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Journal articles on the topic 'Thiamin analog'

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Published: 4 June 2021

Last updated: 5 February 2022

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1

Kwan, E., G. B. Baker, A. Shuaib, L. Ling, and K. G. Todd. "N-methyl,N-propargyl-2-phenylethylamine (MPPE), an analog of deprenyl, increases neuronal cell survival in thiamin deficiency encephalopathy." Drug Development Research 51, no. 4 (December 1, 2000): 244–52. http://dx.doi.org/10.1002/ddr.5.

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2

Chiu, Chingfan C., Ke Pan, and Frank Jordan. "Modeling an Elementary Step of the Enzyme Pyruvate Oxidase: Oxidation of a Thiamin Diphosphate-Bound Enamine Intermediate by a Flavin Analog." Journal of the American Chemical Society 117, no. 26 (July 1995): 7027–28. http://dx.doi.org/10.1021/ja00131a036.

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3

Feng, Lingling, Junbo He, Haifeng He, Lulu Zhao, Lingfu Deng, Li Zhang, Lin Zhang, Yanliang Ren, Jian Wan, and Hongwu He. "The design, synthesis and biological evaluation of novel thiamin diphosphate analog inhibitors against the pyruvate dehydrogenase multienzyme complex E1 from Escherichia coli." Org. Biomol. Chem. 12, no. 44 (2014): 8911–18. http://dx.doi.org/10.1039/c4ob01347f.

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4

Kale, Sachin, Palaniappa Arjunan, William Furey, and Frank Jordan. "A Dynamic Loop at the Active Center of the Escherichia coli Pyruvate Dehydrogenase Complex E1 Component Modulates Substrate Utilization and Chemical Communication with the E2 Component." Journal of Biological Chemistry 282, no. 38 (July 17, 2007): 28106–16. http://dx.doi.org/10.1074/jbc.m704326200.

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Our crystallographic studies have shown that two active center loops (an inner loop formed by residues 401-413 and outer loop formed by residues 541-557) of the E1 component of the Escherichia coli pyruvate dehydrogenase complex become organized only on binding a substrate analog that is capable of forming a stable thiamin diphosphate-bound covalent intermediate. We showed that residue His-407 on the inner loop has a key role in the mechanism, especially in the reductive acetylation of the E. coli dihydrolipoamide transacetylase component, whereas crystallographic results showed a role of this residue in a disorder-order transformation of these two loops, and the ordered conformation gives rise to numerous new contacts between the inner loop and the active center. We present mapping of the conserved residues on the inner loop. Kinetic, spectroscopic, and crystallographic studies on some inner loop variants led us to conclude that charged residues flanking His-407 are important for stabilization/ordering of the inner loop thereby facilitating completion of the active site. The results further suggest that a disorder to order transition of the dynamic inner loop is essential for substrate entry to the active site, for sequestering active site chemistry from undesirable side reactions, as well as for communication between the E1 and E2 components of the E. coli pyruvate dehydrogenase multienzyme complex.

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5

Hultin, Philip G., and Walter A. Szarek. "Heterocyclic analogs of nucleosides: synthesis and biological evaluation of some 1-(3-thianyl)uracil and 9-(3-thianyl)adenine derivatives." Canadian Journal of Chemistry 72, no. 1 (January 1, 1994): 208–13. http://dx.doi.org/10.1139/v94-032.

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The 1-(3-thianyl)uracil (9) and 9-(3-thianyl)adenine (14) nucleoside analogs have been prepared from the key intermediate, (±)-(3β,5β)-3-amino-5-(hydroxymethyl)thiane (6). Analog 9 was converted into a mixture of diastereomeric sulfoxides (10) that afforded, by a Pummerer reaction, a mixture of (±)-1-{(2′β,3′β,,5′β)-2′-acetoxy-5′-(acetoxymethyl)thian-3′-yl}-2,4(1H,3H)-pyrimidinedione (11a) and its 6′-β isomer (11b). The EI mass spectra of the nucleoside analogs are discussed. The uracil nucleoside analogs have been evaluated also for their anti-HIV and antitumor activities.

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6

Kim, Jaeah, Christopher P. Hopper, Kelsey H. Connell, Parisa Darkhal, Jason A. Zastre, and Michael G. Bartlett. "Development of a novel method for the bioanalysis of benfotiamine and sulbutiamine in cancer cells." Analytical Methods 8, no. 28 (2016): 5596–603. http://dx.doi.org/10.1039/c6ay01387b.

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Quantification of benfotiamine and sulbutiamine, synthetic thiamine analogs, in biological samples is an essential step toward understanding the role of these thiamine analogs on cancer cell proliferation.

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7

Thamm, Antje M., Gengnan Li, Marlene Taja-Moreno, Svetlana Y. Gerdes, Valérie de Crécy-Lagard, Steven D. Bruner, and Andrew D. Hanson. "A strictly monofunctional bacterial hydroxymethylpyrimidine phosphate kinase precludes damaging errors in thiamin biosynthesis." Biochemical Journal 474, no. 16 (August 10, 2017): 2887–95. http://dx.doi.org/10.1042/bcj20170437.

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The canonical kinase (ThiD) that converts the thiamin biosynthesis intermediate hydroxymethylpyrimidine (HMP) monophosphate into the diphosphate can also very efficiently convert free HMP into the monophosphate in prokaryotes, plants, and fungi. This HMP kinase activity enables salvage of HMP, but it is not substrate-specific and so allows toxic HMP analogs and damage products to infiltrate the thiamin biosynthesis pathway. Comparative analysis of bacterial genomes uncovered a gene, thiD2, that is often fused to the thiamin synthesis gene thiE and could potentially encode a replacement for ThiD. Standalone ThiD2 proteins and ThiD2 fusion domains are small (∼130 residues) and do not belong to any previously known protein family. Genetic and biochemical analyses showed that representative standalone and fused ThiD2 proteins catalyze phosphorylation of HMP monophosphate, but not of HMP or its toxic analogs and damage products such as bacimethrin and 5-(hydroxymethyl)-2-methylpyrimidin-4-ol. As strictly monofunctional HMP monophosphate kinases, ThiD2 proteins eliminate a potentially fatal vulnerability of canonical ThiD, at the cost of the ability to reclaim HMP formed by thiamin turnover.

