180160-91-2Relevant academic research and scientific papers
Nitroimidazole compound as well as preparation method and application thereof
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Paragraph 0140-0142; 0150-0151, (2021/02/10)
The invention discloses a novel nitroimidazole compound as well as a preparation method and application thereof. The nitroimidazole compound has a general formula (I) shown in the specification.
Cobalt-Catalyzed Electrophilic Amination of Aryl- and Heteroarylzinc Pivalates with N-Hydroxylamine Benzoates
Chen, Yi-Hung,Gra?l, Simon,Knochel, Paul
supporting information, p. 1108 - 1111 (2018/01/01)
Aryl- and heteroarylzinc pivalates can be aminated with O-benzoylhydroxylamines at 25 °C within 2–4 h in the presence of 2.5–5.0 % CoCl2?2 LiCl to furnish the corresponding tertiary arylated or heteroarylated amines in good yields. This electrophilic amination also provides access to diarylamines and aryl(heteroaryl)amines. A new tuberculosis drug candidate (Q203) was prepared in six steps and 56 % overall yield by using this cobalt-catalyzed amination as the key step.
Alcohols as Latent Coupling Fragments for Metallaphotoredox Catalysis: Sp3-sp2 Cross-Coupling of Oxalates with Aryl Halides
Zhang, Xiaheng,MacMillan, David W.C.
supporting information, p. 13862 - 13865 (2016/11/06)
Alkyl oxalates, prepared from their corresponding alcohols, are engaged for the first time as carbon radical fragments in metallaphotoredox catalysis. In this report, we demonstrate that alcohols, native organic functional groups, can be readily activated with simple oxalyl chloride to become radical precursors in a net redox-neutral Csp3-Csp2 cross-coupling with a broad range of aryl halides. This alcohol-activation coupling is successfully applied to the functionalization of a naturally occurring steroid and the expedient synthesis of a medicinally relevant drug lead.
Pyrazolo[1, 5-a]pyridine compound and use thereof
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Paragraph 0084; 0092; 0093; 0094; 0095, (2016/10/08)
The invention discloses a pyrazolo[1, 5-a]pyridine compound with the structure characteristic shown in the formula (I) or its pharmaceutically acceptable salt, stereoisomer or prodrug molecule and a use thereof. The compound has good in-vitro anti-tubercle bacillus activity, has the minimal inhibitory concentration (MIC) less than 0.1 micrograms per milliliter and partial MIC of 0.01 micrograms per milliliter and has strong inhibition effects on a clinically sorted multi-drug-resistant tuberculosis (MDR-TB) strain. In an in-vivo experiment, at a dosage of 20mg/kg/d, the pyrazolo[1, 5-a]pyridine compound can effectively eliminate H37Ra infection in a mouse and is a novel anti-tuberculosis compound.
Design, Synthesis, and Biological Evaluation of Pyrazolo[1,5-a]pyridine-3-carboxamides as Novel Antitubercular Agents
Tang, Jian,Wang, Bangxing,Wu, Tian,Wan, Junting,Tu, Zhengchao,Njire, Moses,Wan, Baojie,Franzblauc, Scott G.,Zhang, Tianyu,Lu, Xiaoyun,Ding, Ke
supporting information, p. 814 - 818 (2015/07/15)
A series of pyrazolo[1,5-a]pyridine-3-carboxamide derivatives were designed and synthesized as new anti-Mycobacterium tuberculosis (Mtb) agents. The compounds exhibit promising in vitro potency with nanomolar MIC values against the drug susceptive H37Rv s
ANTI-INFECTIVE COMPOUNDS
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Page/Page column 39; 40, (2015/02/25)
The present invention relates to small molecule compounds and their use in the treatment of bacterial infections, in particular Tuberculosis.
4 ( 1H) -PYRIDINONE DERIVATIVES AND THEIR USE AS ANTIMALARIA AGENTS
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Page/Page column 38, (2010/08/08)
4-pyridone (4-pyridinone) derivatives of Formula (I) and pharmaceutically acceptable derivatives thereof, processes for their preparation, pharmaceutical formulations thereof and their use in chemotherapy of certain parasitic infections such as malaria, are provided.
SULFONAMIDE DERIVATIVES FOR THERAPEUTIC USE AS FATTY ACID SYNTHASE INHIBITORS
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Page/Page column 177, (2008/12/06)
A compound of formula (I) or a pharmaceutically acceptable salt thereof, processes for preparing such compounds, their use as Fatty Acid Synthase inhibitors, methods for their therapeutic use, particularly in the treatment of obesity and diabetes mellitus
Tricyclic benzimidazoles and their use as metabotropic glutamate receptor modulators
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Page/Page column 44, (2008/06/13)
The invention provides for a compound of formula (I) or a pharmaceutically acceptable salt thereof: wherein R1, R2, R3, A, B, D, m, n, x, and y are defined as described in the specification. The invention additionally provides a pharmaceutically composition comprising the compound of formula I, together with a method of using the same to treat or prevent neurological and psychiatric disorders. The compounds are useful in therapy related to the treatment or prevention of mGluR2 receptor-mediated disorders.
