- Design, synthesis and identification of novel substituted 2-amino thiazole analogues as potential anti-inflammatory agents targeting 5-lipoxygenase
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Human 5-Lipoxygenase (5-LOX) is a key enzyme targeted for asthma and inflammation. Zileuton, the only drug against 5-LOX, was withdrawn from the market due to several problems. In the present study, the performance of rationally designed conjugates of thi
- Sinha, Shweta,Doble, Mukesh,Manju
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- Expanding the donor-acceptor toolbox with a minimal 5-(thiophen-2-yl)-1,3-thiazole core: Transition metal-free synthesis and molecular design for HOMO-LUMO energy modulations
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Synthesis of a minimal 5-(thiophen-2-yl)-1,3-thiazole core through a transition metal-free, versatile [4+1] route is reported. DFT calculations on a prototype library of D-A-D-A tetrads established the exquisite HOMO-LUMO energy modulation by varying peri
- Radhakrishnan, Rakesh,Sreejalekshmi, Kumaran G.
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supporting information
p. 3036 - 3039
(2016/05/09)
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- Crystal structures and antimicrobial and cytotoxic activities of zinc(II), nickel(II) and copper(II) complexes of N-(piperidylthiocarbonyl)benzamide
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A new zinc(II) complex of N-(piperidylthiocarbonyl)benzamide, [ZnL2], has been synthesized and characterized using elemental analysis, Fourier transform infrared and 1H NMR spectroscopies. X-ray diffraction indicates that [ZnL2
- Xie, Juan,Cheng, Zhongqin,Yang, Wen,Liu, Huanhuan,Zhou, Weiqun,Li, Mengying,Xu, Yunlong
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p. 157 - 164
(2015/03/30)
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- Crystal structures and antifungal activities of fluorine-containing thioureido complexes with nickel(II)
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Ni(II) complexes with N-2-fluorobenzoylpiperidine-1-carbothioimidate (L2-), N-4-fluorobenzoylpiperidine-1-carbothioimidate (L3-), N-2- fluorobenzoylmorpholine- 1-carbothioimidate (L5-) and N-4- fluorobenzoylmorpholine-1-carbothioimidate (L6-) have been synthesized and characterized by elemental analysis, FTIR and 1H-NMR. The crystal structures of three ligands (HL2, HL3 and HL6) and the corresponding Ni(II) complexes ([Ni(L2)2], [Ni(L3)2] and [Ni(L6)2]) have been determined by X-ray diffraction. The antifungal activities of the Ni(II) complexes together and the corresponding ligands against the fungi Botrytis cinerea, Trichoderma spp., Myrothecium and Verticillium spp. have been investigated. The experimental results showed that the ligands and their complexes have antifungal abilities. When the fluorine was substituted on the para-benzoyl moiety, the antifungal activity of the ligands was obviously increased. Moreover, the ligands were stronger than their complexes in inhibiting fungal activities. The antifungal ability of HL6 is especially strong, and similar to that of the commercial fungicide fluconazole.
- Li, Chun,Yang, Wen,Liu, Huanhuan,Li, Mengying,Zhou, Weiqun,Xie, Juan
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p. 15737 - 15749
(2014/01/17)
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- Efficient one-pot synthesis of alkyl 2-(dialkylamino)-4-phenylthiazole-5- carboxylates and single-crystal x-ray structure of methyl 2-(diisopropylamino)- 4-phenylthiazole-5-carboxylate
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The reaction between secondary amines, benzoyl isothiocyanate, and dialkyl acetylenedicarboxylates (=dialkyl but-2-ynedioates) in the presence of silica gel (SiO2) led to alkyl 2-(dialkylamino)-4-phenylthiazole-5- carboxylates in fairly high yi
- Souldozi, Ali,Ramazani, Ali,Dadrass, Ali Reza,Slepokura, Katarzyna,Lis, Tadeusz
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scheme or table
p. 339 - 348
(2012/04/10)
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- Facile synthesis of 3-aryl/alkylamino 5-aryl/alkyl 1,2,4-oxadiazoles from acylthiourea
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Facile and selective synthesis of 3-aryl/alkylamino 5-aryl/alkyl 1,2,4-oxadiazoles starting from N-acylthioureas has been demonstrated. The regio-selectivity is achieved by simply selecting an appropriate base used for the generation of hydroxyl amine fro
- Chennakrishnareddy, Gundala,Debasis, Hazra,Jayan, Rapai,Manjunatha, Sulur G.
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experimental part
p. 6170 - 6173
(2011/11/30)
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- A rapid, four-component synthesis of functionalized thiazoles
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An efficient synthesis of 2-(dialkylamino)-4-phenyl)-1,3-thiazol-5-yl) (phenyl)methanone using acid chlorides, secondary amines, 2-bromoacethophenone and ammonium thiocyanate is described.