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8

Zilles, Julie L., Laura R. Croal, and Diana M. Downs. "Action of the Thiamine Antagonist Bacimethrin on Thiamine Biosynthesis." Journal of Bacteriology 182, no. 19 (October 1, 2000): 5606–10. http://dx.doi.org/10.1128/jb.182.19.5606-5610.2000.

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ABSTRACT Bacimethrin is an analog of the 4-amino-5-hydroxymethyl-2-methylpyrimidine (HMP) moiety of thiamine and inhibits the growth of Salmonella enterica serovar Typhimurium on a defined medium. Two classes of mutants that had increased bacimethrin resistance were isolated and characterized. Results showed that overexpression of the thioperon or specific lesions in thiD resulted in a bacimethrin-resistant phenotype. Phenotypic analyses of thethiD mutants suggested that they had a specific defect in one of the two kinase activities associated with this gene product and, further, that ThiD and not PdxK was primarily responsible for salvage of HMP from the medium.

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9

Mee, Lisa, Svetlana M. Nabokina, V. Thillai Sekar, Veedamali S. Subramanian, Kathrin Maedler, and Hamid M. Said. "Pancreatic beta cells and islets take up thiamin by a regulated carrier-mediated process: studies using mice and human pancreatic preparations." American Journal of Physiology-Gastrointestinal and Liver Physiology 297, no. 1 (July 2009): G197—G206. http://dx.doi.org/10.1152/ajpgi.00092.2009.

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Thiamin is essential for the normal function of the endocrine pancreas, but very little is known about uptake mechanism(s) and regulation by beta cells. We addressed these issues using mouse-derived pancreatic beta-TC-6 cells, and freshly isolated primary mouse and human pancreatic islets. Results showed that thiamin uptake by beta-TC-6 cells involves a pH (but not Na+)-dependent carrier-mediated process that is saturable at both the nanomolar (apparent Km = 37.17 ± 9.9 nM) and micromolar (apparent Km = 3.26 ± 0.86 μM) ranges, cis-inhibited by thiamin structural analogs, and trans-stimulated by unlabeled thiamin. Involvement of carrier-mediated process was also confirmed in primary mouse and human pancreatic islets. Both THTR-1 and THTR-2 were found to be expressed in these mouse and human pancreatic preparations. Maintaining beta-TC-6 cells in the presence of a high level of thiamin led to a significant ( P < 0.01) decrease in thiamin uptake, which was associated with a significant downregulation in level of expression of THTR-1 and THTR-2 at the protein and mRNA levels and a decrease in transcriptional (promoter) activity. Modulators of intracellular Ca2+/calmodulin- and protein-tyrosine kinase-mediated pathways also altered thiamin uptake. Finally, confocal imaging of live beta-TC-6 cells showed that clinical mutants of THTR-1 have mixed expression phenotypes and all led to impairment in thiamin uptake. These studies demonstrate for the first time that thiamin uptake by the endocrine pancreas is carrier mediated and is adaptively regulated by the prevailing vitamin level via transcriptional mechanisms. Furthermore, clinical mutants of THTR-1 impair thiamin uptake via different mechanisms.

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10

Ashokkumar, Balasubramaniem, Nosratola D. Vaziri, and Hamid M. Said. "Thiamin uptake by the human-derived renal epithelial (HEK-293) cells: cellular and molecular mechanisms." American Journal of Physiology-Renal Physiology 291, no. 4 (October 2006): F796—F805. http://dx.doi.org/10.1152/ajprenal.00078.2006.

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Thiamin (vitamin B1) is essential for normal cellular functions. The kidneys play a critical role in regulating body thiamin homeostasis, by salvaging the vitamin via reabsorption from the glomerular filtrate, but little is known about the mechanism(s) and regulation of thiamin transport in the human renal epithelia at cellular and molecular levels. Using the human-derived renal epithelial HEK-293 cells as a model, we have addressed these issues. Our results showed [3H]thiamin uptake to be 1) temperature and energy dependent but Na+ independent, 2) pH dependent with higher uptake at alkaline/neutral buffer pH compared with acidic pH, 3) saturable as a function of concentration over the nanomolar (apparent Km = 70.0 ± 18.4 nM) and micromolar (apparent Km = 2.66 ± 0.18 μM) ranges, 4) cis-inhibited by unlabeled thiamin and its structural analogs but not by unrelated organic cations, 5) trans-stimulated by unlabeled thiamin, and 6) competitively inhibited by amiloride with an apparent Ki of 0.6 mM. Using a gene-specific small-interference RNAs (siRNAs) approach, human thiamin transporters 1 and 2 (hTHTR-1 and hTHTR-2) were both found to be expressed and contributed toward total carrier-mediated thiamin uptake. Maintaining the cells in thiamin-deficient medium led to a significant ( P < 0.01) and specific upregulation in [3H]thiamin uptake, which was associated with an increase in hTHTR-1 and hTHTR-2 protein and mRNA levels as well as promoter activities. Uptake of thiamin by HEK-293 cells also appeared to be under the regulation of an intracellular Ca2+/calmodulin-mediated pathway. These studies demonstrate for the first time that thiamin uptake by HEK-293 cells is mediated via a specific pH-dependent process, which involves both the hTHTR-1 and hTHTR-2. In addition, the uptake process appears to be under the regulation of an intracellular Ca2+/CaM-mediated pathway and also adaptively upregulated in thiamin deficiency via transcriptional regulatory mechanism(s) that involves both the hTHTR-1 and hTHTR-2.

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11

Nakanishi, Ikuo, Shinobu Itoh, Tomoyoshi Suenobu, Hiroo Inoue, and Shunichi Fukuzumi. "Redox Behavior of Active Aldehydes Derived from Thiamin Coenzyme Analogs." Chemistry Letters 26, no. 8 (August 1997): 707–8. http://dx.doi.org/10.1246/cl.1997.707.

