Sinteza i biološko djelovanje novih supstituiranih derivata tiazolin-kinolina

5-Acyl-8-hydroxyquinoline-2-(3\u27-substituted-4\u27-aryl-2,3-dihydrothiazol-2\u27-ylide- ne)hydrazones, 5a-e to 10a-c, were prepared by the reaction of the appropriate 5-acyl-8-hydroxyquinoline-4-substituted thiosemicarbazones 3a-e and phenacyl bromides 4a-e. Structures of the new compounds were verified on the basis of spectral and elemental analyses. Twenty-eight new compounds were tested for their possible antimicrobial activities. Most of the tested compounds showed weak to moderate antibacterial activity against most of the bacterial strains used in comparison with gatifloxacin as a reference drug. The test compounds showed weak to moderate antifungal activity against tested fungi in comparison with ketoconazole as a reference drug. On the other hand, the newly synthesized compounds were tested for their anti-inflammatory effects and most of them showed good to excellent anti-inflammatory activity compared to indomethacin. Moreover, ulcerogenicity and the median lethal dose (LD50) of the most active anti-inflammatory compounds 6b and 9e were determined in mice; they were non-toxic at doses up to 400 mg kg-1 after i.p. administration.5-Acil-8-hidroksikinolin-2-(3\u27-supstituirani-4\u27-aril-2,3-dihidrotiazol-2\u27-ilid- ne)hidrazoni 5a-e do 10a-c pripravljeni su reakcijom odgovarajućih 5-acil-8-hidroksikinolin-4-supstituiranih tiosemikarbazona 3a-e i fenacil bromida 4a-e. Strukture novih spojeva potvrđene su na temelju spektralnih i elementarnih analiza. Dvadeset osam novih spojeva testirano je na potencijalno antimikrobno djelovanje. Većina spojeva pokazuje slabo do umjereno antibakterijsko djelovanje protiv većine testiranih bakterijskih sojeva u usporedbi s gatifloksacinom kao referentim lijekom, te slabo do umjereno antifungalno djelovanje protiv gljivica u usporedbi s ketokonazolom kao referentnim lijekom. Testovi na protuupalno djelovanje pokazuju da većina spojeva posjeduje dobro ili snažno protuupalno djelovanje u usporedbi s indometacinom. Ulcerogeno djelovanje i srednje letalne doze (LD50) najaktivnijih spojeva 6b i 9e određeni su na miševima. Rezultati pokazuju da su netoksični u dozama do 400 mg kg-1 nakon i.p. primjene

Further evidence for an HLA-related recessive mutation in nasopharyngeal carcinoma among the Chinese

We typed 247 cases of nasopharyngeal carcinoma (NPC), a disease predominantly of the southern Chinese, and 274 controls from the Chao Shan region of China's Guangdong province for HLA A and B. Besides confirming the established associations with A2, A33, B46 and B58 (positive associations) and A11 (negative association), the results demonstrated a number of rarer alleles with strong negative association with NPC. Our data, combined with those from the previous studies in Southern Chinese, displayed the protective effects for A31 (odds ratio (OR)=0.0; 95% confidence interval (CI)=0–0.11), B13 (OR=0.50; 95% CI=0.35–0.69), B27 (OR=0.49; 95% CI=0.25–0.92), B39 (OR=0.18; 95% CI=0.06–0.48) and B55 (OR=0.32; 95% CI=0.14–0.68), the ORs comparing individuals with or without each allele. Other ethnic groups do not display such large HLA-associated variation in NPC risk. We show that a linked NPC gene with dominant mode of action could not generate such large protective effects. The results provide strong supporting evidence for the existence of a southern Chinese specific, recessive NPC gene closely linked to the HLA region as a major determinant of the Chinese risk for the disease

Ziv-Zakai bound on time-of-arrival estimation with statistical channel knowledge at the receiver

Time-of-arrival (TOA) based localization plays an important role due to the possibility to exploit the fine delay resolution property when wideband signals are adopted. This paper investigates lower bounds on TOA estimation error for wideband and ultrawide bandwidth (UWB) ranging systems operating in realistic multipath environments. In particular, analytical expressions for the Ziv-Zakai bound (ZZB) on TOA estimation error for multipath channels are provided and discussed under different operating conditions. Using these bounds it is shown how the a priori knowledge about the multipath characteristics can be accounted for in the TOA estimation performance. These bounds serve as useful performance benchmarks for the design of practical TOA estimators.FP7 Network of Excellence in Wireless Communications NEWCom++ (contract no. 216715)FP7 European Project EUWB (Grant no. 215669

Time-of-Arrival Estimation in the Presence of Narrow and Wide Bandwidth Interference in UWB Channels

Ultrawide bandwidth (UWB) positioning techniques have gained significant interest in recent years especially for cluttered environments where signals from satellite navigation systems are not reliable. Range measurements required by UWB positioning systems are usually obtained from the time-of-arrival (ToA) estimation of the first path, which could be a challenging task in the presence of multipath and interference. This paper proposes a practical ToA estimator to mitigate both narrowband and wideband interference. The performance of this estimator is compared with various other ToA estimators for UWB ranging systems. The effect of the interference is evaluated for different system parameters configurations in realistic multipath environments. For the case of simple ToA estimator based on thresholding with averaging filter, we provide a criteria to determine the suitable threshold level when narrowband interference (NBI) is present