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Journal articles on the topic 'Amino derivative'

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Published: 5 June 2025

Last updated: 1 August 2025

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1

Easton, CJ, and SC Peters. "Synthesis of Novel Cross-Linked Amino Acid Derivatives." Australian Journal of Chemistry 43, no. 1 (1990): 87. http://dx.doi.org/10.1071/ch9900087.

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Reactions of the derivatives of cysteine (6), serine (7) and lysine (8a), with the bromide (1), afforded the corresponding cross-linked amino acid derivatives (11), (12) and (13). Of the linked species (11)-(13), the cysteine derivative (11) was found to be the most stable under a variety of conditions. A mixture of the cross-linked serine derivative (12) and the cysteine derivative (6) in chloroform containing triethylamine reacted to give the cross-linked cysteine derivative (11) and the serine derivative (7). Similarly, a mixture of (13) and (6) in chloroform reacted to give (11).

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2

Burgess, VA, та CJ Easton. "Reaction of N-Benzoyl-2-bromoglycine Methyl Ester With Deprotonated Nitroalkanes: Synthesis of β-Nitro and α,β-Dehydro Amino Acid Derivatives". Australian Journal of Chemistry 41, № 7 (1988): 1063. http://dx.doi.org/10.1071/ch9881063.

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N-Benzoyl-2-bromoglycine methyl ester (1) reacted with the alkyl nitronates (2a-e) to give the corresponding β-nitro amino acid derivatives (4a-e). Elimination reactions of (4a-d) afforded the α,β-dehydro amino acid derivatives (5a-d). Treatment of the β- nitrovaline derivative (4b) with tributyltin hydride gave the valine derivative (8). Reduction of the β- nitroalanine derivative (4a) gave the β- aminoalanine derivative (9), characterized by hydrolysis to 2,3- diaminopropionic acid hydrochloride.

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3

K. Abdullah, Ebtihal. "Synthesis of New (1-alkylamino-4-phenyldithio-2-bntanol amine) andderivatives." Tikrit Journal of Pharmaceutical Sciences 6, no. 1 (2023): 78–82. http://dx.doi.org/10.25130/tjphs.2010.6.1.12.78.82.

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Anew series of(1-alkylamino-4-phenyldithio-2-bntanol amine) and derivatives,containing two functional groups (pheny ring and NCS2) here been prepared from a reaction by 3steps :- 1-In the first step the preparation of n-phenyl dithio carbamate (A) and derivatives from a reaction between Aniline and carbon disulfide in basic medium. 2-Then , preparation N-3-chloro-2-hydroxy propyl amine tt 3 )) and derivativel from reaction between N-3-chloro-2-hydroxy propylamine and epichloro hydrine in methanolic a queous.3-In three step :-preparation 1-Alkyi amino -4-phenyl dithio-2-butanol amine ( I-IV) fr

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4

Šála, Michal, Hubert Hřebabecký, Milena Masojídková, and Antonín Holý. "Synthesis of Novel Racemic Conformationally Locked Carbocyclic Nucleosides Derived from 7-Substituted Bicyclo[2.2.1]hept-5-ene-2,2-dimethanols." Collection of Czechoslovak Chemical Communications 71, no. 5 (2006): 635–49. http://dx.doi.org/10.1135/cccc20060635.

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(1R*,4R*,7S*)-7-Aminobicyclo[2.2.1]hept-5-ene-2,2-dimethanol (15) was prepared in four easy steps from bicyclo[2.2.1]hept-5-ene-2,2-dimethanol (10). Reaction of amine 15 with ethyl N-((E)-3-ethoxymethacryloyl)carbamate afforded thymine derivatives 17a. The amine 15 was used to construct 6-chloro-9H-purine derivative 19a, 2-amino-6-chloro-9H-purine derivative 22a. Ammonolysis of 19a led to the adenine derivative 20a. Treatment of 22a with trifluoroacetic acid afforded guanine nucleoside 23a. (1R*,4R*,7S*)-7-[6-(Cyclopropylamino)-9H-purin-9-yl]bicyclo[2.2.1]hept-5-ene-2,2-dimethanol (21a) and (1

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5

Konečný, Václav, Jozefína Žúžiová, Štefan Kováč, and Tibor Liptaj. "Synthesis of Novel 4-Amino-5-(disubstituted amino)-2-phenyl-2H-pyridazin-3-ones." Collection of Czechoslovak Chemical Communications 62, no. 5 (1997): 800–808. http://dx.doi.org/10.1135/cccc19970800.

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Substituted 4-amino-2-phenyl-2H-pyridazin-3-ones 5a-5j have been prepared from 4-amino-5-chloro-2-phenyl-2H-pyridazin-3-one 1 which on reactions with acetyl chloride or acetic anhydride gives 4-acetylamino derivative 2 or 4-diacetylamino derivative 3, respectively. Derivatives 2 and 3 with dialkylamines and cyclic amines yielded appropriate 4-acetylamino-5-(disubstituted amino)-2-phenyl-2H-pyridazin-3-ones 4a-4j. Subsequent alkaline hydrolysis of the acetylamino derivatives 4a-4j let to the title compounds 5a-5j, which were screened for pesticidal activity, but none of them reached activity of

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6

Veeranki, Krishna Chaitanya, Jalapathi Pochampally, and Ravi Chander Maroju. "Synthesis of Novel Biaryl Fused Thiazolo[3,2-b][1,2,4]triazol-2-amines from Thiazole Amine Involving Suzuki Coupling Reaction under Microwave Irradiation." Asian Journal of Chemistry 35, no. 2 (2023): 431–34. http://dx.doi.org/10.14233/ajchem.2023.26998.

