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Journal articles on the topic 'Substituted Nicotinic acid'

Author: Grafiati

Published: 3 June 2025

Last updated: 31 July 2025

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1

Sokolenko, Taras M., and Yurii L. Yagupolskii. "5-Trifluoromethoxy-substituted Nicotinic Acid, Nicotinamide and Related Compounds." Журнал органічної та фармацевтичної хімії 22, no. 1 (2024): 22–30. http://dx.doi.org/10.24959/ophcj.24.302435.

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A practical and convenient method for synthesizing nicotinic acid and nicotinamide with the trifluoromethoxy group in position 5 of the ring has been developed. A series of related compounds, for example, nicotinic aldehyde and nicotinic alcohol, have been synthesized. It has been shown that 3-bromo-5-trifluoromethoxypyridine is a convenient and efficient synthon for palladium-catalyzed coupling reactions. The trifluoromethoxy group has been found to be remarkably stable against hydroiodic acid in contrast to the methoxy group.

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2

N., Hariraj1* N. Kannappan2 Siju.E.N3. "Synthesis of certain Pyrazoline 5-One Derivatives of 6-Methyl Nicotinicacid and Evaluation of their Antimicrobial activities." Journal of Pharma Research 1, no. 2 (2012): 16–17. https://doi.org/10.5281/zenodo.1098657.

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<strong><em>ABSTRACT</em></strong> <em>Pyrazolines are known to possess a wide variety of biological activities. Due to the wide range of biological activities that Pyrazolines posses, it was our aim to prepare pyrazolin-5-one derivatives containing substituted Nicotinic acid and to explore, their therapeutic advantage. Among the six newly synthesized pyrazoline-5-one derivatives MPZ-1 showed promising antimicrobial activity even at a concentration 250mcg/disc. and MPZ-2 showed moderate antimicrobial activity at a concentration 500mcg/disc.</em> <strong><em>Keywords: </em></strong><em>Pyrazoli

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3

Nandi, Goutam, Ranjit Thakuria, Hatem M. Titi, Ranjan Patra, and Israel Goldberg. "Synthesis, structure, topology and magnetic properties of new coordination polymers based on 5(–Br/–COOH)-substituted nicotinic acid." CrystEngComm 16, no. 24 (2014): 5244–56. http://dx.doi.org/10.1039/c4ce00300d.

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4

Jain, Pooja, James T. Slama, LeRoy A. Perez-Haddock, and Timothy F. Walseth. "Nicotinic Acid Adenine Dinucleotide Phosphate Analogues Containing Substituted Nicotinic Acid: Effect of Modification on Ca2+Release." Journal of Medicinal Chemistry 53, no. 21 (2010): 7599–612. http://dx.doi.org/10.1021/jm1007209.

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5

Nenajdenko, Valentine G., Sergey V. Druzhinin, and Elizabeth S. Balenkova. "Efficient route to 6-CF3-substituted nicotinic acid derivatives." Journal of Fluorine Chemistry 127, no. 7 (2006): 865–73. http://dx.doi.org/10.1016/j.jfluchem.2006.03.007.

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6

Kmoníček, Vojtěch, Martin Valchář, and Zdeněk Polívka. "Some 4-Substituted 1-(3-Pyridylmethyl)piperazines with Antihistamine Activity." Collection of Czechoslovak Chemical Communications 59, no. 10 (1994): 2343–50. http://dx.doi.org/10.1135/cccc19942343.

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Several compounds derived from nicotinic acid were prepared within a more extensive programme aiming at the synthesis of new substances with expected antihistamine and antidepressant activity. Some of these compounds display certain structural resemblance with the antidepressant agent piberaline (EGYT 475, Trelibet®, I) and its analogues. The products were used as intermediates for the synthesis of further compounds and most of them were subjected to pharmacological testing. Substituted nicotinic acid piperazides IIa - IId and IVa - IVe were obtained by reactions of nicotinoyl chloride (prepar

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7

Akishina, E. A., D. V. Kazak, and E. A. Dikusar. "Synthesis of functionally substituted esters of nicotinic and isonicotinic acid." Proceedings of the National Academy of Sciences of Belarus, Chemical Series 56, no. 3 (2020): 301–10. http://dx.doi.org/10.29235/1561-8331-2020-56-3-301-310.

