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Journal articles on the topic 'N-(2-(hydrazinecarbonyl) phenyl) benzamide derivatives'

Author: Grafiati

Published: 5 June 2025

Last updated: 2 August 2025

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1

Charanjeet, Singh, Yaswant, and Sharma Mukesh. "SYNTHESIS AND ASSESSMENT THE IN-VITRO ANTIOXIDANT ACTIVITY OF 2,3-DISUBTITUTED QUINAZOLIN-4(3H)-ONE DERIVATIVES." International Journal of Current Pharmaceutical Review and Research 12, no. 2 (2020): 01–11. https://doi.org/10.5281/zenodo.12667459.

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Quinazolinones have various biological activities such as anticancer, antibacterial,antidiabetic, anticonvulsant, antihistaminic, antiinflammatory, antifungal, anthelmintics andantiviral activities. In this research some of compounds 2,3-disubtituted quinazolin-4(3H)-one derivatives had been synthesized under microwave irradiation. The compounds wereobtained from reaction some of benzoxazine derivatives with hydrazine hydrate usingmicrowave irradiation and the result of reaction we obtained 82-96%. The products had beentested by IR, 1H-NMR, 13C-NMR and Mass Spectroscopy analysis. The using mic

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2

Sulistyowaty, Melanny Ika, Galih Satrio Putra, Tutuk Budiati, and Katsuyoshi Matsunami. "Synthesis, In Vitro Anticancer Activity and In Silico Study of some Benzylidene Hydrazide Derivatives." Key Engineering Materials 840 (April 2020): 277–83. http://dx.doi.org/10.4028/www.scientific.net/kem.840.277.

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Some benzylidenehydrazides (3a-e) have been synthesized in three reaction steps from anthranilic acid in good yields, about 70% - 99%. The structures of the synthesized compounds were analyzed using spectroscopic methods. The compounds were evaluated its activity against human lung cancer, A549 cell line by MTT method and studied its molecular docking onto the protein tyrosine kinase (PDB ID: 1M17) by using Molegro® vs. 5.5. The data showed that N-(2-(2-(4-nitrobenzylidene)hydrazinecarbonyl)phenyl)benzamide (3d) which synthesized in 70% yield and has the highest activity on inhibiting the grow

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3

Elkaeed, Eslam B., Reda G. Yousef, Hazem Elkady, et al. "Design, Synthesis, Docking, DFT, MD Simulation Studies of a New Nicotinamide-Based Derivative: In Vitro Anticancer and VEGFR-2 Inhibitory Effects." Molecules 27, no. 14 (2022): 4606. http://dx.doi.org/10.3390/molecules27144606.

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A nicotinamide-based derivative was designed as an antiproliferative VEGFR-2 inhibitor with the key pharmacophoric features needed to interact with the VEGFR-2 catalytic pocket. The ability of the designed congener ((E)-N-(4-(1-(2-(4-benzamidobenzoyl)hydrazono)ethyl)phenyl)nicotinamide), compound 10, to bind with the VEGFR-2 enzyme was demonstrated by molecular docking studies. Furthermore, six various MD simulations studies established the excellent binding of compound 10 with VEGFR-2 over 100 ns, exhibiting optimum dynamics. MM-GBSA confirmed the proper binding with a total exact binding ene

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4

Mohamed, Shaaban K., Joel T. Mague, Mehmet Akkurt, Herman Potgieter, and Mustafa R. Albayati. "A new polymorph ofN-(2-{N′-[(1E)-2-hydroxybenzylidene]hydrazinecarbonyl}phenyl)benzamide." Acta Crystallographica Section E Structure Reports Online 70, no. 6 (2014): o645—o646. http://dx.doi.org/10.1107/s1600536814010010.

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The title compound, C21H17N3O3, is a new polymorph of an already published structure [Shashidharet al.(2006).Acta Cryst.E62, o4473–o4475]. The previously reported structure crystallizes in the monoclinic space groupC2/c, whereas the structure reported here is in the tetragonal space groupI41/a. The bond lengths and angles are similar in both structures. The molecule adopts an extended conformationviaintramolecular N—H...O and O—H...N hydrogen bonds; the terminal phenyl ring and the hydroxylphenyl ring are twisted with respect to the central benzene ring by 44.43 (7) and 21.99 (8)°, respectivel

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5

Ienascu, Ioana Maria Carmen, Tiberius Balaes, Cristiana Virginia Petre, et al. "Novel N-(2-bromo-phenyl)-2-hydroxy-benzamide Derivatives with Antifugal Activity." Revista de Chimie 69, no. 7 (2018): 1876–80. http://dx.doi.org/10.37358/rc.18.7.6435.

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In order to increase the biological activity, some novel molecules, esters, hydrazides, hydrazones of N-(2-bromo-phenyl)-2-hydroxy-benzamide, were obtained in good yields (86-93%), working at 150 �C, 500 W, 7-11 min, under microwave irradiation. All synthesized compounds were characterized using modern physico-chemical methods (FTIR, 1H-NMR, 13C-NMR and elemental analysis). Eight dilutions in dimethyl sulfoxide of these derivatives were tested against two phyto-pathogenic fungi, Fusarium oxysporum, Sclerotinia sclerotiorum and one common yeast, Saccharomyces cerevisiae. The antifungal activity

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6

Nagarsha, K. M., T. M. Sharanakumar, D. Ramesh, et al. "NOVEL SYNTHESIS, CHARACTERIZATION AND ANTIMICROBIAL ACTIVITY OF N-(5BROMO-2-(5-PHENYL1,3,4-OXADIAZOL-2-YL)NAPHTHA[2,1-B]FURAN-1- YL)ACETAMIDE AND N-(5-NITRO-2-(5-PHENYL-1,3,4- OXADIAZOL-2-YL)NAPHTHA[2,1-BFURAN-1-YL]ACETAMIDE AND THEIR DERIVATIVES." RASAYAN Journal of Chemistry 16, no. 01 (2023): 167–75. http://dx.doi.org/10.31788/rjc.2023.1618088.