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Novel series of fused heterocycles in which amino triazole fused to biphenyl thiazole were synthesized in a multistep reaction starting from 2-aminothiazole. The amino compound with ethoxy carbonyl isothiocyanate afforded the ethyl carbamate thiomide derivative of thiazole, which further underwent intramolecular cyclization with hydroxyl amine hydrochloride in presence of DIPEA to furnish the fused thiazolotriazole amine. Haloaryl group in the fused heterocycle under Suzuki coupling condition afforded biphenyl derivatives of fused thiazolotriazole amines. All the synthesized compounds were con

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7

Harnden, MR, and DT Hurst. "The Chemistry of Pyrimidinethiols. III. The Synthesis of Some Substituted Pyrimidinthiols and Some Thiazolo[5,4-D]pyrimidines." Australian Journal of Chemistry 43, no. 1 (1990): 55. http://dx.doi.org/10.1071/ch9900055.

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The preparation of a number of pyrimidinethiols and (substituted) thiopyrimidines has been carried out. The reaction of 5-acetylamino-2-aminopyrimidine-4,6-diol with phosphorus penta -sulfide in pyridine gave 5-amino-2-methylthiazolo[5,4-d]pyrimidine-7-thiol which was used to prepare several additional novel pyrimidine derivatives. Hydrolysis of the 4-carboxymethylthio derivative by using 5M hydrochloric acid gave 2,5-diamino-6-mercaptopyrimidin-4-ol hy -drochloride whilst hydrolysis of 2-methyl-7-methylthiothiazolo[5,4-d]pyrimidin-5-amine gave the corresponding 4-hydroxy derivative. Several 4

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8

Julianto, T. S., F. J. Rachmawaty, H. A. Tamhid, and B. S. Putri. "THE POTENTIAL ANTIMALARIAL DRUG OF ARYL AMINO ALCOHOL DERIVATIVES FROM EUGENOL: SYNTHESIS, in-vitro AND in-silico ANALYSIS OF BIOACTIVITY." RASAYAN Journal of Chemistry 16, no. 03 (2023): 1425–34. http://dx.doi.org/10.31788/rjc.2023.1636940.

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Malaria is a significant cause of death in numerous countries, and the discovery of effective drugs is crucial. In this research, a new method was employed to synthesize a derivative of aryl amino alcohol using eugenol. Initially, an epoxide compound called 2-methoxy-4-(oxiran-2-ylmethyl) phenol was synthesized from eugenol by reacting it with peroxyacetic acid in dichloromethane. Subsequently, the epoxide compound was subjected to a reaction with various amine compounds, including aniline, naphthylamine, and diphenylamine for 10 minutes under 100 W microwave conditions, resulting in the produ

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9

Khalifa, Nagy M., Ahmed M. Naglah, Mohamed A. Al-Omara, and Abd El-Galil E. Amr. "Synthesis and Reactions of New Chiral Linear Dipeptide Candidates Using Nalidixic Acid as Starting Material." Zeitschrift für Naturforschung B 69, no. 6 (2014): 728–36. http://dx.doi.org/10.5560/znb.2014-4031.

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A series of dipeptide heterocyclic derivatives 4-15 were synthesized using methyl 2-{[(1-ethyl- 7-methyl-4-oxo-1,4-dihydro-1,8-naphthyridin-3-yl)carbonyl]amino}-3-ethylbutanoate (3) as starting material. Treatment of 3 with L-phenylalanine methyl ester hydrochloride afforded the corresponding dipeptide methyl ester derivative 4, which was treated with hydrazine hydrate to afford the dipeptide acid hydrazide 5. Compound 5 was coupled with aldehyde and acetophenone derivatives to afford the corresponding Schiff bases 6a-f. The hydrazide derivative 5 was reacted with ethyl acetoacetate or acetone

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10

Saadi, Lina, and Shaimaa Adnan. "Synthesis, Antibacterial and Antioxidant Evaluation of 2-Substituted-4-arylidene-5(4<i>H</i>)-oxazolone Derivatives." Indonesian Journal of Chemistry 23, no. 5 (2023): 1463. http://dx.doi.org/10.22146/ijc.83052.

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In this research, the synthesis of new substituted oxazolone derivatives is described via Erlenmeyer synthesis of N-acyl amino acid. Firstly, the azo derivative 1 was prepared by coupling the diazonium salt of 3-amino-4-methoxybenzoic acid with 4,5-dichloroimidazole in sodium hydroxide solution. Benzoyl chloride derivative 2, the key intermediate of the synthesis, was synthesized by the acylation of azo-carboxylic acid derivative 1 with thionyl chloride. The resulting acyl chloride derivative reacted with glycine in a basic catalyst to form a hippuric acid derivative 3. After that, oxazolone d

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11

Janeba, Zlatko, Antonín Holý, and Milena Masojídková. "Transformation of 8-[(2-Hydroxyalkyl)sulfanyl]adenines to 6-Amino-7H-purin-8(9H)-one Derivatives." Collection of Czechoslovak Chemical Communications 66, no. 9 (2001): 1393–406. http://dx.doi.org/10.1135/cccc20011393.

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Alkylation of 6-amino-7H-purin-8(9H)-thione (8-sulfanyladenine, 1) with one equivalent of (R)-[(trityloxy)methyl]oxirane gave its S-alkyl derivative 2, which was converted to the 6-amino-7H-purin-8(9H)-one (3), while alkylation of 1 with two equivalents of (S)-[(trityloxy)methyl]oxirane afforded a mixture of N3,S-dialkylated product 4a, N9-monoalkyl and N7,N9-dialkyl derivatives of 6-amino-7H-purin-8(9H)-one, 5a and 6a, respectively. This approach can be used for rapid and easy transformation of 8-[(2-hydroxyalkyl)sulfanyl]adenines to the derivatives of 6-amino-7H-purin-8(9H)-one (8-hydroxyade

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12

Konno, Hiroyuki, Yasuhiro Sasaki, Ryota Sato, XiuMei Zhu, Yusuke Otsuki та Megumi Ikoma. "Synthesis of β-Hydroxytyrosine, A Component of Burkholdines". Natural Product Communications 11, № 2 (2016): 1934578X1601100. http://dx.doi.org/10.1177/1934578x1601100221.