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8

Dikusar, E. A., S. V. Dubovik, N. G. Kozlov, and A. P. Yuvchenko. "Salts of Nicotinic Acid with a Series of Substituted Amines." Chemistry of Natural Compounds 39, no. 6 (2003): 607–8. http://dx.doi.org/10.1023/b:conc.0000018124.22112.7f.

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9

Kazak, D. V., E. A. Dikusar, and S. G. Stepin. "NEW APPROACHES TO SYNTHESIS OF HETEROCYCLIC DERIVATIVES OF PYRIDINE CARBOXYLIC ACIDS, ACRIDINE AND PYRAZOLONE." Vestnik Farmacii 91, no. 1 (2021): 65–85. http://dx.doi.org/10.52540/2074-9457.2021.1.65.

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The urgent task of modern pharmaceutical chemistry is the development of new methods of synthesis, the study of chemical properties, as well as the search for biologically active compounds among derivatives of nicotinic and isonicotinic acids. The review examines synthetic approaches to the production of carboxylic acid esters including nicotinic and isonicotinic acids, gives examples of the biological activity of nicotinic and isonicotinic acids and their derivatives. The methods for the synthesis of azomethines, substituted acridines and pyrazolones are discussed, examples of their biologica

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10

Trabbic, Christopher J., Fan Zhang, Timothy F. Walseth, and James T. Slama. "Nicotinic Acid Adenine Dinucleotide Phosphate Analogues Substituted on the Nicotinic Acid and Adenine Ribosides. Effects on ReceptorMediated Ca2+Release." Journal of Medicinal Chemistry 58, no. 8 (2015): 3593–610. http://dx.doi.org/10.1021/acs.jmedchem.5b00279.

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11

Makhmudova, A. A. "Synthesis and Biological Activity of Sulfamidoand Alkoxycarbonyl-substituted Nicotinic Acid Esters." Russian Journal of Organic Chemistry 56, no. 2 (2020): 246–50. http://dx.doi.org/10.1134/s1070428020020104.

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12

Drmanic, Sasa, Bratislav Jovanovic, Aleksandar Marinkovic, and Milica Misic-Vukovic. "The kinetics of the reactions of 2-substituted nicotinic acids with diazodiphenylmethane in various alcohols." Journal of the Serbian Chemical Society 68, no. 7 (2003): 515–24. http://dx.doi.org/10.2298/jsc0307515d.

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The rate constants of 2-substituted nicotinic acids in reaction with diazodiphenylmethane (DDM) in eight alcohols at 30 ?C have been determined. In order to explain the obtained results through solvent effects, the second order reaction rate constants (k) of the examined acids were correlated using the appropriate solvent parameters by the equation: logk=logk0 af(?) + b?* + cn?H where f(?) is the measure of solvent ability as a dielectric to stabilize the separation of opposite charges in the activated complex, ?* is the measure of solvent ability to stabilize proton in the initial state and n

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13

Drmanic, Sasa, Jasmina Nikolic, Aleksandar Marinkovic, and Bratislav Jovanovic. "The comparative study of linear solvatation energy relationship for the reactivity of pyridine carboxylic acids with diazodiphenylmethane in protic and aprotic solvents." Journal of the Serbian Chemical Society 77, no. 10 (2012): 1311–38. http://dx.doi.org/10.2298/jsc120713078d.

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Protic and aprotic solvent effects on the reactivity of picolinic, nicotinic and isonicotinic acid, as well as of some substituted nicotinic acids with diazodiphenylmethane (DDM) were investigated. In order to explain the kinetic results through solvent effects, the second-order rate constants for the reaction of the examined acids with DDM were correlated using the Kamlet-Taft solvatochromic equation. The correlations of the kinetic data were carried out by means of the multiple linear regression analysis and the solvent effects on the reaction rates were analyzed in terms of the contribution

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14

Drmanic, Sasa, Jasmina Nikolic, and Bratislav Jovanovic. "Effects of solvent and structure on the reactivity of 2-substituted nicotinic acids with diazodiphenylmethane in aprotic solvents." Journal of the Serbian Chemical Society 77, no. 5 (2012): 569–79. http://dx.doi.org/10.2298/jsc120223019d.

