Abstract:
:Annulated thienopyrimidine derivatives attracted big interest of the scientific community due to their broad spectrum of biological activities among which are the inhibition of phosphodiesterase, antiproliferative and antimicrobial activities. As a continuation of our studies on the synthesis and biological activity of fused thieno[3,2-d]pyrimidine derivatives, the goal of this paper is the synthesis and study of the properties of compounds containing different heterocycles such as fused thieno[2,3-b]pyridine and tetrazolo[1,5-c]pyrimidine in the same molecule. Thus, starting from the ethyl 1-amino-5-isopropyl-8,8-dimethyl-8,9-dihydro-6H-pyrano[4,3-d]thieno[2,3-b]pyridine-2-carboxylate 1, efficient methods for obtaining new 8-amino-5-isopropyl-2,2-dimethyl-10-(methylthio)-1,4-dihydro-2H-pyrano[4'',3'':4',5']pyrido[3',2':4,5]thieno[3,2-d]pyrimidines 6 and thieno[2,3-e]tetrazolo[1,5-c]pyrimidine 8 are described. The spectroscopic results showed that compound 8 in the solid state is exclusively in the tetrazolo tautomeric form, while in solution an azide-tetrazole equilibrium is present 8A/T. The possible antimicrobial activity of newly synthesized compounds against some gram-positive and gram-negative bacilli strains has been evaluated. The biological tests evidenced that some of them showed promising antimicrobial activity. Two compounds showed similar activity to the one of the used reference drug. The study of structure-activity relationships revealed that the activity of a compound depends mostly on the nature of substituent R1R2. According to the predicted docking studies our compounds could be DnaG inhibitors.
journal_name
An Acad Bras Ciencjournal_title
Anais da Academia Brasileira de Cienciasauthors
Sirakanyan SN,Geronikaki A,Spinelli D,Hakobyan EK,Kartsev VG,Petrou A,Hovakimyan AAdoi
10.1590/0001-3765201820170798subject
Has Abstractpub_date
2018-04-23 00:00:00pages
1043-1057issue
1 Suppl 2eissn
0001-3765issn
1678-2690pii
S0001-37652018005007107journal_volume
90pub_type
杂志文章abstract::Membrane protein patterns in SDS-PAGE clearly characterized Azospirillum amazonense, A. brasilense, A. lipoferum, and Herbaspirillum seropedicae. Each species showed also a typical major band with approximate molecular weights (AMWs) of 44, 39.5, 35.5, and 37.5 Kdaltons for the four species respectively. Characteristi...
journal_title:Anais da Academia Brasileira de Ciencias
pub_type: 杂志文章
doi:
更新日期:1989-06-01 00:00:00
abstract::The objective of this study was to estimate variance components for performance and carcass traits in a paternal broiler line. The (co)variance components were estimated by the restricted maximum likelihood method applied to the animal model, including the fixed effect of group (sex and hatch) and additive genetic and...
journal_title:Anais da Academia Brasileira de Ciencias
pub_type: 杂志文章
doi:10.1590/0001-3765202020180697
更新日期:2020-01-01 00:00:00
abstract::The golden mussel, Limnoperna fortunei, is among the most devastating invasive species in freshwater habitats worldwide, leading to severe environmental disturbances and economic losses. Therefore, management efforts would be greatly improved by methods that efficiently detect and quantify the abundance of the golden ...
journal_title:Anais da Academia Brasileira de Ciencias
pub_type: 杂志文章
doi:10.1590/0001-3765201720160723
更新日期:2017-04-01 00:00:00
abstract::Sea anemones are considered as polyphagous opportunistic predators and it has been suggested that their diet reflects the structure of the community they inhabit. The feeding ecology of intertidal species is an interesting topic to study due to their wide variety of strategies to obtain food. In this sense, we studied...
journal_title:Anais da Academia Brasileira de Ciencias
pub_type: 杂志文章
doi:10.1590/0001-3765202020190520
更新日期:2020-10-19 00:00:00
abstract::This study suggests the employment of accumulated sediments in the reservoir of Tucuruí (Pará /Brazil) to remineralize the surrounding degraded soils. The approach was based on the principles of stonemeal technology. It suggests that the soil can be rejuvenated by crushed rocks rich in macro and micronutrients. Remova...
