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Journal articles on the topic '4-oxadiazole derivatives containing R-phenyl moiety'

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Published: 7 June 2025

Last updated: 2 August 2025

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1

Markov, Andrey V., Aleksandra V. Sen’kova, Irina I. Popadyuk та ін. "Novel 3′-Substituted-1′,2′,4′-Oxadiazole Derivatives of 18βH-Glycyrrhetinic Acid and Their O-Acylated Amidoximes: Synthesis and Evaluation of Antitumor and Anti-Inflammatory Potential In Vitro and In Vivo". International Journal of Molecular Sciences 21, № 10 (2020): 3511. http://dx.doi.org/10.3390/ijms21103511.

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A series of novel 18βH-glycyrrhetinic acid (GA) derivatives containing 3′-(alkyl/phenyl/pyridin(-2″, -3″, and -4″)-yl)-1′,2′,4′-oxadiazole moieties at the C-30 position were synthesized by condensation of triterpenoid’s carboxyl group with corresponding amidoximes and further cyclization. Screening of the cytotoxicity of novel GA derivatives on a panel of tumor cell lines showed that the 3-acetoxy triterpenoid intermediates—O-acylated amidoxime 3a-h—display better solubility under bioassay conditions and more pronounced cytotoxicity compared to their 1′,2′,4′-oxadiazole analogs 4f-h (median IC

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2

Wang, Lei, Xia Zhou, Hui Lu, Xianfu Mu, and Linhong Jin. "Synthesis and Antibacterial Evaluation of Novel 1,3,4-Oxadiazole Derivatives Containing Sulfonate/Carboxylate Moiety." Molecules 25, no. 7 (2020): 1488. http://dx.doi.org/10.3390/molecules25071488.

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In order to discover new lead compounds with high antibacterial activity, a series of new derivatives were designed and synthesized by introducing a sulfonate or carboxylate moiety into the 1,3,4-oxadiazole structure. Antibacterial activity against two phytopathogens, Xanthomonas oryzae pv. oryzae (Xoo) and Xanthomonas axonopodis pv. citri (Xac), was assayed in vitro. The preliminary results indicated that ten compounds including 4a-1-4a-4 and 4a-11-4a-16 had good antibacterial activity against Xoo, with EC50 values ranging from 50.1-112.5 µM, which was better than those of Bismerthiazol (253.

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3

Adimule, Vinayak, Sudha Medapa, AdarshaHaraballi Jagadeesha, LalitaSanjeev Kumar, and Prakash Kumar Rao. "Synthesis, characterization and cytotoxic evaluation of novel derivatives of 1, 3, 4-oxadiazole containing 5-phenyl thiophene moiety." IOSR Journal of Pharmacy and Biological Sciences 9, no. 5 (2014): 42–48. http://dx.doi.org/10.9790/3008-09544248.

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4

*Ashwini, H. Pagare, and Anwar R. Shaikh Dr. "CONVENTIONAL SYNTHESIS AND STRUCTURAL ELUCIDATION OF NEWER 1,3,4-OXADIAZOLE DERIVATIVES BIO FUNCTIONING AS ANTI-BACTERIAL AND ANTI-FUNGAL." World Journal of Pharmaceutical Science and Research 4, no. 1 (2025): 836–44. https://doi.org/10.5281/zenodo.14940193.

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5

Li, Feng-Yun, Jing-Bo Liu, Jia-Ning Gong, and Gen Li. "(R)-2-Phenyl-4,5-Dihydrothiazole-4-Carboxamide Derivatives Containing a Diacylhydrazine Group: Synthesis, Biological Evaluation, and SARs." Molecules 24, no. 24 (2019): 4440. http://dx.doi.org/10.3390/molecules24244440.

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A series of (R)-2-phenyl-4,5-dihydrothiazole-4-carboxamide derivatives containing a diacylhydrazine moiety were designed and synthesized. Their structures were confirmed by melting points, 1H NMR, 13C NMR, and elemental analysis (EA). Their antifungal and insecticidal activities were evaluated. The antifungal activity result indicated that most title compounds against Cercospora arachidicola, Alternaria solani, Phytophthora capsici, and Physalospora piricola exhibited apparent antifungal activities at 50 mg/L, and better than chlorothalonil or carbendazim. The EC50 values of (R)-N’-benzoyl-2-(

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6

Liu, Jingbo, Fengyun Li, Yuanhong Wang, Haoxuan Zhang, Yuxin Li, and Zhengming Li. "Synthesis, biological activities, and 3D-QSAR studies of (R)-2-phenyl-4,5-dihydrothiazole-4-carboxamide derivatives containing a sulfonohydrazide moiety." Medicinal Chemistry Research 29, no. 3 (2020): 495–503. http://dx.doi.org/10.1007/s00044-020-02499-3.

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7

Liu, Jingbo, Fengyun Li, Yuanhong Wang, et al. "Synthesis, biological activities and 3D-QSAR studies of (R)-2-phenyl-4,5-dihydrothiazole-4-carboxamide derivatives containing a sulfur ether moiety." Chinese Chemical Letters 30, no. 3 (2019): 668–71. http://dx.doi.org/10.1016/j.cclet.2018.11.001.

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8

Irfan, Ali, Shah Faisal, Ameer Fawad Zahoor, et al. "In Silico Development of Novel Benzofuran-1,3,4-Oxadiazoles as Lead Inhibitors of M. tuberculosis Polyketide Synthase 13." Pharmaceuticals 16, no. 6 (2023): 829. http://dx.doi.org/10.3390/ph16060829.

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Benzofuran and 1,3,4-oxadiazole are privileged and versatile heterocyclic pharmacophores which display a broad spectrum of biological and pharmacological therapeutic potential against a wide variety of diseases. This article reports in silico CADD (computer-aided drug design) and molecular hybridization approaches for the evaluation of the chemotherapeutic efficacy of 16 S-linked N-phenyl acetamide moiety containing benzofuran-1,3,4-oxadiazole scaffolds BF1–BF16. This virtual screening was carried out to discover and assess the chemotherapeutic efficacy of BF1–BF16 structural motifs as Mycobac

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9

Ölmez, Nevin Arıkan, and Faryal Waseer. "New Potential Biologically Active Compounds: Synthesis and Characterization of Urea and Thiourea Derivativpes Bearing 1,2,4-oxadiazole Ring." Current Organic Synthesis 17, no. 7 (2020): 525–34. http://dx.doi.org/10.2174/1570179417666200417112106.