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The novel derivatives of naphtho-furan such N-(5bromo-2-(5-phenyl-1,3,4-oxadiazol-2-yl)naphtha[2,1-b]furan-1- yl)acetamide (8), N-(5-bromo-2-(hydrazinecarbonyl)naphtha[2,1-b]furan-1-yl]acetamide (7), ethyl-1-acetamido-5- bromonaphtho[2,1-b]furan-2-carboxylate (6), N-(5-nitro-2-(5-phenyl-1,3,4-oxadiazol-2-yl)naphtha[2,1-bfuran-1- yl]acetamide (5),N-(2-(hydrazinecarbonyl)-5-nitronaphtho[2,1-b]furan-1-yl)acetamide (4), ethyl-1-acetamido-5- nitrpnaphtho[2,1-b]furan-2-carboxylate (3), are prepared by ethyl-1-acetamidonaphtho[2,1-b]furan-2-carboxyate and ethyl 1-aminonaphtho[2,1-b]furan-2-carboxylat

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7

Ienascu, Ioana Maria Carmen, Diana Obistioiu, Iuliana Maria Popescu, et al. "In Vitro Testing of Salicylanilide Derivatives Against Some Fungal and Bacterial Strains." Revista de Chimie 70, no. 4 (2019): 1496–99. http://dx.doi.org/10.37358/rc.19.4.7157.

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In the dental office, disinfection and sterilization are a matter of utmost importance for both the physician, the medical staff and the patient. Twelve N-(2-bromo-phenyl)-2-hydroxy-benzamide and N-(4-bromo-phenyl)-2-hydroxy-benzamide derivatives were synthesized and tested for antimicrobial activity against 6 bacterial and 2 fungal strains using the Disk diffusion method for susceptibility testing. The obtained results indicated that the N-(2-bromo-phenyl)-2-hydroxy-benzamide derivatives were more active against the tested microbes, inhibition zones of 6-12 mm being obtained, although the mos

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8

Sawamura, Masaya, Yohei Shimizu, Ryotaro Niizeki, Kosuke Higashida, and Emna Mejri. "Synthesis of C,N,N-Cyclometalated Gold(III) Complexes with Anionic Amide Ligands." Synlett 33, no. 03 (2021): 288–92. http://dx.doi.org/10.1055/a-1673-9236.

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AbstractA series of neutral C,N,N Au(III) complexes were synthesized with N-(8-quinolinyl)benzamide derivatives or chiral N-[2-(1,3-oxazolin-2-yl)phenyl]benzamide derivatives. The convenient synthesis method for the amide ligands, together with their operationally simple complexation by direct C–H auration, permitted changes to both the steric and electronic properties of Au(III) complexes for promoting the catalytic three-component couplings of an aldehyde, an amine, and an alkyne.

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9

Ienascu, Ioana M. c., Alfa X. Lupea, Iuliana M. Popescu, Stefan Th Tomas, and Alina D. Zamfir. "Synthesis and Characterization of Some New 2-Hydroxy-N-(3-Trifluoromethyl-Phenyl)-Benzamide Derivatives." Revista de Chimie 59, no. 1 (2008): 56–60. http://dx.doi.org/10.37358/rc.08.1.1707.

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In the reaction between 2-hydroxy-N-(3-trifluoromethyl-phenyl)-benzamide and chloro-acetic acid ethyl ester, [2-(3-trifluoromethyl-phenylcarbamoyl)-phenoxy]-acetic acid ethyl ester was obtained. The ethyl ester was condensed with hydrazine giving 2-hydrazinocarbonylmethoxy-N-(3-trifluoromethyl-phenyl)-benzamide. This hydrazide is considered the key intermediate for the synthesis of new compounds. So, in the reaction between hydrazide and chloro-substituted benzaldehydes hydrazones were obtained. In order to establish their structures, all new synthesized compounds were analyzed by modern physi

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10

Singh, Sonia, Alireza Hassanabadi, and Mohammad H. Mosslemin. "Synthesis of N-(3-Methyl-4-Phenyl-3H-Selenazol-2-Ylidene)Benzamide Derivatives." Journal of Chemical Research 42, no. 9 (2018): 474–75. http://dx.doi.org/10.3184/174751918x15359643889826.

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A three-component and one-pot reaction between phenacyl bromide and aroyl isoselenocyanates in the presence of methylamine gave N-(3-methyl-4-phenyl-3 H-selenazol-2-ylidene)benzamide derivatives in good yields.

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11

Yang, Huiyong, Jun Xu, Yilan Zhang, Lei He, Pengfei Zhang, and Wanmei Li. "Synthesis of quinazoin-4-ones through an acid ion exchange resin mediated cascade reaction." Organic & Biomolecular Chemistry 18, no. 23 (2020): 4406–14. http://dx.doi.org/10.1039/d0ob00881h.