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12

Said, Hamid M., Alvaro Ortiz, Veedamali S. Subramanian, Ellis J. Neufeld, Mary Pat Moyer, and Pradeep K. Dudeja. "Mechanism of thiamine uptake by human colonocytes: studies with cultured colonic epithelial cell line NCM460." American Journal of Physiology-Gastrointestinal and Liver Physiology 281, no. 1 (July 1, 2001): G144—G150. http://dx.doi.org/10.1152/ajpgi.2001.281.1.g144.

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Thiamine (vitamin B1) is essential for normal cellular functions and growth. Mammals cannot synthesize thiamine and thus must obtain the vitamin via intestinal absorption. The intestine is exposed to a dietary thiamine source and a bacterial source in which the vitamin is synthesized by the normal microflora of the large intestine. Very little is known about thiamine uptake in the large intestine. The aim of this study was, therefore, to address this issue. Our results with human-derived colonic epithelial NCM460 cells as a model system showed thiamine uptake to be 1) temperature- and energy dependent, 2) Na+ independent, 3) increased with increasing buffer pH from 5 to 8 and after cell acidification but inhibited by amiloride, 4) saturable as a function of concentration, 5) inhibited by thiamine structural analogs but not by unrelated organic cations, and 6) inhibited by modulators of a Ca2+/calmodulin-mediated pathway. NCM460 cells and native human colonic mucosa expressed the recently cloned human thiamine transporter THTR-1 (product of the SLC19A2 gene) at both mRNA and protein levels. These results demonstrate for the first time that human NCM460 colonocytes possess a specific carrier-mediated system for thiamine uptake that appears to be under the regulation of an intracellular Ca2+/calmodulin-mediated pathway. It is suggested that bacterially synthesized thiamine in the large intestine may contribute to thiamine nutrition of the host, especially toward cellular nutrition of the local colonocytes.

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13

Dudeja, Pradeep K., Sangeeta Tyagi, Reena J. Kavilaveettil, Ravinder Gill, and Hamid M. Said. "Mechanism of thiamine uptake by human jejunal brush-border membrane vesicles." American Journal of Physiology-Cell Physiology 281, no. 3 (September 1, 2001): C786—C792. http://dx.doi.org/10.1152/ajpcell.2001.281.3.c786.

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Thiamine, a water-soluble vitamin, is essential for normal cellular functions, growth and development. Thiamine deficiency leads to significant clinical problems and occurs under a variety of conditions. To date, however, little is known about the mechanism of thiamine absorption in the native human small intestine. The objective of this study was, therefore, to characterize the mechanism of thiamine transport across the brush-border membrane (BBM) of human small intestine. With the use of purified BBM vesicles (BBMV) isolated from the jejunum of organ donors, thiamine uptake was found to be 1) independent of Na+but markedly stimulated by an outwardly directed H+gradient (pH 5.5in/pH 7.5out); 2) competitively inhibited by the cation transport inhibitor amiloride (inhibitor constant of 0.12 mM); 3) sensitive to temperature and osmolarity of the incubation medium; 4) significantly inhibited by thiamine structural analogs (amprolium, oxythiamine, and pyrithiamine), but not by unrelated organic cations (tetraethylammonium, N-methylnicotinamide, or choline); 5) not affected by the addition of ATP to the inside and outside of the BBMV; 6) potential insensitive; and 7) saturable as a function of thiamine concentration with an apparent Michaelis-Menten constant of 0.61 ± 0.08 μM and a maximal velocity of 1.00 ± 0.47 pmol · mg protein−1· 10 s−1. Carrier-mediated thiamine uptake was also found in BBMV of human ileum. These data demonstrate the existence of a Na+-independent, pH-dependent, amiloride-sensitive, electroneutral carrier-mediated mechanism for thiamine absorption in native human small intestinal BBMV.

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14

Said, Hamid M., Alvaro Ortiz, Chandira K. Kumar, Nabendu Chatterjee, Pradeep K. Dudeja, and Stanley Rubin. "Transport of thiamine in human intestine: mechanism and regulation in intestinal epithelial cell model Caco-2." American Journal of Physiology-Cell Physiology 277, no. 4 (October 1, 1999): C645—C651. http://dx.doi.org/10.1152/ajpcell.1999.277.4.c645.

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The present study examined the intestinal uptake of thiamine (vitamin B1) using the human-derived intestinal epithelial cells Caco-2 as an in vitro model system. Thiamine uptake was found to be 1) temperature and energy dependent and occurred with minimal metabolic alteration; 2) pH sensitive; 3) Na+independent; 4) saturable as a function of concentration with an apparent Michaelis-Menten constant of 3.18 ± 0.56 μM and maximal velocity of 13.37 ± 0.94 pmol ⋅ mg protein−1⋅ 3 min−1; 5) inhibited by the thiamine structural analogs amprolium and oxythiamine, but not by unrelated organic cations tetraethylammonium, N-methylnicotinamide, and choline; and 6) inhibited in a competitive manner by amiloride with an inhibition constant of 0.2 mM. The role of specific protein kinase-mediated pathways in the regulation of thiamine uptake by Caco-2 cells was also examined using specific modulators of these pathways. The results showed possible involvement of a Ca2+/calmodulin (CaM)-mediated pathway in the regulation of thiamine uptake. No role for protein kinase C- and protein tyrosine kinase-mediated pathways in the regulation of thiamine uptake was evident. These results demonstrate the involvement of a carrier-mediated system for thiamine uptake by Caco-2 intestinal epithelial cells. This system is Na+independent and is different from the transport systems of organic cations. Furthermore, a CaM-mediated pathway appears to play a role in regulating thiamine uptake in these cells.

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15

Alston, Theodore A., and Robert H. Abeles. "Enzymatic conversion of the antibiotic metronidazole to an analog of thiamine." Archives of Biochemistry and Biophysics 257, no. 2 (September 1987): 357–62. http://dx.doi.org/10.1016/0003-9861(87)90577-7.