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Background: Urea, thiourea, and 1,2,4-oxadiazole compounds are of great interest due to their different activities such as anti-inflammatory, antiviral, analgesic, fungicidal, herbicidal, diuretic, antihelminthic and antitumor along with antimicrobial activities. Objective: In this work, we provide a new series of potential biologically active compounds containing both 1,2,4-oxadiazole and urea/thiouprea moiety. Materials and Methods: Firstly, 5-chloromethyl-3-aryl-1,2,4-oxadiazoles (3a-j) were synthesized from the reaction of different substituted amidoximes (2a-j) and chloroacetyl chloride i

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10

Bhat, Mashooq Ahmad, Mohamed A. Al-Omar, Ahmed M. Naglah, Atef Kalmouch, and Abdullah Al-Dhfyan. "Synthesis and Characterization of Novel Biginelli Dihydropyrimidinone Derivatives Containing Imidazole Moiety." Journal of Chemistry 2019 (May 13, 2019): 1–7. http://dx.doi.org/10.1155/2019/3131879.

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Enaminone, (2E)-1-[4-(1H-imidazol-1-yl) phenyl]-4-methylpent-2-en-1-one (II) was synthesized by refluxing 1-[4-(1H-imidazol-1-yl) phenyl] ethan-1-one (I) with dimethylforamide dimethylacetal (DMF–DMA) under solvent-free condition for 12 hours. Finally, the dihydropyrimidinone derivatives containing imidazole moiety (1–15) were obtained by reacting enaminone, (2E)-1-[4-(1H-imidazol-1-yl) phenyl]-4-methylpent-2-en-1-one (II) with urea and different substituted benzaldehydes in the presence of glacial acetic acid. Dihydropyrimidinone derivatives containing imidazole moiety were synthesized in exc

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11

Bhat, Mashooq A., Mohamed A. Al-Omar, Ahmed M. Naglah, and Abdullah Al-Dhfyan. "Biginelli Synthesis of Novel Dihydropyrimidinone Derivatives Containing Phthalimide Moiety." Journal of Chemistry 2020 (March 9, 2020): 1–5. http://dx.doi.org/10.1155/2020/4284628.

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A new series of novel Biginelli compounds, 5-benzoyl-substituted phenyl-3,4-dihydropyrimidin-2(1H)-one-1H-isoindole-1,3(2H)-dione (1−10), were synthesized from enaminone, 2-{4-[(2E)-3-(dimethylamino)prop-2-enoyl]phenyl}-1H-isoindole-1,3(2H)-dione (IV), which was synthesized by refluxing 2-(4-acetylphenyl)-1H-isoindole-1,3(2H)-dione (III), with dimethylformamide-dimethylacetal (DMF-DMA) without solvent for 12 h. The compound 2-(4-acetylphenyl)-1H-isoindole-1,3(2H)-dione (III) was obtained by reacting phthalic anhydride (I) with para-aminoacetophenone (II) in glacial acetic acid for 2 h. The dih

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12

Alsaedi, Farghaly, and Shaaban. "Synthesis and Antimicrobial Evaluation of Novel Pyrazolopyrimidines Incorporated with Mono- and Diphenylsulfonyl Groups." Molecules 24, no. 21 (2019): 4009. http://dx.doi.org/10.3390/molecules24214009.

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A novel series of pyrazolo[1,5-a]pyrimidine ring systems containing phenylsulfonyl moiety have been synthesized via the reaction of 2-(phenylsulfonyl)-1-(4-(phenylsulfonyl) phenyl)ethan-1-one, 2-benzenesulfonyl-1-(4-benzenesulfonyl-phenyl)-3-dimethylamino-propenone and 3-(dimethylamino)-1-(4-(phenylsulfonyl)phenyl)prop-2-en-1-one each with various substituted aminoazopyrazole derivatives in one pot reaction strategy. The proposed structure as well as the mechanism of their reactions were discussed and proved with all possible spectral data. The results of antimicrobial activities of the new su

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13

Patel, H. S., H. D. Desai, and H. J. Mistry. "Synthesis and Antimicrobial Activity of Some New Piperazine Derivaties Containing Aryl Sulfonyloxy Group." E-Journal of Chemistry 1, no. 2 (2004): 93–98. http://dx.doi.org/10.1155/2004/732420.

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NovelN-substituted piperazine derivatives containing sulfonyloxy aniline moiety have been prepared. The various 4-sulfonyloxy aniline (SA) derivatives (2a-h) have been prepared by the condensation reaction ofN-Acetyl Sulfanilyl chloride (ASC) and sodium phenates followed by hydrolysis. The SA derivatives are then reacted with chloro acetyl chloride to give corresponding (N-Chloroacetyl) derivatives (3a-h). These derivatives are then reacted withN-phenyl piperazine to yield the corresponding piperazine derivatives (4a-h).

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14

Drzewiecka-Antonik, Aleksandra, Marta Struga, Agnieszka Głogowska, et al. "Synthesis, Structural Characterization and Biological Activity Evaluation of Novel Cu(II) Complexes with 3-(trifluoromethyl)phenylthiourea Derivatives." International Journal of Molecular Sciences 23, no. 24 (2022): 15694. http://dx.doi.org/10.3390/ijms232415694.

