The new HIV-1 NNRTI drug Etravirine (TMC125) and a promising drug candidate Rilpivirine (TMC278) in phase III clinical trial are compounds belonging to the diarylpyrimidine (DAPY) family. They are extremely high potent against both wild-type and many drug-resistant HIV-1 strains, providing new hope for HIV-infected patients who fail to use current drugs due to the emergence of drug-resistant HIV mutants. The discovery and development of DAPY derivatives as next-generation NNRTI drugs depend on multidisciplinary coordination and their success has encouraged new researches to explore more next-generation NNRTIs with new scaffolds. This review described the story of discovery and development of DAPY derivatives as next-generation NNRTIs and related progress.

Objective A meta-analysis of clinical trials of prehospital thrombolysis versus in-hospital thrombolysis or PCI for acute myocardia infarction (AMI). Method We collected the literature on prehospital thrombolysis for AMI published at home and abroad from January 1989 to April 2009. Recanalization rate of infarct-related arter, complication incidence and mortality ( ＜ 30 d) were regarded as result indicators. Software RevMan 4.2.8 was used to process meta-analysis. Results There were only 27 literatures selected. Prehospital thrombolysis was associated with higher recanalization rate of infarct-related arter[OR 2.67,95%CI(1.86 ～ 3.85);P ＜0.01] and lower mortality ( ＜ 30 d ) [OR 0.71,95%CI(0.64 ～ 0.78); P ＜ 0.01] than in-hospital thrombolysis. There was no significant difference in complications between them. Compared with PCI, prehospital thrombolysis was associated with higher complication incidence [OR 2.91,95% CI ( 1.26 ～ 3.80); P = O.005]. There was no significant statistical difference of mortality ( ＜30 d ),but the sensitivity analysis was not good. Conchusions The effect and prognosis of prehospital thrombolytic are superior to that of in-hospital thrombolysis,and the same with PCI,but prehospital thrombolytic has higher incidences of complications,and the sensitivity is not good.

Objective To study the treatment effect of joint nitric acid imidazole and itraconazole on recurrent candida vaginitis.Methods 200 confirmed cases of patients with recurrent candida vaginitis in our hospital during October 2014 to June 2015 were selected and divided into research group and the control group with random indicator method,with 100 cases in each group.The control group were treated by nitric acid imidazole vaginal soft capsule,with vaginal drug delivery,which shoud put suppository in vaginal depths after washing,for one times a night and one soft capsule every time,and a week was a period of treatment.The patients in the research group received basis treatment of the control group adding itraconazole capsules(200mg per day,oral).8 weeks after treatment,the patients in this process were reviewed to analyzed clinical efficacy and adverse reactions occured.Results The total effective rate of the research group was 98%,which of the control group was 73%,the difference was statistically significant(χ2 =25.21,P <0.01).The incidence of adverse of patients in the research group was 13%,which of the control group was 14%,there was no statistically significant difference (χ2 =0.04,P >0.05 ).Conclusion The curative effect of itraconazole joint miconazole nitratet to recurrent monilial vaginitis is superior to the use of miconazole nitrate alone, with less adverse reaction,and is easy to use.It is worth clinical application.

By structural modifications of our previous leads 1-3, 18 diarylamines were designed, synthesized and evaluated with a human tumor cell line panel, including A549, DU145, KB, and KB-vin cell lines, resulting in the discovery of new antitumor agents A6 and B2 with low micromolar G50 values ranging from 1.55-2.10 micromol x L(-1) for above cell lines, and A9 with GI50 values ranging from 1.55-2.10 micromol x L(-1) specially for DU145, KB, and KB-vin cells. Current structure-activity relationships are helpful for further lead optimization.

Animals ; Bone Marrow ; metabolism ; Cell Division ; physiology ; Hematologic Diseases ; therapy ; Hematopoiesis ; physiology ; Hematopoietic Stem Cells ; cytology ; Humans ; Renin-Angiotensin System ; physiology

Objective:To observe the effect of electroacupuncture(EA)combined with routine language and motor training on limb and language function,depression,and serum brain injury markers in patients with ischemic stroke. Methods:A total of 86 patients with ischemic stroke were selected and divided into an observation group and a control group using the random drawing method,with 43 cases in each group.Both groups received routine stroke treatments.The control group was additionally treated with routine language and motor training,and the observation group was additionally treated with EA treatment on the basis of the intervention of the control group.Changes in the limb function score,language function score,depression score,and brain injury marker protein were compared between the two groups,and the treatment safety of the two groups was evaluated. Results:The Fugl-Meyer assessment scale scores of both groups were higher than those before treatment(P<0.05),and the Fugl-Meyer assessment scale score of limb function of the observation group was higher than that of the control group(P<0.05).The language function score of the observation group was higher than that of the control group after treatment(P<0.05).The Montgomery-Asberg depression rating scale(MADRS)scores of the observation group were lower than those of the control group after treatment(P<0.05).The levels of brain injury markers heart-type fatty acid-binding protein(H-FABP),glial fibrillary acidic protein(GFAP),and annexin a7(ANXA7)of the observation group were lower than those of the control group(P<0.05).The incidence rate of adverse reactions in the two groups was 14.0%and 9.3%,respectively,with no statistically significant difference between the groups(P>0.05). Conclusion:EA combined with language and motor training is effective in the treatment of ischemic stroke.It can promote the recovery of limb motor function and language function,inhibit the occurrence of depression,and reduce the levels of brain injury markers,with good safety.

