40546-45-0Relevant academic research and scientific papers
DNA-Encoded Libraries: Hydrazide as a Pluripotent Precursor for On-DNA Synthesis of Various Azole Derivatives
Ma, Fei,Li, Jie,Zhang, Shuning,Gu, Yuang,Tan, Tingting,Chen, Wanting,Wang, Shuyue,Ma, Peixiang,Xu, Hongtao,Yang, Guang,Lerner, Richard A.
supporting information, p. 8214 - 8220 (2021/05/03)
DNA-encoded combinatorial chemical library (DEL) technology, an approach that combines the power of genetics and chemistry, has emerged as an invaluable tool in drug discovery. Skeletal diversity plays a fundamental importance in DEL applications, and relies heavily on novel DNA-compatible chemical reactions. We report herein a phylogenic chemical transformation strategy using DNA-conjugated benzoyl hydrazine as a common versatile precursor in azole chemical expansion of DELs. DNA-compatible reactions deriving from the common benzoyl hydrazine precursor showed excellent functional group tolerance with exceptional efficiency in the synthesis of various azoles, including oxadiazoles, thiadiazoles, and triazoles, under mild reaction conditions. The phylogenic chemical transformation strategy provides DELs a facile way to expand into various unique chemical spaces with privileged scaffolds and pharmacophores.
Colchicine derivatives, and preparation method and medical application thereof
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Paragraph 0092; 0093; 0100; 0102; 0103, (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.
PREPARATION OF CERTAIN (SUBSTITUTED PHENYL)-TRIAZOLYL-(SUBSTITUTED PHENYL) MOLECULES, AND INTERMEDIATES AND INSECTICIDES RELATED THERETO
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Paragraph 0026; 0027, (2014/09/30)
This disclosure is related to the field of preparation of certain (substituted phenyl)-triazolyl-(substituted phenyl) molecules, and intermediates related thereto, where said intermediates are useful in the preparation of certain insecticides.
PREPARATION OF HALOALKOXYARYLHYDRAZINES AND INTERMEDIATES THEREFROM
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Paragraph 0046; 0047, (2014/09/30)
This document is related to the field of preparation of haloalkoxyarylhydrazines and certain intermediates derived therefrom, where said intermediates are useful in the preparation of certain pesticides disclosed in U.S. Pat. No. 8,178,658.
PREPARATION OF HALOALKOXYARYLHYDRAZINES AND INTERMEDIATES THEREFROM
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Paragraph 0031; 0032, (2014/09/30)
The invention in this document is related to the field of preparation of haloalkoxyarylhydrazines and certain intermediates derived therefrom, where said intermediates are useful in the preparation of certain pesticides disclosed in U.S. Pat. No. 8,178,65
PREPARATION OF CERTAIN (SUBSTITUTED-PHENYL)-TRIAZOLYL-(SUBSTITUTED PHENYL) MOLECULES, AND INTERMEDIATES AND INSECTICIDES RELATED THERETO
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Paragraph 0049; 0050, (2014/09/30)
This document is related to the preparation of certain (substituted-phenyl)-triazolyl-(substituted phenyl) molecules, and intermediates related thereto, where said intermediates are useful in preparing certain insecticides.
Synthesis and structure of aroylamidines and N-arylbenzamidines hydrochlorides
Kuvaeva,Fedorova,Zaitsev,Yakovlev,Zakharov,Semakova
experimental part, p. 209 - 213 (2012/06/01)
Aroylamidines can be obtained as salts in a reaction of the corresponding arylcarbonitriles with anhydrous ethanol in the presence of dry HCl followed by treating intermediate imidoesters with alcoholic solution of ammonia. N-Arylbenzamidines are obtained by reacting benzonitrile with arylamines in the presence of AlCl3. The structure of arylamines and the reaction conditions signifi cantly affect the yield of the target product, and sometimes the very possibility of its preparation. Pleiades Publishing, Ltd., 2012.
Reverse-benzamidine antimalarial agents: Design, synthesis, and biological evaluation
Berger, Olivier,Wein, Sharon,Duckert, Jean-Frederic,Maynadier, Marjorie,Fangour, Siham El,Escale, Roger,Durand, Thierry,Vial, Henri,Vo-Hoang, Yen
scheme or table, p. 5815 - 5817 (2010/11/17)
In the frame of the development of bis-cationic choline analogs, the RSA of bis-N-alkylamidines were studied and a new series of reverse-benzamidine derivatives was designed. Contrary to the lipophilicity, the basicity of alkylamidine compounds directly influences their antimalarial potencies.
HETEROCYCLIC AMIDE COMPOUNDS AND PHARMACEUTICAL USE OF THE SAME
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, (2008/06/13)
Heterocyclic amide compounds of the formula (I) STR1 wherein each symbol is as defined in the specification, pharmacologically acceptable salts thereof, pharmaceutical compositions thereof and pharmaceutical use thereof. The heterocyclic amide compounds and pharmacologically acceptable salts thereof of the present invention have superior inhibitory activity against chymase groups in mammals inclusive of human, and can be administered orally or parenterally. Therefore, they are useful as chymase inhibitors and can be effective for the prophylaxis and treatment of various diseases caused by chymase, such as those caused by angiotensin II.
DNA Binding Compounds. VI. Synthesis and Characterization of 2,5'-Disubstituted Bibenzimidazoles Related to the DNA Minor Groove Hoechst 33258
Kelly, David P.,Bateman, Stuart A.,Hook, Robert J.,Martin, Roger F.,Reum, Monica E.,et al.
, p. 1751 - 1770 (2007/10/02)
A series of compounds have been synthesized in which the basic 2-phenylbibenzimidazole structure of Hoechst 33258 has been modified to include various combinations of bromo, iodo, methoxy, amino, alkylamino and nitro groups in the terminal phenyl ring.Both sequential and convergent synthetic routs have been followed using coupling reactions of both imino ethers and aldehydes to 1,2-diamines.All these compounds were characterized by a combination of f.a.b. mass spectrometry and 1H and 13C n.m.r. spectroscopy including inverse detection of long-range heteronuclear CH correlations (HMBC).