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Copper complexes with 1,3-disubstituted thiourea derivatives, all containing 3-(trifluoromethyl)phenyl tail and 1-alkyl/halogen-phenyl substituent, were synthesized. The experimental spectroscopic studies and theoretical calculation revealed that two ligands coordinate to Cu(II) in a bidentate fashion via thiocarbonyl S and deprotonated N atoms of thiourea moiety. Such monomers are characteristic of alkylphenylthiourea complexes, whereas the formation of a sandwich-type dimer is observed for halogeno derivatives. For the first time, the structural identifications of CuN2S2-based complexes usin

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15

da Silva Lima, Camilo Henrique, Júlio César de Araujo Vanelis Soares, Joana Lucius de Sousa Ribeiro, Estela Maris Freitas Muri, Sérgio de Albuquerque, and Luiza Rosaria Sousa Dias. "Anti-Trypanosoma cruzi Activity and Molecular Docking Studies of 1Hpyrazolo[ 3, 4-b]pyridine Derivatives." Letters in Drug Design & Discovery 17, no. 2 (2020): 184–91. http://dx.doi.org/10.2174/1570180816666190305141733.

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Background: Untargeted studies led to the development of some pyrazolopyridine derivatives for the antiparasitic profile, particularly the derivatives containing the structural carbohydrazide subunit. In this work, we proceeded in the biological screening of 27 N’- (substitutedphenylmethylene)- 4-carbohydrazide-3-methyl-1-phenyl-1H-pyrazolo[3, 4-b]pyridine derivatives against T. cruzi as well as the cytotoxic evaluation. To obtain more information about the trypanocidal activity of this class of compounds, we carried out molecular docking simulations to get an insight into putative targets in

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16

H., D. Navadiya, K. Undavia N., and S. Patwa B. "Studies on synthesis of 2-methyl-3,1-benzoxazine-4(4H)-one dyes and their application on nylon and polyester fibres." Journal of Indian Chemical Society Vol. 86, Oct 2009 (2009): 1118–20. https://doi.org/10.5281/zenodo.5820642.

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Department of Chemistry, Department of Industrial Chemistry, Sir P. P. Institute of Science, Bhavnagar University, Bhavnagar-364 002, Gujarat, India <em>E-mail </em>: dr.navadiya@yahoo.com <em>Manuscript received 15 December 2008, accepted 3 July 2009</em> A series of 3-{4-[4-(4-arylazo)-benzenesulfonyl]phenyl}-2-methyl-3H-quinazolin-4-one derivatives (3) have been obtained by a reaction of a various coupling agent (a-g) with diazonium salt containing 4-oxo-quinazolin moiety (2). The diazonium salt 2 is obtained by the reaction of 4-(2-methyl-4-oxo-3-quinazolinyl)-4<em>'</em>-aminodiphenyl

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17

Darwish, Elham S. "Facile Synthesis and Antimicrobial Evaluation of Some New Heterocyclic Compounds Incorporating a Biologically Active Sulfamoyl Moiety." Scientific World Journal 2014 (2014): 1–10. http://dx.doi.org/10.1155/2014/165495.

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A facile and convenient synthesis of new heterocyclic compounds containing a sulfamoyl moiety suitable for use as antimicrobial agents was reported. The precursor 3-oxo-3-phenyl-N-(4-sulfamoylphenyl)propionamide was coupled smoothly with arenediazonium salt producing hydrazones which reacted with malononitrile or triethylorthoformate affording pyridazine and triazine derivatives, respectively. Also, the reactivity of the same precursor with DMF-DMA was followed by aminotriazole; aromatic aldehydes was followed by hydrazine hydrate, triethylorthoformate, or thiourea affording triazolo[1,5-a]pyr

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18

Makhova, N. N., I. V. Ovchinnikov, A. S. Kulikov, S. I. Molotov, and E. L. Baryshnikova. "Monocyclic and cascade rearrangements of furoxans." Pure and Applied Chemistry 76, no. 9 (2004): 1691–703. http://dx.doi.org/10.1351/pac200476091691.

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Monocyclic rearrangements of azoles are extensively studied as alternative methods for the preparation of new heterocyclic systems. The present work is devoted to investigation of monocyclic and cascade rearrangements of 1,2,5-oxadiazole 2-oxide (furoxan) derivatives. It was found during investigations that rearrangements of furoxan ring had some peculiarities in comparison with analogous rearrangements of other azoles. Therefore, three different kinds of rearrangements were found. The first of them occurred through a dinitroso-ethylene intermediate and resulted in the synthesis of 1,2,3-triaz

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19

Lu, Hui, Xia Zhou, Lei Wang, and Linhong Jin. "Synthesis and Antibacterial Evaluation of N-phenylacetamide Derivatives Containing 4-Arylthiazole Moieties." Molecules 25, no. 8 (2020): 1772. http://dx.doi.org/10.3390/molecules25081772.

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A series of new N-phenylacetamide derivatives containing 4-arylthiazole moieties was designed and synthesized by introducing the thiazole moiety into the amide scaffold. The structures of the target compounds were confirmed by 1H-NMR, 13C-NMR and HRMS. Their in vitro antibacterial activities were evaluated against three kinds of bacteria—Xanthomonas oryzae pv. Oryzae (Xoo), Xanthomonas axonopodis pv. Citri (Xac) and X.oryzae pv. oryzicola (Xoc)—showing promising results. The minimum 50% effective concentration (EC50) value of N-(4-((4-(4-fluoro-phenyl)thiazol-2-yl)amino)phenyl)acetamide (A1) i

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20

Gupta, Sakuntala, Tanmay Choudhury, Ewelina Dmochowska, Przemyslaw Kula, Fabio Borbone, and Roberto Centore. "Crystal structure and mesogenic behaviour of a new fluorene derivative: 9,9-dimethyl-2,7-bis(4-pentylphenyl)-9H-fluorene." Acta Crystallographica Section C Structural Chemistry 75, no. 11 (2019): 1459–64. http://dx.doi.org/10.1107/s2053229619013007.

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The title compound, C37H42, is a new mesogenic compound containing the fluorene moiety. It exhibits enantiotropic nematic liquid crystalline behaviour with melting at 125 °C and isotropization at 175 °C. The crystallographically independent unit contains two molecules oriented face-to-edge with respect to each other. The two molecules have nearly the same conformation of the bis-phenyl fluorene moiety. The molecular packing in the crystal phase is nematic-like.