Objective We discussed the nursing management measures to improve the qualified rate of sputum culture specimen of patients with pulmonary infection. Methods We monitored the qualified rate of sputum culture specimen, positive rate, pathogen distribution and drug resistance for patients with pulmonary infection in our hospital. Data collected from January 2007 to February 2008 were set as the test group. Data collected from January 2005 to December 2006 were set as the control group. The monitoring effect was compared in the two groups. Results The qualified rate of sputum culture specimen and the distribution of bacteria and fungus in the test group were different from those of the control group (P<0.01). Conclusions To strengthen the quality control of sputum culture specimen, comprehensively improve the cognition of nurses to the significance of qualified rate of sputum culture specimen and the techique of collecting sputum culture specimen could ensure the qualified rate of sputum culture specimen.

Objective To investigate the safety and effectiveness of endoscopical therapy for small grastric stromal tumor( d<2 cm) . Methods Clinical records of 80 patients dignosed as having small grastric stromal tumor by pathology and immunohistochemistry were retrospectively analyzed. Endoscopic or laparo?scopic or open surgery was performed, so patients were divided into endoscopic treatment group ( n=37) and surgical treatment group ( n=43) accordingly. Perioperative period data, effectiveness and follow?up data were analysed. Results Thirty?five cases( 94?6%) of endoscopic treatment group were successfully treated by endoscopic surgery. Intraoperative perforation occurred in 8 cases, among which 2 cases transferred for conventional operations.Pneumoperitoneum occurred in 2 cases (better after symptomatic treatment), while no serious infection or perioperative death occurred. There were no significant differences in the complete re?section rate[ 91?89% ( 34/37) VS 100?0%( 43/43) , P=0?095) , the incidence of postoperative complica?tions[5?71%(2/35)VS 2?33%(1/43),P=0?855)or the improvement of postoperative symptoms[93?10%( 27/29) VS 85?71% ( 30/35) , P=0?589] ,while statistically significant differences were found in operation time[(37?41±13?45)min VS(84?56±38?37)min, P=0?000], intraoperative blood loss[(5?65±5?88)ml VS(31?48 ±39?57)ml, P=0?000], postoperative feeding time[(2?47±0?61)d VS(3?26 ±1?27)d, P=0?001], postoperative hospital stay[(5?76 ±2?28)d VS(7?64±2?99)d,P=0?022],and medical expenses [(18 554?4±9 736?45)yuan VS(31 138?11±1 206?24)yuan, P=0?000]. Conclusion Endoscopic re?section is safe and effective for small grastric stromal tumor with minimal invasion,simple procedure, faster recovery and less economic burden for the patients.

Objective To observe the clinical effect of the Placenta Polypeptides injection combined with paclitaxel plus paraplatin(TC)chemotherapy in the treatment of advanced ovarian cancer.Methods Eighty patients with advanced ovarian cancer receiving tumor cytoreductive surgery were divided into the treatment group and control group,40 cases in each group.The control group accepted single TC chemotherapy,while on this basis the treatment group was added with the Placenta Polypeptides injection.The short-term effect,KPS scores and occurrence of chemotherapeutic toxic reactions were observed in both groups.Results The short-term effective rates in the treatment group and control group were 90.00％ and 87.50 ％ respectively,the difference was not statistically significant (P＞0.05);the living quality KPS score in the treatment group was significantly better than that in the control group,the difference indicated statistical significance(P＜0.05).The occurrence rates of adverse reactions,including leukopenia,nausea and vomiting,liver function damage,heart toxicity,muscle and joint pain were significantly lower than those in the control group (P＜0.05).Conclusion The Placenta Polypeptides injection combined with TC chemotherapeutic regimen in the treatment of advanced ovarian cancer could improve the quality of life of the patients,reduce the toxic and adverse reactions of chemotherapeutic drugs.

Objective To explore micro-trauma and hig h effective method in treating arterial and venous obstruction diseases. Methods Seven patients with lower limbs arterial sclerosis obstruction (ASO) and 33 patients with deep vein thrombosis (DVT) had been treated by ultrasound thrombus ablation. The short-term curative effects were observed. Results All patients achieved vessels recanalization without puncture. Arterial straightness of seven ASO cases was reduced from 93%?12% to 35%?6%. While observing from angiogram, their symptoms and signs ameliorated remarkably. Venous straightness in thirty-three DVT patients was reduced from 100% to 28%?8% by observing from angiogram and disappearance of their limb tumidness. Conclusions Ultrasound thrombus ablation is an effective , safe and micro-trauma method for arterials and venous obstructive diseases.