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16

Thomas, Allen A., J. De Meese, Y. Le Huerou, Steven A. Boyd, Todd T. Romoff, Steven S. Gonzales, Indrani Gunawardana, et al. "Non-charged thiamine analogs as inhibitors of enzyme transketolase." Bioorganic & Medicinal Chemistry Letters 18, no. 2 (January 2008): 509–12. http://dx.doi.org/10.1016/j.bmcl.2007.11.098.

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17

Le Huerou, Yvan, Indrani Gunawardana, Allen A. Thomas, Steven A. Boyd, Jason de Meese, Walter deWolf, Steven S. Gonzales, et al. "Prodrug thiamine analogs as inhibitors of the enzyme transketolase." Bioorganic & Medicinal Chemistry Letters 18, no. 2 (January 2008): 505–8. http://dx.doi.org/10.1016/j.bmcl.2007.11.100.

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18

Kandiko, Charles T., Daniel Smith, and Bryan K. Yamamoto. "Inhibition of rat brain pyruvate dehydrogenase by thiamine analogs." Biochemical Pharmacology 37, no. 22 (November 1988): 4375–80. http://dx.doi.org/10.1016/0006-2952(88)90620-x.

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19

Sugimori, Naomi, J. Luis Espinoza, Ly Quoc Trung, Akiyoshi Takami, Yukio Kondo, Dao Thi An, Motoko Sasaki, Tomohiko Wakayama, and Shinji Nakao. "Paraptosis Cell Death Induction by the Thiamine Analog Benfotiamine in Leukemia Cells." PLOS ONE 10, no. 4 (April 7, 2015): e0120709. http://dx.doi.org/10.1371/journal.pone.0120709.

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20

König, S., A. Schellenberger, H. Neef, and G. Schneider. "Specificity of coenzyme binding in thiamin diphosphate-dependent enzymes. Crystal structures of yeast transketolase in complex with analogs of thiamin diphosphate." Journal of Biological Chemistry 269, no. 14 (April 1994): 10879–82. http://dx.doi.org/10.1016/s0021-9258(17)34140-6.

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21

Brown, Scott B., Lisa R. Brown, Mitra Brown, Kristin Moore, Maria Villella, John D. Fitzsimons, Bill Williston, et al. "Effectiveness of Egg Immersion in Aqueous Solutions of Thiamine and Thiamine Analogs for Reducing Early Mortality Syndrome." Journal of Aquatic Animal Health 17, no. 1 (March 2005): 106–12. http://dx.doi.org/10.1577/h03-075.1.

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22

Uray, Georg, and Ingo Kriessmann. "Reaction of thiamin analogs with sulfite ion: an example of zero-order kinetics." Journal of Organic Chemistry 52, no. 5 (March 1987): 802–5. http://dx.doi.org/10.1021/jo00381a018.

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23

KOMATA, Yasuko, Akiko KANEKO, and Tadao FUJIE. "Solubilization of Thiamine Disulfide by Fatty Acid or Its Analog in 1,2-Dichloroethane." CHEMICAL & PHARMACEUTICAL BULLETIN 40, no. 12 (1992): 3311–13. http://dx.doi.org/10.1248/cpb.40.3311.

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24

Begum, Afshan, Julia Drebes, Alexey Kikhney, Ingrid B. Müller, Markus Perbandt, Dmitri Svergun, Carsten Wrenger, and Christian Betzel. "Staphylococcus aureusthiaminase II: oligomerization warrants proteolytic protection against serine proteases." Acta Crystallographica Section D Biological Crystallography 69, no. 12 (November 19, 2013): 2320–29. http://dx.doi.org/10.1107/s0907444913021550.

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Staphylococcus aureusTenA (SaTenA) is a thiaminase type II enzyme that catalyzes the deamination of aminopyrimidine, as well as the cleavage of thiamine into 4-amino-5-hydroxymethyl-2-methylpyrimidine (HMP) and 5-(2-hydroxyethyl)-4-methylthiazole (THZ), within thiamine (vitamin B1) metabolism. Further, by analogy with studies ofBacillus subtilisTenA,SaTenA may act as a regulator controlling the secretion of extracellular proteases such as the subtilisin type of enzymes in bacteria. Thiamine biosynthesis has been identified as a potential drug target of the multi-resistant pathogenS. aureusand therefore all enzymes involved in theS. aureusthiamine pathway are presently being investigated in detail. Here, the structure ofSaTenA, determined by molecular replacement and refined at 2.7 Å resolution to anRfactor of 21.6% with one homotetramer in the asymmetric unit in the orthorhombic space groupP212121, is presented. The tetrameric state of wild-type (WT)SaTenA was postulated to be the functional biological unit and was confirmed by small-angle X-ray scattering (SAXS) experiments in solution. To obtain insights into structural and functional features of the oligomericSaTenA, comparative kinetic investigations as well as experiments analyzing the structural stability of the WTSaTenA tetramerversusa monomericSaTenA mutant were performed.

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25

Nabokina, Svetlana M., and Hamid M. Said. "A high-affinity and specific carrier-mediated mechanism for uptake of thiamine pyrophosphate by human colonic epithelial cells." American Journal of Physiology-Gastrointestinal and Liver Physiology 303, no. 3 (August 1, 2012): G389—G395. http://dx.doi.org/10.1152/ajpgi.00151.2012.