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The preparation of four stereoisomers of β-hydroxytyrosine containing burkholdines is described. Enantio-pure syn β-hydroxytyrosine was synthesized using Sharpless aminohydroxylation. To obtain anti β-hydroxytyrosine, the cinnamate derivative was oxidized to give the optical active diol derivative by the AD-mix and subsequently, the α-hydroxy group was converted to amine. Deprotection of the acid-sensitive β-hydroxytyrosine derivatives was successively accomplished by brief immersion in 4N HCl/dioxane. All prepared stereoisomers of β-hydroxytyrosine were available for solid and solution phase

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13

Garg, Ajay Kumar, Ranjan Kumar Singh, Vaibhav Saxena, Saurabh Kr Sinha, and Sanjay Rao. "Synthesis, Characterization, and Anti-inflammatory activity of Some Novel Oxazole Derivatives." Journal of Drug Delivery and Therapeutics 13, no. 1 (2023): 26–28. http://dx.doi.org/10.22270/jddt.v13i1.5719.

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A series of novel oxazole derivatives (A, A1, A2) were synthesized starting from acetone and urea. The compound (A) was obtained by heating it with acetophenone and urea in iodine. Compound (A) on treatment with 4-amino benzaldehyde (Z)-N-(4-amino benzylidine)-4-((E)-Penta-2, 4-diene-2) oxazole-2-amine afforded (A1). Acylation of compound (A) with 4-amino benzoyl chloride to obtain the corresponding N-(4 phenyl oxazole-2- yl)- benzamide (A2). The structures of compounds have been established employing FTIR and 1H-NMR spectral analysis. All oxazole derivatives were evaluated for anti-inflammato

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14

Mohssen Khudair, Marwa. "An in Silico Molecular Docking and in Vitro Investigation of the Bioactivity of Amoxicillin Derivatives Against Staphylococcus Aureus and Escherichia Coli." Al-Nahrain Journal of Science 28, no. 1 (2025): 29–39. https://doi.org/10.22401/anjs.28.1.05.

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Antimicrobial resistance happens when germs like bacteria and fungi develop the ability to defeat the drugs designed to kill them. We developed an amoxicillin drug via modification with different aldehyde compounds. Evaluation of the bioactivity of synthesized derivatives against Staphylococcus aureus and Escherichia coli. The derivatives A1–A4exhibited more excellent biological activity than the parent drug, and derivative A2 had the most significant biological activity by higher zone inhibition. Derivative 2 tested as against prostate cancer PC3,and the IC50 rates of derivative A2 give (5.75

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15

Choe, Deokyeong, Soo Min Song, Chul Soo Shin, et al. "Production and Characterization of Anti-Inflammatory Monascus Pigment Derivatives." Foods 9, no. 7 (2020): 858. http://dx.doi.org/10.3390/foods9070858.

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The prevention and treatment of chronic inflammation using food-derived compounds are desirable from the perspectives of marketing and safety. Monascus pigments, widely used as food additives, can be used as a chronic inflammation treatment. Orange Monascus pigments were produced by submerged fermentation in a 5 L bioreactor, and multiple orange Monascus pigment derivatives with anti-inflammatory activities were synthesized using aminophilic reaction. A total of 41 types of pigment derivatives were produced by incorporating amines and amino acids into the orange pigments. One derivative candid

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16

Wzorek, Alicja, Jianlin Han, Nataliya V. Lyutenko та ін. "Enzymatic approaches for preparation of α-aminophosphonic acids and fluorine-containing β-amino acids". Ukrainica Bioorganica Acta 19, № 1 (2024): 21–29. https://doi.org/10.15407/bioorganica2024.01.021.

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In this perspective review article, we discuss application of penicillin acylase for biocatalytic resolution of tailor-made amino acids, in particular α-aminophosphonic acids and fluorine-containing β-amino acids. The method includes preparation of the corresponding N-phenylacetyl derivatives followed by the enzyme-catalyzed hydrolysis of one of the enantiomers. The free amino acid and the remaining N-phenylacetyl derivative are separated simply by cation-exchange chromatography or extraction. The final step is a chemical hydrolysis of the enzymatically unreactive N-phenylacetyl derivative. Th

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17

Pervaiz, Muhammad, Ikram Ahmad, Zohaib Saeed, et al. "Amalgamation and Scrutinizing of Leucine Derivatives Schiff Bases Complexes as Antimicrobial Agent." Combinatorial Chemistry & High Throughput Screening 25, no. 7 (2022): 1167–80. http://dx.doi.org/10.2174/1386207325666210927092623.

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: The enhanced applications of Schiff bases metal complexes of amino acid derivatives have captured the attention of researchers for the synthesis of leucine derivatives of Schiff bases metal complexes. Amino acids are considered to be essential part of food supplements as well as derivatives of Schiff bases in coordination chemistry due to their donor ability. The leucine derivatives Schiff bases ligand have been synthesized by condensation reaction between amine of leucine with aldehyde or ketone bearing molecules attached with them. These complexes were characterized by different spectrosco

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18

Duggan, BM, RL Laslett, and JFK Wilshire. "Studies in Thiohydantoin Chemistry. I. Some Aspects of the Schlack-Kumpf Reaction." Australian Journal of Chemistry 49, no. 5 (1996): 541. http://dx.doi.org/10.1071/ch9960541.

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An investigation has been carried out into the Schlack-Kumpf reaction, i.e., the reaction of amino acids with a mixture of acetic anhydride, acetic acid and sodium thiocyanate (occasionally ammonium thiocyanate was used). Particular emphasis was placed on the reactions with amino acids containing sensitive or functional side chains, i.e., serine, threonine , arginine , proline , lysine, histidine , cysteine , and aspartic and glutamic acids. The reaction of serine, and of certain of its O- and N-substituted derivatives, takes an unusual course to give an acetylated thiohydantoin derivative of

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19

Lin, Lizhen, Yuqing Zhao, Peng Wang, et al. "Amino Acid Derivatives of Ginsenoside AD-2 Induce HepG2 Cell Apoptosis by Affecting the Cytoskeleton." Molecules 28, no. 21 (2023): 7400. http://dx.doi.org/10.3390/molecules28217400.