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The rate constants for the reactions of diazodiphenylmethane (DDM) with 2-substituted nicotinic acids in nine aprotic solvents at 30?C were determined. The obtained second order rate constants in aprotic solvents were correlated using the Kamlet?Taft solvatochromic equation in the complete form: log k = log k0 + s?* + a??+ b?. The correlations of the kinetic data were realized by means of multiple linear regression analysis. The obtained results were analyzed in terms of the initial and the transition state of the reaction and compared with previously determined kinetic data for nicotinic acid

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15

van Veldhoven, J. P. D., C. C. Blad, C. M. Artsen, et al. "Structure–activity relationships of trans-substituted-propenoic acid derivatives on the nicotinic acid receptor HCA2 (GPR109A)." Bioorganic & Medicinal Chemistry Letters 21, no. 9 (2011): 2736–39. http://dx.doi.org/10.1016/j.bmcl.2010.11.091.

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16

Su, Peiling, James D. Bretz, Gihan S. Gunaratne, Jonathan S. Marchant, Timothy F. Walseth, and James T. Slama. "Chemo-enzymatic synthesis of adenine substituted nicotinic acid adenine dinucleotide phosphate (NAADP) analogs." Bioorganic & Medicinal Chemistry 30 (January 2021): 115901. http://dx.doi.org/10.1016/j.bmc.2020.115901.

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17

Mood, Shilpa, Uma Boda, and Hanmanthu Guguloth. "Synthesis of Substituted 5-Phenyltriazolylquinazolinylamino Nicotinic Acid Esters, Screened their Antibacterial Activity and Molecular Docking Studies." Asian Journal of Chemistry 34, no. 7 (2022): 1799–803. http://dx.doi.org/10.14233/ajchem.2022.23740.

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Quinazolines and imidazoles are substantial attention because of the several varieties of their biological activities. Substituted 5-phenyl-[1,2,4]triazolo[4,3-c]quinazolin-3-yl)amino)nicotinates were synthesized from anthranilamide as starting material by cyclization with benzaldehyde gave 2-phenyl-2,3-dihydroquinazolin-4(1H)-one, then followed by treated with Lawesson’s reagent and hydrazine hydrate to produce hydrazine by replaced the sulfur atom. 5-Phenyl-[1,2,4]triazolo[4,3- c]quinazolin-3-amine obtained by cyclization of hydrazine compound with cyanogen bromide, followed by amidation wit

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18

Akishina, E. A., E. A. Dikusar, G. N. Lysenko, et al. "Catalytic Synthesis of 14-Substituted 14H-Dibenzo[a,j]xanthenes Using Sulfonic Cation Exchanger FIBAN K-1." Russian Journal of General Chemistry 95, no. 6 (2025): 1559–68. https://doi.org/10.1134/s1070363225602182.

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Abstract A new method was developed for obtaining dibenzo[a,j]xanthenylphenols by condensation of natural and synthetic hydroxybenzaldehydes with β-naphthol in boiling trichloroethylene using the sulfonic cation exchanger FIBAN-K1 as a catalyst. The esters were prepared by acylation of dibenzo[a,j]xanthenylphenols with nicotinic, isonicotinic and 1,2-azole-3-carboxylic acid chlorides in methylene chloride in the presence of triethylamine.

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19

Barlin, GB, and W. Tan. "Potential Antimalarials. III. N4-Substituted 7-Bromo-1,5-naphthyridin-4-amines." Australian Journal of Chemistry 38, no. 3 (1985): 459. http://dx.doi.org/10.1071/ch9850459.

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A series of new N4-substituted 7-bromo-1,5-naphthyridin-4-amines has been prepared from nicotinic acid through 3-bromo-8-chloro- 1,5- naphthyridine by nucleophilic replacement of the 8-chloro substituent with appropriate amines. Several of these compounds, namely 7-bromo-N- (4′-diethylamino-1′-methylbutyl)-1,5-naphthy-ridin-4-amine (′5-azabromoquine'), 4-(7′-bromo-1′,5′-naphthyridin-4′-ylamino)-2-(diethylamino-methyl)phenol and 7-bromo-N-(2′-diethylaminoethyl)-1,5- naphthyridin-4-amine showed significant antimalarial acivity. Apparent cures were effected when these test chemicals were injected

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20

Fernàndez, Joan-Carles, Laia Solé-Feu, Dolors Fernández-Forner, Natalia de la Figuera, Pilar Forns, and Fernando Albericio. "Suzuki coupling reaction for the solid-phase preparation of 5-substituted nicotinic acid derivatives." Tetrahedron Letters 46, no. 4 (2005): 581–85. http://dx.doi.org/10.1016/j.tetlet.2004.11.153.

