Design and Synthesis of an Indole-Estrogen Derivative

There are several methods reported for synthesis of aromatic-condensed derivatives; nevertheless, expensive reagents and special conditions are required. Therefore, in this study, an indole-estrogen derivative (3-[4-(2-butyl-3-cyclohexylimino-4-piperidin-1-yl-cyclobutylidencarbamoyl)]-phenoxy-NH-indolo[2′,3′:17,16]estra-1,3,5(10)triene) was synthesized using some strategies. The structure of all compounds obtained was confirmed by spectroscopic and spectrometric methods. In conclusion, a facile procedure for the formation of an indole-estrogen derivative was developed in this study

Design and Synthesis of Two Oxazine Derivatives Using Several Strategies

Several oxazine derivatives have been synthesized; nevertheless, expensive reagents and special conditions are required. Therefore, in this study, two oxazine derivatives (2-chloro-3-{{2-[-(3-chloro-2-oxo-cyclobutyl)-(2,3-dimethoxy-9,10-dihydrostrychnid-10-yl)-amino]-ethyl}-[1,5-dimethyl-4-(1H-naphtho[1,2-e][1,3-oxazin-2-yl)-2-phenyl-2,3-dihydro-1H-pyrazol-3-yl]-amino}-cyclobutanone and 2-chloro-3-{{2-[(3-chloro-2-oxo-cyclobutyl)-(1,7,7-trimethyl-bicyclo[2.2.1]hept-2-yl)-amino]-ethyl}-[1,5-dimethyl-4-(1H-naphtho[1,2-e][1,3]oxazin-2-yl)-2-phenyl-2,3-dihydro-1H-pyrazol-3-yl]-amino}-cyclobutanone) were synthesized using several strategies. The structure of compounds obtained was confirmed by elemental analysis, spectroscopy, and spectrometry data. In conclusion, the methods used offer some advantages such as good yields, simple procedure, low cost, and ease of workup

Activity Exerted by a Testosterone Derivative on Myocardial Injury Using an Ischemia/Reperfusion Model

Some reports indicate that several steroid derivatives have activity at cardiovascular level; nevertheless, there is scarce information about the activity exerted by the testosterone derivatives on cardiac injury caused by ischemia/reperfusion (I/R). Analyzing these data, in this study, a new testosterone derivative was synthetized with the objective of evaluating its effect on myocardial injury using an ischemia/reperfusion model. In addition, perfusion pressure and coronary resistance were evaluated in isolated rat hearts using the Langendorff technique. Additionally, molecular mechanism involved in the activity exerted by the testosterone derivative on perfusion pressure and coronary resistance was evaluated by measuring left ventricular pressure in the absence or presence of the following compounds: flutamide, prazosin, metoprolol, nifedipine, indomethacin, and PINANE TXA2. The results showed that the testosterone derivative significantly increases P=0.05 the perfusion pressure and coronary resistance in isolated heart. Other data indicate that the testosterone derivative increases left ventricular pressure in a dose-dependent manner (0.001–100 nM); however, this phenomenon was significantly inhibited P=0.06 by indomethacin and PINANE-TXA2  P=0.05 at a dose of 1 nM. In conclusion, these data suggest that testosterone derivative induces changes in the left ventricular pressure levels through thromboxane receptor activation

Atividade biológica de um benzeno sulfonamida na pressão de perfusão e na resistência coronariana utilizando um modelo isolado de coração de rato

There are studies which indicate that some sulfonamide derivatives can produce changes in the cardiovascular system; however, their biological activity on perfusion presure and coronary resistance is not clear. The aim of this research was to evaluate the effect exerted by benzenesulfonamide, and  their derivatives (2,5-dichloro- N-(4-nitro-phenyl)-benzene-sulfonamide, 2-hydrazino-carbonyl-benzenesulfonamide, 4-(2-amino-ethyl)-benze- ne-sulfonamide, and 4-[3-(4-nitro-phenyl)-ureido]-benzene- sulfonamide) on perfusion pressure and coronary reistance.  To evaluate the biological activity of benzenesulfonamide and their derivatives on perfusion pressure and coronary reistance an isolated rat heart model was used. Furthermore, theoretical interaction of 4-(2-amino-ethyl)-benzenesul- fonamide with Calcium channel surface was determined using 6jp5 protein, nifedipine, amlodipine, verapamil and BayK 8644 as theoretical tools in a DockingServer program. The Results showed that 4-(2-amino-ethyl)-ben- zenesulfonamide decreased perfusion pressure and coronary resistance compared to benzenesulfonamide, 2,5-dichloro- N-(4-nitro-phenyl)-benzene-sulfonamide, 2-hydrazinocar- bonyl-benze-nesulfonamide, 4-[3-(4-nitro-phenyl)-ureido]- benenesulfonamide and the control conditions. Besides, theoretical data suggest that 4-(2-aminoethyl)benzenesulfo- namide could interact with aminoacid residues such as Glu614 and Ala320 involved in 6jp5 protein surface. This phenomenon could result in an ligand-Calcium channel  complex  formation to produce a decrease in perfusion pressure and vascular resistance. It is noteworthy that  biological and experimental  models used in this study is an invaluable research tool for investigating questions across the spectrum of physiologic functions of cardiovascular system such as perfusion pressure and coronary resistanceExistem estudos que indicam que alguns derivados das sulfonamidas podem produzir alterações no sistema cardiovascular entretanto, sua atividade biológica na pressão de perfusão e na resistência coronariana não está clara. O objetivo desta pesquisa foi avaliar o efeito exercido pela benzenossulfonamida e seus derivados (2,5-dicloro-N-(4-nitro-fenil)-benzeno-sulfonamida, 2-hidrazino-carbonil-benzenossulfonamida, 4-(2-amino- etil)-benzeno-sulfonamida e 4-[3-(4-nitro-fenil)-ureido]-benzeno-sulfonamida) na pressão de perfusão e na resistência coronariana. Para avaliar a atividade biológica da benzenossulfonamida e seus derivados na pressão de perfusão e na resistência coronariana, foi utilizado um modelo isolado de coração de rato. Além disso, a interação teórica da 4-(2-amino-etil)-benzenossulfonamida com a superfície do canal de Cálcio foi determinada usando a proteína 6jp5, nifedipina, amlodipina, verapamil e BayK 8644 como ferramentas teóricas em um programa DockingServer. Os resultados mostraram que a 4-(2-amino-etil)-benzenossulfonamida diminuiu a pressão de perfusão e a resistência coronariana em comparação com a benzenossulfonamida, 2,5-dicloro-N-(4-nitro-fenil)-benzeno-sulfonamida, 2-hidrazinocarbonil-benze-nessulfonamida, 4-[3-(4-nitro- fenil)-ureido]-benenossulfonamida e as condições de controlo. Além disso, dados teóricos sugerem que a 4-(2-aminoetil)benzenossulfonamida poderia interagir com resíduos de aminoácidos como Glu614 e Ala320 envolvidos na superfície da proteína 6jp5. Este fenômeno pode resultar na formação de um complexo ligante-canal de Cálcio para produzir uma diminuição na pressão de perfusão e na resistência vascular. Vale ressaltar que, os modelos biológicos e experimentais utilizados neste estudo são uma ferramenta de pesquisa inestimável para investigar questões em todo o espectro de funções fisiológicas do sistema cardiovascular, como pressão de perfusão e resistência coronariana