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All mammals require exogenous sources of thiamine (vitamin B1), as they lack the ability to synthesize the vitamin. These sources are dietary and bacterial (the latter is in reference to the vitamin, which is synthesized by the normal microflora of the large intestine). Bacterially generated thiamine exists in the free, as well as the pyrophosphorylated [thiamine pyrophosphate (TPP)], form. With no (or very little) phosphatase activity in the colon, we hypothesized that the bacterially generated TPP can also be taken up by colonocytes. To test this hypothesis, we examined [3H]TPP uptake in the human-derived, nontransformed colonic epithelial NCM460 cells and purified apical membrane vesicles isolated from the colon of human organ donors. Uptake of TPP by NCM460 cells occurred without metabolic alterations in the transported substrate and 1) was pH- and Na+-independent, but energy-dependent, 2) was saturable as a function of concentration (apparent Km = 0.157 ± 0.028 μM), 3) was highly specific for TPP and not affected by free thiamine (or its analogs) or by thiamine monophosphate and unrelated folate derivatives, 4) was adaptively regulated by extracellular substrate (TPP) level via what appears to be a transcriptionally mediated mechanism(s), and 5) appeared to be influenced by an intracellular Ca2+/calmodulin-mediated regulatory pathway. These findings suggest the involvement of a carrier-mediated mechanism for TPP uptake by colonic NCM460 cells, which was further confirmed by results from studies of native human colonic apical membrane vesicles. The results also suggest that the bacterially synthesized TPP in the large intestine is bioavailable and may contribute to overall body homeostasis of vitamin B1 and, especially, to the cellular nutrition of the local colonocytes.

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B, Ravindar, Srinivasa Murthy M, and Afzal Basha Shaik. "DESIGN, FACILE SYNTHESIS, AND BIOLOGICAL EVALUATION OF NOVEL 1,3-THIAZINE DERIVATIVES AS POTENTIAL ANTICONVULSANT AGENTS." Asian Journal of Pharmaceutical and Clinical Research 9, no. 5 (September 1, 2016): 272. http://dx.doi.org/10.22159/ajpcr.2016.v9i5.13676.

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ABSTRACTObjective: Chalcones and their heterocyclic analogs represent an important class of small molecules having anticonvulsant activities. Therefore, inthis study, the synthesis and anticonvulsant activity of some new chalcones and 1,3-thiazines were described.Methods: The reaction of 1-acetylnaphthalene with substituted aromatic aldehydes in the presence of aq. NaOH afforded corresponding chalconeswhich upon further cyclization with thiourea resulted in 1,3-thiazine derivatives. The newly synthesized compounds were tested for anticonvulsantactivity by pentylenetetrazole-induced seizures method using diazepam as standard.Results: Most of the compounds showed good anticonvulsant activity but is less than diazepam. 1,3-thiazines were more potent than chalconesand among them, compound P4 containing 4-fluorophenyl substituents on the thiazine moiety was more potent as it has prolonged the onset ofconvulsions by 155.2 seconds.Conclusion: We described the synthesis and anticonvulsant activity of novel chalcones and 1,3-thiazine derivatives. 1,3-thiazines are more activeanticonvulsant agents than chalcones and in particular compounds with electron withdrawing substituents.Keywords: Chalcone, 1,3-thiazine, Pentylenetetrazole.

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27

Zoltewicz, John A., George Uray, Thomas D. Baugh, and Hanna Schultz. "Mechanism of nucleophilic substitution of thiamine and its analogs: Methanol and water solvents." Bioorganic Chemistry 13, no. 2 (June 1985): 135–49. http://dx.doi.org/10.1016/0045-2068(85)90016-1.

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28

Uray, G., I. Kriessmann, and J. A. Zoltewicz. "Dual Mechanisms of Nucleophilic Substitution of Thiamin Analogs: Estimating the Special Kinetic Effect of Sulfite Ion." Bioorganic Chemistry 21, no. 3 (September 1993): 294–308. http://dx.doi.org/10.1006/bioo.1993.1025.

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Yamashiro, Takahiro, Tomoya Yasujima, Hamid M. Said, and Hiroaki Yuasa. "pH-dependent pyridoxine transport by SLC19A2 and SLC19A3: Implications for absorption in acidic microclimates." Journal of Biological Chemistry 295, no. 50 (October 2, 2020): 16998–7008. http://dx.doi.org/10.1074/jbc.ra120.013610.

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SLC19A2 and SLC19A3, also known as thiamine transporters (THTR) 1 and 2, respectively, transport the positively charged thiamine (vitamin B1) into cells to enable its efficient utilization. SLC19A2 and SLC19A3 are also known to transport structurally unrelated cationic drugs, such as metformin, but whether this charge selectivity extends to other molecules, such as pyridoxine (vitamin B6), is unknown. We tested this possibility using Madin-Darby canine kidney II (MDCKII) cells and human embryonic kidney 293 (HEK293) cells for transfection experiments, and also using Caco-2 cells as human intestinal epithelial model cells. The stable expression of SLC19A2 and SLC19A3 in MDCKII cells (as well as their transient expression in HEK293 cells) led to a significant induction in pyridoxine uptake at pH 5.5 compared with control cells. The induced uptake was pH-dependent, favoring acidic conditions over neutral to basic conditions, and protonophore-sensitive. It was saturable as a function of pyridoxine concentration, with an apparent Km of 37.8 and 18.5 μm, for SLC19A2 and SLC19A3, respectively, and inhibited by the pyridoxine analogs pyridoxal and pyridoxamine as well as thiamine. We also found that silencing the endogenous SLC19A3, but not SLC19A2, of Caco-2 cells with gene-specific siRNAs lead to a significant reduction in carrier-mediated pyridoxine uptake. These results show that SLC19A2 and SLC19A3 are capable of recognizing/transporting pyridoxine, favoring acidic conditions for operation, and suggest a possible role for these transporters in pyridoxine transport mainly in tissues with an acidic environment like the small intestine, which has an acidic surface microclimate.

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30

Ketola, H. George, Gary R. Isaacs, Jeffrey S. Robins, and Russell C. Lloyd. "Effectiveness and Retention of Thiamine and Its Analogs Administered to Steelhead and Landlocked Atlantic Salmon." Journal of Aquatic Animal Health 20, no. 1 (March 2008): 29–38. http://dx.doi.org/10.1577/h07-012.1.

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31

Bender, R. A. "The Danger of Annotation by Analogy: Most "thiI" Genes Play No Role in Thiamine Biosynthesis." Journal of Bacteriology 193, no. 18 (July 8, 2011): 4574–75. http://dx.doi.org/10.1128/jb.05666-11.