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21

Han, Xu, Yun Long Yu, Duo Ma, Zhao Yan Zhang, and Xin Hua Liu. "Synthesis, telomerase inhibitory and anticancer activity of new 2-phenyl-4H-chromone derivatives containing 1,3,4-oxadiazole moiety." Journal of Enzyme Inhibition and Medicinal Chemistry 36, no. 1 (2020): 344–60. http://dx.doi.org/10.1080/14756366.2020.1864630.

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22

Zhang, Guoqi. "4-vinylpyridine derivatives: Protonation, methylation and silver(I) coordination chemistry." Journal of Chemical Research 45, no. 7-8 (2021): 687–93. http://dx.doi.org/10.1177/1747519821989659.

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( E)-4-[2-(Pyridin-4-yl)vinyl]benzaldehyde, containing both a 4-vinylpyridine and an aldehyde functionality, is utilized to develop new, highly conjugated chalcone compounds and a bis-Schiff base azine compound. The chalcone-containing compounds are further explored for their protonation, methylation and silver(I) coordination chemistry using the pyridine moiety. In parallel, a cyano-containing analogue, ( E)-4-[2-(pyridin-4-yl)vinyl]benzonitrile is also synthesized and studied for its silver(I) coordination chemistry. These new compounds are fully characterized by mass spectrometry, elemental

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23

Holla, Bantwala S., Channamata S. Prasanna, Boja Poojary, Mithun Ashok, Kottapalli S. Rao, and Kanakamajalu Shridhara. "Synthesis, Characterization and Antibacterial Studies of Some 1,2,4-Triazole Derivatives Containing a 6-Chloropyridin-3-yl methyl Moiety." Zeitschrift für Naturforschung B 61, no. 3 (2006): 334–38. http://dx.doi.org/10.1515/znb-2006-0315.

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Abstract5-(6-Chloropyridin-3-yl methyl)-4-phenyl-1,2,4-triazole-3-thiol (2) and 5-substituted-4-phenyl- 1,2,4-triazole-3-thiols (3) were synthesized. Alkylation and aminomethylation reactions of these triazoles were also carried out. Some of the newly synthesized compounds were screened for their antibacterial activities.

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24

Kliegel, Wolfgang, Lutz Preu, Ute Schumacher, Steven J. Rettig, and James Trotter. "Structural studies of organoboron compounds L. 4-(2-Hydroxy-2,2-diphenylacetyl)- 6,6-pentamethylene-2-phenyl-1,3-dioxa-4-aza-2-boracyclohexane and 4-[2,2-difluoro-5,5-bis(4-methoxyphenyl)-1,3-dioxa-2-borata-4-cyclopentylidene]- 6,6-pentamethylene-2-phenyl-1,3-dioxa-4-azonia-2-boracyclohexane." Canadian Journal of Chemistry 70, no. 4 (1992): 1176–87. http://dx.doi.org/10.1139/v92-154.

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The preparation of the organoboron compounds 4-(2-hydroxy-2,2-diphenylacetyl)-6,6-pentamethylene-2-phenyl-1,3-dioxa-4-aza-2-boracyclohexane, 6, 4-(2,2-difluoro-5,5-diphenyl-1,3-dioxa-2-borata-4-cyclopentylidene)-6,6-pentamethylene-2-phenyl-1,3-dioxa-4-azonia-2-boracyclohexane, 14a, and 4-[2,2-difluoro-5,5-bis(4-methoxyphenyl)-1,3-dioxa-2-borata-4-cyclopentylidene]-6,6-pentamethylene-2-phenyl-1,3-dioxa-4-azonia-2-boracyclohexane, 14b, are reported. Crystals of 6 are triclinic, [Formula: see text], a = 8.7348(5), b = 11.0529(6), c = 14.104(1) Å, α = 65.781(5)°, β = 72.147(6)°, γ = 79.928(6)°, Z

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25

Selvaraj, Revathy, J. Suresh, E. Vakees, and A. Arun. "Synthesis of Novel Organic Compounds from Cyanuric Chloride Containing 1-(4-(7-Chloroquinolin-4-ylamino)phenyl)-3-(4-hydroxyphenyl)prop-2-en-1-one Chalcone for Biological Applications." Asian Journal of Chemistry 34, no. 5 (2022): 1139–44. http://dx.doi.org/10.14233/ajchem.2022.23662.

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This article reported the synthesis of triazine having quinoline chalcone moiety and its derivatives. Cyanuric chloride, 1-(4-(7-chloroquinolin-4-ylamino)phenyl)-3-(4-hydroxyphenyl)prop-2-en-1-one (KKC), aniline, 4-nitro aniline and 1-naphthol used for the synthesis. Triazine having chlorine atom was periodically replaced by the above materials to synthesize the desired product. Synthesized triazine based organic molecules were characterized using elemental analysis, FT-IR, 1H NMR and UV-visible spectroscopic techniques. Antibacterial activity of synthesized compounds was found on Gram-positiv

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26

Dr., Faizan Sayeed1* Abdul Sayeed1 MD Akram1 Mohd Waseem Akram2. "DESIGN, SYNTHESIS AND PHARMACOLOGICAL EVALUATION OF NEW SUBSTITUTED THIAZOLIDIN-4- ONE DERIVATIVES." Indo American Journal of Pharmaceutical Sciences 04, no. 08 (2017): 2461–72. https://doi.org/10.5281/zenodo.846845.

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4-thiazolidinones are among t h e most extensively investigated class of organic compounds. Thiazolidin-4-one has been considered as magic moiety, which is a core structure in various synthetic pharmaceuticals displaying a broad spectrum of biological activities.They are widely used as anti-inflammatory, anticonvulsant, analgesic, antimicrobial,anti-HIV,CNS depressant, carcinostatic, antihypertensive and cytotoxic. In view of the wide spectrum activities of condensed 4-thiazolidinones, it was thought worthwhile to undertake the synthesis of heterocyclic systems in which 4-thiazolidinone nucleu

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27

Alsayari, Abdulrhman, Yahya I. Asiri, Abdullatif Bin Muhsinah, and Mohd Zaheen Hassan. "Synthesis and antimicrobial activity of aryldiazenyl/arylhydrazono pyrazoles." Journal of Chemical Research 45, no. 11-12 (2021): 1093–99. http://dx.doi.org/10.1177/17475198211057461.