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We report the use of 2-(2-oxazolyl)aniline to prepare quinazolin-4-one derivatives by an acid ion exchange resin mediated cascade reaction of N-(2-(4,5-dihydrooxazol-2-yl)phenyl)benzamide for the first time.

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12

Konovalova, S. A., A. P. Avdeenko, V. I. Lubenets, O. Z. Komarovska-Porokhnyavets, I. Yu Yakymenko, and E. N. Lysenko. "BIOLOGICAL ACTIVITY OF N-{3-[(4-METHYLBENZENE-1- SULFONYL)IMINO]-6-OXOCYCLOHEXA-1,4-DIEN-1-YL}ARYLAMIDES AND THEIR DERIVATIVES." Odesa National University Herald. Chemistry 26, no. 1(77) (2021): 37–47. http://dx.doi.org/10.18524/2304-0947.2021.1(77).226136.

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N-{3-[(4-Methylbenzene-1-sulfonyl)imino]-6-oxocyclohexa-1,4-dien-1-yl}arylamides and their derivatives were synthesized by the reaction of the corresponding N-(4-oxocyclohexa-2,5-dien-1-ylidene)arylsulfonamides with N-chloramides. The biological activity of the synthesized compounds was studied on test cultures of Escherichia coli 67, Staphylococcus aureus 209-p, Mycobacterium luteum VKM B-868 and fungi Candida tenuis VKM Y-70, Aspergillus niger VKM F-1119 by the method of diffusion of substances into agar on a solid nutrient medium. The degree of activity of the test compounds was determined

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13

Ienașcu, Ioana Maria Carmen, Adina Căta, Antonina Evelina Lazăr, et al. "Antimicrobial and Anti-Inflammatory Activity of N-(2-Bromo-phenyl)-2-hydroxy-benzamide Derivatives and Their Inclusion Complexes." Pharmaceutics 17, no. 7 (2025): 869. https://doi.org/10.3390/pharmaceutics17070869.

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Background/Objectives: In order to enhance the biological activity, novel complexes of N-(2-bromo-phenyl)-2-hydroxy-benzamide derivatives and β-cyclodextrin were obtained. Methods: The inclusion complexes were characterized using spectral and thermal analyses. The antimicrobial activity was determined using the disk diffusion agar method, and completed with the minimum inhibitory concentration (MIC) values obtained by the broth microdilution method. The in vitro anti-inflammatory activity was evaluated using the protease inhibition assay. Results: The computed supramolecular architectures of t

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14

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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15

Tran Hoai Tu, Nguyen Trung Nhan, and Dang Hoang Phu. "Synthesis of benzamide derivatives and evaluation of their in vitro and in silico tyrosinase inhibitory activities." Vietnam Journal of Science and Technology 62, no. 4 (2024): 660–69. http://dx.doi.org/10.15625/2525-2518/18302.

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In this research, six benzamide derivatives were traditionally synthesized using hydrazine, carbazide, and hydroxylamine derivatives through the pre- or in situ activation of the carboxylic acid functionality. Their chemical structures were identified as N′-phenylbenzohydrazide, N′-(2,4-dinitrophenyl)benzohydrazide, N′-(benzoyloxy)benzamide, N-dibenzoylurea, 2-amino-5-(4-phenyl)-1,3,4-thiadiazole, and benzohydrazide based on the interpretation of NMR spectroscopic data. Among these products, N′-phenylbenzohydrazide and N-(benzoyloxy)benzamide showed potent tyrosinase inhibitory activity with t

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16

Laskowska, Anna, Agata J. Pacuła-Miszewska, Magdalena Obieziurska-Fabisiak та ін. "Synthesis of New Chiral β-Carbonyl Selenides with Antioxidant and Anticancer Activity Evaluation—Part I". Materials 17, № 4 (2024): 899. http://dx.doi.org/10.3390/ma17040899.

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A series of unsymmetrical phenyl β-carbonyl selenides with o-amido function substituted on the nitrogen atom with chiral alkyl groups was obtained. The compounds form a series of enantiomeric and diastereomeric pairs and present the first examples of this type of chiral Se derivatives. All obtained selenides were further evaluated as antioxidants and anticancer agents to define the influence of the particular stereochemistry of the attached functional groups on the bioactivity of the molecules. The highest H2O2 reduction potential was observed for N-(cis-2-hydroxy-1-indanyl)-2-((2-oxopropyl)se

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17

Jabber, Mohammed Muhsin, and mohammed k. Hadi. "Synthesis, Characterization, and Antimicrobial Evaluation of new Ibuprofen Derivatives." Pakistan Journal of Medical and Health Sciences 16, no. 3 (2022): 689–92. http://dx.doi.org/10.53350/pjmhs22163689.

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A new series of ibuprofen derivatives were synthesized and tested against the microbial activity. P_amino ethyl benzoate (compound I) was prepared, then coupled with ibuprofen acyl chloride (compound II) to give ethyl 4-(2-(4-isobutylphenyl) propanamido) benzoate (compounds III). Hydrazine hydrate 99% was added to compound III to synthesized N-(4-(hydrazinecarbonyl) phenyl)-2-(4-isobutylphenyl) propenamide (compound IV). Finally compound IV coupled with different aldehydes (1. Benzaldehyde (Va) 2. Salicylaldehyde (Vb) 3. 4_hydroxybenzaldehyde (Vc) 4. Vanillin (Vd) respectively to form target c

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18

Avunoori, Sravanthi, Mater H. Mahnashi, Ibrahim Ahmed Shaikh, et al. "Synthesis and in silico studies of some new pyrrolyl benzamides as antitubercular agents." INDIAN JOURNAL OF HETEROCYCLIC CHEMISTRY 35, no. 02 (2025): 255. https://doi.org/10.59467/ijhc.2025.35.255.

