Design, synthesis, and PPARgamma agonistic activity of novel indenone derivatives / 药学学报

Agonists of peroxisome proliferator-activated receptor gamma (PPARgamma) are of interest as a treatment of type II diabetes, and indenone derivatives are a new class of non-TZD PPARgamma agonists. Based on existing indenone derivatives, a series of novel ones have been designed and synthesized. Meanwhile the structures have been comfirmed with 1H NMR and MS. Among them, 17b and 19 showed higher agonistic activities than rosiglitazone.

Design, synthesis and biological assay of novel tripeptidic tetrazoles as inhibitors of 20S proteasome / 药学学报

Ubiquitin-proteasome pathway (UPP) is one of the ways utilized for selective degradation of many proteins in cells, and the 20S proteasome takes the functional machinery where hydrolysis of targeted proteins takes place. Based on existing peptide inhibitors, a series of novel tripeptidic tetrazoles have been designed, synthesized, and the structures have been confirmed with 1H NMR, MS and elemental analysis. Among them, three compounds (6b, 6d and 6h) showed inhibitory activities of ChT-L of 20S proteasome.

Comparison of propofol-fentanyl and propofoi-ketamine anesthesia for painless artificial abortion / 中国基层医药

Objective To observe and compare the efficacy and safety between propofol-fentanyl and propo- fol-ketamine for anesthesia of artificial abortion.Methods 450 ASA physical statusⅠandⅡpatients scheduled for elective artificial abortion were randomized into three groups:P group were given intravenous normal saline 2ml be- fore propofol(n=150) ;PF group were given intravenous fentanyl 1?g/kg then propofol(n=150);PK group were given intravenous ketamine 0.4mg/kg then propofol(n=150).Total dose of propofol,extinction time of lash reflex, heart rate(HR),mean arterial pressure(MAP),pulse oxygen saturation(SpO_2),time to open the eye when called, time of full recovery(answering correctly and walking unaided),discomfort,awareness during operation,self-feeling were recorded.Analysis of date was with SPSS 12.0.P＜0.05 was considered significant.Results No episodes of nausea,vomiting,cardio-cerebral syndrome or awareness were noted in all patients;Total dose of propofol,and extinc- tion time of lash reflex in P group were significantly more than those in PK or PF group(P＜0.05),but there was no difference between PK and PF group;MAP,minimum HR and SpO_2 during operation were obviously lower than preoperation or postoperation in those in P or PF group,minimum HR and SpO_2 during operation in P group were significantly lower than in PF or PK group;Minimum HR and SpO_2 during operation in PK group were lower than preoperation,but its decrease extent was less than that in P or PF group(P＜0.05);Time to eye opening in PF or PK group was significantly less than that in P group(P＜0.05);Time to full recovery were not different in three groups;Incidence of pain on injection in PF group(10%)or PK group(8%)was obviously lower than P group (80%);Incidence of coughing and moving during operation in PF group(8%)or PK group(6%)was obviously less than P group(30%);No difference were noted with respect to degree of comfort,time of full recovery,bleeding vol- ume during operation,time to operation.Conclusion Painless artificial abortion can be preformed effectively and safely with propofol-fentanyl or propofol-ketamine,propofol-ketamine especially fits for painless artificial abortion compared with propofol-fantanyl.