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We report the design, synthesis, and in vitro antimicrobial evaluation of functionalized pyrazoles containing a hydrazono/diazenyl moiety. Among these newly synthesized derivatives, 4-[2-(4-chlorophenyl)hydrazono]-5-methyl-2-[2-(naphthalen-2-yloxy)acetyl]-2,4-dihydro-3 H-pyrazol-3-one is a promising antimicrobial agent against Staphylococcus aureus (minimum inhibitory concentration 0.19 μg mL−1). Structure–activity relationship studies reveal that the electronic environment on the distal phenyl ring has a considerable effect on the antimicrobial potential of the hybrid analogues. Molecular doc

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28

Vu Quoc, Trung, Duong Tran Thi Thuy, Thuan Dang Thanh, et al. "Some chalcones derived from thiophene-3-carbaldehyde: synthesis and crystal structures." Acta Crystallographica Section E Crystallographic Communications 75, no. 7 (2019): 957–63. http://dx.doi.org/10.1107/s2056989019007503.

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The synthesis, spectroscopic data and crystal and molecular structures of four 3-(3-phenylprop-1-ene-3-one-1-yl)thiophene derivatives, namely 1-(4-hydroxyphenyl)-3-(thiophen-3-yl)prop-1-en-3-one, C13H10O2S, (1), 1-(4-methoxyphenyl)-3-(thiophen-3-yl)prop-1-en-3-one, C14H12O2S, (2), 1-(4-ethoxyphenyl)-3-(thiophen-3-yl)prop-1-en-3-one, C15H14O2S, (3), and 1-(4-bromophenyl)-3-(thiophen-3-yl)prop-1-en-3-one, C13H9BrOS, (4), are described. The four chalcones have been synthesized by reaction of thiophene-3-carbaldehyde with an acetophenone derivative in an absolute ethanol solution containing potass

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29

Apostol, Theodora-Venera, Mariana Carmen Chifiriuc, Constantin Draghici, et al. "Synthesis, In Silico and In Vitro Evaluation of Antimicrobial and Toxicity Features of New 4-[(4-Chlorophenyl)sulfonyl]benzoic Acid Derivatives." Molecules 26, no. 16 (2021): 5107. http://dx.doi.org/10.3390/molecules26165107.

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The multi-step synthesis, physico-chemical characterization, and biological activity of novel valine-derived compounds, i.e., N-acyl-α-amino acids, 1,3-oxazol-5(4H)-ones, N-acyl-α-amino ketones, and 1,3-oxazoles derivatives, bearing a 4-[(4-chlorophenyl)sulfonyl]phenyl moiety are reported here. The structures of the newly synthesized compounds were confirmed by spectral (UV-Vis, FT-IR, MS, 1H- and 13C-NMR) data and elemental analysis results, and their purity was determined by RP-HPLC. The new compounds were assessed for their antimicrobial activity and toxicity to aquatic crustacean Daphnia m

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Ozolins, Reinis, Mara Plotniece, Karlis Pajuste, et al. "1,1′-{[3,5-Bis((dodecyloxycarbonyl)-4-phenyl-1,4-dihydropyridine-2,6-diyl]bis(methylene)}bis[4-(anthracen-9-yl)pyridin-1-ium] Dibromide." Molbank 2022, no. 3 (2022): M1438. http://dx.doi.org/10.3390/m1438.

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A synthesis of a cationic moiety and fluorescent moieties containing amphiphilic 1,4-dihydropyridine (1,4-DHP) derivatives was performed starting with the Hantzsch-type cyclization of dodecyl acetoacetate, phenylaldehyde and ammonium acetate. Bromination of the 2,6-dimethyl groups of a parent 1,4-DHP compound, followed by nucleophilic substitution of bromine with 4-(anthracen-9-yl)pyridine, produced the desired 1,1′-{[3,5-bis((dodecyloxycarbonyl)-4-phenyl-1,4-dihydropyridine-2,6-diyl]bis(methylene)}bis[4-(anthracen-9-yl)pyridin-1-ium] dibromide. The obtained target compound was fully character

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Yang, DaEun, Kyutae Seo, and Hyo Kang. "Effect of Position and Structure of the Terminal Moieties in the Side Group on the Liquid Crystal Alignment Behavior of Polystyrene Derivatives." Polymers 13, no. 16 (2021): 2822. http://dx.doi.org/10.3390/polym13162822.

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We synthesized a series of polystyrene derivatives containing various side groups, such as the 4-(tert-butyl)-phenoxymethyl, 3-(tert-butyl)-phenoxymethyl, 2-(tert-butyl)-phenoxymethyl, 4-cumyl-phenoxymethyl, and 4-trityl-phenoxymethyl groups, through a polymer modification reaction to examine the liquid crystal (LC) alignment of these derivatives. In general, the vertical LC alignment on polymer films can be affected by the position and structure of the terminal moiety of the polymer side group. For example, the LC cells fabricated with 4-(tert-butyl)-phenoxymethyl-substituted polystyrene havi

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32

Apostol, Theodora-Venera, Mariana Carmen Chifiriuc, Laura-Ileana Socea, et al. "Synthesis, Characterization, and Biological Evaluation of Novel N-{4-[(4-Bromophenyl)sulfonyl]benzoyl}-L-valine Derivatives." Processes 10, no. 9 (2022): 1800. http://dx.doi.org/10.3390/pr10091800.