journal_title:Anais da Academia Brasileira de Ciencias
pub_type: 杂志文章
doi:10.1590/s0001-37652013000100003
更新日期:2013-03-01 00:00:00
abstract::Cesium atomic beam clocks have been the workhorse for many demanding applications in science and technology for the past four decades. Tests of the fundamental laws of physics and the search for minute changes in fundamental constants, the synchronization of telecommunication networks, and realization of the satellite...
journal_title:Anais da Academia Brasileira de Ciencias
pub_type: 杂志文章
doi:10.1590/s0001-37652008000200002
更新日期:2008-06-01 00:00:00
abstract::The aim of this study was to evaluate the effect of phosphorus (P) on the toxicity of zinc (Zn) for the alga Raphidocelis subcapitata. P was provided in three concentrations: 2.3 x 10-4 mol L-1, 2.3 x 10-6 mol L-1 and 1.0 x 10-6 mol L-1. Algal cells were acclimated to the specific P concentrations before the start of ...
journal_title:Anais da Academia Brasileira de Ciencias
pub_type: 杂志文章
doi:10.1590/0001-3765202020190050
更新日期:2020-11-06 00:00:00
abstract::The acceleration of the anthropogenic activity has increased the atmospheric carbon concentration, which causes changes in regional climate. The Gross Primary Production (GPP) is an important variable in the global carbon cycle studies, since it defines the atmospheric carbon extraction rate from terrestrial ecosystem...
journal_title:Anais da Academia Brasileira de Ciencias
pub_type: 杂志文章
doi:10.1590/0001-3765201520140457
更新日期:2015-09-01 00:00:00
abstract::There is growing evidence that, during song learning, birds do not only acquire 'what to sing' (the inventory of behavior), but also 'how to sing' (the singing program), including order-features of song sequencing. Common Nightingales Luscinia megarhynchos acquire such serial information by segmenting long strings of ...
journal_title:Anais da Academia Brasileira de Ciencias
pub_type: 杂志文章
doi:10.1590/s0001-37652004000200005
更新日期:2004-06-01 00:00:00
abstract::The objective of this study was to investigate the effects of 2% L-glutamine supplementation on myenteric innervation in the ileum of diabetic rats, grouped as follows: normoglycemic (N); normoglycemic supplemented with L-glutamine (NG); diabetic (D); and diabetic supplemented with L-glutamine (DG). The ileums were su...
journal_title:Anais da Academia Brasileira de Ciencias
pub_type: 杂志文章
doi:10.1590/0001-3765201620150228
更新日期:2016-01-01 00:00:00
abstract::Leaves of Psidium guajava L. (guava) have been widely used in the popular way for prevention and treatment of various diseases. Thus, the objective of this study was to evaluate the inhibitory potential of leaves aqueous extract from three cultivars of P. guajava (Pedro Sato, Paluma and Século XXI) on α-amylase, α-gly...
journal_title:Anais da Academia Brasileira de Ciencias
pub_type: 杂志文章
doi:10.1590/0001-3765201720160067
更新日期:2017-01-01 00:00:00
abstract::Rotifers have often been used as indicators of sudden changes in physical and chemical features of the aquatic environment. Such features vary greatly during flood pulse events in small lakes connected to major floodplains. However, few are the studies that investigate the consequences of the flood pulse in rotifer sp...
journal_title:Anais da Academia Brasileira de Ciencias
pub_type: 杂志文章
doi:10.1590/0001-3765201420130323
更新日期:2014-09-01 00:00:00
abstract::Candida is a human fungal pathogen that causes a wide range of diseases. Candida albicans is the main etiologic agent in these diseases; however, infections can be caused by non-albicans Candida species. Virulence factors such as biofilm production, which protect the fungus from host immunity and anti-fungal drugs, ar...
