ABSTRACT
A series of 4-(N-aryl)amino-6-alkoxyl pteridine derivatives was designed and synthesized via the bio-isostere principle using anti-cancer drugs with quinazoline cores as lead compounds.The proliferative inhibitory activities of the synthesized compounds against tumor cells A549,KG1a and HGC-27 were also performed by MTT assay.Using methyl 3-aminopyrazine-2-carboxylate as the starting material,12 target compounds(7a-7l)were synthesized through six-step reaction, and characterized by 1H NMR, 13C NMR and MS.It was showed that antitumor activity of pteridines with 2-chloro-5-nitro-anilino substituted in position 4 was more potent than that of others.The activity of compound 7b on A549 cells(IC50=11.55 μmol/L)was closely approximate to that of positive control gefitinib(IC50=5.95 μmol/L).IC50values of compound 7k on three cell lines were all close to those of gefitinib.A 2-chloro-5-nitro-anilino fragment was contained in preferred compounds which might be modified for further investigation.
ABSTRACT
Objective To study family typology of stroke survivors′spouse and its relationship with perceived social support and offer a basic reference for family intervention. Methods A total of 327 qualified spouses of stroke survivors were investigated in the Family Cohesion and Adaptability Questionnaire (FACESII-CV) and Perceived Social Support Scale (PSSS) for their family typology proportion and relationship with PSSS. Results Compared with normal group, the ratios of extremity type family and middle family type were increased in this study: 23.9%(78/327)vs. 16.4%(20/122), 45.0%(147/327) vs. 29.5%(36/122), while the equilibrium family type were decreased:31.1% (102/327) vs. 54.1%(66/122), and there were significant differences (χ2=23.089, P 0.05). Family typology was the most important factor to PSSS (β=0.212, P 0.05). Conclusions Among the spouses of stroke survivors, the ratios of extremity and middle family type are increased but equilibrium family type are decreased. Family typology is the most important factor to PSSS of survivors′spouse. The PSSS of survivors′spouse in extremity type families is higher than that in middle and equilibrium type families. Intervention should be offered to the families, guiding the conversion of family typology from other types to extremity.
ABSTRACT
OBJECTIVE To evaluate bacterial drug resistance detection value in lower respiratory tract infection treatment.METHODS The data of distribution and antimicrobial resistance of clinical strains in sputum samples in patients with lower respiratory tract infection within some periods were collected and analyzed by WHONET software.Meanwhile,the delivery rates and detection positive rates of clinical species and antibiotics application status in clinic were retrospectively analyzed.RESULTS The delivery rates and detection positive rates of clinical species in patients with lower respiratory tract infection within some periods were 67.8% and 55.9%,respectively.The proportion of Gram-negative bacilli and Gram-positive cocci was 82.39% and 14.18%,respectively.Different drug resistance was displayed in different pathogenic bacteria.Resistant rate of Enterobacteriaceae bacteria and non-ferment bacteria against ciprofloxacin and piperacillin/tazobactam was 47.8%,34.8%and 31.5%,44.7%,respectively and resistant rate of S.aureus against levofloxacin was 63.9%.CONCLUSIONS Although the pathogenic bacteria in patients with lower respiratory tract infection show higher drug resistance to general antibiotics,most of patients with lower respiratory tract infection are treated according to clinical experience of doctors,not based on the results of bacterial culture and antimicrobial susceptibility test.Therefore,the results of bacterial culture and antimicrobial susceptibility test do not play a proper role to direct anti-infective therapy in clinic.