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In this article, we present the design and synthesis of novel compounds, containing in their molecules an L-valine residue and a 4-[(4-bromophenyl)sulfonyl]phenyl moiety, which belong to N-acyl-α-amino acids, 4H-1,3-oxazol-5-ones, 2-acylamino ketones, and 1,3-oxazoles chemotypes. The synthesized compounds were characterized through elemental analysis, MS, NMR, UV/VIS, and FTIR spectroscopic techniques, the data obtained are in accordance with the assigned structures. Their purities were verified by reversed-phase HPLC. The new compounds were tested for antimicrobial action against bacterial an

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Zagórska, Agnieszka, Anna Czopek, Anna Jaromin, et al. "Design, Synthesis, and In Vitro Antiproliferative Activity of Hydantoin and Purine Derivatives with the 4-Acetylphenylpiperazinylalkyl Moiety." Materials 14, no. 15 (2021): 4156. http://dx.doi.org/10.3390/ma14154156.

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Cancer represents one of the most serious health problems and the second leading cause of death around the world. Heterocycles, due to their prevalence in nature as well as their structural and chemical diversity, play an immensely important role in anti-cancer drug discovery. In this paper, a series of hydantoin and purine derivatives containing a 4-acetylphenylpiperazinylalkyl moiety were designed, synthesized, and biologically evaluated for their anticancer activity on selected cancer cell lines (PC3, SW480, SW620). Compound 4, a derivative of 3′,4′-dihydro-2′H-spiro[imidazolidine-4,1′-naph

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34

Bharathi, Sharanappa Veerapur, L. N. Netravati, and K. M. Basavaraja. "Synthesis and molecular docking investigations of some benzofuran derivatives containing 1,2,4-triazole moiety as potent antibacterial and antifungal agents." Research Journal of Chemistry and Environment 27, no. 3 (2023): 20–26. http://dx.doi.org/10.25303/2703rjce20026.

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Inspired by the pharmacological activities of 1, 2, 4-triazoles, a new series of 1, 2, 4-triazoles derivatives was prepared by using the key intermediate 3-amino-5-nitro-1-benzofuran-2-yl) (phenyl) methanone (2). Compound-2 on acetylation and benzoylation yielded corresponding derivatives 3a-b, which were then treated with hydrazine hydrate to produce compound (4a-b). Compounds (4a-b) when refluxed with glacial acetic acid, produce targeted molecules of 1, 2, 4-triazoles compounds (5a-b). All the newly synthesized compounds were characterized by FT IR, 1H NMR and mass spectral analysis. All th

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35

Rishipathak, Dinesh, Sushil Vaidya, and Shantanu Ghodke. "Synthesis and Evaluation of Anticonvulsant Activity of Some 5,5-Disubstituted-N3-[(2-aryl thiazolidine-4-one-3-yl)amino]hydantoins." Asian Journal of Chemistry 35, no. 3 (2023): 591–97. http://dx.doi.org/10.14233/ajchem.2023.27282.

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According to the World Health Organization, the majority of people with epilepsy who live in developing countries do not have access to high-quality treatment. Modern anticonvulsants are in high demand since the unwanted effects of those compounds already in use make therapy difficult. The synthesis of derivatives of 5,5-disubstituted-N3-[(2-aryl thiazolidine-4-one-3-yl)amino]hydantoins has been reported. The position N3 of the hydantoin nucleus was substituted with 4-thiazolidinone moiety containing aryl substituent at 2nd position with the goal of achieving the enhanced anticonvulsant effect

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36

Padrtová, Tereza, Pavlína Marvanová, Renáta Kubínová, et al. "Indol-2-Carboxylic Acid Esters Containing N-Phenylpiperazine Moiety - Preparation and Cholinesterase-inhibiting Activity." Current Organic Synthesis 17, no. 7 (2020): 576–87. http://dx.doi.org/10.2174/1570179417666200619132218.

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Background: The indole derivatives and the N-phenylpiperazine fragment represent interesting molecular moieties suitable for the research of new potentially biologically active compounds. This study was undertaken to identify if indol-2-carboxylic acid esters containing N-phenylpiperazine moiety possess acetylcholinesterase and butyrylcholinesterase inhibitory activity. Materials and Methods: The study dealt with the synthesis of a novel series of analogs of 1H-indole-2- carboxylic acid and 3-methyl-1H-indole-2-carboxylic acid. The structure of the derivatives was represented by the indolylcar

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37

Ghorab, Mostafa M., and Mansour S. Alsaid. "Anti-breast cancer activity of some novel quinoline derivatives." Acta Pharmaceutica 65, no. 3 (2015): 271–83. http://dx.doi.org/10.1515/acph-2015-0030.

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Abstract To discover new bioactive lead compounds for medicinal purposes, 2-cyano-3-(4-substituted)-N-(quinolin-3-yl) acrylamide derivatives 2–24, chromenes 25, 26 and benzochromenes 27, 28 were synthesized. The structures of the newly synthesized compounds were confirmed by elemental analyses, IR, 1H NMR and 13C NMR spectroscopies. In addition, the structure of compound 1 was confirmed through X-ray crystallography. All the newly synthesized compounds were evaluated for their cytotoxic activity against the breast cancer cell line MCF7. The corresponding 2-cyano-3-(4-hydroxy-3-methoxyphenyl)-N

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38

Singh, Shiv Dev, Arvind Kumar, Firoz Babar, Neetu Sachan, and Arun Kumar Sharma. "Synthesis of Novel 3(N,N-dialkylamino)alkyl/phenyl Substituted Thieno [2,3-d]pyrimidinones as H1-Anti-Histaminic and Antimicrobial Agents." Current Bioactive Compounds 15, no. 1 (2019): 63–70. http://dx.doi.org/10.2174/1573407214666180226130957.

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Background: Thienopyrimidines are the bioisoster of quinazoline and unlike quinazoline exist in three isomeric forms corresponding to the three possible types annulation of thiophene to the pyrimidine ring viz thieno[2,3-d] pyrimidine, thieno[3,2-d] pyrimidine and thieno[3,4-d]pyrimidine. Heterocyclic containing the thienopyrimidinone moiety exhibits various pronounced activities such as anti-hypertensive, analgesic and anti-inflammatory, antiviral, platelet aggregation inhibitory, antiprotozoal bronchodilatory, phosphodiesterase inhibitory, antihistaminic, antipsychotic and antimicrobial acti

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39

T., Bansal, Sharma S., Gaba J., and Behal R. "Eco-friendly synthesis of amides and their microbial activity." Journal of Indian Chemical Society Vol. 92, Feb 2015 (2015): 255–61. https://doi.org/10.5281/zenodo.5602803.