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21

Drmanic, Sasa, Aleksandar Marinkovic, and Bratislav Jovanovic. "Effects of solvent and structure on the reactivity of 6-substituted nicotinic acids with diazodiphenylmethane in aprotic solvents." Journal of the Serbian Chemical Society 74, no. 12 (2009): 1359–70. http://dx.doi.org/10.2298/jsc0912359d.

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The rate constants for the reactions of diazodiphenylmethane (DDM) with 6-substituted nicotinic acids in aprotic solvents at 30?C were determined. The obtained second order rate constants in aprotic solvents, together with literature data for benzoic and nicotinic acids in protic solvents, were used for the calculation of solvent effects, employing the Kamlet-Taft solvatochromic equation (linear solvation energy relationship - LSER) in the form: log k = log k0 + + s?*+ a? + b?. The correlations of the kinetic data were performed by means of multiple linear regression analysis taking appropriat

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22

Ganesh, M. Sai. "Conventional Method for the Synthesis of series of N-phenyl Nicotinamide Analogous Promoted by Iodine." INTERANTIONAL JOURNAL OF SCIENTIFIC RESEARCH IN ENGINEERING AND MANAGEMENT 09, no. 04 (2025): 1–9. https://doi.org/10.55041/ijsrem44863.

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In the present study, the conventional process of bioactive synthesis of N-phenyl Nicotinamide analogous. These derivatives (4) can be synthesized from nicotinoylchloride (2) with the different substituted aromatic amines (3) in the presence of I2/K2CO3 ethanol at reflux. The nicotinoylchloride (2) can be prepared by nicotinic acid with thionyl chloride in the presence of MDC at 400C. All desired compounds were evaluated by 1H-NMR and 13CNMR spectroscopy and LCMS. These new N-phenyl Nicotinamide derivatives were examination pharmacological activities in microbial activity. Some of tested compo

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23

Al-Ghulikah, H. A., A. S. El-Azab, M. S. AL-Saleem, M. S. AL-Towayan, and S. A. Al-Issa. "Green synthesis, characterization, biological evaluation and docking study of some pyrazoline and pyrimidine derivatives." Research Journal of Chemistry and Environment 25, no. 12 (2021): 88–97. http://dx.doi.org/10.25303/2512rjce8897.

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Green and classical techniques have been utilized for preparing of a variety of aryl - substituted pyrazoline and pyrimidine derivatives (2-8). Reactions of chalcones 1 with semicarbazide and thiosemicarbazide, nicotinic acid hydrazide and amino guanidine hydrochloride afforded the corresponding N-substituted pyrazoline derivatives 2-5. Pyrimidine derivatives 6-8 were achieved via reaction of chalcone derivatives 1 with several reagents namely: guanidine nitrate, thiourea and 6-amino-2-thioxo-2,3- dihydropyrimidin-4(1H)-one under conventional and ultrasonic conditions. Ultrasonic method was fo

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24

Ali, Ramadan A., Tetyana Zhelay, Christopher J. Trabbic, et al. "Activity of nicotinic acid substituted nicotinic acid adenine dinucleotide phosphate (NAADP) analogs in a human cell line: Difference in specificity between human and sea urchin NAADP receptors." Cell Calcium 55, no. 2 (2014): 93–103. http://dx.doi.org/10.1016/j.ceca.2013.12.004.

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25

Dyachenko, V. D., O. S. Bityukova, and A. D. Dyachenko. "Synthesis of new functionally substituted 2-oxo(thioxo)nicotinic acid amides and nitriles by SNVin reaction." Russian Journal of Organic Chemistry 47, no. 9 (2011): 1335–40. http://dx.doi.org/10.1134/s1070428011090132.

