RESUMO
INTRODUCTION: Golden standard of acute stroke treatment is recanalisation therapy. However, opening the occluded blood vessel sometimes does not show the expected clinical result or leads to haemorrhagic complications. As neuroinflammation and neurotoxicity play an important role in the pathophysiology of stroke, neuroprotective agents might preserve brain tissue after futile recanalisation. PATIENTS AND METHODS: After recanalisation therapy and not later than 24 h after symptoms onset, patients with initial NIHSS of ≥ 8 were assigned to the investigational and control group. The investigational group received intravenous Cerebrolysin as add-on therapy. The primary objective was to assess the clinical efficacy of Cerebrolysin. The secondary objective was to investigate its effect on haemorrhagic transition and to confirm its safety profile. RESULTS: Baseline characteristics of patients showed no significant differences between the two groups. No difference could be detected between the two groups in the mRS scale though the Cerebrolysin group showed descriptive superiority over the control group. We found a statistically significant difference considering haemorrhagic transition and mortality rate in favour of the Cerebrolysin group. DISCUSSION: The multimodal neurotrophic agent Cerebrolysin holds promise to impact on the late consequences of a reperfusion syndrome. Its influence on reducing neuroinflammation, promoting neuronal cell viability and neurogenesis as well as the stabilising effect on the blood-brain barrier suggests a protective effect on the neurovascular unit even when no recanalisation occurs. We confirmed the excellent safety profile of Cerebrolysin. CONCLUSION: Cerebrolysin as add-on therapy might be beneficial and safe for patients with acute stroke in terms of lowering risk for haemorrhagic complications after recanalisation therapy.
Assuntos
Aminoácidos/uso terapêutico , Hemorragias Intracranianas/epidemiologia , Fármacos Neuroprotetores/uso terapêutico , Acidente Vascular Cerebral/tratamento farmacológico , Acidente Vascular Cerebral/cirurgia , Idoso , Idoso de 80 Anos ou mais , Feminino , Humanos , Masculino , Futilidade Médica , Pessoa de Meia-Idade , Estudos Prospectivos , Acidente Vascular Cerebral/complicações , Resultado do TratamentoRESUMO
Starting from 3-hydroxy-1,4-benzodiazepin-2-ones 1--3, via 3-chloro derivatives 4--6, 13 new C(3)-substituted 1,4-benzodiazepin-2-ones were synthesized. Reaction of 4--6 with ethylene glycol yielded 3-(beta-hydroxyethyl) derivatives 7--9. Similar reaction with the isopropylidene derivative of glycerol afforded 10--12, which on hydrolysis of the isopropylidene group hielded glycerol derivatives 13--15. Reaction of trichloroacetyl chloride with oxazepam and temazepam yielded the corresponding trichloroacetyl esters 16 and 17. The beta-hydroxyethyl derivative 7 was conjugated with an acetylated glucopyranose derivative to give isomeric 18 and 19. Partition coefficients (log Poct) and central nervous system activities (in six stranded tests) were determined for 7--15 as well as several standard compounds. Most of the compounds exhibiting beneficial central nervous system activity had Poct values between 1.71 and 2.48. No correlation between lipophilicity and central nervous system activity could be discerned for these compounds.
Assuntos
Benzodiazepinonas/síntese química , Sistema Nervoso Central/efeitos dos fármacos , Animais , Benzodiazepinonas/farmacologia , Ésteres/síntese química , Éteres/síntese química , Feminino , Masculino , Camundongos , SolubilidadeRESUMO
The authors describe the synthesis of I-aminomethylisatin (3) from [I-chloromethylisatin] (1) by means of the Delépine reaction. On condensation with aromatic aldehydes, 3 yields the azomethines 5--7. The azomethine 5 is converted into the corresponding thiosemicarbazone 9. Testing for mitodepressive activity showed that the compounds 5--7 are active. On testing in vitro for tuberculostatic effects, the compound 9 proved exceptionally potent.
Assuntos
Compostos Azo/síntese química , Indóis/síntese química , Isatina/síntese química , Antituberculosos/síntese química , Compostos Azo/farmacologia , Isatina/análogos & derivados , Isatina/farmacologia , Mitose/efeitos dos fármacos , Plantas/efeitos dos fármacosAssuntos
Anti-Infecciosos/farmacologia , Monoterpenos , Óleos Voláteis/farmacologia , Plantas/química , Antibacterianos , Anti-Infecciosos/química , Bactérias/efeitos dos fármacos , Cromatografia Gasosa , Monoterpenos Cicloexânicos , Fungos/efeitos dos fármacos , Mentol/análogos & derivados , Mentol/farmacologia , Testes de Sensibilidade Microbiana , Óleos Voláteis/química , Extratos Vegetais/química , Extratos Vegetais/farmacologiaRESUMO
The electron impact mass spectra of some benzo[1,2-b:4,5-b']dithiophene-2,6-dicarboxylic acid dianilides and dithieno[3,2-b:2',3'-d]thiophene-2,6-dicarboxylic acid dianilides are discussed. Dominant peaks in these dianilides are formed by the cleavage of a C-N bond on one side of an anilino group. These ions fragment further by the cleavage of a C-C bond on the other side of an anilino group and a CONRPhR' group may be lost directly. After loss of CO, the characteristic benzodithiophene radical cation, C10H2S2Cl2[symbol: see text], at m/z 256 and the dithienothiophene radical cation, C8S3Cl2[symbol: see text], at m/z 262 are formed from their respective precursor compounds.