Synthesis and antifungal activity of 3-[2-substituted-5-oxo-3.5-dihydro-6.8-dicarbonitriles-1,2,4-triazolo [1,5-a] pyridin-7-y1] indole derivatives

Base catalyzed reaction of 1-substituted indole-3-carboxaldehydes 2a-d with malononitrile gave the corresponding 3-indolylidene malononitriles 3a-d. Heterocyclization of the latter compounds with 2-cyano-acetohydrazide, 2- acetyl-2-cyanoacetohydrazide and alpha-cyano acetyl arylaldehyde hydrazone derivatives gave the corresponding 1,6-diamino pyridine derivatives 4a-d, 3-[2-methyl-5-oxo-3,5-dihydro-6,8- dicarbonitriles-1,2,4-triazolo[1,5-a] pyridine-7-y1] indoles 5a-d and 3-[2-ary1-5-oxo-3,5-dihydro-6,8-dicarbonitriles-1,2,4-triazolo[1,5-a] pyridin-7-y1] indoles 6a-t, respectively. The target compounds 4a-d, 5a-d and 6a-t were evaluated in vitro against two strains of fungi, Candida albicans [AUCC-1720] and Aspergillus fumigatus [AUMC-1924], Fluconazole and Itraconazole were used as references. All compounds which contain the nitro group were found inefficient [MIC > 100 microg/mL], while the rest of the tested compounds exerted a slight activity [MIC 60-80 microg/mL] against each of C. albicans and A. fumigatus compared with the control

Parathormone, calcitonin and osteocalcin in chronic renal failure with and without schistosomiasis

The present study was conducted on 28 male patients suffering from chronic renal failure aged from 20-40 years, 16 of them were bilharzial and 12 were non bilharzial. Healthy 14 males matching for age were selected as control, 8 of them were bilharzial and 6 were non bilharzial. Serum parathormone, calcitonin and osteocalcin levels were estimated. Serum levels of parathormone and osteocalcin showed significant increase in uremic patients while calcitonin level showed insignificant changes. On the other hand, parathormone, osteocalcin and calcitonin levels in chronic renal failure on top of schistosomal infestation showed insignificant results. It is concluded that the significant increased levels of parathormone and osteocalcin in chronic renal failure can be attributed to disturbance in renal functions due to chronic renal failure

methodological approach to beta-endorphin assay in biological samples

In this study, a methodological approach to B-endorphin in biological fluids [seminal plasma, blood plasma and serum] was done. Measurement of beta-endorphin was performed by immunoassay method [immunoradiometric assay [IRMA] and radioimmunoassay [RIA]], either directly or proceeded by extraction procedures, e.g. Sep Pak [C18], affinity columns of sepharose particles and HPLC. A recovery study of B-endorphin was done to assess the binding effect of endogenous proteins in test samples on assay performance. It can be concluded that measurement of B-endorphin in peripheral blood samples [plasma and serum] can be performed by a direct immunoradiometric assay without extraction methods. As regards the measurement of B-endorphin in seminal plasma by IRMA and RIA, it must be proceeded by acidification of the sample, boiling and extraction by Sep Pak [C18] cartridges

study of parathyroid hormone, calcitonin, and calcium in blood of psoriatic patients

This study was done to evaluate serum calcium, phosphorus, albumin, parathyroid hormone [PTH] and calcitonin [CT] in 40 psoriatic patients [20 with generalized and 20 with localized psoriasis] and their results were compared with a healthy control group [n = 20]. Serum calcium and albumin were significantly reduced in patients with generalized psoriasis compared with control and with localized psoriasis, while psoriatics with localized skin lesions showed hypoalbuminemia with normocalcemia. The correlation between serum calcium and albumin in the studied psoriatic groups was positively highly significant [r = 0.708, P <0.001], so there is a clear correlation between the extent of skin involvement by psoriasis and the reported degree of hypocalcemia and hypoalbuminemia. Serum phosphorus, PTH and CT did not alter in both psoriatic patient groups vs the control group

Urinary N-acetyl-B-D-glucosaminidase, microalbuminuria, and microtransferrinuria as indicators of diabetic nephropathy

