63190-44-3Relevant academic research and scientific papers
Synthesis and molecular docking study of some 5,6-dichloro-2-cyclopropyl-1H-benzimidazole derivatives bearing triazole, oxadiazole, and imine functionalities as potent inhibitors of urease
Mente?e, Emre,Bekta?, Hakan,Sokmen, Bahar Bilgin,Emirik, Mustafa,?ak?r, Demet,Kahveci, Bahittin
, p. 3014 - 3018 (2017)
A new series of benzimidazole compounds including hydrazinecarbothioamide, 1,2,4-triazole, 1,3,4-oxadiazole and imine function were synthesized starting from 5,6-dichloro-2-cyclopropyl-1H-benzimidazole. All of the benzimidazole derivatives exhibited good urease inhibitor activity. Compound 6a proved to be the most potent showing an enzyme inhibitory activity with an IC50?=?0.06?μM. Molecular docking studies were also conducted on enzyme extracted from Jack bean urease to identify the binding mode of the newly synthesized compounds.
NOVEL HETEROARYL-TRIAZOLE COMPOUNDS AS PESTICIDES
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Page/Page column 133, (2021/06/04)
The present invention relates to novel heteroaryl-triazole compounds of the general formula (I), in which the structural elements X, R1, R2, R3, R4 and R5 have the meaning given in the description, to
ASK1 inhibitor, derivative, preparation method, pharmaceutical composition and application thereof
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Paragraph 0170-0175, (2021/02/10)
The invention discloses an ASK1 inhibitor, a derivative, a preparation method, a pharmaceutical composition and application thereof. The structure of the compound is shown as a formula I. The ASK1 inhibitor derivative relates to an isomer, a diastereoisom
NOVEL HETEROARYL-TRIAZOLE COMPOUNDS AS PESTICIDES
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Page/Page column 97, (2021/11/13)
The present invention relates to novel heteroaryl-triazole compounds of the general formula (I), in which the structural elements X, R1, R2, R3 and R4 have the meaning given in the description, to formulations and compositions comprising such compounds and for their use in the control of animal pests including arthropods and insects in plant protection and to their use for control of ectoparasites on animals.
IMIDAZOPIPERAZINONE INHIBITORS OF TRANSCRIPTION ACTIVATING PROTEINS
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Paragraph 0514; 0515, (2019/10/20)
The present disclosure relates to heterocyclic compounds and methods which may be useful as inhibitors of transcription activating proteins such as CBP and P300 for the treatment or prevention of diseases such as proliferative diseases, inflammatory disorders, autoimmune diseases, and fibrotic diseases.
SYNTHESIS OF A COMPOUND THAT MODULATES THE ACTIVITY OF BROMODOMAIN-CONTAINING PROTEINS
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Paragraph 0110, (2018/06/12)
The present disclosure provides processes for the preparation of a compound of formula I: or a salt or co-crystal thereof, that modulates the activity of bromodomain-containing proteins. The disclosure also provides compounds and processes for the preparation of the compounds that are synthetic intermediates to the compound of formula I.
Colchicine derivatives, and preparation method and medical application thereof
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Paragraph 0092; 0093; 0231; 0233; 0234, (2018/09/14)
The invention specifically relates to colchicine derivatives (I) as described in the specification and a preparation method thereof, and pharmaceutical compositions containing the colchicine derivatives, belonging to the field of medicinal chemistry. The results of pharmacodynamic experiments prove that the colchicine derivatives of the invention have treatment effect on lumbar disc herniation andliver fibrosis.
Identification of a novel 5-amino-3-(5-cyclopropylisoxazol-3-yl)-1-isopropyl-1H-pyrazole-4-carboxamide as a specific RET kinase inhibitor
Yoon, Hojong,Shin, Injae,Nam, Yunju,Kim, Nam Doo,Lee, Kyung-Bok,Sim, Taebo
, p. 1145 - 1155 (2016/11/18)
Activating mutations of REarrange during Transfection (RET) kinase frequently occur in human thyroid and lung cancers. An enormous effort has been devoted to discover potent and selective inhibitors of RET. Selective and potent inhibitors against constitutively active RET mutants are rare to date as identification of selective RET inhibitors is challenging. In a recent effort we identified a novel and specific RET inhibitor of 5-aminopyrazole-4-carboxamide scaffold, which was designed to enhance the metabolic stability of the pyrazolopyrimidine scaffold. In the SAR study described in the current report, we identified the 5-aminopyrazole-4-carboxamide analog 15l, which displays high metabolic stability. Compound 15l is potent against gatekeeper mutant (IC50= 252 nM) of RET as well as against wild-type RET (IC50= 44 nM). This substance effectively suppresses growth of Ba/F3 cells transformed with wild-type RET and its gatekeeper mutant (V804M), and thyroid-cancer derived TT cells while it does not affect parental Ba/F3 cells and Nthy ori-3-1, normal thyroid cells. Also, the results of a global kinase profiling assay on a panel of 369 kinases, show that 15l exclusively inhibits RET. Based on its exceptional kinase selectivity, great potency and metabolic stability, 15l represents a promising lead for the discovery of RET directed therapeutic agent and should be a key tool in studies aimed at understanding RET biology.
Synthesis of 3,5-disubstituted 1,2,4-triazoles containing an amino group
Khromova, N. Yu.,Fedorov,Malekin,Kutkin
, p. 1490 - 1495 (2016/11/29)
3,5-Disubstituted 1,2,4-triazoles containing linear and cyclic amine fragments have been synthesized by thermal cyclization of N′-(1-iminoalkyl) hydrazides prepared by condensation of imido esters with carboxylic acid hydrazides. The initial imido esters have been synthesized by the Pinner reaction, as well as by reaction of nitriles with methanol in the presence of a catalytic amount of sodium methoxide. A procedure has been developed for the synthesis of 5-substituted 3-(3-nitrophenyl)-1,2,4-triazoles which have been converted to 3-aminophenyl derivatives by reduction with hydrazine hydrate over Raney nickel.
Pyrrole inhibitors of S-nitrosoglutathione reductase as therapeutic agents
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Page/Page column 292, (2015/11/16)
The present invention is directed to inhibitors of S-nitrosoglutathione reductase (GSNOR), pharmaceutical compositions comprising such GSNOR inhibitors, and methods of making and using the same.
