The urban centers of developing countries like Karachi city in Pakistan are facing the menace of air pollution and atmospheric wet deposition can be used as a tool for monitoring the quality of air.
A series of exploratory investigations with multiple agents was carried out in normal rats and in rats with uranyl nitrate-induced acute renal failure to understand the disposition characteristics of intravenous topotecan (TPT) used as a model substrate. The disposition of TPT was unaltered in normal rats when treated with methotrexate, whereas treatment with probenecid increased the systemic exposure of TPT. In case of uranyl nitrate-induced acute renal failure (UN-ARF) rats, the systemic exposure of TPT was increased when compared with normal rats, whereas in UN-ARF rats treated with probenecid a further reduction in renal clearance of TPT was noted as compared with that of UN-ARF induced rats. Thus, TPT may be involved in the tubular secretory pathway when a passive glomerular filtration pathway for elimination was not possible. The disposition of TPT did not normalize in UN-ARF rats when treated with caffeine, a non-selective adenosine A1 receptor antagonist, whereas the selective adenosine A1 receptor antagonist (1,3-dipropyl-8-phenylxanthine, DPPX) normalized TPT pharmacokinetic disposition by improving renal function. Renal excretion studies demonstrated that CLR improved by almost fivefold following DPPX treatment in ARF rats. In addition, the qualitative stability/metabolism pattern of TPT in liver microsomes prepared from various groups of rats (normal rats, UN-ARF rats, rats treated with DPPX, and UN-ARF rats treated with DPPX) was found to be similar. In summary, using a pharmacokinetic tool as a surrogate, it has been shown that the pharmacokinetic disposition of TPT improved considerably upon treatment with DPPX, a selective adenosine A1 antagonist.
In this study, seventeen urea derivatives, including the five new and N-(2-methylphenyl)-2-oxo-1--pyrrolidinecarboxamide (15), were synthesized by reacting ortho-, meta-and para-tolyl isocyanate with primary and secondary amines using a previously reported method. All the series 1-17 were subjected to urease, β-glucuronidase and snake venom phosphodiesterase enzyme inhibition assays. The ranges of inhibition of urease, β-glucuronidase and phosphodiesterase enzymes were 0.30-45.3, 4.9-44.9 and 1.2-46.4 %, respectively. Moreover, an effect of these compounds on a prostate cancer cell line was observed. The new compound N-(1,3-benzothiazol-2-yl)-N′-(3-methylphenyl)urea (9) showed in vitro anticancer activity with an IC 50 value of 78.28±1.2 μM. All the compounds were characterized by state of art spectroscopic techniques. са примарним и секундарним аминима. Испитана је инхибиторна активност добијених деривати према уреази, β-глукуронидази и фосфодиестерази змијског отрова. Утрвђено је да је опсег инхибиције према уреази, β-глукуронидази и фосфодиестерази ѕмијског отрова. 0, 3-45,3, 4,9-44,9 и 1,2-46,4 %, редом. Осим тога, испатан је и ефекат синтетисаних једињења према ћелијској линији рака простате. Нов дериват N-(1,3-бензотиазол-2-ил)-N′-(3-метилфенил)уреа (9) показује in vitro активност IC 50 од 78,3±1,2 μM. Сва синтетисана једињења окаратактерисана су стандардним спектроскопским техникама.
A series of fourteen (14) N-nitrophenyl-N'-(alkyl/aryl)urea and symmetrical 1,3-disubstituted urea derivatives were synthesized and evaluated for their antidepressant activity in mice. Among them, N-(4-nitrophenyl)-N'-(1'-phenylethyl)urea (1), demonstrated profound antidepressant property as reflected by significant reduction in the immobility time (89.83%), whereas compounds 2-6 showed activity values between 36 to 59% which were also larger than the standard phenelzine. Compounds 7-9 were less effective in reducing the immobility period of mice 26.20 to 31.01%). This variable magnitude of antidepressant activity appears to be related to the position of the nitro group to the parent molecules 1, 2, and 8. Compound 1 with the nitro group at para position showed to be the most effective antidepressant. However, the activity declined, if the nitro is attached to ortho and meta positions.
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