- Conjugates with an antimicrobial effect based on new derivatives of mercaptobenzoxazole esterified onto poly(maleic anhydride-alt-vinyl acetate)
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New compounds with biological activity based on hydroxy-amino derivatives of benzoxazolyl-2-mercaptoformic acid, benzoxazolyl-2-mercaptoacetic acid, and chloracetyl-2-mercaptobenzoxazole have been synthesized. The chemical bonding of these compounds to po
- Aparaschivei, Radita,Sunel, Valeriu,Popa, Marcel,Desbrieres, Jacques
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- Green synthesis of therapeutically active 1,3,4-oxadiazoles as antioxidants, selective COX-2 inhibitors and their in silico studies
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A modest, competent and green synthetic procedure for novel coumarinyl-1,3,4-oxadiazolyl-2-mercaptobenzoxazoles 8i-t has been reported. Analysis of the docked (PDB ID: 5IKR; A-Chain) poses of the compounds illustrated that they adopt identical conformations to the extremely selective COX-2 inhibitor. The biological outcomes as well as computational study suggested that the compounds originated to have elevated resemblance towards COX-2 enzyme than COX-1. The compounds 8i, 8l, 8q, 8r, 8s and 8t emerged as most potent and selective COX-2 inhibitors in contrast with Mefenamic acid. The selectivity index of 8l, 8n and 8r was respectively found to be 33.95, 20.25 and 24.98 which manifested their high selectivity against COX-2. Interestingly, the compounds which were active as COX-2 inhibitors were also active as antioxidant agents.
- Nesaragi, Aravind R.,Kamble, Ravindra R.,Dixit, Shruti,Kodasi, Barnabas,Hoolageri, Swati R.,Bayannavar, Praveen K.,Dasappa, Jagadeesh Prasad,Vootla, Shyamkumar,Joshi, Shrinivas D.,Kumbar, Vijay M.
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supporting information
(2021/06/09)
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- Preparation method of thioether
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The invention relates to a preparation method of thioether, which comprises the following steps: adding mercaptan/phenol and alpha-diazoacetate into an acetonitrile-water mixed solvent, stirring at room temperature under the irradiation of visible light u
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Paragraph 0018; 0039-0040
(2020/11/01)
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- Catalyst-free, visible-light-promoted S-H insertion reaction between thiols and α-diazoesters
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A visible-light-promoted S-H insertion reaction between thiols and α-diazoesters was developed. The reaction proceeded smoothly at room temperature with a broad substrate scope, affording various thioethers in moderate to excellent yields. The catalyst- A
- Chen, Shuwen,Huo, Congde,Liu, Cai,Ma, Ben,Song, Menghui,Wang, Ganggang,Yang, Jingya,Zhou, Hongyan
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supporting information
p. 9494 - 9498
(2020/12/15)
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- Rhodium-Catalyzed Rearrangement of S/Se-Ylides for the Synthesis of Substituted Vinylogous Carbonates
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An efficient rhodium-catalyzed unprecedented oxa-[2,3]-sigmatropic rearrangement of sulfur ylide derived from α-thioesters/ketones and diazo carbonyl compounds has been accomplished for the synthesis of various sulfur-tethered vinylogous carbonates in good to excellent yields. Important features of the developed reaction include wide functional group tolerance, excellent chemo- and regioselectivity, and efficient rearrangement involving the carbonyl motif. The present reaction also equally works well with α-selenoesters for the synthesis of seleno-containing vinylogous carbonates.
- Reddy, Angula Chandra Shekar,Anbarasan, Pazhamalai
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supporting information
p. 9965 - 9969
(2019/12/24)
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- Binding characterization, synthesis and biological evaluation of RXRα antagonists targeting the coactivator binding site
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Previously we identified the first retinoid X receptor-alpha (RXRα) modulators that regulate the RXRα biological function via binding to the coregulator-binding site. Here we report the characterization of the interactions between the hit molecule and RXRα through computational modeling, mutagenesis, SAR and biological evaluation. In addition, we reported studies of additional new compounds and identified a molecule that mediated the NF-κB pathway by inhibiting the TNFα-induced IκBα degradation and p65 nuclear translocation.
- Xu, Dingyu,Guo, Shangjie,Chen, Ziwen,Bao, Yuzhou,Huang, Fengyu,Xu, Dan,Zhang, Xindao,Zeng, Zhiping,Zhou, Hu,Zhang, Xiaokun,Su, Ying
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p. 3846 - 3849
(2016/08/01)
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- Polymer conjugates with potential biological activity based on new derivatives of 2-mercaptobenzoxazole-synthesis and characterization
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New potentially biologically active compounds derived from 2-mercapto-benzoxazole were synthesized and coupled on polymeric support of poly (maleic anhydride-alt-vinyl acetate) for the preparation of polymer-drug conjugates with controlled drug release. All compounds were characterized by elemental and spectroscopy (FT-IR, 1H-NMR) analysis. The toxicological tests recommend the products for further laboratory screening. [Figure not available: see fulltext.]
- Aparaschivei, Rcadita,Sunel, Valeriu,Holban, Mihaela,Popa, Marcel,Desbrieres, Jacques
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p. 1808 - 1815
(2013/09/23)
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- Antimicrobial and analgesic evaluation of newly synthesized benzoxazole incorporated azitidinones
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The cyclocondensation of the Schiff s bases 5(a-j) with chloroacetyl chloride in presence of triethyl amine resulted in the formation of 2-(1,3-benzoxazole-2-yl thio)-N-(3-chloro-2-oxo-4-phenylazetidin-1-yl) acetamide analogs 6(a-j). The structures of the newly synthesized compounds have been established by IR, 1H NMR and mass spectral studies. All the synthesized compounds have been screened for antimicrobial and analgesic activities.