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AD-2 (20(R)-dammarane-3β, 12β, 20, 25-tetrol, 25-OH-PPD) was structurally modified to introduce additional amino groups, which can better exert its anti-tumor effects in MCF-7, A549, LoVo, HCT-116, HT -29, and U-87 cell lines. We investigated the cellular activity of 15 different AD-2 amino acid derivatives on HepG2 cells and the possible mechanism of action of the superior derivative 6b. An MTT assay was used to detect the cytotoxicity of the derivatives. Western blotting was used to study the signaling pathways. Flow cytometry was used to detect cell apoptosis and ghost pen peptide staining

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20

Mullersman, Jerald E., та James F. Preston III. "Conjugation of N-acylated amino sugars to protein by reductive alkylation using sodium cyanoborohydride: application to an azo derivative of α-amanitin". Biochemistry and Cell Biology 69, № 7 (1991): 418–27. http://dx.doi.org/10.1139/o91-064.

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Reductive alkylation mediated by cyanoborohydride is an attractive approach to the conjugation of small molecules, such as drugs, to proteins. This reaction is specific for protein amino groups and can be conducted under mild conditions with little risk of protein polymerization. However, the lability of the aldehyde function that is needed in such reactions presents a difficulty. We have investigated the use of derivatives of D-galactosamine and D-glucosamine in reductive alkylation, since these sugars contain aldehyde groups that are inherently protected and that may be readily linked to oth

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21

Shukkur, A. Hamed, Athraa Thaker, Bilal Majid Rudaini, Hasanain Salah Naeem, Muntaz Abu Bakar, and Siti Aishah Hasbullah. "Synthesis and Characterization of Hexahydropyrimidines and Their New Derivatives." Sains Malaysiana 53, no. 4 (2024): 839–50. http://dx.doi.org/10.17576/jsm-2024-5304-09.

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Three new hexahydropyrimidine derivatives 1a – 1c were successfully synthesized using the Mannich-type reaction. Furthermore, the synthesis of three amino bases 2a – 2c was achieved through the reduction reaction of pyrimidine compounds using hydrazine, followed by the substitution reaction of nitro groups at diverse positions. Subsequently, one of the synthesized amino base derivatives 2c underwent conversion into seven Schiff bases 3a – 3g via a condensation reaction involving the aforementioned amino base derivative and a selection of benzaldehyde derivatives. Four amide compounds 4a – 4d h

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22

Cumpstey, Ian, Jens Frigell, Elias Pershagen, et al. "Amine-linked diglycosides: Synthesis facilitated by the enhanced reactivity of allylic electrophiles, and glycosidase inhibition assays." Beilstein Journal of Organic Chemistry 7 (August 16, 2011): 1115–23. http://dx.doi.org/10.3762/bjoc.7.128.

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Diglycose derivatives, consisting of two monosaccharides linked at non-anomeric positions by a bridging nitrogen atom, have been synthesised. Conversion of one of the precursor monosaccharide coupling components into an unsaturated derivative enhances its electrophilicity at the allylic position, facilitating coupling reactions. Mitsunobu coupling between nosylamides and 2,3-unsaturated-4-alcohols gave the 4-amino-pseudodisaccharides with inversion of configuration as single regio- and diastereoisomers. A palladium-catalysed coupling between an amine and a 2,3-unsaturated 4-trichloroacetimidat

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23

Osolоdchenko, T., I. Andreieva, N. Zavada, I. Ryabova, and A. Volyansky. "Spectrum and levels of antimicrobial activity of modified amino acids." Annals of Mechnikov Institute, no. 4 (December 12, 2019): 62–65. https://doi.org/10.5281/zenodo.3572576.

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<strong>Introduction</strong><strong>. </strong>Antimicrobial resistance  threatens the effective prevention and treatment of an ever-increasing range of infections and  is rising to dangerously high levels in all parts of the world. The search among the natural and synthetic biologically active compounds that influence the development of resistance in against antibacterial agents in the clinically relevant strains acquires increasingly greater significance. <strong>Material & methods</strong><strong>. </strong>Were studied the spectrum and levels of antimicrobial activity of 10

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24

Dabaeva, V. V., M. R. Bagdasaryan, E. G. Paronikyan, et al. "Synthesis of new condensed pyrano[4,3-<i>b</i>]pyridines based on ethyl-3-aminopyrano[4,3-<i>b</i>]thieno[3,2-<i>e</i>]pyridine2-carboxylate derivative." Журнал органической химии 59, no. 1 (2023): 119–27. http://dx.doi.org/10.31857/s051474922301010x.

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Methods for the synthesis of new fused pyrano[4,3- b ]pyridine derivatives based on the ethyl-3-amino-pyrano[4,3- b ]thieno[3,2- e ]pyridine-2-carboxylate derivative have been developed. The interaction reactions of the condensed 3-(phenoxycarbonyl)-amino derivative with primary and secondary amines have been studied. It has been established that in the case of primary amines, the reaction is accompanied by cyclization with the formation of fused pyrimidines. However, when secondary amines are used, the structure of the final product depends on the reaction conditions. The antibacterial proper

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25

Phutdhawong, Weerachai, Siwaporn Inpang, Thongchai Taechowisan, and Waya S. Phutdhawong. "Synthesis and Biological Activity Studies of Methyl-5-(Hydroxymethyl)-2-Furan Carboxylate and Derivatives." Oriental Journal of Chemistry 35, no. 3 (2019): 080–1085. http://dx.doi.org/10.13005/ojc/350322.

