{"status":"ok","message-type":"work","message-version":"1.0.0","message":{"indexed":{"date-parts":[[2026,4,24]],"date-time":"2026-04-24T23:15:41Z","timestamp":1777072541978,"version":"3.51.4"},"reference-count":22,"publisher":"Wiley","issue":"8","license":[{"start":{"date-parts":[[2019,7,29]],"date-time":"2019-07-29T00:00:00Z","timestamp":1564358400000},"content-version":"vor","delay-in-days":0,"URL":"http:\/\/onlinelibrary.wiley.com\/termsAndConditions#vor"}],"content-domain":{"domain":["onlinelibrary.wiley.com"],"crossmark-restriction":true},"short-container-title":["Archiv der Pharmazie"],"published-print":{"date-parts":[[2019,8]]},"abstract":"<jats:title>Abstract<\/jats:title><jats:p>A series of 1,2,4\u2010triazolo[1,5\u2010<jats:italic>a<\/jats:italic>]pyrimidine derivatives was designed, synthesized, and screened for their phosphodiesterase (PDE 4B) inhibitory activity and bronchodilation ability. Compound <jats:bold>7e<\/jats:bold> showed 41.80% PDE 4B inhibition at 10\u2009\u00b5M. Eight compounds were screened for their bronchodilator activity, where compounds <jats:bold>7f<\/jats:bold> and <jats:bold>7e<\/jats:bold> elicited promising bronchodilator activity with EC<jats:sub>50<\/jats:sub> values of 18.6 and 57.1\u2009\u00b5M, respectively, compared to theophylline (EC<jats:sub>50<\/jats:sub>\u2009=\u2009425\u2009\u00b5M). Molecular docking at the PDE 4B active site revealed a binding mode and docking scores comparable to those of a reference ligand, consistent with their PDE 4B inhibition activity.<\/jats:p>","DOI":"10.1002\/ardp.201900002","type":"journal-article","created":{"date-parts":[[2019,7,29]],"date-time":"2019-07-29T08:00:39Z","timestamp":1564387239000},"update-policy":"https:\/\/doi.org\/10.1002\/crossmark_policy","source":"Crossref","is-referenced-by-count":15,"title":["Design and synthesis of 1,2,4\u2010triazolo[1,5\u2010<i>a<\/i>]pyrimidine derivatives as PDE 4B inhibitors endowed with bronchodilator activity"],"prefix":"10.1002","volume":"352","author":[{"given":"Rehab H.","family":"Abd El\u2010Aleam","sequence":"first","affiliation":[{"name":"Pharmaceutical Chemistry Department, Faculty of Pharmacy Nahda University  Beni Suef Egypt"}],"role":[{"role":"author","vocabulary":"crossref"}]},{"ORCID":"https:\/\/orcid.org\/0000-0002-2493-1315","authenticated-orcid":false,"given":"Riham F.","family":"George","sequence":"additional","affiliation":[{"name":"Pharmaceutical Chemistry Department, Faculty of Pharmacy Cairo University  Cairo Egypt"}],"role":[{"role":"author","vocabulary":"crossref"}]},{"given":"Kevin J.","family":"Lee","sequence":"additional","affiliation":[{"name":"USA Mitchell Cancer Institute Drug Discovery Laboratory University of South Alabama  Mobile Alabama"}],"role":[{"role":"author","vocabulary":"crossref"}]},{"given":"Adam B.","family":"Keeton","sequence":"additional","affiliation":[{"name":"USA Mitchell Cancer Institute Drug Discovery Laboratory University of South Alabama  Mobile Alabama"}],"role":[{"role":"author","vocabulary":"crossref"}]},{"given":"Gary A.","family":"Piazza","sequence":"additional","affiliation":[{"name":"USA Mitchell Cancer Institute Drug Discovery Laboratory University of South Alabama  Mobile Alabama"}],"role":[{"role":"author","vocabulary":"crossref"}]},{"given":"Amr A.","family":"Kamel","sequence":"additional","affiliation":[{"name":"Pharmacology and Toxicology Department, Faculty of Pharmacy Minia University  El\u2010Minia Egypt"}],"role":[{"role":"author","vocabulary":"crossref"}]},{"given":"Mahmoud E.","family":"El\u2010Daly","sequence":"additional","affiliation":[{"name":"Pharmacology and Toxicology Department, Faculty of Pharmacy Minia University  El\u2010Minia Egypt"}],"role":[{"role":"author","vocabulary":"crossref"}]},{"given":"Ghaneya S.","family":"Hassan","sequence":"additional","affiliation":[{"name":"Pharmaceutical Chemistry Department, Faculty of Pharmacy Cairo University  Cairo Egypt"},{"name":"Pharmaceutical Chemistry Department, Faculty of Pharmacy Badr University  Badr City Cairo Egypt"}],"role":[{"role":"author","vocabulary":"crossref"}]},{"given":"Hamdy M.","family":"Abdel\u2010Rahman","sequence":"additional","affiliation":[{"name":"Pharmaceutical Chemistry Department, Faculty of Pharmacy Nahda University  Beni Suef Egypt"},{"name":"Medicinal Chemistry Department, Faculty of Pharmacy Assiut University  Assiut Egypt"}],"role":[{"role":"author","vocabulary":"crossref"}]}],"member":"311","published-online":{"date-parts":[[2019,7,29]]},"reference":[{"key":"e_1_2_6_1_2_1","doi-asserted-by":"publisher","DOI":"10.1016\/S0140-6736(16)31679-8"},{"key":"e_1_2_6_1_3_1","doi-asserted-by":"publisher","DOI":"10.1016\/j.bmcl.2012.09.028"},{"key":"e_1_2_6_1_4_1","doi-asserted-by":"publisher","DOI":"10.1021\/jm300514y"},{"key":"e_1_2_6_1_5_1","doi-asserted-by":"publisher","DOI":"10.1021\/jm800582j"},{"key":"e_1_2_6_1_6_1","doi-asserted-by":"publisher","DOI":"10.1038\/onc.2016.469"},{"key":"e_1_2_6_1_7_1","doi-asserted-by":"publisher","DOI":"10.1016\/j.ejmech.2018.03.046"},{"key":"e_1_2_6_1_8_1","doi-asserted-by":"publisher","DOI":"10.3797\/scipharm.1404-08"},{"issue":"52","key":"e_1_2_6_1_9_1","doi-asserted-by":"crossref","first-page":"87232","DOI":"10.18632\/oncotarget.13601","volume":"7","author":"Wang W.","year":"2016","journal-title":"Oncotarget"},{"key":"e_1_2_6_1_10_1","doi-asserted-by":"publisher","DOI":"10.2174\/1381612823666170214105651"},{"key":"e_1_2_6_1_11_1","doi-asserted-by":"publisher","DOI":"10.1378\/chest.09-2363"},{"key":"e_1_2_6_1_12_1","doi-asserted-by":"publisher","DOI":"10.1016\/j.bmcl.2009.01.045"},{"key":"e_1_2_6_1_13_1","doi-asserted-by":"publisher","DOI":"10.1021\/jm00346a017"},{"key":"e_1_2_6_1_14_1","doi-asserted-by":"publisher","DOI":"10.1002\/cjoc.200990161"},{"key":"e_1_2_6_1_15_1","doi-asserted-by":"publisher","DOI":"10.3390\/molecules16098083"},{"key":"e_1_2_6_1_16_1","doi-asserted-by":"crossref","first-page":"109","DOI":"10.21608\/bfsa.2008.64214","author":"El Koussi N. 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