- Sabbaghan, Maryam,Alidoust, Mostafa,Hossaini, Zinatossadat
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experimental part
p. 824 - 828
(2012/04/23)
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- Silica-gel-catalyzed conversion of stabilized phosphorus ylides to benzo[e][1,3]thiazocin derivatives
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The reaction between triphenylphosphine, dialkylacetylenedicarboxylates, and N-benzoyl thiourea derivatives leads to intermediates such as vinyltriphenylphosphonium salts, which undergo Michael addition to produce the highly functionalized phosphorus ylid
- Souldozi, Ali,Dadrass, Ali Reza
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experimental part
p. 1921 - 1925
(2010/11/19)
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- One-pot synthesis of functionalized thioureas by reaction of benzoyl isothiocyanates, secondary amines, and alkyl propiolates
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An efficient one-pot synthesis of functionalized thioureas is described via three-component reaction of benzoyl isothiocyanates, secondary amines, and alkyl propiolates in the presence of triphenylphosphine (20∈mol%).
- Yavari, Issa,Sayyed-Alangi, S. Zahra,Sabbaghan, Maryam,Hajinasiri, Rahimeh,Iravani, Nasir
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experimental part
p. 1025 - 1028
(2009/11/30)
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- Versatile novel syntheses of imidazoles
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A novel ring transformation/desulfurization of substituted 2-methyl-1,2,4-thiadiazolium salts 2 provides a versatile entry to imidazoles 3 with a variety of substituents. Simple one-pot procedures combine the preparation of starting 1,2,4-thiadiazolium salts 2 from N-(thiocarbonyl)-N'-methylamidines 1 or 1,2,4-dithiazolium triiodides 6 with the ring transformation/desulfurization to the imidazoles 3. Alternatively, N-(thiocarbonyl)-N'-methylamidines 1 can be transformed to imidazoles 3 or to 1-substituted imidazoles 5 via S-methylation and elimination of methylthiol. In the same manner, a new entry to 4H-imidazoles 8 could be developed.
- Rolfs, Andreas,Liebscher, Juergen
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p. 3480 - 3487
(2007/10/03)
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- SYNTHESIS AND STUDY OF NEW N-BENZOYLTHIOUREA DERIVATIVES
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A series of new derivatives of N-benzoylthiourea were synthesized and characterized, and the kinetics of their reactions with cumene hydroperoxide was studied.
- Mukmeneva, N. A.,Khabikher, V. Kh.,Cherkasova, O. A.,Cherezova, E. N.,Tuzova, N. G.
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p. 925 - 927
(2007/10/02)
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- N'-Substituted N-Acyl- and N-Imidoyl-thioureas: Preparation and Conversion of N',N'-Disubstituted Compounds into 2-(N,N-Disubstituted Amino)thiazol-5-yl Ketones
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Known methods were developed to give convenient general procedures for preparing N-acyl-N'-mono- and -N',N'-disubstituted thioureas from acid chlorides, and related N-imidoyl thioureas from imidoyl chlorides.In the products from three acid chlorides and ammonium thiocyanate the acyl isothiocyanates did not appear to be accompained by the isomeric thiocyanates.Treatment of N-(anilino)benzylidene-N',N'-disubstituted thioures with chloroacetone in the presence of triethylamine leads to 5-acetyl-4-phenyl-2-(N,N-disubstituted amino)thiazoles.In contrast, the corresponding N-benzoyl thioureas form only small amounts of these compounds; the main products are the 5-benzoyl-4-methyl isomers, and this unexpected outcome requires a revision of the literature.It is thought that formation of the 5-benzoyl-4-methylthiazoles involves N-C(4) fission of a cyclic intermediate to give an open-chain intermediate in which nucleophilic attack can occur at either the acetyl or the benzoyl group.One of the latter intermediates was generated directly from 2-acetyl-2-bromoacetophenone and N-methyl-N-phenylthiourea, and found to give the 5-benzoyl-4-methyl- and 5-acetyl-4-phenyl-thiazoles as the major and minor products, respectively.
- Brindley, Jocelyn C.,Caldwell, Jennifer M.,Meakins, G. Denis,Plackett, Simon J.,Price, Susan J.
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p. 1153 - 1158
(2007/10/02)
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- Reaction of β-Nitro Enamines with Isocyanates, Isothiocyanates and Dimethyl Acetylenedicarboxylate
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β-Nitro enamines (1) reacted with isocyanates and isothiocyanates to give β-(substituted carbamoyl) and β-(substituted thiocarbamoyl) β-nitro enamines, respectively.The reaction of 1 with benzoyl isothiocyanate gave β-(benzoylthiocarbamoyl) β-nitro enamines (8) and/or a mixture of 8 and 4(1H)-pyrimidinethione derivatives (9), which were cyclization products of 8.The isolated 8 afforded the corresponding 9 in high yields upon heating in DMF.The reaction of 1 with dimethyl acetylenedicarboxylate gave cycloadducts (12) and/or a mixture of 12 and δ-nitro dienamino diesters (13) which were ring cleavage products of 12.Compounds 12 afforded 13 upon heating in toluene or xylene.
- Tokumitsu, Takao
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p. 3871 - 3876
(2007/10/02)
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