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Methyl-5-(hydroxymethyl)-2-furan carboxylate and derivatives were prepared from furfuryl alcohol and their biological activities were studied for cytotoxicity against cancer cell lines HeLa, HepG2 and Vero, and Gram (+) and Gram (-) bacteria. The amine derivative, (5-(((2-(1H-indol-3-yl)ethyl)amino)methyl) furan-2-yl)methyl acetate, was found to have the most potent biological activity with IC50 62.37 µg/mL against the HeLa cell line and MIC 250 µg/mL against the photogenic bacteria.

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26

Saeed, Sadaf, Saba Munawar, Sajjad Ahmad, et al. "Recent Trends in the Petasis Reaction: A Review of Novel Catalytic Synthetic Approaches with Applications of the Petasis Reaction." Molecules 28, no. 24 (2023): 8032. http://dx.doi.org/10.3390/molecules28248032.

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The Petasis reaction, also called the Petasis Borono–Mannich reaction, is a multicomponent reaction that couples a carbonyl derivative, an amine and boronic acids to yield substituted amines. The reaction proceeds efficiently in the presence or absence of a specific catalyst and solvent. By employing this reaction, a diverse range of chiral derivatives can easily be obtained, including α-amino acids. A broad substrate scope, high yields, distinct functional group tolerance and the availability of diverse catalytic systems constitute key features of this reaction. In this review article, attent

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27

Smrčková, Svatava, Kristina Juricová, and Viktor Prutianov. "Study of Amino-Imino Tautomerism in Derivatives of 2-, 4- and 6-Aminonicotinic Acid." Collection of Czechoslovak Chemical Communications 59, no. 9 (1994): 2057–68. http://dx.doi.org/10.1135/cccc19942057.

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13C NMR spectra of p-nitrobenzoyl 2-, 4-, and 6-aminopyridine-3-carboxylates, their hydrochlorides, trifluoroacetates and 1-benzyl derivatives were studied. As found from the chemical shifts of pyridine carbon atoms C-2, C-4 and C-6, the free bases exist in the amino form whereas hydrochlorides and 1-substituted pyridinium derivatives in the imino form. Trifluoroacetates of the 2- and 6-amino derivatives have structure similar to that of amidiniumcarboxylates (parallel hydrogen bonds and partially ionic character) whereas trifluoroacetate of the 4-amino derivative is structurally close to the

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28

Müller, P., S. Huck, H. Köppel, H. Pritzkow, and W. Siebert. "Synthese und Strukturen von 9,10-Dihydro-9,10-diboraanthracen-Derivaten / Synthesis and Structures of 9,10-Dihydro-9,10-diboraanthracene Derivatives." Zeitschrift für Naturforschung B 50, no. 10 (1995): 1476–84. http://dx.doi.org/10.1515/znb-1995-1008.

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A series of alkyl and amino derivatives of the tricyclic organoborane system 9,10-dihydro- 9.10-diboraanthracene was synthesized and examined. The reactions of 9,10-dichlor-9,10-dihydro- 9,10-diboraanthracene ( la ) with suitable reagents yield the corresponding alkyl, aryl or amino derivatives 1c-h , respectively. The compounds have been characterized by 1H, 13C and 11B NMR spectroscopy. X-ray structure analyses have shown that the amino derivatives have bent structures, while the H2N compound 1h is planar. Calculations were carried out to study the reasons for the deformation of some of the

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29

Patil, Pravin, and Frederick Luzzio. "Unnatural Amino Acid Derivatives through Click Chemistry: Synthesis of Triazolylalanine Analogues." Synlett 28, no. 14 (2017): 1729–32. http://dx.doi.org/10.1055/s-0036-1588510.

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A novel tert-butyl 2-(1-oxoisoindolin-2-yl)acetate derivative is selectively alkylated with propargyl bromide in the presence of lithium hexamethyldisilazide. After removal of the tert-butyl protecting group, the resulting N-isoindolinyl (ethynylalanine) derivative is reacted with a series of azides under ‘click conditions’. The click reactions afford an array of N-isoindolinyl- 1,2,3-triazolylalanine derivatives as the free carboxylic acids. Following esterification, the N-isoindolinone protecting group is then transformed into the more easily removable phthaloyl group by selective oxidation

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30

Easton, CJ, та SC Peters. "Reactions of α-Substituted Glycine Derivatives With Stannanes in the Presence of Disulfides". Australian Journal of Chemistry 47, № 5 (1994): 859. http://dx.doi.org/10.1071/ch9940859.

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Reactions of α- bromo -, α- benzoyloxy - and α- methoxy -substituted glycine derivatives with stannanes afforded the corresponding α- centred glycinyl radical, which reacted with di -t-butyl disulfide and diphenyl disulfide by homolytic substitution to give the corresponding α-t- butylthio- and α-phenylthio -substituted glycine derivatives, respectively. The glycinyl radical reacted with dibenzyl disulfide by displacement of benzyl radical to give a mixed disulfide, which was subsequently reduced to the corresponding α- benzylthio-substituted glycine derivative. In related reactions of a cysti

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31

B., DINDA, BANERJEE J. та GUHA S. "Triterpenes from Ajugα mαcrospermα Wall." Journal of Indian Chemical Society Vol. 74, May 1997 (1997): 424. https://doi.org/10.5281/zenodo.5885957.

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Department of Chemistry, Tripura University, Agartala-799 004 <em>Manuscript received 6 December 1994, revised 29 November 1995, accepted 19 January 1996</em> Triterpenes from Ajugα mαcrospermα Wall.   

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32

Marinov, Marin. "SYNTHESIS OF AMINO DERIVATIVES OF MONOTHIO- AND DITHIO- ANALOGUES OF CYCLOHEXANESPIRO-5-HYDANTOIN." Journal scientific and applied research 2, no. 1 (2012): 66–73. http://dx.doi.org/10.46687/jsar.v2i1.45.

