ABSTRACT
Objective To design and investigate an effective synthetic route of the antivirus compound favipiravir(T-705) with a stable and high yield. Methods The commercial available diethyl aminomalonate hydrochloride was selected as the starting material. The product of aminolysis was cyclized with glyoxal to yield 3-hydroxy-2-pyraziamide, which was subjected to nitration with KNO3, chlorination and dehydration with POCl3 and fluorination with KF to afford 3, 6-difluoropyrazin-2-carbonnitrile. The difluorate product was further hydrolyzed and oxidized to give favipiravir. Results The target compound was efficiently prepared by the above synthetic route. Conclusion The reaction conditions are mild except the fluoro-substitution, in which all reagents should be dried completely. The synthetic procedure is simple, high-yield and suitable for scale preparation.
ABSTRACT
OBJECTIVE To evaluate the efficacy and safety of levofloxacin in the treatment of respiratory tract infection in elderly patients. METHODS An open clinical trial was conducted for the treatment of respiratory tract infection in elderly patients.The dosage of the drug was 0.5g once daily injection,the duration of treatment was 7-14 days. RESULTS The total cure rate,the total response rate and the bacterial clearance rate were 56.7%,83.3%,and 82.1%,respectively. CONCLUSIONS Levofloxacin is a drug both effective and safe for respiratory tract infection in elderly patients.The dosage of the drug(0.5g/day) can reach higher clinical effective rate,best tolerance and compliancy.
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<p><b>OBJECTIVE</b>To investigate the role of adrenomedullin (AM) in the development of hypoxic pulmonary hypertension (HPH), and to assess the expression of AM and adrenomedullin receptor (AMR) in the lungs of rats with HPH.</p><p><b>METHODS</b>We exposed 10 rats to normobaric hypoxic conditions for 3 weeks to establish rat model of pulmonary hypertension; and 10 other rats were used as normoxic controls. Mean pulmonary arterial pressure (mPAP) was measured by a right cardiac catheterization. The thickness of pulmonary arterioles was measured by a computerized image analyzer. We used the reverse transcription-polymerase chain reaction (RT-PCR) to assess the change of expression of AM and AMR in lung of HPH rat model.</p><p><b>RESULTS</b>Compared with the control group, hypoxic rats developed remarkable pulmonary hypertension, increment in the thickness of pulmonary arterioles and right ventricular hypertrophy (P < 0.01). Chronic hypoxia elicited a considerable increment in expression of AM and AMR in the lungs of rats, and the ratio of AM/beta-actin and AMR/beta-actin in lungs of rats treated with hypoxia were significantly higher (P < 0.01).</p><p><b>CONCLUSIONS</b>The AM plays an important role in regulating pulmonary vascular tone and can ameliorate the development of hypoxic pulmonary hypertension in rats.</p>