journal_title:Anais da Academia Brasileira de Ciencias
pub_type: 杂志文章
doi:10.1590/0001-3765202020200703
更新日期:2020-12-11 00:00:00
abstract::This study investigated the dynamics of cyanobacteria in two deep, eutrophic reservoirs in a semi-arid region of Brazil during periods of stratification and destratification. Four collections were carried out at each reservoir at two depths at three-month intervals. The following abiotic variables were analyzed: water...
journal_title:Anais da Academia Brasileira de Ciencias
pub_type: 杂志文章
doi:10.1590/s0001-37652011000400019
更新日期:2011-12-01 00:00:00
abstract::A simple methodology for the synthesis of enynes by indium mediated diastereoselective allylation of aromatic N-tert-butanesulfinylimines bearing alkenyl groups at ortho-position with allyl bromide has been developed. The addition of the allyl indium intermediate to the chiral imine took place with excellent diastereo...
journal_title:Anais da Academia Brasileira de Ciencias
pub_type: 杂志文章
doi:10.1590/0001-3765201720170756
更新日期:2018-01-01 00:00:00
abstract::Eimeriosis is caused by a protozoan parasite of the genus Eimeria and infection affecting most domestic animal species. The aim of this research was to comprehend the impact of selenium nanoparticles (SeNPs) on eimeriosis induced by Eimeria papillata in mouse jejunum, and how they work as antioxidants and anti-apoptot...
journal_title:Anais da Academia Brasileira de Ciencias
pub_type: 杂志文章
doi:10.1590/0001-3765202020191107
更新日期:2020-06-03 00:00:00
abstract::Agapanthus (Agapanthaceae) has 10 species described. However, most taxonomists differ respect to this number because the great phenotypic plasticity of the species. The cytogenetic has been an important tool to aid the plant taxon identification, and to date, all taxa of Agapanthus L'Héritier studied cytologically, pr...
journal_title:Anais da Academia Brasileira de Ciencias
pub_type: 杂志文章
doi:10.1590/0001-3765201620150514
更新日期:2016-01-01 00:00:00
abstract::Castor bean (Ricinus communis L.) is cultivated mainly for biodiesel production because of its oil-rich seeds; it is assumed to be an anemophylous species. But pollination deficit can lead to low productivity often attributed to other reasons. In this paper, we investigated pollination requirements, pollination mechan...
journal_title:Anais da Academia Brasileira de Ciencias
pub_type: 杂志文章
doi:10.1590/s0001-37652012005000057
更新日期:2012-12-01 00:00:00
abstract::A new azhdarchoid pterosaur from the Upper Cretaceous of Patagonia is described. The material consists of an incomplete edentulous lower jaw that was collected from the upper portion of the Portezuelo Formation (Turonian-Early Coniacian) at the Futalognko site, northwest of Neuquén city, Argentina. The overall morphol...
journal_title:Anais da Academia Brasileira de Ciencias
pub_type: 杂志文章
doi:10.1590/0001-3765201720170478
更新日期:2017-01-01 00:00:00
abstract::A multivariable deterministic extremum seeking (ES) is being evaluated to construct an adaptive Proportional-Integral-Derivative (PID) control law for the functional Neuromuscular Electrical Stimulation (NMES) of stroke patients. The developed scheme is applied to control the position of the patient's arm so that move...
journal_title:Anais da Academia Brasileira de Ciencias
pub_type: 杂志文章
doi:10.1590/0001-3765201820180544
更新日期:2019-02-14 00:00:00
abstract::This article analyzes the existing collaboration networks in the Brazilian scientific output in Evolutionary Biology, considering articles published during the period from 2000 to 2012 in journals indexed by Web of Science. The methodology integrates bibliometric techniques and Social Network Analysis resources to des...
journal_title:Anais da Academia Brasileira de Ciencias
pub_type: 杂志文章
doi:10.1590/0001-3765201620140620
更新日期:2016-03-01 00:00:00
abstract::A total of 30 animals of the genus Dasyprocta were cytogenetically studied. They belong to the following species: D. prymnolopha (N=20), D. leporina (N=6), D. fuliginosa (N=1) and Dasyprocta sp. (N=3) (Dasyproctidae, Hystricognathi). Cell suspensions were obtained by peripheral blood culture, besides bone marrow and s...