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This article presents methods for synthesis of 3-amino derivatives of cyclohexanespiro-5-(2-thiohydantoin) and cyclohexanespiro-5-(2,4-dithiohydantoin). It was found out that the treatment of cyclohexanespiro-5-(2-thiohydantoin) with hydrazine hydrate under different reaction conditions led to obtaining of 3-amino derivative and 2-hydrazone of the initial compound. As a result of thionation of 3-aminocyclohexanespiro-5-hydantoin with P4S10 or Lawesson’s reagent, the corresponding dithio-analogue was synthesized. The structures of the products obtained were verified by IR, 1H NMR, 13C NMR and m

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33

Stanetty, Christian, Andrea Wolkerstorfer, Hassan Amer, et al. "Synthesis and antiviral activities of spacer-linked 1-thioglucuronide analogues of glycyrrhizin." Beilstein Journal of Organic Chemistry 8 (May 8, 2012): 705–11. http://dx.doi.org/10.3762/bjoc.8.79.

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The influenza virus infection remains a significant threat to public health and the increase of antiviral resistance to available drugs generates an urgent need for new antiviral compounds. Starting from the natural, antivirally active compound glycyrrhizin, spacer-bridged derivatives were generated with improved antiviral activity against the influenza A virus infection. Simplified analogues of the triterpene saponin glycyrrhizin containing 1-thio-β-D-glucuronic acid residues have been prepared in good yields by alkylation of 3-amino and 3-thio derivatives of glycyrrhetinic acid with a 2-iodo

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34

Lu, Gang, and Yue Huang. "Study on the Polyaspartic Acid Derivative Synthesis and the Scale Inhibition Performance of Calcium Carbonate." Advanced Materials Research 610-613 (December 2012): 1513–17. http://dx.doi.org/10.4028/www.scientific.net/amr.610-613.1513.

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Intermediate vector polysuccinimide (PSI) was prepared by polymerization of malefic acid and ammonia at 180°Cin this article. Hydrophilic polyaspartic acid (PASP) derivative was prepared from amino-sulfonic and PSI; Lipophilic PASP derivative was prepared from PSI and diisopropylamine. Their scale inhibition rates of calcium carbonate were evaluated by static scale experiments. The inhibition rate of calcium carbonate was 90.2% when n(amino-sulfonic): n(PSI) =1:14 and the dosage of pharmaceutical was 12mg / L. The inhibition rate of calcium carbonate was 87.6% when n(diisopropylamine):n(PSI)=1

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35

Maryna, Samilyk, Korniienko Daria, Bolgova Natalia, Sokolenko Viktoriia, and Boqomol Nadija. "Using derivative products from processing wild berries to enrich pressed sugar." Eastern-European Journal of Enterprise Technologies 3, no. 11 (117) (2022): 39–44. https://doi.org/10.15587/1729-4061.2022.258127.

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This paper reports a study addressing the issue of enriching pressed sugar in order to improve its biological value. As additives to sugar, the use of derivative products of processing wild berries Hippophaerhamnoides L., Viburnumopulus, Sambucusnigra, Sorbusaucuparia is suggested. The technology of processing wild berries includes their preliminary freezing, partial dehydration by osmotic dehydration, and subsequent drying. The resulting osmotic solution is proposed to be used to moisten sugar before its pressing and drying. An important practical aspect of this technological advancement is t

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36

Harnden, MR, and DT Hurst. "The Synthesis and Chlorination of Some Pyrimidin-4-ols Having 5-Nitrogen Functionality." Australian Journal of Chemistry 43, no. 1 (1990): 47. http://dx.doi.org/10.1071/ch9900047.

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Syntheses of a number of pyrimidin-4-ols having 5-nitrogen functionality are described. Phosphorus oxychloride/diethylaniline chlorination of 6-amino-2-methylthio-5-nitropyrimidin-4-ol gave the corresponding 6-chloro derivative. However, 2-amino-6-methylthio-5-nitropyrimidin-4-ol failed to yield a 4-chloro derivative under the same conditions. Similar chlorination of 2,5-diaminopyrimidine-4,6-diol gave a poor yield of the 4,6-dichloro product but under these conditions 2-amino-5-benzoylaminopyrimidine-4,6-diol* gave 7-chloro-2-phenyloxazolo[5,4-d]pyrimidin-5-amine. 5-Acetylamino-2-methylthiopy

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37

Rodríguez, Ricaurte, Felipe Quiroga-Suavita, and Mónica Yadira Dotor Robayo. "Unexpected Formation of 4-[(1-Carbamoyl-3-oxo-1,3-dihydro-2-benzofuran-1-yl)amino]benzoic Acid from 4-[(3-Amino-1-oxo-1H-2-benzopyran-4-yl)amino]benzoic Acid." Molbank 2022, no. 3 (2022): M1407. http://dx.doi.org/10.3390/m1407.

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With the aim of obtaining derivatives belonging to 2′,3′-diphenyl-3H-spiro[[2]benzofuran-1,4′-imidazole]-3,5′(3′H)-dione nucleus, we synthesized 4-[(3-amino-1-oxo-1H-2-benzopyran-4-yl)amino]benzoic acid (a 3,4-diaminoisocoumarine derivative), a known precursor of 4-[(1-carbamoyl-3-oxo-1,3-dihydro-2-benzofuran-1-yl)amino]benzoic acid (a phthalide–carboxamide-bearing system) by a novel methodology that we report here. The reaction conditions were optimized to afford the latter in 62% yield.

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38

Abdelhamid, Abdou Osman, and A. S. Shawali. "Synthesis of Some New 2-Imino-2,3-dihydro-1,3,4-thiadiazole and Selenadiazole Derivatives." Zeitschrift für Naturforschung B 42, no. 5 (1987): 613–16. http://dx.doi.org/10.1515/znb-1987-0516.