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26

Abdel-Aziz, Hatem A., Tarek Aboul-Fadl, Abdul-Rahman M. Al-Obaid, Mohamed Ghazzali, Abdullah Al-Dhfyan, and Alessandro Contini. "Design, synthesis and pharmacophoric model building of novel substituted nicotinic acid hydrazones with potential antiproliferative activity." Archives of Pharmacal Research 35, no. 9 (2012): 1543–52. http://dx.doi.org/10.1007/s12272-012-0904-2.

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27

Mohammad, Haneen K., Muhammed H. Alzweiri, Mohammad A. Khanfar, and Yusuf M. Al-Hiari. "6-Substituted nicotinic acid analogues, potent inhibitors of CAIII, used as therapeutic candidates in hyperlipidemia and cancer." Medicinal Chemistry Research 26, no. 7 (2017): 1397–404. http://dx.doi.org/10.1007/s00044-017-1825-x.

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28

Hara, Koji, Edmond I. Eger, Michael J. Laster, and R. Adron Harris. "Nonhalogenated Alkanes Cyclopropane and Butane Affect Neurotransmitter-gated Ion Channel and G-protein–coupled Receptors." Anesthesiology 97, no. 6 (2002): 1512–20. http://dx.doi.org/10.1097/00000542-200212000-00025.

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Background Anesthetic mechanisms of nonhalogenated alkanes cyclopropane and butane are not understood. This study was designed to look at which neurotransmitter receptors are possible targets for these anesthetics. Methods Effects of cyclopropane and butane on eight recombinant receptors expressed in Xenopus oocytes were examined electrophysiologically. To address molecular mechanisms of interaction with glycine and gamma-aminobutyric acid type A (GABA(A)) receptors, cyclopropane was further tested on alpha1(S267C) glycine receptor and alpha2(S270X)beta1 GABA(A) receptors that were mutated to

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29

Kumar, Sukeerthi, Aarti A. Sawant, Rajendra P. Chikhale, Keya Karanjai, and Abraham Thomas. "One-Pot Synthesis of Highly Substituted Nicotinic Acid Derivatives Based on a Formylation Strategy of Enamino Keto Esters." Journal of Organic Chemistry 81, no. 4 (2016): 1645–53. http://dx.doi.org/10.1021/acs.joc.5b02796.

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30

Dyachenko, V. D., O. S. Bityukova, and A. D. Dyachenko. "ChemInform Abstract: Synthesis of New Functionally Substituted 2-Oxo(thioxo)nicotinic Acid Amides and Nitriles by SNVin Reaction." ChemInform 43, no. 18 (2012): no. http://dx.doi.org/10.1002/chin.201218165.

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31

Yu, Jinpeng, Junjie Xie, Yuting Ma та ін. "Single Amino Acid Substitution in Loop1 Switches the Selectivity of α-Conotoxin RegIIA towards the α7 Nicotinic Acetylcholine Receptor". Marine Drugs 22, № 9 (2024): 390. http://dx.doi.org/10.3390/md22090390.

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α-Conotoxins are disulfide-rich peptides obtained from the venom of cone snails, which are considered potential molecular probes and drug leads for nAChR-related disorders. However, low specificity towards different nAChR subtypes restricts the further application of many α-conotoxins. In this work, a series of loop1 amino acid-substituted mutants of α-conotoxin RegIIA were synthesized, whose potency and selectivity were evaluated by an electrophysiological approach. The results showed that loop1 alanine scanning mutants [H5A]RegIIA and [P6A]RegIIA blocked rα7 nAChR with IC50s of 446 nM and 45

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32

Challa, Chandra Sekhar, Naresh Kumar Katari, Varadacharyulu Nallanchakravarthula, Devanna Nayakanti, Ravikumar Kapavarapu, and Manojit Pal. "Sonochemical synthesis of 2-substituted nicotinic acid ethyl ester derivatives: Their in vitro and in silico evaluation against SIRT1." Journal of Molecular Structure 1245 (December 2021): 131069. http://dx.doi.org/10.1016/j.molstruc.2021.131069.

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33

Li, Tianmiao, Han-Shen Tae, Jiazhen Liang та ін. "Rational Design of Potent α-Conotoxin PeIA Analogues with Non-Natural Amino Acids for the Inhibition of Human α9α10 Nicotinic Acetylcholine Receptors". Marine Drugs 22, № 3 (2024): 110. http://dx.doi.org/10.3390/md22030110.

