4237-48-3Relevant academic research and scientific papers
The unusual influence of hetaryl groups on the direct conversion of some secondary alcohols into thiols with Lawesson’s reagent: elucidation of the reaction mechanism
Mlostoń, Grzegorz,Hamera-Fa?dyga, Ró?a,Celeda, Ma?gorzata,Linden, Anthony,Heimgartner, Heinz
, p. 475 - 487 (2017/09/27)
A series of hetaryl-substituted methanols were used for direct conversion into the corresponding thiols by treatment with Lawesson’s reagent in boiling toluene. Unexpectedly, the respective sulfides were formed exclusively. In the case of chiral alcohols,
6-member aromatic cyclic or heteroaromatic cyclic compound as well as preparation method and application thereof
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Paragraph 0239; 0240; 0243, (2018/01/19)
The invention relates to a 6-member aromatic cyclic or heteroaromatic cyclic compound as well as a preparation method and application thereof. A general formula of the 6-member aromatic cyclic or heteroaromatic cyclic compound is shown as a formula I, whe
Two-step three-component process for one-pot synthesis of 8-alkylmercaptocaffeine derivatives
Rad, M. N. Soltani,Maghsoudi
, p. 70335 - 70342 (2016/08/06)
A highly efficient, odourless and two-step three-component process for one-pot synthesis of some 8-alkylmercaptocaffeine derivatives has been described. The catalyst-free three-component reaction of alkyl bromides, thiourea, and 8-bromocaffeine gave 8-alkylmercaptocaffeine products in excellent to quantitative yields. In addition, the impact of parameters on sample reaction is discussed.
HETEROCYCLIC COMPOUNDS WITH WORKING MEMORY ENHANCING ACTIVITY
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Page/Page column 33; 34, (2016/02/29)
The present invention relates to a chemical compound having the general formula (I): wherein R1 and R2 are, equal or independently, aryl, heteroaryl; wherein RTA is a 2-1,3-, or 4- 1,3- or 5-1,3-thiazole ring and its use in for improving; the short term memory and/or the working memory.
Synthesis and structure of dinitrosyl iron complexes with secondary thiolate bridging ligands [Fe2(μ-SCHR2)2(NO)4], R = Me, Ph
Davidovich,Gurzhiy,Sanina,Shchukarev,Garabadzhiu,Belyaev
, p. 197 - 201 (2015/03/14)
New dinitrosyl iron complexes of binuclear structure [Fe2(μ-SCHMe2)2(NO)4] and [Fe2(μ-SCHPh2)2(NO)4] were first synthesized employing new method from Fe(CO)5, corresponding thiol, and EtONO. Complexes structures were determined by XRD technique. DFT calculations were performed to probe the cis-conformer structures in gas and solution phases. NO donor ability of the complex with isopropyl thiolate ligand was studied.
Simple synthesis of modafinil derivatives and their anti-inflammatory activity
Jung, Jae-Chul,Lee, Yeonju,Son, Jee-Young,Lim, Eunyoung,Jung, Mankil,Oh, Seikwan
, p. 10446 - 10458 (2012/11/07)
Simple synthesis of modafinil derivatives and their biological activity are described. The key synthetic strategies involve substitution and coupling reactions. We determined the anti-inflammatory effects of modafinil derivatives in cultured BV2 cells by measuring the inhibition of nitrite production and expression of iNOS and COX-2 after LPS stimulation. It was found that for sulfide analogues introduction of aliphatic groups on the amide part (compounds 11a-d) resulted in lower anti-inflammatory activity compared with cyclic or aromatic moieties (compounds 11e-k). However, for the sulfoxide analogues, introduction of aliphatic moieties (compounds 12a-d) showed higher anti-inflammatory activity than cyclic or aromatic fragments (compounds 12e-k) in BV-2 microglia cells.
Structure-activity relationships in the binding of chemically derivatized CD4 to gp120 from human immunodeficiency virus
Xie, Hui,Ng, Danny,Savinov, Sergey N.,Dey, Barna,Kwong, Peter D.,Wyatt, Richard,Smith III, Amos B.,Hendrickson, Wayne A.
, p. 4898 - 4908 (2008/03/11)
The first step in HIV infection is the binding of the envelope glycoprotein gp120 to the host cell receptor CD4. An interfacial "Phe43 cavity" in gp120, adjacent to residue Phe43 of gp120-bound CD4, has been suggested as a potential target for therapeutic intervention. We designed a CD4 mutant (D1D2F43C) for site-specific coupling of compounds for screening against the cavity. Altogether, 81 cysteine-reactive compounds were designed, synthesized, and tested. Eight derivatives exceeded the affinity of native D1D2 for gp120. Structure-activity relationships (SAR) for derivatized CD4 binding to gp120 revealed significant plasticity of the Phe43 cavity and a narrow entrance. The primary contacts for compound recognition inside the cavity were found to be van der Waals interactions, whereas hydrophilic interactions were detected in the entrance. This first SAR on ligand binding to an interior cavity of gp120 may provide a starting point for structure-based assembly of small molecules targeting gp120-CD4 interaction.
Development of dual-acting benzofurans for thromboxane A2 receptor antagonist and prostacyclin receptor agonist: Synthesis, structure-activity relationship, and evaluation of benzofuran derivatives
Ohno, Michihiro,Miyamoto, Mitsuko,Hoshi, Kazuhiro,Takeda, Takahiro,Yamada, Naohiro,Ohtake, Atsushi
, p. 5279 - 5294 (2007/10/03)
Prostacyclin (PGI2) is an unstable, powerful endogenous inhibitor of platelet aggregation, and thromboxane A2 (TXA 2) is an unstable endogenous arachidonic acid metabolite that plays a pivotal role in platelet aggregation and vasoconstriction. The balance between TXA2 and PGI2 greatly affects maintenance of the homeostasis of the circulatory system. A novel series of benzofuran-7- yloxyacetic acid derivatives was discovered as potent dual-acting agents to block the thromboxane A2 receptor and to activate the prostacyclin receptor. Synthesis, structure-activity relationship, and in vitro and ex vivo pharmacology of this series of compounds are described. The most potent in the series was {3-[2-(1,1-diphenylethylsulfanyl)ethyl]-2-hydroxymethylbenzofuran-7- yloxy}acetic acid diethanolamine salt (7) with Ki of 4.5 nM for thromboxane receptor antagonism and Ki of 530 nM for prostacyclin receptor agonism. Remarkably, compound 7 is a promising candidate for novel treatment as an antithrombotic agent with other cardiovascular actions to avoid hypotensive side effects.
Adsorption equilibria of novel phthalocyaninatomagnesium(II) derivatives with thioethers at the toluene/water interface
Adachi, Kenta,Watarai, Hitoshi
, p. 2011 - 2020 (2007/10/03)
Three novel phthalocyaninatomagnesium(II) derivatives with eight peripheral thioethers (MgPc(SR)8) such as (2,3,9,10,16,17,23,24-octakis- ethylthiophthalocyaninato)magnesium(II) (MgPc(SEt)8), (2,3,9,10,16,17,23,24-octakisbenzylthioph
PREPARATIONS OF A SULFINYL ACETAMIDE
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Page 12, (2008/06/13)
The present invention provides processes for the preparation of modafinil which includes the step of reacting benzhydrylthiol and chloroacetamide.
