152434-86-1Relevant articles and documents
Discovery of 1,3,4-oxadiazol-2-one-containing benzamide derivatives targeting FtsZ as highly potent agents of killing a variety of MDR bacteria strains
Bi, Fangchao,Song, Di,Qin, Yinhui,Liu, Xingbang,Teng, Yuetai,Zhang, Na,Zhang, Panpan,Zhang, Nan,Ma, Shutao
, p. 3179 - 3193 (2019/06/17)
The spread of infections caused by multidrug-resistant (MDR) pathogens, such as methicillin-resistant Staphylococcus aureus (MRSA) and vancomycin-resistant S. aureus (VRSA), has created a need for new antibiotics with novel mechanisms of action. The bacterial division protein FtsZ has been identified as a novel drug target that can be exploited clinically. As part of an ongoing effort to develop FtsZ-targeting antibacterial agents, we describe herein the design, synthesis and bioactivity of six series of novel 1,3,4-oxadiazol-2-one-containing, 1,2,4-triazol-3-one-containing and pyrazolin-5-one-containing benzamide derivatives. Among them, compound A14 was found to be the most potent antibacterial agent, much better than clinical drugs such as ciprofloxacin, linezolid and erythromycin against all the tested gram-positive strains, particularly methicillin-resistant, penicillin-resistant and clinical isolated S. aureus. Subsequent studies on biological activities and docking analyses proved that A14 functioned as an effective compound targeting FtsZ. Preliminary SAR indicated a general direction for further optimization of these novel analogues. Taken together, this research provides a promising chemotype for developing newer FtsZ-targeting bactericidal agents.
Isoxazoline benzamide compounds as well as preparation method and application thereof
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Paragraph 0068-0070, (2019/09/17)
The invention provides isoxazoline benzamide compounds as well as a preparation method and application thereof. The isoxazoline benzamide compounds have a structure shown by a formula (I) in the specification, wherein R1 is selected from a phenyl group, a substituted phenyl group and a heteroaryl group; R2, R3, R4 and R5 are each independently selected from hydrogen, alkyl and heteroalkyl groups;or, an isomer or solvate or pharmaceutically acceptable salt of the compounds is shown by the formula (I) in the specification. The compounds provided by the invention have good bacteriostatic and/orbactericidal activity, can prevent and cure bacterial infections and have good FtsZ inhibitory activity.
SYNTHETIC PROCESSES AND SYNTHETIC INTERMEDIATES
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Page/Page column 11-12, (2018/10/25)
The invention provides synthetic intermediates and synthetic processes that are useful for preparing the antibacterial agent TXA709:
Substitution of terminal amide with 1H-1,2,3-triazole: Identification of unexpected class of potent antibacterial agents
Bi, Fangchao,Ji, Shengli,Venter, Henrietta,Liu, Jingru,Semple, Susan J.,Ma, Shutao
supporting information, p. 884 - 891 (2018/02/15)
3-Methoxybenzamide (3-MBA) derivatives have been identified as novel class of potent antibacterial agents targeting the bacterial cell division protein FtsZ. As one of isosteres for the amide group, 1,2,3-triazole can mimic the topological and electronic features of the amide, which has gained increasing attention in drug discovery. Based on these considerations, we prepared a series of 1H-1,2,3-triazole-containing 3-MBA analogues via isosteric replacement of the terminal amide with triazole, which had increased antibacterial activity. This study demonstrated the possibility of developing the 1H-1,2,3-triazole group as a terminal amide-mimetic element which was capable of both keeping and modulating amide-related bioactivity. Surprisingly, a different action mode of these new 1H-1,2,3-triazole-containing analogues was observed, which could open new opportunities for the development of antibacterial agents.
SYNTHETIC PROCESSES AND INTERMEDIATES
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Page/Page column 13, (2017/09/21)
The invention provides synthetic processes and synthetic intermediates that can be used to prepare a compound of formula (I): or a salt thereof.
Macrocyclic compounds and methods for their production
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Page/Page column 44, (2015/11/10)
There is provided inter alia compounds of formula (I): for use in treatment of viral infection or as an immunosuppressant.
Sanglifehrin Derivatives and Methods for Their Production
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Paragraph 0171; 0172, (2014/04/03)
There are provided inter alia compounds of formula (I) and (II) and their use in therapy, particularly for the treatment of viral infection.
Novel Dosage Form
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Paragraph 0276; 0277, (2014/09/03)
There is provided inter alia a pharmaceutical dosage form for oral administration comprising a sanglifehrin as active ingredient in which the sanglifehrin active ingredient is protected from acid degradation in the stomach environment following oral admin
NOVEL DOSAGE FORM
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Page/Page column 66, (2013/05/21)
There is provided inter alia apharmaceutical dosage form fororal administration comprising a sanglifehrin as active ingredient in which the sanglifehrin active ingredient is protected from acid degradation in the stomach environment following oral adminis
PYRROLO[2,3-B] PYRIDINE DERIVATIVES AS PROTEIN KINASE INHIBITORS
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Page/Page column 142, (2010/11/25)
Compounds of formula III which are active on protein kinases are described, as well as methods of using such compounds to treat diseases and conditions associated with aberrant activity of protein kinases.
