1283706-81-9Relevant academic research and scientific papers
Synthesis and biological evaluation of indole core-based derivatives with potent antibacterial activity against resistant bacterial pathogens
Hong, Wei,Li, Jingyang,Chang, Zhe,Tan, Xiaoli,Yang, Hao,Ouyang, Yifan,Yang, Yanhui,Kaur, Sargit,Paterson, Ian C,Ngeow, Yun Fong,Wang, Hao
, p. 832 - 844 (2017/07/04)
The emergence of drug resistance in bacterial pathogens is a growing clinical problem that poses difficult challenges in patient management. To exacerbate this problem, there is currently a serious lack of antibacterial agents that are designed to target extremely drug-resistant bacterial strains. Here we describe the design, synthesis and antibacterial testing of a series of 40 novel indole core derivatives, which are predicated by molecular modeling to be potential glycosyltransferase inhibitors. Twenty of these derivatives were found to show in vitro inhibition of Gram-positive bacteria, including methicillin-resistant Staphylococcus aureus. Four of these strains showed additional activity against Gram-negative bacteria, including extended-spectrum beta-lactamase producing Enterobacteriaceae, imipenem-resistant Klebsiella pneumoniae and multidrug-resistant Acinetobacter baumanii, and against Mycobacterium tuberculosis H37Ra. These four compounds are candidates for developing into broad-spectrum anti-infective agents.
Indole compounds and preparation method and application thereof as drug-resistant bacteria resistant drugs
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Paragraph 0179; 0180; 0183, (2016/10/09)
The invention discloses indole compounds represented by the general formula defined in the specification and salts and preparation method thereof, corresponding medical uses of the compounds and the salts thereof, and drugs and disinfectants containing the compounds and the salts thereof. A lot of experiments prove that the compounds and the salts thereof have good bacteriostatic and bactericidal activity on MRSA (drug-resistant staphylococcus aureus), MDR K.pneumonia (drug-resistant klebsiella pneumonia), and MDR A.baumanii (drug-resistant acinetobacter baumannii). In the formula, X is methylene, carbonyl or sulfonyl; R1 is fluorine, chlorine, bromine, methoxy acyl, nitro or hydrogen; R2 is methoxyl acyl, (p-methoxyl acyl)phenyl, (p-trifluoro oxy)phenyl, (p-trifluoro)phenyl, (m-methoxy acyl)phenyl, (m-trifluoro oxy)phenyl, (p-fluoro m-chloro)phenyl or hydrogen; and HA is inorganic acid or a part of organic acid with strong acidity, preferably hydrochloric acid or hydrobromic acid.
Synthesis and anti-proliferative activity of aromatic substituted 5-((1-benzyl-1H-indol-3-yl)methylene)-1,3-dimethylpyrimidine-2,4,6(1H,3H,5H) -trione analogs against human tumor cell lines
Madadi, Nikhil Reddy,Penthala, Narsimha Reddy,Janganati, Venumadhav,Crooks, Peter A.
, p. 601 - 603 (2014/01/23)
Based on previous SAR studies on N-benzylindole and barbituric acid hybrid molecules, we have synthesized a series of aromatic substituted 5-((1-benzyl-1H-indol-3-yl)methylene)-1,3-dimethylpyrimidine-2,4,6(1H,3H,5H) -trione analogs (3a-i) and evaluated th
Synthesis and in vitro screening of novel N-benzyl aplysinopsin analogs as potential anticancer agents
Penthala, Narsimha Reddy,Yerramreddy, Thirupathi Reddy,Crooks, Peter A.
scheme or table, p. 1411 - 1413 (2011/04/23)
A series of novel substituted (Z)-5-((1-benzyl-1H-indol-3-yl)methylene) imidazolidin-2,4-diones (3a-f) and (Z)-5-((1-benzyl-1H-indol-3-yl)methylene)-2- iminothiazolidin-4-ones (3g-o) have been synthesized utilizing microwave irradiation. These analogs wer
