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Inhibition of this enzyme will locally in the bone lead to an increase in E2 and T levels, two key players in the maintenance of the balance between bone resorption and bone formation. In this study, a new class of 17\u03b2HSD2 inhibitors with a 1<jats:italic>H<\/jats:italic>\u20101,2,4\u2010triazole scaffold was identified; the three best compounds <jats:bold>8b<\/jats:bold>, <jats:bold>8f<\/jats:bold>, and <jats:bold>13a<\/jats:bold> showed moderate 17\u03b2HSD2 inhibitory activity and a good selectivity toward 17\u03b2HSD1. They could be a useful tool to map the unexplored enzyme active site.<\/jats:p>","DOI":"10.1002\/ardp.201200025","type":"journal-article","created":{"date-parts":[[2012,4,25]],"date-time":"2012-04-25T11:05:22Z","timestamp":1335351922000},"page":"610-621","source":"Crossref","is-referenced-by-count":12,"title":["Synthesis and Biological Evaluation of Phenyl Substituted 1<i>H<\/i>\u20101,2,4\u2010Triazoles as Non\u2010Steroidal Inhibitors of 17\u03b2\u2010Hydroxysteroid Dehydrogenase Type 2"],"prefix":"10.1002","volume":"345","author":[{"given":"Yaseen A.","family":"Al\u2010Soud","sequence":"first","affiliation":[],"role":[{"role":"author","vocabulary":"crossref"}]},{"given":"Sandrine","family":"Marchais\u2010Oberwinkler","sequence":"additional","affiliation":[],"role":[{"role":"author","vocabulary":"crossref"}]},{"given":"Martin","family":"Frotscher","sequence":"additional","affiliation":[],"role":[{"role":"author","vocabulary":"crossref"}]},{"given":"Rolf W.","family":"Hartmann","sequence":"additional","affiliation":[],"role":[{"role":"author","vocabulary":"crossref"}]}],"member":"311","published-online":{"date-parts":[[2012,4,25]]},"reference":[{"key":"e_1_2_6_2_2","doi-asserted-by":"publisher","DOI":"10.1016\/j.jsbmb.2010.12.013"},{"key":"e_1_2_6_3_2","doi-asserted-by":"publisher","DOI":"10.1126\/science.2845584"},{"key":"e_1_2_6_4_2","doi-asserted-by":"publisher","DOI":"10.1021\/jm058042r"},{"key":"e_1_2_6_5_2","doi-asserted-by":"publisher","DOI":"10.1016\/j.bmcl.2005.11.099"},{"key":"e_1_2_6_6_2","doi-asserted-by":"publisher","DOI":"10.1021\/jm0702938"},{"key":"e_1_2_6_7_2","doi-asserted-by":"publisher","DOI":"10.1016\/S0960-0760(03)00070-0"},{"key":"e_1_2_6_8_2","doi-asserted-by":"publisher","DOI":"10.1016\/j.bmc.2007.10.094"},{"key":"e_1_2_6_9_2","doi-asserted-by":"publisher","DOI":"10.1021\/jm100400a"},{"key":"e_1_2_6_10_2","doi-asserted-by":"publisher","DOI":"10.1016\/j.ejmech.2009.01.002"},{"key":"e_1_2_6_11_2","doi-asserted-by":"publisher","DOI":"10.1021\/jm701447v"},{"key":"e_1_2_6_12_2","doi-asserted-by":"publisher","DOI":"10.1021\/jm800367k"},{"key":"e_1_2_6_13_2","doi-asserted-by":"publisher","DOI":"10.1021\/jm1009082"},{"key":"e_1_2_6_14_2","doi-asserted-by":"publisher","DOI":"10.1021\/jm8006917"},{"key":"e_1_2_6_15_2","doi-asserted-by":"publisher","DOI":"10.1016\/j.bmc.2008.04.073"},{"key":"e_1_2_6_16_2","doi-asserted-by":"publisher","DOI":"10.1021\/jm901195w"},{"key":"e_1_2_6_17_2","doi-asserted-by":"publisher","DOI":"10.1016\/j.bmc.2010.03.065"},{"key":"e_1_2_6_18_2","doi-asserted-by":"publisher","DOI":"10.1021\/jm101073q"},{"key":"e_1_2_6_19_2","doi-asserted-by":"publisher","DOI":"10.1002\/cmdc.201000457"},{"key":"e_1_2_6_20_2","doi-asserted-by":"publisher","DOI":"10.1016\/S0960-894X(99)00234-6"},{"key":"e_1_2_6_21_2","doi-asserted-by":"publisher","DOI":"10.1016\/S0223-5234(00)01167-3"},{"key":"e_1_2_6_22_2","doi-asserted-by":"publisher","DOI":"10.1016\/S0968-0896(00)00070-5"},{"key":"e_1_2_6_23_2","doi-asserted-by":"publisher","DOI":"10.1021\/jm0208471"},{"key":"e_1_2_6_24_2","doi-asserted-by":"publisher","DOI":"10.1016\/S0968-0896(01)00293-0"},{"key":"e_1_2_6_25_2","doi-asserted-by":"publisher","DOI":"10.1021\/ml100071j"},{"key":"e_1_2_6_26_2","doi-asserted-by":"publisher","DOI":"10.1021\/ml100283h"},{"key":"e_1_2_6_27_2","doi-asserted-by":"publisher","DOI":"10.1021\/jm800377h"},{"key":"e_1_2_6_28_2","doi-asserted-by":"publisher","DOI":"10.1021\/jm800683c"},{"key":"e_1_2_6_29_2","doi-asserted-by":"publisher","DOI":"10.1021\/jm800888q"},{"key":"e_1_2_6_30_2","doi-asserted-by":"publisher","DOI":"10.1021\/jm101470k"},{"key":"e_1_2_6_31_2","doi-asserted-by":"publisher","DOI":"10.1016\/S0021-9258(18)31480-7"},{"key":"e_1_2_6_32_2","doi-asserted-by":"publisher","DOI":"10.1097\/MED.0b013e3282fe6ca9"},{"key":"e_1_2_6_33_2","doi-asserted-by":"publisher","DOI":"10.1210\/er.2003-0003"},{"key":"e_1_2_6_34_2","first-page":"267","volume":"8","author":"Bagi C. 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