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The present study explored the relationship among urban and rural residence living and level of exercise in the Republic of Korea. The study analysed the data from the 2012 Korean Survey of Citizens’ Sports Participation project with a total of 4,479 males and 4,521 females participating. The sampling method used the square root of the proportional allocation design with clustering and stratifications in such way that the survey sampled represented all the people of the Republic of Korea. Multivariate logistic regression analyses were carried out to examine whether residence was related to frequency, intensity, time and duration of exercise, adjusting for the covariate age. The results show that Korean women in rural areas had lower levels of exercise than their urban counterparts in terms of frequency, time, duration and intensity of the exercise. However, there was little or no relationship among exercise levels and place of residence among Korean men. In addition, Korean men and women in rural areas had lower levels of access to “systematic fitness management”, such as fitness instructors and exercise facilities. [ABSTRACT FROM AUTHOR]

Abstract: The discovery, in vitro and in vivo studies of the highly potent AT1 antagonist 12a (BR-A-657, Fimasartan) antagonists are presented. A series of pyrimidin-4(3H)-one derivatives as losartan analogue were synthesized and evaluated for a novel class of AT1 receptor antagonists. Among them, 12a containing thioamido moiety displayed both high in vitro functional antagonism and binding affinity [IC50 =0.42 and 0.13nM, respectively] and inhibited strongly in vivo AngII-induced pressor response in pithed rats with an ED50 of 0.018mg/kg. Moreover, in vivo evaluation in furosemide-treated rat and conscious renal hypertensive rat models and the pharmacokinetic study showed that 12a is a highly potent and orally active AT1 selective antagonist having stronger in vivo potency than losartan. [Copyright &y& Elsevier]

Abstract: As a development strategy for backups of Fimasartan (1), a comparative molecular similarity indices analysis (CoMSIA) of a set of sixty-five 5-(biphenyl-2-yl)-1H-tetrazole derivatives has been performed to find out the pharmacophore elements for angiotensin II receptor type 1 (AT1) blockade. The most potent compound containing pyrimidin-4(3H)-one ring, Fimasartan (1) was used to align the molecules. As a result, we obtained 3D-QSAR model which provided good predictivity for both the training set (q 2 =0.846, r 2 =0.975) and the external test set . This model would guide the design of backups for Fimasartan (1), a launched oral antihypertensive agent. [Copyright &y& Elsevier]