An article Design, synthesis, molecular modeling, and biological evaluation of acrylamide derivatives as potent inhibitors of human dihydroorotate dehydrogenase for the treatment of rheumatoid arthritis WOS:000629336800015 published article about MULTICENTER PHASE-II; BREQUINAR SODIUM; IMMUNOSUPPRESSIVE DRUG; PLASMODIUM-FALCIPARUM; PYRIMIDINE SYNTHESIS; DHODH; VIDOFLUDIMUS; LEFLUNOMIDE; DISCOVERY; BLOCKADE in [Zeng, Fanxun; Yang, Guantian; Zhang, Letian; Xu, Xiaoyong] East China Univ Sci & Technol, Sch Pharm, Shanghai Key Lab Chem Biol, Shanghai 200237, Peoples R China; [Li, Shiliang; Luo, Yating; Qi, Tiantian; Liang, Yingfan; Yang, Tingyuan; Wang, Rui; Zhu, Lili; Li, Honglin] East China Univ Sci & Technol, Sch Pharm, Shanghai Key Lab New Drug Design, State Key Lab Bioreactor Engn, Shanghai 200237, Peoples R China in 2021, Cited 62. The Name is 4-Methoxybenzaldehyde. Through research, I have a further understanding and discovery of 123-11-5. SDS of cas: 123-11-5
Human dihydroorotate dehydrogenase (DHODH) is a viable target for the development of therapeutics to treat cancer and immunological diseases, such as rheumatoid arthritis (RA), psoriasis and multiple sclerosis (MS). Herein, a series of acrylamide-based novel DHODH inhibitors as potential RA treatment agents were designed and synthesized. 2-Acrylamidobenzoic acid analog 11 was identified as the lead compound for structure-activity relationship (SAR) studies. The replacement of the phenyl group with naphthyl moieties improved inhibitory activity significantly to double-digit nanomolar range. Further structure optimization revealed that an acrylamide with small hydrophobic groups (Me, Cl or Br) at the 2-position was preferred. Moreover, adding a fluoro atom at the 5-position of the benzoic acid enhanced the potency. The optimization efforts led to potent compounds 42 and 53.55 with IC50 values of 41, 44, 32, and 42 nmol/L, respectively. The most potent compound 54 also displayed favorable pharmacokinetic (PK) profiles and encouraging in vivo anti-arthritic effects in a dose-dependent manner. (C) 2021 Chinese Pharmaceutical Association and Institute of Materia Medica, Chinese Academy of Medical Sciences. Production and hosting by Elsevier B.V.
SDS of cas: 123-11-5. About 4-Methoxybenzaldehyde, If you have any questions, you can contact Zeng, FX; Li, SL; Yang, GT; Luo, YT; Qi, TT; Liang, YF; Yang, TY; Zhang, LT; Wang, R; Zhu, LL; Li, HL; Xu, XY or concate me.
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Indole alkaloid derivatives as building blocks of natural products from Bacillus thuringiensis and Bacillus velezensis and their antibacterial and antifungal activity study,
,Preparation of Indole Containing Building Blocks for the Regiospecific Construction of Indole Appended Pyrazoles and Pyrroles