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32

Chernyak, S. A., O. V. Shekhter, N. L. Sergovskaya, and Yu S. Tsizin. "Synthesis of 1,3,4,6,7,11b-hexahydro[1,4]thiazino[3,4,-a]-isoquinolin-4-one, an analog of prasiquantel." Chemistry of Heterocyclic Compounds 28, no. 7 (July 1992): 832–34. http://dx.doi.org/10.1007/bf00474503.

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33

Dixon, Seth, Xiaobing Wang, Kit S. Lam, and Mark J. Kurth. "Solid-phase synthesis of quinoxaline, thiazine, and oxazine analogs through a benzyne intermediate." Tetrahedron Letters 46, no. 43 (October 2005): 7443–46. http://dx.doi.org/10.1016/j.tetlet.2005.08.061.

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34

Abele, E., R. Abele, P. Arsenyan, S. Belyakov, M. Veveris, and E. Lukevics. "Phase-transfer catalytic synthesis and hypocholesterolemic activity of thiazino[3,2-a]benzimidazole and its silicon analog." Chemistry of Heterocyclic Compounds 43, no. 2 (February 2007): 220–24. http://dx.doi.org/10.1007/s10593-007-0034-9.

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35

Ponce-Monter, Héctor A., Mario I. Ortiz, Alexis F. Garza-Hernández, Raúl Monroy-Maya, Marisela Soto-Ríos, Lourdes Carrillo-Alarcón, Gerardo Reyes-García, and Eduardo Fernández-Martínez. "Effect of Diclofenac with B Vitamins on the Treatment of Acute Pain Originated by Lower-Limb Fracture and Surgery." Pain Research and Treatment 2012 (October 31, 2012): 1–5. http://dx.doi.org/10.1155/2012/104782.

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The aim of this study was to compare the efficacy of diclofenac, for the treatment of acute pain originated by lower-limb fracture and surgery, with that of diclofenac plus B vitamins. This was a single-center, prospective, randomized, and double-blinded clinical trial. Patients with lower-limb closed fractures rated their pain on a 10 cm visual analog scale (VAS). Patients were then randomized to receive diclofenac or diclofenac plus B vitamins (thiamine, pyridoxine, and cyanocobalamin) intramuscularly twice daily. Patient evaluations of pain intensity were recorded throughout two periods: twenty-four hours presurgery and twenty-four hours postsurgical. One hundred twenty-two patients completed the study. The subjects' assessments of limb pain on the VAS showed a significant reduction from baseline values regardless of the treatment group. Diclofenac plus B vitamins combination was more effective to reduce the pain than diclofenac alone. The results showed that the addition of B vitamins to diclofenac increased its analgesic effect. The novelty of this paper consists in that diclofenac and diclofenac plus B vitamins were useful for treatment of acute pain originated by lower-limb fracture and surgery.

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36

Edwards, Thomas E., and Adrian R. Ferré-D'Amaré. "Crystal Structures of the Thi-Box Riboswitch Bound to Thiamine Pyrophosphate Analogs Reveal Adaptive RNA-Small Molecule Recognition." Structure 14, no. 9 (September 2006): 1459–68. http://dx.doi.org/10.1016/j.str.2006.07.008.

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37

Marcus, E. Ted, Afaf Gundy, Corey H. Levenson, and Rich B. Meyer. "Nucleosides of 1,4-thiazin-3-one and derivatives as tetrahedral intermediate analogs of enzymes in pyrimidine nucleoside metabolism." Journal of Medicinal Chemistry 31, no. 8 (August 1988): 1575–79. http://dx.doi.org/10.1021/jm00403a015.

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38

Shapoval, G. S., L. V. Babii, O. S. Kruglyak, and A. I. Vovk. "Antioxidant activity of thiamine and its structural analogs in reactions with electrochemically generated hydroxyl radicals and hydrogen peroxide." Theoretical and Experimental Chemistry 47, no. 1 (March 2011): 55–60. http://dx.doi.org/10.1007/s11237-011-9185-y.

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39

Gutiérrez-Tarriño, Silvia, Javier Espino, Francisco Luna-Giles, Ana B. Rodríguez, José A. Pariente, and Emilio Viñuelas-Zahínos. "Synthesis, Characterization and Antiproliferative Evaluation of Pt(II) and Pd(II) Complexes with a Thiazine-Pyridine Derivative Ligand." Pharmaceuticals 14, no. 5 (April 22, 2021): 395. http://dx.doi.org/10.3390/ph14050395.

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Chemical, pharmacological, and clinical research on anticancer coordination complexes has led to noteworthy anticancer drugs such as cisplatin, carboplatin and oxaliplatin. Although these compounds are effective chemotherapeutic agents in the treatment of different tumors, they are associated with high toxicity and numerous side effects. Several studies have shown that the range of platinum complexes with antitumor activity is not limited to structural analogs of cisplatin. Therefore, the development of convenient anticancer drugs that can be effectively used for the treatment of human tumors has become the main goal of most research groups in this field. In this sense, active platinum complexes without NH groups, transplatinum complexes, multinuclear complexes, cationic complexes, and several classes of palladium(II) complexes have emerged. Herein, the synthesis and characterization of two Pt(II) or Pd(II) complexes with PyTz (2-(2-pyridyl)iminotetrahydro-1,3-thiazine), a thiazine derivative ligand, with the formula [MCl2(PyTz)]·C2H6O (M = Pt(II) or Pd(II)) were reported. The potential anticancer ability of both complexes was evaluated in epithelial cervix carcinoma HeLa, human ovary adenocarcinoma SK-OV-3, human histiocytic lymphoma U-937, and human promyelocytic leukemia HL-60 cell lines. Interestingly, the Pt(II) complex showed great cytotoxic potential against all tumor cell lines tested, whereas the Pd(II) complex displayed slight antitumor actions.

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40

Shukla, Upendra K., Raieshwar Singh, J. M. Khanna, Anil K. Saxena, Hemant K. Singh, Ravindra N. Sur, Bhola N. Dhawan, and Nitya Anand. "Synthesis of trans-2-[N-(2-Hydroxy-1,2,3,4-tetrahydronaphthalene-1-yl)]iminothiazolidine and Related Compounds - A New Class of Antidepressants." Collection of Czechoslovak Chemical Communications 57, no. 2 (1992): 415–24. http://dx.doi.org/10.1135/cccc19920415.