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Department of Chemistry, Punjab Agricultural University, Ludhiana-141 004, Punjab, India E-mail : taniabansal2@yahoo.com, jyotgcw@gmail.com Department of Plant Breeding and Genetics, Punjab Agricultural University, Ludhiana-141 004, Punjab, India <em>E-mail</em> : sunita_sharma@pau.edu <em>Manuscript received online 23 July 2014, accepted 18 August 2014</em> A series of <em>N</em>-(1,5-dimethyl-3-oxo-2-phenyl-2,3-dihydro-1<em>H</em>-pyrazol-4-yl)-2-phenoxy-3-phenylacrylamide 5a-e, 1-morpholino-2-phenoxy-3-phenyl prop-2-ene-1-one 7a-e and 2-phenoxy-3-phenyl-N-(4<em>H</em>-1,2,4-triazole-4-yl)ac

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40

Yurttaş, Leyla, Yusuf Özkay, Gülşen Akalın-Çiftçi, and Şafak Ulusoylar-Yıldırım. "Synthesis and anticancer activity evaluation of N-[4-(2-methylthiazol-4-yl)phenyl]acetamide derivatives containing (benz)azole moiety." Journal of Enzyme Inhibition and Medicinal Chemistry 29, no. 2 (2013): 175–84. http://dx.doi.org/10.3109/14756366.2013.763253.

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41

Supuran, Claudiu T. "Complexes With Biologically Active Ligands. Part 2. Preparation of Copper(II) Complexes of Positively-Charged Derivatives of Aminoglutethimide." Metal-Based Drugs 3, no. 2 (1996): 57–62. http://dx.doi.org/10.1155/mbd.1996.57.

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Cu(II) complexes of 1-[4-(3-ethyl-piperidine-2,6-dione)-3-yl]-phenyl-2,4,6-trisubstituted pyridinium perchlorates, containing alkyl, aryl and combinations of these two types of moieties in their molecule were synthesized and characterized by elemental analysis, spectroscopy, magnetic, thermogravimetric and conductimetric measurements. In these complexes, Cu(II) ions are in octahedral geometry with four water molecules occupying the equatorial coordination sites and the two organic ligands in deprotonated state the remaining axial ones. The donor atom of these ligands is constituted by the ioni

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42

El-Gaby, Mohamed S. A., Mohamed I. Hassan, Modather F. Hussein, Ahmed M. Ali, Mahmoud M. Elaasser, and Faraghally A. Faraghally. "Synthesis, characterization and in vitro biological screening of 4-hydroxy naphthalen-1-yl, naphtho[1,2-b]furan, benzo[h]chromene and 5,6-dihydropyridazine derivatives containing sulfonamide moiety." Mediterranean Journal of Chemistry 7, no. 5 (2018): 346–58. http://dx.doi.org/10.13171/mjc751912061355msaeg.

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In this study, a series of 4-((4-hydroxynaphthalen-1-yl)diazenyl)benzenesulfonamides have been prepared by subsequent diazotization of sulfonamide derivatives and coupling with 1-naphthol in alkaline medium. Cyclization of 4-((4-hydroxynaphthalen-1-yl)diazenyl)benzenesulfonamides with cinnamic acid in the presence of a basic catalyst afforded the novel naphtho[1,2-b]furans. Also, 4-((4-hydroxynaphthalen-1-yl)diazenyl)benzenesulfonamides can be cyclized with α‐cyanocinnamonitriles to afford 2-amino-3-cyano-4-phenyl-4H-benzo[h]chromenes. 4-(4-amino-3,5- dicyano-6-iminopyridazin-1(6H)-yl)benzenes

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43

Koralla, Sravani, and Asha Deepti Choppala. "Novel Pyridopyrimidine-Based Compounds: Design, Synthesis and Cytotoxic Evaluation." Asian Journal of Chemistry 37, no. 7 (2025): 1577–86. https://doi.org/10.14233/ajchem.2025.33671.

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In this study, fifteen novel pyrido[2,3-d]pyrimidine derivatives (11a-o) were successfully designed, synthesized and characterized using spectroscopic techniques. The synthesized compounds were evaluated for their anticancer activity against three human cancer cell lines: MDA-MB-231 (breast cancer), HeLa (cervical cancer) and MCF-7 (breast cancer). The MTT assay results revealed that while some compounds exhibited low to moderate activity, the majority demonstrated potent anticancer effects, with pyrido[2,3-d]pyrimidine derivatives standing out as particularly effective. Among the synthesized

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44

SG, Jawarkar, and Game MD. "Synthesis, Characterization and Antimicrobial Evaluation of New Substituted Thiazolidinones Bearing Triazole Moiety." INTERNATIONAL JOURNAL OF PHARMACEUTICAL QUALITY ASSURANCE 15, no. 02 (2024): 796–802. http://dx.doi.org/10.25258/ijpqa.15.2.39.

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Series of thiazolidinone derivatives containing triazole moiety have been synthesized by condensing various substituted aldehydes to form Schiff bases which further reacts with thioglycolic acid undergoes ring condensation to form 3-(3-mercapto-5-((5-methoxy-1H-indol-1-yl)methyl)-4H-1,2,4-triazol-4-yl)-2-substituted phenylthiazolidin-4-one followed by reaction with ethyl chloroacetate to form ethyl 2-((4-(2-subtituted phenyl-4-oxothiazolidin-3-yl)-5-((5-methoxy-1H-indol-1-yl)methyl)-4H-1,2,4-triazol-3-yl)thio)acetate. The synthesized compounds were characterized by elemental analysis, fourier-

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45

Avendaño Leon, Oscar Leonardo, Christophe Curti, Fabiana Maia Santos Urbancg Moncorvo, et al. "Diethyl (5-Benzyl-2-(4-(N′-hydroxycarbamimidoyl)phenyl)-5-methyl-4,5-dihydrofuran-3-yl)phosphonate." Molbank 2023, no. 4 (2023): M1736. http://dx.doi.org/10.3390/m1736.

