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1.
BMJ Case Rep ; 14(7)2021 Jul 13.
Artigo em Inglês | MEDLINE | ID: mdl-34257118

RESUMO

Neonatal Dieulafoy's lesion is a rare but serious condition that can be life-threatening if not diagnosed and intervened in a timely manner. It presents with episodes of sudden acute gastrointestinal haemorrhage in the form of blood in vomit and/or blood in stool. In general, most of the lesions are successfully treated with endoscopic or angiographic intervention. Surgery is usually reserved for cases that fail endoscopic or angiographic intervention. We present a neonatal case of duodenal Dieulafoy's lesion that occurred in a 29-week-old male baby with birth weight of 1.2 kg. He developed melena and haematemesis at 4 weeks of life. He required normal saline boluses and transfusion of blood products for acute blood loss. The lesion was successfully treated with endoscopic intervention.


Assuntos
Duodeno , Hemorragia Gastrointestinal , Angiografia , Hemorragia Gastrointestinal/etiologia , Hematemese/etiologia , Humanos , Recém-Nascido , Masculino , Melena/etiologia
2.
Indian J Biochem Biophys ; 50(4): 278-83, 2013 Aug.
Artigo em Inglês | MEDLINE | ID: mdl-24772946

RESUMO

A quantitative structure-activity relationship (QSAR) study was performed on a large series of thiourea derivatives reported by Kang et al. [Bioorg Med Chem Lett (2009), 19, 1950-55 & 6063-68], acting as anti-hepatitis C virus (anti-HCV) agents. The activity of the compounds was found to be significantly correlated with their hydrophobic property and three indicator variables I1, I2 and I3, the first two specifying a negative effect of an alkyl and an aromatic group, respectively on their R-moiety and the third one specifying a negative effect of their Ar-moiety having a nitrogen-containing heterocyclic ring. The whole set containing 85 compounds was divided into two subsets: the training set and the test set containing 61 and 24 compounds, respectively. For the training set, the correlation coefficient (r) and the square of cross-validated correlation coefficient (r2cv) were found to be 0.926 and 0.83, respectively. The correlation obtained suggested that anti-HCV activity of the compounds would depend on their hydrophobic property, conformational flexibility and the steric effects of an alkyl or an aromatic group on the R-moiety. This suggested that the molecules might have significant hydrophobic interactions with the receptor which might be aided by their conformational flexibility, but hindered sterically by an alkyl or an aromatic group on their R-moiety. Using the correlation obtained, some new compounds having activity higher (> 8.0) than the most active compound in the existing series were predicted.


Assuntos
Antivirais/química , Antivirais/farmacologia , Hepacivirus/efeitos dos fármacos , Relação Quantitativa Estrutura-Atividade , Tioureia/química , Tioureia/farmacologia , Descoberta de Drogas
3.
Arch Pharm (Weinheim) ; 340(1): 41-6, 2007 Jan.
Artigo em Inglês | MEDLINE | ID: mdl-17206609

RESUMO

A variety of 3-(4-methyl phenyl)-2-substituted amino-3H-quinazolin-4-ones were synthesized by reacting the amino group of 2-hydrazino-3-(4-methyl phenyl)-3H-quinazolin-4-one with a variety of aldehydes and ketones. The starting material 2-hydrazino-3-(4-methyl phenyl)-3H-quinazolin-4-one was synthesized from 4-methyl aniline. The title compounds were investigated for analgesic, anti-inflammatory, and ulcerogenic index activities. While the test compounds exhibited significant activity, compounds Al, A2, and A3 showed more potent analgesic activity and the compound A3 showed more potent anti-inflammatory activity when compared to the reference standard diclofenac sodium. Interestingly, the test compounds showed only mild ulcerogenic potential when compared to aspirin.


Assuntos
Analgésicos/síntese química , Anti-Inflamatórios/síntese química , Quinazolinonas/síntese química , Analgésicos/farmacologia , Analgésicos/toxicidade , Animais , Anti-Inflamatórios/farmacologia , Anti-Inflamatórios/toxicidade , Aspirina/toxicidade , Carragenina , Diclofenaco/farmacologia , Modelos Animais de Doenças , Edema/induzido quimicamente , Edema/prevenção & controle , Masculino , Camundongos , Estrutura Molecular , Medição da Dor , Limiar da Dor/efeitos dos fármacos , Quinazolinonas/farmacologia , Quinazolinonas/toxicidade , Ratos , Ratos Wistar , Úlcera Gástrica/induzido quimicamente
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