Urinary levels of total protein, albumin and transferrin [as estimates of glomerular function] and urinary N-acetyl-B-D-glucosaminidase [NAG] activity [as estimate of tubular function] were determined in 10 healthy control persons [GI] and in 40 insulin-dependent diabetic patients, 10 patients with clinical proteinuria [GIII] and the other 30 patients without clinical proteinuria [GII]. Group II was further subgrouped according to the duration of diabetes into three subgroups: GIIa [10 patients with duration of less than 2 years], GIIb [10 patients with duration of 2 to 10 years, and GIIc [10 patients with duration of more than 10 years]. The patients and controls were also investigated for fasting blood glucose, glycosylated hemoglobin and creatinine clearance. In diabetics with clinical proteinuria, urinary levels of total protein, albumin and NAG activity were significantly increased when compared with other groups. Also, urinary transferrin was only detected in this group. In diabetics without clinical proteinuria creatinine clearance was significantly increased in group IIa and IIb when compared with controls and in group IIb when compared with group IIc. There was a significant increase in microalbuminuria in group IIc when compared with the control, group IIa and group IIb. Also, urinary NAG activity was significantly increased in group IIc when compared with the control and group IIa. Urinary albumin and transferrin were found to be negatively correlated to the creatinine clearance in group III, while there was a positive correlation between urinary transferrin and urinary albumin and total urinary protein in the same group

Comparative study of the levels of B2-microglobulin in serum and synovial fluid in patients with rheumatoid arthritis and osteoarthritis

B2-microglobulin [B2-m], as a low molecular weight protein, was evaluated in serum and synovial fluid of 10 patients with rheumatoid disease [RD], 10 patients with osteoarthritis [OA], and 10 age and sex matched controls. These investigations were done after excluding all patients with renal diseases. It was found that the serum level of B2-m was significantly elevated, in both RD and OA with more increase in the former, when compared with the control group. The synovial fluid/serum ratio of B2-m was a better diagnostic tool that could be used for differentiation between RD and OA, rather than using the serum level of B2-m in each disease alone

Effect of opioids and opioid receptors antagonists on the anterior pituitary hormone secretions in man

The effects of morphine and nafloxone [Opioid receptor antagonist] on secretion of LH, FSH, GH and prolactin hormone were studied in twenty male subjects aged 35-45 years. The results revealed that morphine injection increased FSH, GH and prolactin hormone secretion without a significant effect on LH release, while naloxone injection increased LH and decreased prolactin hormone release without a significant change on FSH and GH release. These data show that both opioids and opioid receptors antagonists exert a rariety of effects on the anterior pituitary secretions in man and this is due to the multiplicity of opiate receptors in pituitary gland cells

Effect of chronic oral zinc administration on serum-prolactin level in chronic renal failure patients

Hyperprolactinaemia and low serum zinc levels are common findings in chronic renal failure patients. In this study, fourteen chronic renal failure men on chronic haemodialysis were given 400 mg zinc sulphate [equivalent to 5 mEq zinc] per day for four months. Serum prolactin and zinc levels were measured before and after oral zinc administration. Statistical analysis of the results revealed a highly significant decrease [P < 0.001] in serum prolactin level after zinc administration [20.01 +/- 1 6 vs 31.74 +/- 2.61 ng/ml]. On the other hand, a highly significant increase [P < 0.001] in serum zinc level was found after zinc administration [16.96 +/- 0.86 vs 10.03 +/- 0.47 mEq/L]. Also, a marked improvement in sexual function was found. So, chronic oral zinc administration may be important in the treatment at hyperprolactinaemia in chronic renal failure men with its sequele as impotence, diminished libido, gynaecomastia and infertility since zinc may play an important role in inhibition of prolactin secretion by pituitary lactotrophes. On conclusion, this study suggests that chronic zinc administration in chronic renal failure patients may be of importance in treatment of hyperprolactinaemia with its sequele of sexual dysfunctoin as diminished libido, impotence. gynaecomastia and infertility

effect of different hypoglycemic agents on plasma lipid pattern

Fifty nine maturity onset diabetic patients with hyperlipemia have been studied as regards the effects of hypoglycemic agents on their blood lipid pattern. Insulin, metformin and diamicron led to significant decrease of serum free fatty acids, triglycerides, cholesterol and B-lipoproteins level, diet control or tolbutamide had no such an effect on blood lipids

Serum copper levels in epilepsy

Estimation of serum copper level in forty epileptic cases together with normal controls. The effect of treatment with diphenyl-hydantoin on the serum copper level was also studied. Significant elevation of serum copper level was demonstrated in untreated cases, while low levels were also observed in cases treated with diphenyl-hydantoin. Possible underlying mechanisms were discussed