[Control of blood pressure morning surge in a lebanese hypertensive population]

The primary endpoint of this prospective clinical study is to ascertain the degree of blood pressure control in the early-morning hours after 8 weeks of treatment with telmisartan in hypertensive patients using home blood pressure measurements. Two hundred forty Lebanese patients with uncontrolled hypertension are enrolled in the study. The blood pressure is measured at the initial visit, then at week 4 of follow-up [optional visit] and after the 8 weeks period, by the physician at his office [with pulse rate] and by the patient at home in the morning. The blood pressure measured by the patient at home in the morning has a mean value of 129.7/79.1 mmhg, significantly less than 135/85 mmhg [P< 10[-5]], and it is reduced by 31.9/13.5 mmhg [P< 10[-5]]. At the physician's office, the reduction is 34.8/16 mmhg [P< 10[-5]. Heart rate is decreased by 4.7 +/- 0.5 bpm [P< 10[-5]. The drug was well tolerated. This study has demonstrated that Telmisartan, by his long half-life, protects the patients against the early-morning hours blood pressure surge, period during which coronary and cerebral events are the most frequent

Some reactions of 3-methyl- 1- phenyl-4- [phenylamino-thiocarbonyl] -2- pyrazolin-5-one

The title compound 1 was prepared via reaction of 3-methyl-1-phenyl-2-pyrazolin-5-one with phenylisothiocyanate. Then, it was converted to pyrazolopyrazole, pyrazolopyrimidine, pyrazolopyridine, and the amino derivatives through reaction with hydrazines, urea, thiourea, malononitrile and aromatic amines. Compound [1] prepared via addition of activated nucleophilic carbon of 3-methyl-1-phenyl-2-pyrazolin-5-one to the electrophilic carbon of phenylisothiocyanate seemed to be suitable to annulation through its reactive center. The reaction of [1] with hydrazine hydrate and phenyl-hydrazine in boiling ethanol gave the pyrazolopyrazole derivatives [2a] and [2b], respectively. The mass spectrum of [2a] showed the parent ion peak at m/z 289 and the following abundant peaks 185, 105, 91, 77, and 51. Structure of [2a] was further established by its reaction with ethyl bromoacetate to give [3]. The latter afforded the hydrazide derivative [4] on reaction with hydrazine hydrate