220844-73-5Relevant academic research and scientific papers
Amide compound and derivative thereof, preparation method, pharmaceutical composition and application thereof
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Paragraph 0417; 0418; 0421; 0422, (2021/07/09)
The invention discloses an amide compound and derivative thereof, a preparation method, a pharmaceutical composition and application thereof. The structure of the amide compound is shown as a formula (I). The derivatives of theamide compound relate to a stereoisomer, a tautomer, a metabolite, a metabolic precursor, a prodrug, a solvate, a salt of the solvate, a crystal, a pharmaceutically acceptable salt or a mixture of the above of theamide compound. The amide compound and the derivative thereof have an efficient inhibition effect on indoleamine 2, 3-dioxygenase 1, and can be used for preparing medicines for treating indoleamine 2, 3-dioxygenase 1 mediated immunosuppression related diseases, the prepared medicine can exert the medicine effect at the molecular level and is wide in application, and the synthesis method of the compound is simple, convenient and easy to operate.
Synthesis and biological evaluation of novel 4-(6-substituted quinolin-4-yl)-N-aryl thiazol-2-amine derivatives as potential antimicrobial agents
Thakare, Prashant,Shinde, Abhijit,Dakhane, Sagar,Chavan, Abhijit,Bobade, Vivek D.,Mhaske, Pravin C.
, p. 1867 - 1877 (2021/06/21)
Cyclocondensation reaction of 4-(2-bromoacetyl)quinolin-1-ium bromide (4a–d) with substituted arylthiourea, (5a–g) afforded 4-(6-substituted quinolin-4-yl)-N-aryl/pyridyl thiazol-2-amine (6a-ab). These newly synthesized derivatives were evaluated for in vitro antibacterial activity against Escherichia coli (NCIM 2574), Proteus mirabilis (NCIM 2388) (Gram-negative strains), Bacillus subtilis (NCIM 2063), Staphylococcus albus (NCIM 2178) (Gram-positive strains) and in vitro antifungal activity against Aspergillus niger (ATCC 504) and Candida albicans (NCIM 3100). Compounds 6a, 6b, 6d, 6f, 6k, and 6l showed moderate to good antibacterial activity against S. albus. Ten derivatives 6c, 6q, 6r, 6s, 6t, 6v, 6w, 6x, 6y, and 6aa, showed moderate to good activity against A. niger. N-[4-(Quinolin-4-yl)-1,3-thiazol-2-yl]pyridin-2-amine presented comparable activity against A. niger with respect to standard drug Rouconazole.
Quinoline formamide compound as well as preparation method and application thereof
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Paragraph 0130-0132; 0136-0138; 0139-0141; 0145-0147, (2020/11/25)
The invention discloses quinoline formamide compounds as well as a preparation method and application thereof. Specifically, the invention relates to a compound represented by a formula (I) as shown in the specification or a tautomer, a meso-racemate, a r
Amide derivative and preparation method thereof and medical application
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Paragraph 0234; 0235; 0237, (2019/10/01)
The invention relates to an amide derivative and a preparation method thereof and medical application, in particular to a compound in the formula (I) and pharmaceutically acceptable salt thereof or astereisomer, a preparation method of the compound and ap
NOVEL FAP INHIBITORS
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Paragraph 0365; 0366; 0367; 0368, (2014/12/09)
The present invention relates to novel inhibitors having high selectivity and specificity for FAP (fibroblast activation protein). Said inhibitors are useful as a human and/or veterinary medicine, in particular for the treatment and/or prevention of FAP-related disorders such as but not limited to proliferative disorders.
NOVEL FAP INHIBITORS
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Page/Page column 52, (2013/07/31)
The present invention relates to novel inhibitors having high selectivity and specificity for FAP (fibroblast activation protein). Said inhibitors are useful as a human and/or veterinary medicine, in particular for the treatment and/or prevention of FAP-related disorders such as but not limited to proliferative disorders.
Selective inhibitors of fibroblast activation protein (FAP) with a (4-quinolinoyl)-glycyl-2-cyanopyrrolidine scaffold
Jansen, Koen,Heirbaut, Leen,Cheng, Jonathan D.,Joossens, Jurgen,Ryabtsova, Oxana,Cos, Paul,Maes, Louis,Lambeir, Anne-Marie,De Meester, Ingrid,Augustyns, Koen,Van Der Veken, Pieter
supporting information, p. 491 - 496 (2013/07/19)
Fibroblast activation protein (FAP) is a serine protease that is generally accepted to play an important role in tumor growth and other diseases involving tissue remodeling. Currently there are no FAP inhibitors with reported selectivity toward both the closely related dipeptidyl peptidases (DPPs) and prolyl oligopeptidase (PREP). We present the discovery of a new class of FAP inhibitors with a N-(4-quinolinoyl)-Gly-(2-cyanopyrrolidine) scaffold. We have explored the effects of substituting the quinoline ring and varying the position of its sp2 hybridized nitrogen atom. The most promising inhibitors combined low nanomolar FAP inhibition and high selectivity indices (>10 3) with respect to both the DPPs and PREP. Preliminary experiments on a representative inhibitor demonstrate that plasma stability, kinetic solubility, and log D of this class of compounds can be expected to be satisfactory.
Facile and efficient synthesis of quinoline-4-carboxylic acids under microwave irradiation
Zhu, Hui,Yang, Ri Fang,Yun, Liu Hong,Li, Jin
experimental part, p. 35 - 38 (2010/11/04)
A facile and efficient method for the preparation of 2-non-substituted quinoline-4-carboxylic acids is described via the Pfitzinger reaction of isatins with sodium pyruvate following consequent decarboxylation under microwave irradiation.
