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Biomedical subjects

H Akgün

Publications and source records attributed to H Akgün.

10 recordsLinked to original sources

Rapidly relapsing squamous cell carcinoma of the renal pelvis associated with paraneoplastic syndromes of leukocytosis, thrombocytosis and hypercalcemia.

A case history is reported here in which leukocytosis, thrombocytosis and hypercalcemia associated with rapidly relapsing squamous cell carcinoma (SCC) of the renal pelvis were observed. In a 58-year-old man, SCC of the renal pelvis was documented during nephrolithotomy, and right nephrectomy was performed. Local relapse of the tumor occurred rapidly in 2 months' time and hypercalcemia, leukocytosis and thrombocytosis worsened in accordance with tumor volume. Cranial computerized tomography (CT), thorax CT and bone scintigraphy were negative for metastasis. The serum parathyroid hormone level was 28 pg/ml (normal 9- 55 pg/ml). To disclose leukocytosis and thrombocytosis, peripheral smear and bone marrow aspiration were performed and no pathologic finding regarding any hematologic disorder was found; the samples were also BCR-ABL negative and Philadelphia chromosome negative. Production of several factors by tumor cells may be responsible for this paraneoplastic syndrome. The association of SCC of the renal pelvis with this triple paraneoplastic syndrome is an extremely rare occurrence.

Carcinoma, Squamous Cell↗

Quantitative structure-activity relationship study of some 7-substituted theophyllines.

Some novel 7-substituted theophylline derivatives have been investigated for quantitative structure-activity relationship (QSAR). For this purpose, their bronchodilatory activities (in vitro), which were examined by the inhibition of acetylcholine induced contraction in tracheae isolated from guinea pigs, have been correlated with various quantum chemical and physicochemical parameters.

Acetylcholine↗

New beta-diketone and 3,5-dimethyl isoxazole derivatives of theophylline as potential bronchodilator agents.

Ten new compounds having 7-[(2,4-pentanedione-3-yl)alkyl]- and 7-[(3,5-dimethylisoxazole-4-yl)alkyl]-3,7-dihydro-1,3-dimethyl-1H- purine-2, 6-dione structures were synthesized and their bronchodilator activities investigated using the method based on inhibition of acetylcholine and histamine-induced contractions in guinea pig trachea. None of the compounds were effective on acetylcholine-induced contractions. However, the compounds 4d, 4e, 5d and 5c were potent inhibitors of the bronchospasm induced by histamine, whereas the others (4b, 4c, 5b and 5c) were weak inhibitors.

Acetylcholine↗

Synthesis of some 2-arylpropionic acid amides as prodrugs.

The synthesis of amide prodrugs of some 2-arylpropionic acids (ibuprofen, naproxen, diclofenac and ketorolac) and the enantiomeric separation of these compounds are reported in this paper. The compounds were prepared from the corresponding 2-arylpropionic acids and (R-(-)-2-amino-1-butanol in the presence of N,N'-dicyclohexylcarbodiimide (DCC). Enantiomers were separated by preparative chromatography or crystallisation. The structure were confirmed by infrared, nuclear magnetic resonance and elementary analysis. The compounds prepared in the study have significant analgesic activity.

Administration, Topical↗

Synthesis and antifungal activity of some new benzimidazole derivatives.

Synthesis and antifungal evaluation of 5-ethoxycarbonyl-2-(substituted-benzyl or phenoxymethyl)benzimidazoles are reported. Structures of the compounds were elucidated with IR-, 1H-NMR-, 13C-NMR-, mass-spectra and elemental analysis. Preliminary results show that none of the synthesized benzimidazole derivatives has antifungal activity at the concentration of 100 micrograms/ml against Candida parapsilosis, Candida stellatoidea, and Candida pseudotropicalis.

Antifungal Agents↗

Synthesis of some substituted quinazolinediones as potential inhibitors of smooth muscle contraction.

3-Substituted 2,4(1H,3H)-quinazolinediones were prepared from the corresponding N-substituted 2-aminobenzamides by treatment with ethyl chloroformate and KOH in ethanol. Also, a series of 3-substituted and 1-methyl-3-substituted 2,4(1H,3H)-quinazolinediones were synthesized by the reaction of 1-methyl-1,4-dihydro- and 1,4-dihydro-2,4-dioxo-3(2H)-quinazolineacetic acid with the corresponding N-substituted piperazines. The 13C NMR spectra and mass spectra of the compounds were measured and signals were assigned. Some of the compounds showed inhibitory action on contractile function of smooth muscle.

Animals↗

New naphthyloxyalkyl beta-diketone and 3,5-dimethylisoxazole derivatives as potential antiviral agents.

Ten new compounds having 3-[(2-naphthyloxy)alkyl]-2,4-pentanedione and 4-[(2-naphthyloxy)alkyl]-3,5-dimethylisoxazole structures were synthesized and their cytotoxicities and antiviral activities investigated. 3-[6-(2-Naphthyloxy)hexyl]-2,4-pentandione possessing inhibitory activity on the replication of both adenovirus type 5 and poliovirus type 1 at 20 micrograms/ml was the most active compound in the series.

Antiviral Agents↗