Synthesis and Biological Evaluation of Derivatives of 2-{2-Fluoro-4-[(2-oxocyclopentyl)methyl]phenyl}propanoic Acid: Nonsteroidal Anti-Inflammatory Drugs with Low Gastric Ulcerogenic Activity

We previously reported that 2-fluoroloxoprofen has lower gastric ulcerogenic activity than loxoprofen, a nonsteroidal anti-inflammatory drug (NSAID) without selectivity for COX-2. We synthesized derivatives of 2-fluoroloxoprofen and studied their properties. Compared to 2-fluoroloxoprofen, one derivative, <b>11a</b>, exhibited higher anti-inflammatory activity and an equivalent ulcerogenic effect. These results suggest that <b>11a</b> could be therapeutically beneficial for use as an NSAID

Additional file 1: of Blockade of TGF-β/Smad signaling by the small compound HPH-15 ameliorates experimental skin fibrosis

Figure S1. The molecular structure of HPH-15. (PDF 7 kb

Additional file 4: of Blockade of TGF-β/Smad signaling by the small compound HPH-15 ameliorates experimental skin fibrosis

Figure S4. The inverse proportional change of Ly6Chi macrophages and CD206+ M2 macrophages from the inflammation stage (day 7) to the fibrotic stage (day 21). The single-cell suspension obtained from the back skin of bleomycin-injected C57BL/6 mice on day 7 and day 21 was stained with the mAbs against CD45, CD11b, Ly6C, and CD206. Stained samples were analyzed using the FACSCanto II system. Data were analyzed using FlowJo software version 7. All values represent mean ± SEM. n = 3 at each time point. ** p ≤ 0.01. (PDF 49 kb

Additional file 2: of Blockade of TGF-β/Smad signaling by the small compound HPH-15 ameliorates experimental skin fibrosis

Figure S2. HPH-15 treatment did not affect the growing of the mice. The body weight changes of mice treated with vehicle or HPH-15 were assessed every 3 days. All values represent mean Âą SEM; n = 5 in each group. (PDF 6 kb

Additional file 3: of Blockade of TGF-β/Smad signaling by the small compound HPH-15 ameliorates experimental skin fibrosis

Figure S3. Every-other-day injection of bleomycin for 2 weeks induced significant skin fibrosis. Back skin of NaCl- or bleomycin-injected mice was harvested on day 14 and stained with H&E. Scale bar = 100 Îźm. n = 3 in each group. (PDF 80 kb