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Antiparasitic and antidepressant activities exhibited by tetramisole (I) and its enantiomers prompted the study of its structural analogs trans-2-[N-(2-hydroxy-1,2,3,4-tetrahydronaphthalene/indane-1-yl)]iminothiazolidine (VIII/IX) and 2,3,4a,5,6,10b-hexahydronaphtho[1',2':4,5]-imidazo[2,1-b]thiazole (XII), 2,3,4a,5-tetrahydro-9bH-indeno[1',2':4,5]imidazo[2,1-b]thiazole (XIII), and 2,3,4a,5-tetrahydro-9bH-indeno[1',2':4,5]imidazo[2,1-b]thiazole (XVI), and a homolog 3,4,6,7-tetrahydro-7-phenyl-2H-imidazo[2,1-b]-1,3-thiazine (XX). While none of these compounds showed any noteworthy antiparasitic activity, the trans-2-[N-(2-hydroxy-1,2,3,4-tetrahydronaphthalene-1-yl)]iminothiazolidine (VIII) has shown marked antidepressant activity, better than imipramine in the tests used, and provides a new structural lead for antidepressants.

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41

KOMATA, Yasuko, Akiko KANEKO, and Tadao FUJIE. "In Vitro Percutaneous Absorption of Thiamine Disulfide through Rat Skin from a Mixture of Propylene Glycol and Fatty Acid or Its Analog." CHEMICAL & PHARMACEUTICAL BULLETIN 40, no. 8 (1992): 2173–76. http://dx.doi.org/10.1248/cpb.40.2173.

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42

Guo, Xiaolong, Luyao Wang, Jing Hu, and Mengmeng Zhang. "CuI nanoparticle-catalyzed synthesis of tetracyclic benzo[e]benzo[4,5]imidazo[1,2-c][1,3]thiazin-6-imine heterocycles by SNAr-type C–S, C–N bond formation from isothiocyanatobenzenes and benzimidazoles." RSC Advances 8, no. 39 (2018): 22259–67. http://dx.doi.org/10.1039/c8ra02552e.

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We proposed a practical synthesis of analogs of the anti-HIV drug 3,4-dihydro-2H,6H-pyrimido[1,2-c][1,3]benzothiazin-6-imine via a CuI nanoparticle-catalyzed intramolecular C(sp²)–S coupling reaction.

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43

Shin, Whanchul, and Young Chang Kim. "Crystal structure of thiamine thiazolone: a possible transition-state analog with an intramolecular N-H.cntdot..cntdot..cntdot.O hydrogen bond in the V form." Journal of the American Chemical Society 108, no. 22 (October 1986): 7078–82. http://dx.doi.org/10.1021/ja00282a038.

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44

Mimenza Alvarado, Alberto, and Sara Aguilar Navarro. "Clinical Trial Assessing the Efficacy of Gabapentin Plus B Complex (B1/B12) versus Pregabalin for Treating Painful Diabetic Neuropathy." Journal of Diabetes Research 2016 (2016): 1–8. http://dx.doi.org/10.1155/2016/4078695.

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Introduction. Painful diabetic neuropathy (PDN) is a prevalent and impairing disorder. The objective of this study was to show the efficacy and safety of gabapentin (GBP) plus complex B vitamins: thiamine (B1) and cyanocobalamine (B12) compared to pregabalin in patients with moderate to severe intensity PDN.Method. Multicenter, randomized, blind study. Two hundred and seventy patients were evaluated, 147 with GBP/B1/B12 and 123 with PGB, with a 7/10 pain intensity on the Visual Analog Scale (VAS). Five visits (12 weeks) were scheduled. The GBP/B1 (100 mg)/B12 (20 mg) group started with 300 mg at visit 1 to 3600 mg at visit 5. The PGB group started with 75 mg/d at visit 1 to 600 mg/d at visit 5. Different safety and efficacy scales were applied, as well as adverse event assessment.Results. Both drugs showed reduction of pain intensity, without significant statistical difference (P=0.900). In the GBP/B1/B12 group, an improvement of at least 30% on VAS correlated to a 900 mg/d dose, compared with PGB 300 mg/d. Likewise, occurrence of vertigo was lower in the GBP/B1-B12 group, with a significant statistical difference,P=0.014.Conclusions. Our study shows that GPB/B1-B12 combination is as effective as PGB. Nonetheless, pain intensity reduction is achieved with 50% of the minimum required gabapentin dose alone (800 to 1600 mg/d) in classic NDD trials. Less vertigo and dizziness occurrence was also observed in the GBP/B1/B12 group. This trial is registered with ClinicalTrials.govNCT01364298.

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Yuan, Chen, Jie Yan, Chen Song, Fan Yang, Chao Li, Cheng Wang, Huiling Su, et al. "Discovery of [1,2,4]Triazole Derivatives as New Metallo-β-Lactamase Inhibitors." Molecules 25, no. 1 (December 23, 2019): 56. http://dx.doi.org/10.3390/molecules25010056.

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The emergence and spread of metallo-β-lactamase (MBL)-mediated resistance to β-lactam antibacterials has already threatened the global public health. A clinically useful MBL inhibitor that can reverse β-lactam resistance has not been established yet. We here report a series of [1,2,4]triazole derivatives and analogs, which displayed inhibition to the clinically relevant subclass B1 (Verona integron-encoded MBL-2) VIM-2. 3-(4-Bromophenyl)-6,7-dihydro-5H-[1,2,4]triazolo [3,4-b][1,3]thiazine (5l) manifested the most potent inhibition with an IC50 (half-maximal inhibitory concentration) value of 38.36 μM. Investigations of 5l against other B1 MBLs and the serine β-lactamases (SBLs) revealed the selectivity to VIM-2. Molecular docking analyses suggested that 5l bound to the VIM-2 active site via the triazole involving zinc coordination and made hydrophobic interactions with the residues Phe61 and Tyr67 on the flexible L1 loop. This work provided new triazole-based MBL inhibitors and may aid efforts to develop new types of inhibitors combating MBL-mediated resistance.

