{"status":"ok","message-type":"work","message-version":"1.0.0","message":{"indexed":{"date-parts":[[2026,5,11]],"date-time":"2026-05-11T23:35:40Z","timestamp":1778542540148,"version":"3.51.4"},"reference-count":30,"publisher":"MDPI AG","issue":"3","license":[{"start":{"date-parts":[[2022,3,21]],"date-time":"2022-03-21T00:00:00Z","timestamp":1647820800000},"content-version":"vor","delay-in-days":0,"URL":"https:\/\/creativecommons.org\/licenses\/by\/4.0\/"}],"funder":[{"DOI":"10.13039\/501100003725","name":"National Research Foundation of Korea","doi-asserted-by":"publisher","award":["2021R1I1A3A0403710411"],"award-info":[{"award-number":["2021R1I1A3A0403710411"]}],"id":[{"id":"10.13039\/501100003725","id-type":"DOI","asserted-by":"publisher"}]}],"content-domain":{"domain":[],"crossmark-restriction":false},"short-container-title":["Pharmaceutics"],"abstract":"<jats:p>Dapsone (DpS) is an antimicrobial and antiprotozoal agent, especially used to treat leprosy. The drug shares a similar mode of action with sulfonamides. Additionally, it possesses anti-inflammatory activity, useful for treating autoimmune diseases. Here, we developed a \u201cme-better\u201d alternative to sulfasalazine (SSZ), a colon-specific prodrug of mesalazine (5-ASA) used as an anti-inflammatory bowel diseases drug; DpS azo-linked with two molecules of 5-ASA (AS-DpS-AS) was designed and synthesized, and its colon specificity and anti-colitic activity were evaluated. AS-DpS-AS was converted to DpS and the two molecules of 5-ASA (up to approximately 87% conversion) within 24 h after incubation in the cecal contents. Compared to SSZ, AS-DpS-AS showed greater efficiency in colonic drug delivery following oral gavage. Simultaneously, AS-DpS-AS substantially limited the systemic absorption of DpS. In a dinitrobenzene sulfonic acid-induced rat colitis model, oral AS-DpS-AS elicited better efficacy against rat colitis than oral SSZ. Moreover, intracolonic treatment with DpS and\/or 5-ASA clearly showed that combined treatment with DpS and 5-ASA was more effective against rat colitis than the single treatment with either DpS or 5-ASA. These results suggest that AS-DpS-AS may be a \u201cme-better\u201d drug of SSZ with higher therapeutic efficacy, owing to the combined anti-colitic effects of 5-ASA and DpS.<\/jats:p>","DOI":"10.3390\/pharmaceutics14030684","type":"journal-article","created":{"date-parts":[[2022,3,21]],"date-time":"2022-03-21T21:48:42Z","timestamp":1647899322000},"page":"684","update-policy":"https:\/\/doi.org\/10.3390\/mdpi_crossmark_policy","source":"Crossref","is-referenced-by-count":4,"title":["Dapsone Azo-Linked with Two Mesalazine Moieties Is a \u201cMe-Better\u201d Alternative to Sulfasalazine"],"prefix":"10.3390","volume":"14","author":[{"given":"Changyu","family":"Kang","sequence":"first","affiliation":[{"name":"College of Pharmacy, Pusan National University, Busan 46241, Korea"}],"role":[{"role":"author","vocabulary":"crossref"}]},{"given":"Jaejeong","family":"Kim","sequence":"additional","affiliation":[{"name":"College of Pharmacy, Pusan National University, Busan 46241, Korea"}],"role":[{"role":"author","vocabulary":"crossref"}]},{"given":"Sanghyun","family":"Ju","sequence":"additional","affiliation":[{"name":"College of Pharmacy, Pusan National University, Busan 46241, Korea"}],"role":[{"role":"author","vocabulary":"crossref"}]},{"given":"Sohee","family":"Park","sequence":"additional","affiliation":[{"name":"College of Pharmacy, Pusan National University, Busan 46241, Korea"}],"role":[{"role":"author","vocabulary":"crossref"}]},{"ORCID":"https:\/\/orcid.org\/0000-0001-5216-5518","authenticated-orcid":false,"given":"Jin-Wook","family":"Yoo","sequence":"additional","affiliation":[{"name":"College of Pharmacy, Pusan National University, Busan 46241, Korea"}],"role":[{"role":"author","vocabulary":"crossref"}]},{"ORCID":"https:\/\/orcid.org\/0000-0002-0997-5723","authenticated-orcid":false,"given":"In-Soo","family":"Yoon","sequence":"additional","affiliation":[{"name":"College of Pharmacy, Pusan National University, Busan 46241, Korea"}],"role":[{"role":"author","vocabulary":"crossref"}]},{"given":"Min-Soo","family":"Kim","sequence":"additional","affiliation":[{"name":"College of Pharmacy, Pusan National University, Busan 46241, Korea"}],"role":[{"role":"author","vocabulary":"crossref"}]},{"given":"Yunjin","family":"Jung","sequence":"additional","affiliation":[{"name":"College of Pharmacy, Pusan National University, Busan 46241, Korea"}],"role":[{"role":"author","vocabulary":"crossref"}]}],"member":"1968","published-online":{"date-parts":[[2022,3,21]]},"reference":[{"key":"ref_1","doi-asserted-by":"crossref","first-page":"1082","DOI":"10.2174\/13816128113199990416","article-title":"Inflammatory bowel disease: Etiology, pathogenesis and current therapy","volume":"20","author":"Ko","year":"2014","journal-title":"Curr. 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