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A new series of pyrrolyl benzamide derivatives (3a-3j) and Schiff base 4 were synthesized by reacting N-(2,5-dimethyl-1H-pyrrol-1-yl)-4-(2-hydrazenyl-2-oxoethoxy)benzamide (1) with substituted phenylacetic acids (2a-2j) and indole-3-carbaldehyde, respectively. Molecular docking was performed for these synthesized compounds against the InhA and dihydrofolate reductase (DHFR) mycobacterial enzymes. The compounds were biologically screened for antimycobacterial and antibacterial activities along with InhA and DHFR enzyme inhibition studies. The compounds were also analyzed for absorption, distrib

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19

Pandya, Dhananjay, and Yogesh Naliapara. "Microwave-Assisted C-N Coupling for the Synthesis of 2-(2H-1,2,3-Triazol-2-yl)benzoic Acid Scaffold and Novel N-Phenyl-2-(2H-1,2,3-triazol-2-yl)benzamide Derivatives." Asian Journal of Organic & Medicinal Chemistry 4, no. 3 (2019): 189–93. http://dx.doi.org/10.14233/ajomc.2019.ajomc-p211.

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We report a novel methodology for the efficient and rapid synthesis of core intermediate 2-(2H-1,2,3- triazol-2-yl)benzoic acid using trans-N,N’-dimethylcyclohexane-1,2-diamine as a catalyst and copper iodide as co-catalyst under microwave irradiations and a series of novel N-phenyl-2-(2H-1,2,3-triazol- 2-yl)benzamide derivatives via acid-amine coupling reaction using DCC as a dehydrating agent and DMAP as a base. In comparison to the conventional heating procedure and performing the reaction using different combinations of catalysts and bases, the time of synthesis and efforts are significant

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20

Fedotov, S. O., and A. S. Hotsulia. "Evaluation of the pharmacological potential of N-((5-phenyl-6,11-dihydro-[1,2,4]triazolo[1’,5’:1,6]pyrido[3,4-b]indol-2-yl)methyl)benzamides." Current issues in pharmacy and medicine: science and practice 18, no. 2 (2025): 148–59. https://doi.org/10.14739/2409-2932.2025.2.328643.

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The rational design of new biologically active compounds is based on the use of effective structural fragments, capable of ensuring high biosimilarity, favorable pharmacokinetic properties and an appropriate safety profile. Among them, 1,2,4-triazole and indole cores occupy a special place, being widely represented in pharmacologically active molecules due to their ability to participate in various types of molecular interactions. The combination of 1,2,4-triazole and indole fragments within a single molecule promotes the creation of conjugated systems with potentially multifunctional activity

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21

Lutsenko, R. V., V. N. Bobyrev, and T. A. Devyatkina. "Anxiolytic effect of 2-oxyindolin-3-glyoxylic acid derivatives: computer prediction and experimental confirmation." Kazan medical journal 94, no. 4 (2013): 553–60. http://dx.doi.org/10.17816/kmj1970.

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Aim. To complete the computer prediction of possible spectrum of biological activity of simple amides of 2-oxyindolin-3-glyoxylic acid derivatives and to test their anxiolytic activity in experiment. Methods. The prediction of possible spectrum of biological activity of simple amides of 2-oxyindolin-3-glyoxylic acid derivatives was performed using PASS (Prediction of Activity Spectra for Substances) software. The experimental part was performed on 140 adult rats of both sexes. Animals were distributed to subgroups (n=10 in each subgroup) according to age and gender. Experimental screening for

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22

Chen, Taiping, Hongwu Jiang, Jianjun Zhou, et al. "Synthesis of N-Substituted Benzamide Derivatives and their Evaluation as Antitumor Agents." Medicinal Chemistry 16, no. 4 (2020): 555–62. http://dx.doi.org/10.2174/1573406415666190712120611.

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Background: Histone deacetylases inhibitors (HDACIs) with different chemical structures have been reported to play an important role in the treatment of cancer. Objective: The study aims to modify the structure of Entinostat (MS-275) to discover new compounds with improved anti-proliferative activities and perform SAR studies on this class of bioactive compounds. Methods: Fourteen N-substituted benzamide derivatives were synthesized and their antiproliferative activities were tested with four cancer cell lines (MCF-7, A549, K562 and MDA-MB- 231) by MTT assay. Results: Compared with MS-275, six

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23

Sun, Ming, Na Lv, Zeng Li, Qiru Xiong, Liang Xu, and Zongsheng Yin. "N-(4-(quinazolin-2-yl)phenyl)benzamide derivatives with potent anti-angiogenesis activities: synthesis and evaluation." Journal of the Iranian Chemical Society 13, no. 4 (2015): 753–61. http://dx.doi.org/10.1007/s13738-015-0788-4.