journal_title:Anais da Academia Brasileira de Ciencias
pub_type: 杂志文章
doi:10.1590/s0001-37652003000100007
更新日期:2003-03-01 00:00:00
abstract::A performance assessment of active magnetocaloric regenerators using entropy generation minimization is presented. The model consists of the Brinkman-Forchheimer equation to describe the fluid flow and coupled energy equations for the fluid and solid phases. Entropy generation contributions due to axial heat conductio...
journal_title:Anais da Academia Brasileira de Ciencias
pub_type: 杂志文章
doi:10.1590/0001-3765201720160427
更新日期:2017-05-01 00:00:00
abstract::Limnoperna fortunei, an Asiatic rivers bivalve has become a worldwide problematic invasive species causing several water quality and macrofouling problems. In the Neotropical region it was first recorded in 1991 in the Rio de la Plata coast, Buenos Aires province. Since this, it showed a quick upstream invasion into t...
journal_title:Anais da Academia Brasileira de Ciencias
pub_type: 杂志文章
doi:10.1590/s0001-37652005000200004
更新日期:2005-06-01 00:00:00
abstract::The centesimal composition and the physical and chemical analyses of Lentinus strigosus, an edible mushroom occurring in the Brazilian Amazon and produced in alternative substrates based on wood and agroindustrial residues, were evaluated. For this purpose, the C, N, pH, soluble solids, water activity, protein, lipids...
journal_title:Anais da Academia Brasileira de Ciencias
pub_type: 杂志文章
doi:10.1590/0001-3765201399412
更新日期:2013-01-01 00:00:00
abstract::Candidiasis has become an important concern for clinical practice, especially with the increasing incidence of immunocompromised patients. In this scenario, the development resistance to fluconazole presents a challenge for treating these opportunistic infections. The aim of this study was to evaluate some epidemiolog...
journal_title:Anais da Academia Brasileira de Ciencias
pub_type: 杂志文章
doi:10.1590/0001-3765201520140717
更新日期:2015-08-01 00:00:00
abstract::Programs of Science and Technology research have grown significantly in Brazil over the last decades. Until the 1980s the so-called undirected programs, without specific goals and requiring only scientific merit, prevailed. The few programs with defined goals in this period were never objectively assessed. The same si...
journal_title:Anais da Academia Brasileira de Ciencias
pub_type: 杂志文章
doi:10.1590/s0001-37652007000300014
更新日期:2007-09-01 00:00:00
abstract::The amino acid sequence of the "double-headed" trypsin and chymotrypsin inhibitor (BTCI), purified from the cowpea Vigna unguiculata (L.) Walp. cv "Seridó" was determined in our laboratory. Tryptic and chymotryptic peptides were sequenced by the Edman-Gray and Edman-Chang N-terminal manual method as well as the carbox...
journal_title:Anais da Academia Brasileira de Ciencias
pub_type: 杂志文章
doi:
更新日期:1987-01-01 00:00:00
abstract::In this study, geochemical and particle size analyses of thirty-four street sediment samples collected from an urban environment around Guanabara Bay, shows highway run-off to be a potential source of heavy metals for the pollution of near-shore sedimentary deposits. Concentrations of Fe, Mn, Zn, Cu, Pb, Cr and Ni wer...
journal_title:Anais da Academia Brasileira de Ciencias
pub_type: 杂志文章
doi:10.1590/s0001-37652007000400013
更新日期:2007-12-01 00:00:00
abstract::This study aimed to detail the temporal and morphological parameters of the immature stages of Spodoptera albula (Walker 1857) under controlled conditions (25 ± 1°C, 70 ± 10% RH and 14 hour photophase) and to gather information about their larval host plants. For this purpose, a new rearing method and artificial diet ...
journal_title:Anais da Academia Brasileira de Ciencias
pub_type: 杂志文章
doi:10.1590/s0001-37652013000100013
更新日期:2013-03-01 00:00:00