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(2)Diazotized 3(5)amino-5(3)-phenylpyrazole reacts with phenacylthiocyanate (1) and phenacylselenocyanate (10) to give the corresponding 1,3,4-thiadiazoline derivative (5) and 1,3,4- selenadiazoline derivative (12), respectively. A mechanism is proposed and it is substantiated by an alternate synthesis of 5 and 12 from the corresponding hydrazidoyl bromide (6) with potassium thiocyanate and potassium selenocyanate, respectively. The thiadiazoline (5) and selenadiazoline (12) give the respective N-acyl derivatives (7a) and (12) with acetic anhydride. Nitrosation of 5 and 12 gives the correspond

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39

Gupta, Nisha, Gyanesh Kumar Sahu, and Suchita Wamankar. "Molecular Docking Study of Ibuprofen Analogue for Anti-inflammatory and Analgesic Activity." International Journal of Advanced Multidisciplinary Research and Studies 5, no. 3 (2025): 876–82. https://doi.org/10.62225/2583049x.2025.5.3.4372.

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Non-steroidal anti-inflammatory drugs (NSAIDs), such as ibuprofen, are widely used for pain relief and inflammation management. However, their clinical utility is often limited by gastrointestinal side effects arising from non-selective inhibition of both COX-1 and COX-2 enzymes. To address this issue, the ibuprofen derivatives with structural modifications aimed at enhancing COX-2 and Prostaglandin E2 selectivity. The approach involved incorporating of 4-amino Pyrazole ring into the ibuprofen scaffold to modulate its binding affinity and selectivity for the COX-2 and prostaglandin active site

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40

Melano, Ivonne, Li-Lan Kuo, Yan-Chung Lo, Po-Wei Sung, Ni Tien, and Wen-Chi Su. "Effects of Basic Amino Acids and Their Derivatives on SARS-CoV-2 and Influenza-A Virus Infection." Viruses 13, no. 7 (2021): 1301. http://dx.doi.org/10.3390/v13071301.

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Amino acids have been implicated with virus infection and replication. Here, we demonstrate the effects of two basic amino acids, arginine and lysine, and their ester derivatives on infection of two enveloped viruses, SARS-CoV-2, and influenza A virus. We found that lysine and its ester derivative can efficiently block infection of both viruses in vitro. Furthermore, the arginine ester derivative caused a significant boost in virus infection. Studies on their mechanism of action revealed that the compounds potentially disturb virus uncoating rather than virus attachment and endosomal acidifica

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41

Spassova, Maria K., Antonín Holý, and Milena Masojídková. "Ribonucleosides of 3-amino- and 3,5-diaminopyrazole-4-carboxylic acid and their open-chain analogues: Synthesis and reactions." Collection of Czechoslovak Chemical Communications 51, no. 7 (1986): 1512–31. http://dx.doi.org/10.1135/cccc19861512.

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Bis(trimethylsilyl) derivative of ethyl 3-aminopyrazole-4-carboxylate (VI) and tris(trimethylsilyl) derivative of ethyl 3,5-diaminopyrazole-4-carboxylate (VII) on reaction with 2,3,5-tri-O-benzoyl-D-ribofuranolyl chloride and subsequent debenzoylation afforded the respective β-D-ribofuranosyl derivatives VIIIa and Xa. Their alkaline hydrolysis led to 1-(β-D-ribofuranosyl)-3-aminopyrazole-4-carboxylic acid (VIIIc) and 1-(β-D-ribofuranosyl)-3,5-diaminopyrazole-4-carboxylic acid (Xb). The esters VIIIa and Xa were not ammonolyzed under normal conditions. Contrary to nucleosidation of the silyl der

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42

Fan, Yunpeng, Wen Wan, Guobin Ma, et al. "Room-temperature Cu(ii)-catalyzed aromatic C–H azidation for the synthesis of ortho-azido anilines with excellent regioselectivity." Chem. Commun. 50, no. 43 (2014): 5733–36. http://dx.doi.org/10.1039/c4cc01481b.

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An efficient synthesis of ortho-aniline derivatives through aromatic C–H azidation catalyzed by Cu(OAc)<sub>2</sub> have been disclosed. The amino group plays an ortho-directing effect in the azidation reactions, regiospecifically affording the mono-azidated derivative as the sole products.

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43

Widyanti, Monika, Muhammad Idham Darussalam Mardjan, Niko Prasetyo, Alberto Krishna Ksatria Winning Kusuma, and Aldino Javier Saviola. "Substituted Indole Derivatives against Leucine Transporter (LeuT) as SSRI Antidepressant: Molecular Dynamics Study." Key Engineering Materials 990 (October 29, 2024): 145–55. http://dx.doi.org/10.4028/p-bdr6qt.

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Molecular docking and molecular dynamics on substituted indole derivatives-Leucine Trasporter had been performed. Indole derivatives with methoxy and fluorine group are chosen and specific amino acid residue Arg30 and Asp404 are π-alkyl and π-cation interactions. The suggested molecule containing methoxy groups has an RMSD value of 1.95 Å, a binding energy of-4.00 kcal mol-1, and an inhibition constant of 1.17 μM. The hypothesized fluorine-containing compound's RMSD value, binding energy, and inhibition constant were each 1.88 Å; -5.97 kcal mol-1; and 41.88 μM, respectively. The substituted in

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44

Pískala, Alois, Naeem B. Hanna, Jaroslav Zajíček, and Alois Čihák. "Synthesis, molecular conformation and biological activity of 6-amino-5-azacytidine." Collection of Czechoslovak Chemical Communications 54, no. 9 (1989): 2502–12. http://dx.doi.org/10.1135/cccc19892502.

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Reaction of N-ethoxycarbonylguanidine III with 2,3,5-tri-O-benzoyl-β-D-ribosyl isocyanate (II) afforded N-ethoxycarbonylamidinourea IV, which was cyclized by bis(trimethylsilyl)acetamide to the 6-ethoxy derivative VII. Ammono- and methanolysis of intermediate VII yielded 6-amino and 6-methoxy derivatives of 5-azacytidine I and VIII, respectively. Reaction of amidinourea IV with a mixture of chlorotrimethylsilane and triethylamine gave the blocked nucleoside V which was also formed by dealkylation of 6-ethoxy derivative VII with chlorotrimethylsilane or oxidation of tribenzoyl-5-azacytidine IX

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45

Moreno, Leydi, Jairo Quiroga, Rodrigo Abonia, Jonathan Ramírez-Prada, and Braulio Insuasty. "Synthesis of New 1,3,5-Triazine-Based 2-Pyrazolines as Potential Anticancer Agents." Molecules 23, no. 8 (2018): 1956. http://dx.doi.org/10.3390/molecules23081956.