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46

Wakchaure, Padmaja D., and Bishwajit Ganguly. "Molecular level insights into the inhibition of gene expression by thiamine pyrophosphate (TPP) analogs for TPP riboswitch: A well-tempered metadynamics simulations study." Journal of Molecular Graphics and Modelling 104 (May 2021): 107849. http://dx.doi.org/10.1016/j.jmgm.2021.107849.

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47

Imperatore, Concetta, Gerardo Della Sala, Marcello Casertano, Paolo Luciano, Anna Aiello, Ilaria Laurenzana, Claudia Piccoli, and Marialuisa Menna. "In Vitro Antiproliferative Evaluation of Synthetic Meroterpenes Inspired by Marine Natural Products." Marine Drugs 17, no. 12 (December 5, 2019): 684. http://dx.doi.org/10.3390/md17120684.

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Several marine natural linear prenylquinones/hydroquinones have been identified as anticancer and antimutagenic agents. Structure-activity relationship studies on natural compounds and their synthetic analogs demonstrated that these effects depend on the length of the prenyl side chain and on the type and position of the substituent groups in the quinone moiety. Aiming to broaden the knowledge of the underlying mechanism of the antiproliferative effect of these prenylated compounds, herein we report the synthesis of two quinones 4 and 5 and of their corresponding dioxothiazine fused quinones 6 and 7 inspired to the marine natural product aplidinone A (1), a geranylquinone featuring the 1,1-dioxo-1,4-thiazine ring isolated from the ascidian Aplidium conicum. The potential effects on viability and proliferation in three different human cancer cell lines, breast adenocarcinoma (MCF-7), pancreas adenocarcinoma (Bx-PC3) and bone osteosarcoma (MG-63), were investigated. The methoxylated geranylquinone 5 exerted the highest antiproliferative effect exhibiting a comparable toxicity in all three cell lines analyzed. Interestingly, a deeper investigation has highlighted a cytostatic effect of quinone 5 referable to a G0/G1 cell-cycle arrest in BxPC-3 cells after 24 h treatment.

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Csomós, Péter, Lajos Fodor, István Zupkó, Antal Csámpai, and Pál Sohár. "Synthesis and in vitro antiproliferative effect of isomeric analogs of cyclobrassinin phytoalexin possessing 1,3-thiazino[5,6-b]indole-4-one skeleton." Arkivoc 2017, no. 4 (April 18, 2017): 1–11. http://dx.doi.org/10.24820/ark.5550190.p009.962.

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Bairam, Ravindar, Srinivasa Murthy Muppavarapu, and Sivan Sreekanth. "SYNTHESIS, CHARACTERIZATION, BIOLOGICAL EVALUATION AND DOCKING OF SOME NOVEL SUBSTITUTED 1, 3-THIAZINE DERIVATIVES." International Journal of Pharmacy and Pharmaceutical Sciences 9, no. 3 (February 3, 2017): 233. http://dx.doi.org/10.22159/ijpps.2017v9i3.16406.

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Objective: Chalcones and their heterocyclic analogs represent an important class of small molecules which have a wide range of pharmacological activities. Therefore, in this study, synthesis and anticonvulsant and antimicrobial activities of some new 1, 3-thiazines have been extensively discussed.Methods: The reaction mixture of 4-tert-butylcyclohexanone on Claisen-Schmidt condensation with various aromatic aldehydes in the presence of dilute sodium hydroxide afforded the corresponding chalcones. Further, these compounds were subjected to cocondensation with thiourea, in the presence of isopropanol, catalyzed by aqueous potassium hydroxide to form 4-aryl 8-arylidene-5, 6-dihydro-2-imino-6-methyl-4H, 7H-(1, 3) benzothiazines. The structures of the newly synthesized compounds have been established on the basis of their spectral analysis. The newly synthesized compounds have been tested for their biological screening. Antimicrobial activity by cup plate agar diffusion method and antiepileptic activity by pentylenetetrazole (PTZ) induced seizures model, using diphenyl hydantain as standard, and also they are subjected to molecular properties prediction, toxicity, drug-likeness, lipophilicity and solubility parameters determination were done by using Osiris program, Molsoft, Prototox and ALOGPS 2.1 software. The binding mode of the synthesized compounds with active protein site has been predicted using docking method.Results: Most of the compounds have shown good anticonvulsant as well as antimicrobial activities, but it is less than the standard drugs. 1, 3-thiazines derivatives were more potent, and among them, compounds TB5 andTB7 were the most active compounds in these series; TB5 whichcontains isopropyl phenyl moiety, was shown moderate potent activity with onset of convulsion at 14.1 min and TB7 containing 3, 4, 5-trimethoxyphenyl substituents on the thiazine moiety was more potent as it has prolonged the onset of convulsions by 18.7 min. Whereas in the case of antimicrobial activity of the compounds, from the results we have observed that TB5 have been shown greatest antimicrobial activity in all the bacterial and fungal strains, TB2 also shown superior activity, the others have been shown good antimicrobial activity.Conclusion: According to the activity studies, it is observed that the synthesis and antimicrobial as well as anticonvulsant activities of novel 1, 3-thiazine derivatives have been shown better activity. Moreover molecular docking results give an insight into how further modification of the lead compound can be carried out for higher inhibitory activity. In particular, compounds with electron withdrawing substituents along with lipophilic methoxyl and isopropyl groups were more potent.

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Sá, Marcus Mandolesi, Misael Ferreira, Adailton J. Bortoluzzi, Luciano Fernandes, and Silvio Cunha. "Exploring the reaction of multifunctional allylic bromides with N,S-dinucleophiles: isothiouronium salts and analogs as useful motifs to assemble the 1,3-thiazine core." Arkivoc 2010, no. 11 (November 14, 2010): 303–21. http://dx.doi.org/10.3998/ark.5550190.0011.b24.

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