Editor Papa Research September 4, 2019

Highly Enantioselective Aza‐Baylis–Hillman Reactions Catalyzed by Chiral Thiourea Derivatives

We report the invention of uneven aza‐Baylis–Hillman (ABH) reactions of N‐p‐nitrobenzenesulfonylimines with alkyl group salt catalyzed by chiral thiourea derivatives. A series of aromatic imines was found to bear coupling with alkyl group salt with unexampled levels of enantioselectivity (87–99% ee), albeit solely in modest (25–49%) yields. A DABCO‐acrylate‐imine adduct was isolated as a key intermediate within the ABH reaction. we offer a mechanistic analysis supported the identity of this intermediate likewise as kinetic investigations and atom studies, and propose a principle for the determined limitations in yield. artificial applications of the ABH merchandise also are delineate. [1]

Antimicrobial Activity of Some Thiourea Derivatives and Their Nickel and Copper Complexes

Five thiourea spinoff ligands and their Ni2+ and Cu2+ complexes are synthesized. The compounds were screened for his or her in vitro anti-bacterial activity exploitation gram-positive microorganism (two totally different customary strains of cocci aureus, cocci epidermidis, Enterococcus faecalis, true bacteria pyogenes, eubacterium cereus) and gram-negative bacteria (Esherichia coli, genus Pseudomonas aeruginosa, Enterobacter cloacae, Proteus vulgaris, Enterobacter aerogenes) and in vitro anti-yeast activity (Candida albicans, fungus krusei, fungus glabrata, fungus tropicalis, fungus parapsilosis). The minimum repressive concentration resolve for all ligands and their complexes. [2]

Urea and Thiourea Derivatives as Low Molecular‐Mass Organogelators

The properties of a series of organogels consisting of a organic compound or thiourea spinoff with one or 2 n‐alkyl substitutuents at the chemical element atoms (a low molecular‐mass organogelator (LMOG)) ANd an organic liquid area unit delineate. They embody N,N′‐dimethylurea, the LMOG of lowest molecular mass (MW 88) we tend to area unit awake to. The efficiencies of the LMOGs, based mostly the variety of liquids gelated, the minimum quantity needed for gelation of a liquid at temperature, and also the temporal and thermal stabilities of the gels fashioned, are investigated as a operate of the quantity, length, and substitution pattern of their n‐alkyl chains.  [3]

Design, synthesis and antitumor evaluation of a new series of N-substituted-thiourea derivatives

Aim: to style and synthesize a unique category of macromolecule amino acid enzyme inhibitors, that includes the N-(2-oxo-1,2-dihydroquinolin-3-yl-methyl)-thiourea framework.

Methods: 1st, compounds one and a pair of were known exploitation the virtual screening approach in conjunction with binding assay supported surface plasmon resonance. afterwards, three regions of compounds one and a pair of were hand-picked for chemical modification. All compounds were characterised potent repressive activities toward the human respiratory organ carcinoma cell line SPAC1. [4]

Synthesis, Characterization and Antibacterial Studies of Some Metal Complexes of N-DI (Pyridin-2-YL) Thiourea Derivatives

N-(di (pyridin-2-yl) carbamothioyl)-3-nitrobenzamide (L1) and N-(di(pyridin-2-yl) carbamothioyl)-4-nitrobenzamide (L2)) and their copper (II), nickel (II), Co (II) and atomic number 30 (II) complexes are synthesized, characterised and tested for medicinal drug activity. The ligands were synthesized below reflux and characterised with some qualitative analysis techniques. FTIR studies of those 2 nitro-substituted-N-di (pyridin-2-yl) thiourea derivatives showed the presence of >N-H and >C=S teams. The 1HNMR spectra of those compounds, L1 and L2revealed chemical shifts for dipyridyl-protons at seven.13 – 8.37 ppm and vi.89 – 8.03 ppm severally. The 13CNMR spectra, in support, appeared down around ~154 ppm for pyridyl-carbon atoms. [5]

Reference

[1] Raheem, I.T. and Jacobsen, E.N., 2005. Highly Enantioselective Aza‐Baylis–Hillman Reactions Catalyzed by Chiral Thiourea Derivatives. Advanced Synthesis & Catalysis, 347(11‐13), pp.1701-1708. (Web Link)

[2] Arslan, H., Duran, N., Borekci, G., Koray Ozer, C. and Akbay, C., 2009. Antimicrobial activity of some thiourea derivatives and their nickel and copper complexes. Molecules, 14(1), pp.519-527. (Web Link)

[3] George, M., Tan, G., John, V.T. and Weiss, R.G., 2005. Urea and Thiourea Derivatives as Low Molecular‐Mass Organogelators. Chemistry–A European Journal, 11(11), pp.3243-3254. (Web Link)

[4] Design, synthesis and antitumor evaluation of a new series of N-substituted-thiourea derivatives
Jian Li, Jin-zhi Tan, Li-li Chen, Jian Zhang, Xu Shen, Chang-lin Mei, Li-li Fu, Li-ping Lin, Jian Ding, Bing Xiong, Xi-shan Xiong, Hong Liu, Xiao-min Luo & Hua-liang Jiang
Acta Pharmacologica Sinicavolume 27, pages1259–1271 (2006) (Web Link)

[5] M. Fayomi, O., Sha’Ato, R., A. Wuana, R., O. Igoli, J., Moodley, V. and E. Van Zyl, W. (2018) “Synthesis, Characterization and Antibacterial Studies of Some Metal Complexes of N-DI (Pyridin-2-YL) Thiourea Derivatives”, International Research Journal of Pure and Applied Chemistry, 16(3), pp. 1-31. doi: 10.9734/RJPAC/2018/40567. (Web Link)

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