HPLC of Formula: C6H5NO. In 2020.0 BIOORG CHEM published article about BETA-LACTAMASE INHIBITOR; SMALL MOLECULES; IN-VITRO; NDM-1; ASPERGILLOMARASMINE; DEFERIPRONE; RESISTANCE; UPDATE; NOTA; ACID in [Cui, De-Yun; Yang, Yi; Bai, Meng-Meng; Wang, Cong-Cong; Kong, Hong-Tao; Shen, Bo-Yuan; Yan, Da-Chao; Zhang, En] Zhengshou Univ, Sch Pharmaceut Sci, Inst Drug Discovery & Dev, Minist Educ China,Key Lab Adv Pharmaceut Technol, Zhengzhou 450001, Peoples R China; [Han, Jiang-Xue; Xiao, Chun-Ling; Liu, Yi-Shuang] Chinese Acad Med Sci & Peking Union Med Coll, Inst Med Biotechnol, Beijing 100050, Peoples R China; [Zhang, En] Collaborat Innovat Ctr New Drug Res & Safety Eval, Zhengzhou 450001, Henan, Peoples R China in 2020.0, Cited 52.0. The Name is 3-Pyridinecarboxaldehyde. Through research, I have a further understanding and discovery of 500-22-1.
New Delhi Metallo-beta-lactamase-1 (NDM-1), a Zn (II)-dependent enzyme, can catalyze the hydrolysis of almost all beta-lactam antibiotics including carbapenems, resulting in bacterial antibiotic resistance, which threatens public health globally. Based on our finding that H(2)dedpa is as an efficient NDM-1 inhibitor, a series of H-2 dedpa derivatives was systematically prepared. These compounds exhibited significant activity against NDM-1, with IC50 values 0.06-0.94 mu M. In vitro, compounds 6k and 6n could restore the activity of meropenem against Klebsiella pneumoniae, Escherichia coli and Proteus mirabilis possessing either NDM or IMP. In particular, the activity of meropenem against E. coli producing NDM-4 could be improved up to 5333 times when these two compounds were used. Time-kill cell-based assays showed that 99.9% of P. mirabilis were killed when treated with meropenem in combination with compound 6k or 6n. Furthermore, compounds 6k and 6n were non -hemolytic (HC50 > 1280 mu g/mL) and showed low toxicity toward mammalian (HeLa) cells. Mechanistic studies indicated that compounds 6k and 6n inhibit NDM-1 by chelating the Zn2+ ion of the enzyme.
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Reference:
Pyridine – Wikipedia,
,Pyridine | C5H5N – PubChem