Formula: C7H8N2O. In 2021 ACTA PHARMACOL SIN B 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 2-Aminobenzamide. Through research, I have a further understanding and discovery of 88-68-6.
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.
Formula: C7H8N2O. About 2-Aminobenzamide, 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.
Reference:
Thiomorpholine – Wikipedia,
,Thiomorpholine | C4H9NS – PubChem