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24

Wadhwa, Pankaj, Priti Jain, Arpit Patel, Shantanu Shinde, and Hemant R. Jadhav. "Synthesis and Evaluation of 3-(1,3-dioxoisoindolin-2-yl)-N-substituted Phenyl Benzamide Analogues as HIV Integrase Strand Transfer Inhibitors." Anti-Infective Agents 17, no. 2 (2019): 105–14. http://dx.doi.org/10.2174/2211352516666181102121920.

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<P>Background: A series of novel 3-(1,3-dioxoisoindolin-2-yl)-N-substituted phenyl benzamide derivatives was synthesized and tested in vitro against human immunodeficiency virus type-1 Integrase (HIV-1 IN). Methods: Out of the 18 analogues, six (compounds 16c, 16h, 16i, 16m, 16n and 16r) showed significant inhibition of strand transfer by HIV-1 integrase. For these six compounds. IC50 was below 5.0 µM. In silico docking studies revealed that the presence of 2-phenyl isoindoline-1,3-dione motif was essential as it was found to interact with active site magnesium. Results: To further confi

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Obieziurska-Fabisiak, Magdalena, Agata J. Pacuła, Lucia Capoccia, et al. "Phenylselanyl Group Incorporation for “Glutathione Peroxidase-Like” Activity Modulation." Molecules 25, no. 15 (2020): 3354. http://dx.doi.org/10.3390/molecules25153354.

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The ability of organoselenium molecules to mimic the activity of the antioxidant selenoenzyme glutathione peroxidase (GPx) allows for their use as antioxidant or prooxidant modulators in several diseases associated with the disruption of the cell redox homeostasis. Current drug design in the field is partially based on specific modifications of the known Se-therapeutics aimed at achieving more selective bioactivity towards particular drug targets, accompanied by low toxicity as the therapeutic window for organoselenium compounds tends to be very narrow. Herein, we present a new group of Se-bas

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Xu, Yong-Jiang, Hua-Quan Miao, Weitao Pan, et al. "N-(4-{[4-(1H-Benzoimidazol-2-yl)-arylamino]-methyl}-phenyl)-benzamide derivatives as small molecule heparanase inhibitors." Bioorganic & Medicinal Chemistry Letters 16, no. 2 (2006): 404–8. http://dx.doi.org/10.1016/j.bmcl.2005.09.070.

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27

Nimbalkar, Urja, Julio Seijas, Rachna Borkute, et al. "Ultrasound Assisted Synthesis of 4-(Benzyloxy)-N-(3-chloro-2-(substitutedphenyl)-4-oxoazetidin-1-yl) Benzamide as Challenging Anti-Tubercular Scaffold." Molecules 23, no. 8 (2018): 1945. http://dx.doi.org/10.3390/molecules23081945.

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A series of ten novel derivatives of 4-(benzyloxy)-N-(3-chloro-2-(substituted phenyl)-4-oxoazetidin-1-yl) benzamide 6a–j were synthesized in good yield from the key compound 4-(benzyloxy)-N′-(substituted benzylidene) benzo hydrazide, called Schiff ’s bases 5a–j, by Staudinger reaction ([2 + 2] ketene-imine cycloaddition reaction) with chloro acetyl chloride in the presence of catalyst tri ethylamine and solvent dimethyl formamide (DMF), by using ultra-sonication as one of the green chemistry tools. All the synthesised compounds were evaluated for in vitro anti-tubercular activity against Mycob

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28

Wei, Lai, Tao Hou, Chang Lu, et al. "SAR Studies of N-[2-(1H-Tetrazol-5-yl)phenyl]benzamide Derivatives as Potent G Protein-Coupled Receptor-35 Agonists." ACS Medicinal Chemistry Letters 9, no. 5 (2018): 422–27. http://dx.doi.org/10.1021/acsmedchemlett.7b00510.

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29

Szczesio, Małgorzata, Andrzej Olczak, Katarzyna Gobis, Henryk Foks, and Marek L. Główka. "Planarity of benzoylhydrazine–dithiocarbazoate tuberculostatics. I.N′-Methyl-substituted 3,4-dichlorobenzoyl monoesters." Acta Crystallographica Section C Crystal Structure Communications 68, no. 10 (2012): o373—o376. http://dx.doi.org/10.1107/s0108270112036001.

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Methyl 2-(3,4-dichlorobenzoyl)-1-methylhydrazinecarbodithioate, C10H10Cl2N2OS2, (F1), butyl 2-(3,4-dichlorobenzoyl)-1-methylhydrazinecarbodithioate, C13H16Cl2N2OS2, (F2), and 3,4-dichloro-N-(2-sulfanylidene-1,3-thiazinan-3-yl)benzamide, C11H10Cl2N2OS2, (F3), were studied by X-ray diffraction to test our hypothesis that planarity of aryloylhydrazinedithiocarbazic acid esters is a prerequisite for tuberculostatic activity. All compounds examined in this study are inactive and nonplanar due to twists along two specific bonds in the central frame of the molecules. The significant twist at the N—N

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Iliş, Monica, Marilena Ferbinteanu, Cristina Tablet, and Viorel Cîrcu. "Investigation of Mechanochromic and Solvatochromic Luminescence of Cyclometalated Heteroleptic Platinum(II) Complexes with Benzoylthiourea Derivatives." Molecules 30, no. 11 (2025): 2415. https://doi.org/10.3390/molecules30112415.