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α-Conotoxins (α-CTxs) are structurally related peptides that antagonize nicotinic acetylcholine receptors (nAChRs), which may serve as new alternatives to opioid-based treatment for pain-related conditions. The non-natural amino acid analogues of α-CTxs have been demonstrated with improved potency compared to the native peptide. In this study, we chemically synthesized Dab/Dap-substituted analogues of α-CTx PeIA and evaluated their activity at heterologously expressed human α9α10 nAChRs. PeIA[S4Dap, S9Dap] had the most potent half-maximal inhibitory concentration (IC50) of 0.93 nM. Molecular d

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34

Robert, Nicolas, Anne-Laure Bonneau, Christophe Hoarau, and Francis Marsais. "Unusual Sterically Controlled Regioselective Lithiation of 3-Bromo-5-(4,4‘-dimethyl)oxazolinylpyridine. Straightforward Access to Highly Substituted Nicotinic Acid Derivatives." Organic Letters 8, no. 26 (2006): 6071–74. http://dx.doi.org/10.1021/ol062556i.

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35

Baldassarri, Cecilia, Gianfabio Giorgioni, Alessandro Piergentili, et al. "Properly Substituted Benzimidazoles as a New Promising Class of Nicotinate Phosphoribosyltransferase (NAPRT) Modulators." Pharmaceuticals 16, no. 2 (2023): 189. http://dx.doi.org/10.3390/ph16020189.

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The prevention of nicotinamide adenine dinucleotide (NAD) biosynthesis is considered an attractive therapeutic approach against cancer, considering that tumor cells are characterized by an increased need for NAD to fuel their reprogrammed metabolism. On the other hand, the decline of NAD is a hallmark of some pathological conditions, including neurodegeneration and metabolic diseases, and boosting NAD biosynthesis has proven to be of therapeutic relevance. Therefore, targeting the enzymes nicotinamide phosphoribosyltransferase (NAMPT) and nicotinate phosphoribosyltransferase (NAPRT), which reg

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36

Jain, Gourav, and Neha Kawathekar. "Design, synthesis, and characterization of some N-(piperidine-4-yl)benzamide derivatives for the treatment of diabetes." INDIAN JOURNAL OF HETEROCYCLIC CHEMISTRY 35, no. 01 (2025): 181. https://doi.org/10.59467/ijhc.2025.35.181.

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N-(Piperidine-4-yl)benzamide (S3I2) is a key pharmacophore for GPR119 agonists, enhancing insulin secretion and incretin release without hypoglycemia. Its design optimizes receptor binding, bioavailability, and glucose homeostasis, making it a promising antidiabetic agent. A series of N-(piperidine-4-yl)benzamide derivatives (S3F1-S3F6) was synthesized via a two-step process. Benzoyl chloride (1) reacted with tert-butyl 4-aminopiperidine-1-carboxylate (2) to form intermediate-1 (S3I1), followed by deprotection with trifluoroacetic acid to yield intermediate-2 (S3I2). The final compounds were o

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37

Ren, Jie, Xiaopeng Zhu, Pan Xu та ін. "d-Amino Acid Substitution of α-Conotoxin RgIA Identifies its Critical Residues and Improves the Enzymatic Stability". Marine Drugs 17, № 3 (2019): 142. http://dx.doi.org/10.3390/md17030142.

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α-Conotoxin RgIA is a selective and potent competitive antagonist of rat α9α10 nicotinic acetylcholine receptors (nAChR), but it is much less potent towards human α9α10 nAChR. Furthermore, RgIA is susceptible to proteolytic degradation due to containing four arginine residues. These disadvantages greatly limit its use for clinical applications. The purpose of this research was to identify critical stereocenters of RgIA and discover more stable analogues, enhancing its bioavailability by using the d-amino acid scan method. The activity of each variant was investigated against rat and human α9α1

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38

Bellone, M., F. Tang, R. Milius, and B. M. Conti-Tronconi. "The main immunogenic region of the nicotinic acetylcholine receptor. Identification of amino acid residues interacting with different antibodies." Journal of Immunology 143, no. 11 (1989): 3568–79. http://dx.doi.org/10.4049/jimmunol.143.11.3568.

