimicrobial Properties of β-Hydroxy Sulfides, S...
Copini,Suély; Micheletti,Ana C.; Lima,Dênis P. de; Gomes,Roberto S.; Meza,Alisson; Beatriz,AdilsonNatural and synthetic sulfur-bearing organic compounds have many applications in medicinal chemistry. This article reports the preparation of amphiphilic β-hydroxy sulfides, sulfoxides, and sulfones derived from cardanol and glycerol. Thiolysis of cardanol epoxide 3 with various thiols (4a-4j) in ethanol or water yielded the corresponding β-hydroxy sulfides 5a-5j (61-95%). Treatment with 30% H2O2 in acetic acid...
Assessment of genetic integrity, splenic phagocytosis and cell death potential ...
Oliveira,Rodrigo Juliano; da Cruz Leite Santos,Naiara; Pesarini,João Renato; de Oliveira,Beatriz Carneiro; Berno,Claudia RodriguesAbstract The increased incidence of cancer and its high treatment costs have encouraged the search for new compounds to be used in adjuvant therapies for this disease. This study discloses the synthesis of (Z)-4-((1,5-dimethyl-3-oxo-2-phenyl-2,3dihydro-1H-pyrazol-4-yl) amino)-4-oxobut-2-enoic acid (IR-01) and evaluates not only the action of this compound on genetic integrity, increase in splenic phagocytosis a...
Synthesis, Antibacterial and Antitubercular Evaluation of Cardanol and Glycerol...
Manda,Bhaskar R.; Prasad,Avvari N.; Thatikonda,Narendar R.; Lacerda Jr.,Valdemar; Barbosa,Layla R.; Santos,Heloa; Romão,Wanderson; Pavan,Fernando R.The synthesis of novel amino alcohol derivatives based on cardanol and glycerol were achieved in good yields and characterized by 1H and 13C NMR (nuclear magnetic resonance) and MS (mass spectrometry). In addition, we evaluated the in vitro antimicrobial activity against Gram-positive (Staphylococcus aureus, standard and clinical strains), Gram-negative (Escherichia coli) and M. tuberculosis bacterial strains. ...
In vivo chemotherapeutic insight of a novel isocoumarin (3-hexyl-5,7-dimethoxy-...
Araújo,Flávio Henrique Souza de; Figueiredo,Débora Rojas de; Auharek,Sarah Alves; Pesarini,João Renato; Meza,Alisson; Gomes,Roberto da SilvaAbstract Chemotherapy is one of the major approaches for the treatment of cancer. Therefore, the development of new chemotherapy drugs is an important aspect of medicinal chemistry. Chemotherapeutic agents include isocoumarins, which are privileged structures with potential antitumoral activity. Herein, a new 3-substituted isocoumarin was synthesized from 2-iodo-3,5-dimethoxy-benzoic acid and oct-1-yne in a cro...
Cardanol: toxicogenetic assessment and its effects when combined with cyclophos...
Schneider,Beatriz Ursinos Catelan; Meza,Alisson; Beatriz,Adilson; Pesarini,João Renato; Carvalho,Pamela Castilho de; Mauro,Mariana de OliveiraAbstract Cardanol is an effective antioxidant and is a compound with antimutagenic and antitumoral activity. Here, we evaluated the genotoxic and mutagenic potential of saturated side chain cardanol and its effects in combination with cyclophosphamide in preventing DNA damage, apoptosis, and immunomodulation. Swiss mice were treated with cardanol (2.5, 5 and 10 mg/kg) alone or in combination with cyclophosphami...
Synthesis and evaluation of octocrylene-inspired compounds for UV-filter activity
Polonini,Hudson C.; Lopes,Rosângela S.; Beatriz,Adilson; Gomes,Roberto S.; Silva,Adriano O.; Lima,Ricardo V. de; Nunes,Gláucia. A.Octocrylene (2-ethylhexyl 2-cyano-3,3-diphenyl-2-propenoate) is present in several sunscreens and is known to work synergistically with UV filters. We prepared eight octocrylene-related compounds to test their photoprotective activities by measuring diffuse transmittance. The compounds had varied photoprotection profiles, with Sun Protection Factors (SPF) ranging from 1 to 5 and UVA Protection Factors (UVAPF) r...
Synthesis and biological activity of sulfur compounds showing structural analog...
Santos,Edson dos A. dos; Prado,Paulo C.; Carvalho,Wanderley R. de; Lima,Ricardo V. de; Beatriz,Adilson; Lima,Dênis P. de; Hamel,Ernest; Dyba,Marzena A.We extended our previous exploration of sulfur bridges as bioisosteric replacements for atoms forming the bridge between the aromatic rings of combretastatin A-4. Employing coupling reactions between 5-iodo-1,2,3-trimethoxybenzene and substituted thiols, followed by oxidation to sulfones with m-CPBA, different locations for attaching the sulfur atom to ring A through the synthesis of nine compounds were examine...
Total synthesis and allelopathic activity of cytosporones A-C
Zamberlam,Charles E. M.; Meza,Alisson; Leite,Carla Braga; Marques,Maria Rita; de Lima,Dênis P.; Beatriz,AdilsonThe search for efficient, environmentally friendly herbicides has been the focus of numerous studies on the organic synthesis of compounds isolated from natural sources. Cytosporones, which are phenolic lipids isolated from fungi, exhibit noteworthy biological properties. This paper reports the preparation of cytosporones A-C from the same starting material through a short synthetic route, with good yields. All...
Chemical modifications of a natural xanthone and antimicrobial activity against...
Micheletti,Ana Camila; Honda,Neli Kika; Lima,Dênis Pires de; Beatriz,Adilson; Sant'ana,Maria Rita; Carvalho,Nadia Cristina PereiraA series of 15 ω-aminoalkoxylxanthones containing methyl, ethyl, propyl, tert-butylamino and piperidinyl moieties were synthesized from a natural xanthone isolated from a lichen species. These compounds were tested for their in vitro antibacterial properties against Gram-positive and Gram-negative bacteria and cytotoxicity against a number of human tumor cell lines was too evaluated. The newly synthesized deriv...
Glicerol: um breve histórico e aplicação em sínteses estereosseletivas
Beatriz,Adilson; Araújo,Yara J. K.; Lima,Dênis Pires dePresently glycerol is considered a co-product of biodiesel industry. As the biodiesel production is exponentially increasing, glycerol generated from the transesterification of vegetable oils and fats is also being produced on a large scale, and turned out to be essential seeking for novel alternatives to the consumption of the extra volume, in crude and/or as derivatives high added value. This review mainly de...