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Two novel cyclometalated platinum(II) complexes based on 2-phenylpyridine (ppy) and 2,4-difluorophenylpyridine (dfppy) ligands in combination with a benzoylthiourea (4-(decyloxy)-N-((4-(decyloxy)phenyl)carbamothioyl)benzamide, BTU) functionalized with decyloxy alkyl chains as auxiliary ligands were synthesized and characterized for their mechanochromic and photophysical properties. Structural characterization was achieved through IR and NMR spectroscopy, single-crystal X-ray diffraction, and TD-DFT calculations. Both complexes exhibit significant photoluminescence with quantum yields up to 28.

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

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

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Bonache, María Ángeles, Pedro Juan Llabrés, Cristina Martín-Escura та ін. "Phenylalanine-Derived β-Lactam TRPM8 Modulators. Configuration Effect on the Antagonist Activity". International Journal of Molecular Sciences 22, № 5 (2021): 2370. http://dx.doi.org/10.3390/ijms22052370.

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Transient receptor potential cation channel subfamily M member 8 (TRPM8) is a Ca2+ non-selective ion channel implicated in a variety of pathological conditions, including cancer, inflammatory and neuropathic pain. In previous works we identified a family of chiral, highly hydrophobic β–lactam derivatives, and began to intuit a possible effect of the stereogenic centers on the antagonist activity. To investigate the influence of configuration on the TRPM8 antagonist properties, here we prepare and characterize four possible diastereoisomeric derivatives of 4-benzyl-1-[(3′-phenyl-2′-dibenzylamin

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Su, Qing, Baolin Xu, Zhoubin Tian, and Ziling Gong. "Design and development of novel 1,2,3-triazole chalcone derivatives as potential anti-osteosarcoma agents via inhibition of PI3K/Akt/mTOR signalling pathway." Acta Pharmaceutica 72, no. 3 (2022): 389–402. http://dx.doi.org/10.2478/acph-2022-0026.

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Abstract Osteosarcoma (OS) is an uncommon tumour that mainly affects bone in children and adolescents. The current treatment options of OS are of limited significance due to their immense side effects. In the present manuscript, we have developed a novel series of 1,2,3-triazole chalcone derivatives as potential agents against OS. The compounds were synthesized and evaluated for their PI3K and mTOR inhibitory activity using luminescent kinase assay, and Lance ultra assay, resp. The entire set of compounds showed significant to moderate inhibition of both kinases in the nanomolar range. The thr

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Balewski, Łukasz, Franciszek Sączewski, Patrick J. Bednarski, et al. "Synthesis, Structure and Cytotoxicity Testing of Novel 7-(4,5-Dihydro-1H-imidazol-2-yl)-2-aryl-6,7-dihydro-2H-imidazo[2,1-c][1,2,4]triazol-3(5H)-Imine Derivatives." Molecules 25, no. 24 (2020): 5924. http://dx.doi.org/10.3390/molecules25245924.

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The appropriate 1-arylhydrazinecarbonitriles 1a–c are subjected to the reaction with 2-chloro-4,5-dihydro-1H-imidazole (2), yielding 7-(4,5-dihydro-1H-imidazol-2-yl)-2-aryl-6,7-dihydro-2H-imidazo[2,1-c][1,2,4]triazol-3(5H)-imines 3a–c, which are subsequently converted into the corresponding amides 4a–e, 8a–c, sulfonamides 5a–n, 9, ureas 6a–I, and thioureas 7a–d. The structures of the newly prepared derivatives 3a–c, 4a–e, 5a–n, 6a–i, 7a–d, 8a–c, and 9 are confirmed by IR, NMR spectroscopic data, as well as single-crystal X-ray analyses of 5e and 8c. The in vitro cytotoxic potency of these comp

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Jiang, Cheng-Shi, Yong-Xi Ge, Zhi-Qiang Cheng та ін. "Discovery of New Selective Butyrylcholinesterase (BChE) Inhibitors with Anti-Aβ Aggregation Activity: Structure-Based Virtual Screening, Hit Optimization and Biological Evaluation". Molecules 24, № 14 (2019): 2568. http://dx.doi.org/10.3390/molecules24142568.

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In this study, a series of selective butyrylcholinesterase (BChE) inhibitors was designed and synthesized from the structural optimization of hit 1, a 4-((3,4-dihydroisoquinolin-2(1H)-yl)methyl)benzoic acid derivative identified by virtual screening our compound library. The in vitro enzyme assay results showed that compounds 9 ((4-((3,4-dihydroisoquinolin-2(1H)-yl)methyl)phenyl)(pyrrolidin-1-yl)methanone) and 23 (N-(2-bromophenyl)-4-((3,4-dihydroisoquinolin-2(1H)-yl)methyl)benzamide) displayed improved BChE inhibitory activity and good selectivity towards BChE versus AChE. Their binding modes

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Martín-Escura, Cristina, M. Ángeles Bonache, Jessy A. Medina та ін. "β-Lactam TRPM8 Antagonists Derived from Phe-Phenylalaninol Conjugates: Structure–Activity Relationships and Antiallodynic Activity". International Journal of Molecular Sciences 24, № 19 (2023): 14894. http://dx.doi.org/10.3390/ijms241914894.