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A new series of 1,3,5-triazine-containing 2-pyrazoline derivatives (8–11)a–g was synthesized by cyclocondensation reactions of [(4,6-bis((2-hydroxyethyl)amino)-1,3,5-triazin-2-yl)amine]chalcones 7a–g with hydrazine hydrate and derivatives. Chalcones 7a–g were obtained by Claisen-Schmidt condensation between aromatic aldehydes and triazinic derivative 5, which was synthesized in high yield by a microwave-assisted reaction. Seventeen of the synthesized compounds were selected and tested by the US National Cancer Institute (NCI) for their anticancer activity against 58 different human tumor cell

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46

Al-Masoudi, Najim A., Yaseen A. Al-Soud, Erik De Clercq, and Christophe Pannecouque. "Nitroimidazoles Part 6. Synthesis, Structure and in Vitro anti-HIV Activity of New 5-substituted Piperazinyl-4-nitroimidazole Derivatives." Antiviral Chemistry and Chemotherapy 18, no. 4 (2007): 191–200. http://dx.doi.org/10.1177/095632020701800403.

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2-Amino-1-[4-(1-benzyl-2-ethyl-4-nitro-1 H-imidazol-5-yl)piperazin-1-yl]ethanone [6] was prepared from 1-(1-benzyl-2-ethyl-4-nitro-1 H-imidazol-5-yl) piperazine [3]. A series of new 2-oxoethyl-arylamide [9,10] and 2-oxoethyl-arylsulphonamide [11–14] derivatives were synthesized from [6] with the aim of developing new non-nucleoside reverse transcriptase inhibitors. Alternatively, the amine [17] was synthesized from [3] via the phthalimide derivative [16]. The arylsulphonamide derivatives [18–23] and the arylamide analogues [24–26] were synthesized from [17]. The compounds were evaluated for th

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47

Huijuan, Yang, Ren Yujie, Xu Wenqian, and Li Ren. "Design and synthesis of novel pyridinium nitrate-bearing substituted anilines via one-pot tandem reactions." Journal of Chemical Research 41, no. 7 (2017): 384–89. http://dx.doi.org/10.3184/174751917x14967701766950.

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Thirty-two novel 2-amino-1-[3-oxo-3-(substituted-anilino)propyl]pyridinium nitrate derivatives were designed and prepared via one-pot tandem reactions. The structure of the 2-methylanilino derivative was characterised by X-ray crystallographic analysis. In addition, a potential formation mechanism is proposed.

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48

Mistry, Rakesh N., and K. R. Desai. "Studies on Synthesis of Some Novel Heterocyclic Azlactone Derivatives and Imidazolinone Derivatives and their Antimicrobial Activity." E-Journal of Chemistry 2, no. 1 (2005): 42–51. http://dx.doi.org/10.1155/2005/542938.

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p- Methyl benzoic acid on reaction with phosphorus pentachloride gives p - methyl benzoyl chloride derivative which on condensation with glycine gives p - methyl benzoyl glycine derivative. Now, this p - methyl benzoyl glycine derivative on condensation with various substituted aldehydes gives corresponding substituted 4 - [aryl methylidine] - 2 - [p - methyl phenyl] - oxazole - 5 - one derivatives [1(a-j)]. Further, these derivatives [1(a-j)] on condensation with 4 , 4’ - diamino diphenyl sulphone gives corresponding substituted imidazolinone - dibenzsulphone derivatives [2(a-j)], on condensa

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49

Zaki, Remon M., Adel M. Kamal El-Dean, Shaban M. Radwan, and Ahmed F. Saber. "Efficient synthesis, reactions and spectral characterization of pyrazolo[4’,3’:4,5]thieno[3,2-d] pyrimidines and related heterocycles." Heterocyclic Communications 25, no. 1 (2019): 39–46. http://dx.doi.org/10.1515/hc-2019-0004.

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AbstractNew pyrazolothienopyrimidines were synthesized. The key intermediate 4-aminothieno[2,3-c]pyrazole-5-carbonitrile 1 was converted to the chloroacetyl amino derivative 2 followed by nucleophilic substitution and Dimorth rearrangement upon treatment with nitrogen nucleophiles to give the pyrimidinones 3a-c. Treatment of 3a with formaldehyde and with triethyl orthoformate afforded the respective tetracyclic derivatives 4 and 5. Condensation of the amino group in the o-aminocarbonitrile 1 with triethyl orthoformate followed by cycloaddition reaction with hydrazine led to the formation of py

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50

Zhao, Xinyi, Hongge Jia, Qingji Wang, et al. "The oxidative coupling between benzaldehyde derivatives and phenylacetylene catalyzed by rhodium complexes via C-H bond activation." Heterocyclic Communications 26, no. 1 (2020): 20–25. http://dx.doi.org/10.1515/hc-2020-0004.

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AbstractThis paper reports the use of rhodium (Rh) catalysts for the oxidative coupling reaction between phenylacetylene and benzaldehyde derivatives via C-H bond activation. These reactions were catalyzed by Rh(l-amino acid)(cod) (the l-amino acid is l-phenylalanine, l-valine or l-proline; cod is 1,5-cyclooctadiene) to obtain chromones in 12.7–88.3% yield. These new Rh catalysts have excellent activity for the coupling reaction between phenylacetylene and different benzaldehyde derivatives. It was found that the electronic effects of the benzaldehyde derivative substituent affected the reacti

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