4662-03-7Relevant academic research and scientific papers
HETEROAROMATIC INHIBITORS OF ASTACIN PROTEINASES
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Paragraph 0117; 0119, (2020/12/22)
The present invention relates to novel hydroxamic acid derivatives useful as inhibitors of astacin metalloproteinases, in particular procollagen C-proteinase (PCP) enzymes, meprins, ovastacin and/or nematode astacins; more particularly human or mammalian
N-Heterocyclic-Carbene-Catalyzed Umpolung of Imines
Patra, Atanu,Mukherjee, Subrata,Das, Tamal Kanti,Jain, Shailja,Gonnade, Rajesh G.,Biju, Akkattu T.
supporting information, p. 2730 - 2734 (2017/02/26)
N-Heterocyclic carbene (NHC) catalysis has been widely used for the umpolung of aldehydes, and recently for the umpolung of Michael acceptors. Described herein is the umpolung of aldimines catalyzed by NHCs, and the reaction likely proceeds via aza-Breslo
Access to 2-Arylindoles via Decarboxylative C?C Coupling in Aqueous Medium and to Heteroaryl Carboxylates under Base-Free Conditions using Diaryliodonium Salts
Arun, Velladurai,Pilania, Meenakshi,Kumar, Dalip
supporting information, p. 3345 - 3349 (2016/12/14)
Easily accessible heteroaromatic carboxylic acids and diaryliodonium salts were successfully employed to construct valuable 2-arylindoles and heteroaryl carboxylates in a regioselective fashion. C2-arylated indoles were produced using a Pd-catalyzed decarboxylative strategy in water without any base, oxidant, or ligand. Heteroaryl carboxylates were prepared under metal and base-free conditions. This protocol was successfully utilized to synthesize Paullone, a cyclin-dependent kinase (CDK) inhibitor.
PLANT GROWTH REGULATOR COMPRISING COMPOUND HAVING BULKY SUBSTITUENT
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Paragraph 0157; 0160; 0162; 0163, (2018/10/24)
PROBLEM TO BE SOLVED: To provide a plant growth regulator having a more reduced risk of withering plants and to provide a simple plant growth regulating method. SOLUTION: Provided is a plant growth regulator that comprises, as an active ingredient, a compound or agriculturally acceptable salt, hydrate or solvate thereof in which a bulky substituent (optionally substituted aryl group) is introduced into at least one (carbon atom to which carboxy alkyl group is not bonded) of sp2 hybridized carbon atoms which the indole ring in an indole compound having carboxy alkyl group or the naphthalene ring in a naphthalene compound having carboxy alkyl group possesses. COPYRIGHT: (C)2015,JPOandINPIT
Synthesis of C-2 arylated tryptophan amino acids and related compounds through palladium-catalyzed C-H Activation
Preciado, Sara,Mendive-Tapia, Lorena,Albericio, Fernando,Lavilla, Rodolfo
, p. 8129 - 8135 (2013/09/12)
Tryptophan (Trp) and tryptophan derivatives are C2-arylated. A C-H activation process allows the preparation of both protected and unprotected arylated-Trp amino acids, directly from the amino acid precursor and aryl iodides. The obtained compounds are suitable for standard solid-phase peptide synthesis.
Design and synthesis of indomethacin analogues that inhibit P-glycoprotein and/or multidrug resistant protein without Cox inhibitory activity
Arisawa, Mitsuhiro,Kasaya, Yayoi,Obata, Tohru,Sasaki, Takuma,Nakamura, Tomonori,Araki, Takuya,Yamamoto, Koujirou,Sasaki, Akito,Yamano, Akihito,Ito, Mika,Abe, Hiroshi,Ito, Yoshihiro,Shuto, Satoshi
, p. 8152 - 8163 (2012/11/07)
We designed and synthesized conformationally restricted analogues and regioisomers of the nonsteroidal anti-inflammatory drug indomethacin. Evaluation of the inhibitory effects of these compounds on COX, P-glycoprotein, and multidrug resistance indicated that NSAIDS modulation of multidrug-resistant P-glycoprotein and multidrug-resistant protein-1 is not associated with COX-1 and COX-2 inhibitory activities.
Synthesis of N2S2 conjugates of the highly specific mitochondrial diazapam binding inhibitor (DBI) receptor complexes
Li, Guolin,Ma, Bing,Missert, Joseph R.,Grossman, Zachary D.,Pandey, Ravindra K.
, p. 2855 - 2860 (2007/10/03)
A novel approach for the synthesis of N2S2 ligands conjugated with 2- phenylindole analogs known as mitochondrial diazapam binding inhibitor receptor complexes (previously known as peripheral-type benzodiazepine receptor), as possible target specific Tc-99m imaging agents is described.
Chemistry, Binding Affinities, and Behavioral Properties of a New Class of "Antineophobic" Mitochondrial DBI Receptor Complex (mDRC) Ligands
Kozikowski, A. P.,Ma, D.,Brewer, James,Sun, S.,Costa, E.,et al.
, p. 2908 - 2920 (2007/10/02)
The mitochondrial DBI receptor complex (mDRC; previously called the peripheral benzodiazepine receptors) is linked to the production of neurosteroids such as pregnenolone sulfate, dehydroepiandrosterone sulfate, and others.In order to gain further informa