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The protein transient receptor potential melastatin type 8 (TRPM8), a non-selective, calcium (Ca2+)-permeable ion channel is implicated in several pathological conditions, including neuropathic pain states. In our previous research endeavors, we have identified β-lactam derivatives with high hydrophobic character that exhibit potent and selective TRPM8 antagonist activity. This work describes the synthesis of novel derivatives featuring C-terminal amides and diversely substituted N′-terminal monobenzyl groups in an attempt to increase the total polar surface area (TPSA) in this family of compo

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Santos, Jean Leandro, Ednir Vizioli de Oliveira, Maria Elisa Lopes Pires, Thais Regina Ferreira de Melo, Fernando Ferreira Costa, and Chung Man Chin. "Aspirin Hybrid Molecules with Improved Antiplatelet Properties Designed As New Drug Candidates to Prevent Atherothrombosis,." Blood 118, no. 21 (2011): 3364. http://dx.doi.org/10.1182/blood.v118.21.3364.3364.

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Abstract Abstract 3364 Introduction. Platelets are involved in atherothrombosis as a consequence of their inappropriate and sustained activation, being thus considered an important target for pharmacological interventions. Aspirin (ASA) is the current drug standard of care of most patients; however the therapy is limited and presents several inconveniences such as lack of effectiveness and bleeding. The use of hybridization strategy allows obtaining compounds with pharmacokinetic and pharmacodynamic properties improved. In this work, we describe new compounds with significant antiplatelet acti

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Hassanabadi, Alireza. "Synthesis of N-(3-alkyl-4-phenyl-3H-thiazol-2-ylidene)Benzamide Derivatives by Reaction of Phenacyl Bromide and Aroyl Isothiocyanates in the Presence of Primary Amines." Journal of Chemical Research 37, no. 6 (2013): 331–32. http://dx.doi.org/10.3184/174751913x13667104816225.

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Hassanabadi, Alireza. "ChemInform Abstract: Synthesis of N-(3-Alkyl-4-phenyl-3H-thiazol-2-ylidene)benzamide Derivatives by Reaction of Phenacyl Bromide and Aroyl Isothiocyanates in the Presence of Primary Amines." ChemInform 44, no. 51 (2013): no. http://dx.doi.org/10.1002/chin.201351150.

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Ríos Martínez, Carlos H., Florence Miller, Kayathiri Ganeshamoorthy, et al. "A New NonpolarN-Hydroxy Imidazoline Lead Compound with Improved Activity in a Murine Model of Late-Stage Trypanosoma brucei brucei Infection Is Not Cross-Resistant with Diamidines." Antimicrobial Agents and Chemotherapy 59, no. 2 (2014): 890–904. http://dx.doi.org/10.1128/aac.03958-14.

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ABSTRACTTreatment of late-stage sleeping sickness requires drugs that can cross the blood-brain barrier (BBB) to reach the parasites located in the brain. We report here the synthesis and evaluation of four newN-hydroxy and 12 newN-alkoxy derivatives of bisimidazoline leads as potential agents for the treatment of late-stage sleeping sickness. These compounds, which have reduced basicity compared to the parent leads (i.e., are less ionized at physiological pH), were evaluatedin vitroagainstTrypanosoma brucei rhodesienseandin vivoin murine models of first- and second-stage sleeping sickness. Re

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Ighilahriz-Boubchir, Karima, Baya Boutemeur-Kheddis, Cherifa Rabia, Malika Makhloufi-Chebli, Maamar Hamdi, and Artur Silva. "Recyclable Keggin Heteropolyacids as an Environmentally Benign Catalyst for the Synthesis of New 2-Benzoylamino-N-phenyl-benzamide Derivatives under Microwave Irradiations at Solvent-Free Conditions and the Evaluation of Biological Activity." Molecules 23, no. 1 (2017): 8. http://dx.doi.org/10.3390/molecules23010008.

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Qiao, Jennifer X., Tammy C. Wang, Leonard P. Adam, et al. "Triphenylethanamine Derivatives as Cholesteryl Ester Transfer Protein Inhibitors: Discovery of N-[(1R)-1-(3-Cyclopropoxy-4-fluorophenyl)-1-[3-fluoro-5-(1,1,2,2-tetrafluoroethoxy)phenyl]-2-phenylethyl]-4-fluoro-3-(trifluoromethyl)benzamide (BMS-795311)." Journal of Medicinal Chemistry 58, no. 22 (2015): 9010–26. http://dx.doi.org/10.1021/acs.jmedchem.5b01363.

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Friggeri, Laura, Tatiana Y. Hargrove, Zdzislaw Wawrzak та ін. "Sterol 14α-Demethylase Structure-Based Design of VNI ((R)-N-(1-(2,4-Dichlorophenyl)-2-(1H-imidazol-1-yl)ethyl)-4-(5-phenyl-1,3,4-oxadiazol-2-yl)benzamide)) Derivatives To Target Fungal Infections: Synthesis, Biological Evaluation, and Crystallographic Analysis". Journal of Medicinal Chemistry 61, № 13 (2018): 5679–91. http://dx.doi.org/10.1021/acs.jmedchem.8b00641.

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Beksac, Meral, Pinar Ataca, Berna Atesagaoglu, et al. "Expression and in Vitro Binding of Protease Activated Receptor1 (PAR1) with Novel Anti-PAR1 Molecules: Data on Fresh Myeloma Marrow Plasma Cells and Human Myeloma Cell Lines." Blood 126, no. 23 (2015): 4440. http://dx.doi.org/10.1182/blood.v126.23.4440.4440.