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Abstract In myasthenia gravis a highly conserved area of the nicotinic receptor (AcChR) dominates the autoantibody response (main immunogenic region, MIR), and it is formed by residues within the sequence segment 67-76 of the AcChR alpha-subunit. We have studied the binding of eight anti-MIR mAb to synthetic peptides containing the sequence segment 67-76 of the human alpha-subunit, and peptide analogues containing single residue substitutions of this sequence. We used also a peptide where both Asp70 and Asp71 were substituted by glycine residues. The binding of six anti-MIR mAb was strongly in

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39

Redda, Kinfe Ken, Madhavi Gangapuram, Absera W. Haile, and Suresh Eyunni. "Abstract 5742: Synthesis of substituted benzimidazole tetrahydropyridines as anti-breast cancer agents." Cancer Research 85, no. 8_Supplement_1 (2025): 5742. https://doi.org/10.1158/1538-7445.am2025-5742.

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Abstract Breast cancer is the most common type of cancer worldwide. In 2023, the World Health Organization (WHO) reported that 2.3 million women were diagnosed with breast cancer, leading to 670, 000 deaths. Furthermore, the incidence rates of breast cancer have been rising at 3% each year. Overexpression of COX-2 in breast cancer tissues is associated with poor prognosis, including higher tumor grade, increased metastatic potential, and resistance to therapy. Selective COX-2 inhibitors have demonstrated potential in reducing tumor growth in preclinical and some clinical studies. These inhibit

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40

McLane, Kathryn E., Xiadong Wu та Bianca M. Conti-Tronconi. "Amino acid residues forming the interface of a neuronal nicotinic acetylcholine receptor with κ-bungarotoxin: A study using single residue substituted peptide analogs". Biochemical and Biophysical Research Communications 176, № 1 (1991): 11–17. http://dx.doi.org/10.1016/0006-291x(91)90882-8.

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41

Ou, Yu, Min Luo, Yong-Xi Dong, et al. "Permeability of novel 4′-N-substituted (aminomethyl) benzoate-7-substituted nicotinic acid ester derivatives of scutellarein in Caco-2 cells and in an in vitro model of the blood-brain barrier." Medicinal Chemistry Research 25, no. 10 (2016): 2205–13. http://dx.doi.org/10.1007/s00044-016-1659-y.

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McLaughlin, J. T., E. Hawrot, and G. Yellen. "Covalent modification of engineered cysteines in the nicotinic acetylcholine receptor agonist-binding domain inhibits receptor activation." Biochemical Journal 310, no. 3 (1995): 765–69. http://dx.doi.org/10.1042/bj3100765.

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We constructed and characterized a series of nicotinic receptor mutants with a cysteine substituted for one of the amino acid residues in the alpha-subunit between positions 183 and 198. This region of the receptor is known to participate in agonist binding and channel activation. The goal of this ‘cysteine scanning mutagenesis’ is to introduce the reactivity of a free thiol group into functionally important protein domains; modification of the introduced cysteines can then be used to probe the structure and function of the targeted region. Mutants were examined by coexpression with the beta-,

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Xie, Ting, Yuan Qin, Jinyuan Zhao та ін. "Molecular Determinants of Species Specificity of α-Conotoxin TxIB towards Rat and Human α6/α3β4 Nicotinic Acetylcholine Receptors". International Journal of Molecular Sciences 24, № 10 (2023): 8618. http://dx.doi.org/10.3390/ijms24108618.

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Conotoxins are widely distributed and important for studying ligand-gated ion channels. TxIB, a conotoxin consisting of 16 amino acids derived from Conus textile, is a unique selective ligand that blocks rat α6/α3β2β3 nAChR (IC50 = 28 nM) without affecting other rat subtypes. However, when the activity of TxIB against human nAChRs was examined, it was unexpectedly found that TxIB had a significant blocking effect on not only human α6/α3β2β3 nAChR but also human α6/α3β4 nAChR, with an IC50 of 537 nM. To investigate the molecular mechanism of this species specificity and to establish a theoretic

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Chibiryaev, Andrey M., Norbert De Kimpe та Alexey V. Tkachev. "Michael addition of ethyl acetoacetate to α,β-unsaturated oximes in the presence of FeCl3: a novel synthetic route to substituted nicotinic acid derivatives". Tetrahedron Letters 41, № 41 (2000): 8011–13. http://dx.doi.org/10.1016/s0040-4039(00)01391-5.