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As part of our ongoing research into the antileishmanial properties of amidoxime derivatives, we report a preliminary assessment of the antiparasitic properties of a novel compound, diethyl (5-benzyl-2-(4-(N′-hydroxycarbamimidoyl)phenyl)-5-methyl-4,5-dihydrofuran-3-yl)phosphonate. This compound was evaluated in vitro for the first time against the promastigote form of Leishmania amazonensis. Compounds containing both amidoxime and phosphonyl functional groups in dihydrofuran scaffolds are relatively rare, despite the extensive study of this heterocycle in various biological applications. There

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46

Vandresen, Fabio, Sabrina Alencar de Almeida-Batista, Maria Eduarda Bueno Caldeira, et al. "Antitumor and antileishmanial activities of limonene-thiosemicarbazones bearing heterocycles nucleous." Research, Society and Development 11, no. 5 (2022): e11711528152. http://dx.doi.org/10.33448/rsd-v11i5.28152.

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In the present study, we provided the synthesis of a series of R-(+)- and S-(-)-limonene-based thiosemicarbazones containing different pentacyclic heterocyclic nucleus moiety focused in the search of novel antitumor and antileishmanial agents. In the antitumor assay, the derivative imidazole of S-(-)-limonene 8 was the most active compound, especially for U-251, UACC-62 and K562 human tumor cell lines with GI50 ranging from 1.0 to <0.25 µg.mL-1. On the other hand, the imidazole-thiosemicarbazone of R-(+)-limonene 4 was the most promising derivative against the promastigote form of L. amazon

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47

Soni, Hetal I., and Navin B. Patel. "PYRIMIDINE INCORPORATED SCHIFF BASE OF ISONIAZID WITH THEIR SYNTHESIS, CHARACTERIZATION AND IN VITRO BIOLOGICAL EVALUATION." Asian Journal of Pharmaceutical and Clinical Research 10, no. 10 (2017): 209. http://dx.doi.org/10.22159/ajpcr.2017.v10i10.19302.

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Objective: Versatile biological activities of nitrogen containing heterocycles in medicinal chemistry, mainly pyrimidine and pyridine ring based heterocyclic moieties are very important. Pharmaceutical important of pyrimidine and isoniazid moiety prompted us to synthesize isoniazid clubbed pyrimidine derivatives and evaluated for antimicrobial and antituberculosis activity.Method: 2-(2-(3-bromo benzylidene)-1-isonicotinoyl hydrazinyl)-N-(4-(substituted phenyl)-6-(substituted aryl) pyrimidin-2-yl) acetamide 2(A-J) have been synthesized by condensation reaction of 2-chloro-N-[4-(substituted phen

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Samorodov, Aleksandr V., Wang Yi, Dmitry A. Kudlay, et al. "Phosphorus-Derived Isatin Hydrazones: Synthesis, Structure, Thromboelastography, Antiplatelet, and Anticoagulation Activity Evaluation." International Journal of Molecular Sciences 26, no. 13 (2025): 6147. https://doi.org/10.3390/ijms26136147.

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A series of new isatin hydrazones bearing phosphorus-containing moiety was synthesized through a simple, high-yield and easy work-up reaction of phosphine oxide (Phosenazide) or phosphinate (2-chloroethyl (4-(dimethylamino)phenyl)(2-hydrazinyl-2-oxoethyl)phosphinate, CAPAH) hydrazides with aryl-substituted isatins. The 31P NMR technique showed that, in most cases, out of 12 examples in solution, the ratio of the two spatial isomers varied from 1:1 to 1:3. Quantum chemical calculations confirmed the predominance of Z,syn form both in the gas phase and in solution. According to X-ray analysis da

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49

Charoensutthivarakul, Sitthivut, Duangporn Lohawittayanan, Phongthon Kanjanasirirat, et al. "Rational Design and Lead Optimisation of Potent Antimalarial Quinazolinediones and Their Cytotoxicity against MCF-7." Molecules 28, no. 7 (2023): 2999. http://dx.doi.org/10.3390/molecules28072999.

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Quinazolinedione is one of the most outstanding heterocycles in medicinal chemistry thanks to its wide ranges of biological activities including antimalarial, anticancer, and anti-inflammatory. TCMDC-125133 containing a quinazolinedione pharmacophore displays promising antimalarial activity and low toxicity, as described in the GlaxoSmithKline (GSK) report. Herein, the design and synthesis of novel quinazolinedione derivatives is described on the basis of our previous work on the synthesis of TCMDC-125133, where low-cost chemicals and greener alternatives were used when possible. The initial S

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Lelyukh, Maryan, Halyna Halevych, Maria Zhukrovska, Olga n. Semiion-Luchyshyn, and Myroslava Kalytovska. "Synthesis of 5-aryl/heterylidene substituted 2-imino-4-thiazolidinones possessing 1,3,4-thiadiazole moiety and their antitrypanosomal activity." Current Chemistry Letters 12, no. 2 (2023): 413–20. http://dx.doi.org/10.5267/j.ccl.2022.11.005.

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A novel 1,3,4-thiadiazole containing 2-iminothiazolidine-4-ones 4a-b were synthesized through the reaction of 2-chloro-N-(5-ethyl/allylsulfanyl-[1,3,4]thiadiazol-2-yl)-acetamides 1a-b with ammonium thiocyanate in dry acetone. Condensation of 4a-b with various carbonyl compounds according to the standard Knoevenagel procedure yielded the corresponding 5-arylidene- (5a-d), 5-heterylidene- (6a-c), 5-isatinylidene- (7a-b) and 5-(3-phenyl-2-propene-1-ylidene)- (8a-b) derivatives. All the newly synthesized compounds were confirmed by their elemental analysis and spectral data. Synthesized compounds

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