- Hanumanthappa,Vagdevi,Vaidya,Srikrishna,Raghavendra
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p. 121 - 124
(2013/09/23)
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- Synthesis and biological significance of 2-mercaptobenzoxazole derivatives
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Several 2-aryl-3-[(2-mercaptobenzoxazolo)acetamidyl]-4-oxothiazolidines 4, and 2-aryl-3-[(2-mercaptobenzoxazolo)acetamidyl]-5-arylidene-4-oxothiazolidines 5 have been synthesized by the appropriate methods and evaluated for their antibacterial activity ag
- Srivastava, Santosh Kumar,Jain, Ashish,Srivastava, Savitri Devi
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p. 1118 - 1123
(2007/10/03)
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- Organic reactions in ionic liquids: An efficient method for selective S-alkylation of 2-mercaptobenzothia(xa)zole with alkyl halides
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Ionic liquids based on 1-butyl-3-methylimidazolium hexafluorophosphate (BmimPF6) and 1-butyl-3-methylimidazolium tetrafluoroborate (BmimBF4) are used as reusable reaction medium in the selective S-alkylation of 2-mercaptobenzothia(xa)zole with alkyl halides in the presence of potassium carbonate. This procedure is convenient, efficient, and generally gives rise to the S-alkylated product exclusively.
- Hu, Yi,Chen, Zhen-Chu,Le, Zhang-Gao,Zheng, Qin-Guo
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p. 2039 - 2046
(2007/10/03)
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- Electrolytic partial fluorination of organic compounds. Part 29. Anodic mono- and difluorination of 2-benzoxazolyl sulfides
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Anodic fluorination of 2-benzoxazolyl sulfides using various fluoride salts and dimethoxyethane as a supporting electrolyte and a solvent, respectively, resulted in the formation of the corresponding mono- and difluorinated products in reasonable yields. The monofluorination took place selectively at the position α to the sulfur atom while the difluorination resulted at both the α-position and the benzene ring while the expected α,α-difluorination did not take place at all. Moreover, anodic fluorination of the electrolytic solvent, DME, which has never been reported so far, was also observed as a side-reaction and this fluorination was further confirmed by carrying out anodic fluorination of DME itself in the absence of a substrate sulfide.
- Dawood, Kamal M.,Higashiya, Seiichiro,Hou, Yankun,Fuchigami, Toshio
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p. 159 - 164
(2007/10/03)
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- ISOMERISM OF HYDRAZONES OF (2-BENZOTHIAZOLYLTHIO)- AND (2-BENZOXAZOLYLTHIO)ACETIC ACIDS
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PMR spectroscopy was used to shown that the hydrazones of (2-benzothiazolyl) and (2-benzoxazolyl)acetic acids exist in solution as equilibrium mixtures of stereoisomeric forms due to conformational and geometric isomerism.
- Rutavicius, A.,Valiulene, S.,Kuodis, Z.
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p. 629 - 633
(2007/10/03)
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- Synthesis and studies of (2-benzothiazolyl/benzimidazolyl/benzoxazolylthio)acetic acid (3-pyridyl)methylenehydrazides as possible anthelmintics
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Eighteen new (2-benzothiazolyl/benzimidazolyl/benzoxazolylthio)acetic acid (3-pyridil)methylene hydrazides (Va-r) have been synthesized and tested for their anthelmintic activity against H. nana infection in mice at a dose of 250 mg/kg * 3.In the primary screening compounds Va, Ve and Vk exhibit a high order of activity whereas Vc, Vd and Vm show moderate activity.
- Husain, M. Imtiaz,Kumar, Vinay
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p. 905 - 907
(2007/10/02)
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- Synthesis of 2-(2-benzothiazoyl/benzoxazoylthio)-N--5-oxo-2-phenyl/methyl-1H-imidazol-1-yl>acetamides as possible anthelmintics
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Twenty new 2-(2-benzothiazolyl/benzoxazolylthio)-N--5-oxo-2-phenyl/methyl-1H-imidazol-1-yl>acetamides have been synthesised and tested for their anthelmintic activity against H. nana infection in mice.
- Husain, M Imtiaz,Kumar, Vinay
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p. 285 - 288
(2007/10/02)
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- Synthesis and studies of 3--1,2,4-triazolothiadiazol-6-yl substituted phenyl as possible anthelmintics
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A series of 3--1,2,4-triazolothiadiazol-6-yl substituted phenyl (6a-x) has been synthesised and screened for anthelmintic activity against H.nana in mice at a dose of 250 mg/kg * 3.In the primary screening compounds 6c, 6d and 6k exhibited a high order of activity whereas the compounds 6b, 6p and 6r showed moderate activity.
- Husain, M Imtiaz,Kumar, Vinay
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p. 673 - 676
(2007/10/02)
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- Electrochemical Alkylation of Thiols
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Synthesis of functionally substituted sulfides by alkylation of electrochemically generated thiolate on platinum or glassy carbon cathodes with organohalides of various structures is reported.
- Petrosyan, V. A.,Niyazymbetov, M. E.,Konyushkin, L. D.,Litvinov, V. P.
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p. 841 - 842
(2007/10/02)
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- ELECTROCHEMICAL SYNTHESIS OF FUNCTIONALLY SUBSTITUTED SULFIDES
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A method of synthesis of functionally substituted sulfides by cathode electrolysis of thiols on platinum or carbon glass electrodes in the presence of organyl halides was developed.The method of the rotating disk electrode with ring showed that this process passes through the intermediate formation of a thiolate anion on the cathode, and its reaction with the organyl halide results in a high yield of sulfides.
- Niyazymbetov, M. E.,Petrosyan, V. A.,Konyushkin, L. D.,Litvinov, V. P.
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p. 1454 - 1457
(2007/10/02)
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