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Yoshikawa, H., E. H. Lambert, D. R. Walser-Kuntz, Y. Yasukawa, D. J. McCormick, and V. A. Lennon. "A 17-Mer self-peptide of acetylcholine receptor binds to B cell MHC class II, activates helper T cells, and stimulates autoantibody production and electrophysiologic signs of myasthenia gravis." Journal of Immunology 159, no. 3 (1997): 1570–77. http://dx.doi.org/10.4049/jimmunol.159.3.1570.

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Abstract We have identified in an extracellular segment of the alpha1 subunit of nicotinic acetylcholine receptor (AChR) of homologous muscle a 17-residue autoantigen that, without conjugation to a carrier, activates Th lymphocytes and induces production of autoantibodies that cause electrophysiologic signs of experimental autoimmune myasthenia gravis. A panel of overlapping synthetic peptides revealed two T cell epitopes, one encompassed by residues 121-136 and the other by 129-145. Residues 129 (glutamic acid) and 130 (isoleucine) were implicated in a pathogenic B cell epitope. Peptide 129-1

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Chibiryaev, Andrey M., Norbert De Kimpe та Alexey V. Tkachev. "ChemInform Abstract: Michael Addition of Ethyl Acetoacetate to α,β-Unsaturated Oximes in the Presence of FeCl3: A Novel Synthetic Route to Substituted Nicotinic Acid Derivatives." ChemInform 32, № 1 (2001): no. http://dx.doi.org/10.1002/chin.200101151.

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Singh, Sukhdeep, Andreas Schober та G. Alexander Gross. "Direct access to 3-substituted 1,4-oxathiepino[5,6-b]pyridine-5-one through one-pot substitution cyclization reaction of 2-mercapto-3-nicotinic acid with α-bromo ketones". Tetrahedron Letters 55, № 2 (2014): 358–61. http://dx.doi.org/10.1016/j.tetlet.2013.11.030.

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Drmanic, Sasa, Bratislav Jovanovic, and Milica Misic-Vukovic. "The kinetics of the reaction of 6-substituted nicotinic acids and some p-substituted benzoic acids with diazodiphenylmethane in various alcohols." Journal of the Serbian Chemical Society 65, no. 7 (2000): 481–90. http://dx.doi.org/10.2298/jsc0007481d.

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Rate constants have been determined for the reactions of diazodiphenylmethane with a number of 6-substituted nicotinic acids and p-substituted benzoic acids in twelve alcohols. Acomparative study was used to evaluate and compare the Hammett r values and solvent effects. Multiple correlations of the log k values for the reactions of 6-substituted nicotinic acids and p-substituted benzoic acids in 12 alcohols with groups of suitable solvent parameters are very successful. The transmission of electronic effects through the pyridine ring system in compared with that in benzene.

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Singh, Sukhdeep, Andreas Schober та G. Alexander Gross. "ChemInform Abstract: Direct Access to 3-Substituted 1,4-Oxathiepino[5,6-b]pyridine-5-one Through One-Pot Substitution Cyclization Reaction of 2-Mercapto-3-nicotinic Acid with α-Bromo Ketones." ChemInform 45, № 25 (2014): no. http://dx.doi.org/10.1002/chin.201425191.

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Liu, Qing-Song, та Darwin K. Berg. "Extracellular Calcium Regulates Responses of Both α3- and α7-Containing Nicotinic Receptors on Chick Ciliary Ganglion Neurons". Journal of Neurophysiology 82, № 3 (1999): 1124–32. http://dx.doi.org/10.1152/jn.1999.82.3.1124.

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Neuronal nicotinic receptors are generally both permeable to calcium and potentiated by it. We have examined acute calcium regulation of both native α7-containing and the less abundant α3-containing nicotinic receptors on chick ciliary ganglion neurons. Most of the receptors are concentrated on somatic spines tightly overlaid in situ by a large presynaptic calyx. Whole cell patch-clamp recording from dissociated neurons using perforated patch-clamp techniques indicates that the rapidly desensitizing nicotinic response of α7-containing receptors achieves maximum amplitude in 2 mM calcium; both

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