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Abstract Introduction and Aim: Myeloma plasma cells are dependent on stromal support which is mediated through cell adhesion. Heparanase activity has been shown to be associated with aggressive behavior or Bortezomib resistance and can lead to increased levels of proteases as well as shedding of heparan sulfate proteoglycan syndecan-1(CD138) from myeloma cells. We have recently published in vivo anti-myeloma effects of low molecular weight heparin (Beksac et al Acta Haematol 2015). Protease activated Receptor (PAR1) is a thrombin receptor. PAR1 gene and antigen expression on myeloma patient sa

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Wu, Wenneng, Wenjun Lan, Chenyan Wu, and Qiang Fei. "Synthesis and Antifungal Activity of Pyrimidine Derivatives Containing an Amide Moiety." Frontiers in Chemistry 9 (July 12, 2021). http://dx.doi.org/10.3389/fchem.2021.695628.

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In this study, 17 novel pyrimidine derivatives containing an amide moiety were synthesized. Then their in vitro antifungal activities against Botryosphaeria dothidea (B. dothidea), Phomopsis sp., and Botrytis cinereal (B. cinereal) were determined. A preliminary biological test showed that compounds 5-bromo-2-fluoro-N-(2-((2-methyl-6-(trifluoromethyl)pyrimidin-4-yl)oxy)phenyl)benzamide (5f) and 5-bromo-2-fluoro-N-(3-((2-methyl-6-(trifluoromethyl)pyrimidin-4-yl)oxy)phenyl)benzamide (5o) exhibited higher antifungal activity against Phomopsis sp., with an inhibition rate of 100% compared to that

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Bhor, Rohit Jaysing, and Komal Sakharam Sable. "Synthesis; Characterization and Anti-inflammatory Activity of N'-{4-[2-(1H-benzimidazol-2-YL)-2-oxoethyl] phenyl}-2-hydroxyacetohydrazide and it’s Derivatives." Asian Journal of Applied Chemistry Research, August 8, 2022, 40–49. http://dx.doi.org/10.9734/ajacr/2022/v11i330260.

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A fundamental structural feature of benzimidazoles, a group of heterocyclic, aromatic compounds, is the fusion of a six-membered benzene ring with a five-membered imidazole moiety. Formic acid, Acetyl chloride, hydrazine hydrate, Benzene-1,2-diol, Glycolic Acid, Benzoyl chloride, Methyl chloride, Ethyl chloride, Benzamide, and other chemicals were utilized in this research study. In this research study different methods were used such as TLC, IR spectra, 1H-NMR, and MS. These derivatives were tested for their anti-inflammatory activity determined by rat-paw- oedema method. It was determined th

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Miao, Hua-Quan, and et al et al. "N-(4-{[4-(1H-Benzoimidazol-2-yl)-arylamino]-methyl}-phenyl)-benzamide Derivatives as Small Molecule Heparanase Inhibitors." ChemInform 37, no. 16 (2006). http://dx.doi.org/10.1002/chin.200616229.

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Abinash, Pandit*1 S.N. Sriharsha1 N. Habeela Jainab1 Praveen P2 Sheshagiri R. Dixit2. "IN SILICO MOLECULAR DOCKING STUDIES ON SOME NOVEL N-SUBSTITUTED SULFONAMIDE ANTHRANILATE HYDROXAMIC ACID DERIVATIVES FOR ITS CYTOTOXIC POTENTIAL AGAINST CANCER MARKERS." September 7, 2020. https://doi.org/10.5281/zenodo.4017326.

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<em>N</em>-Substituted sulfonamide anthranilate hydroxamic acid derivatives have a better binding affinity towards the Matrix Metalloprotease (MMP) enzyme as per the literature. Based on that we have selected the Matrix Metalloprotease-1 (MMP-1) domain of  MMP enzyme and performed the molecular docking studies using the SYBYL X 2.1 software. We have designed fifteen new chemical new entities for the docking studies and among that two chemical entities were found to have better binding affinities towards the MMP-1 target. By studying the total docking scores of all the new chemical entitie

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Rafique, Hummera, Aamer Saeed, Muhammad Naseem, et al. "Efficient Synthesis of Novel N-[4-Methyl-3-(4-(5-phenyl-1,3,4-oxadiazol-2-yl)phenyl)thiazol-2(3H)-ylidene]benzamide Hybrid Ring System as Potential Antibacterial Agents." Medicinal Chemistry 17 (September 23, 2021). http://dx.doi.org/10.2174/1573406417666210923103209.

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Background: Heterocyclic compounds display versatile biological applications, so the aim of this paper was to prepare biologically important heterocycles with enhanced bacterial resistance and to evaluate for their various structural features that are responsible for their biological properties. Objective: The objective was to synthesize bacterial resistance compounds with enhanced antibacterial properties. Method: Ester moiety containing thiazole ring was converted into its hydrazide derivatives. These heterocyclic derivatives were cyclized into another ring oxadiazole; hence a hybrid ring sy

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Khan, Shabnam, Bhanubhai N. Suhagia, Navnit Prajapati, and Divya Teli. "Design, Synthesis and Biological Evaluation of Novel 6‐Amino‐3‐phenyl‐2H‐chromen‐2‐one Derivatives for Polycystic Ovary Syndrome Management." ChemistrySelect 9, no. 38 (2024). http://dx.doi.org/10.1002/slct.202403268.

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AbstractPolycystic Ovary Syndrome (PCOS) is a widespread and complex hormonal disorder occurs in women of reproductive age, characterized by hormonal imbalances and ovarian dysfunction. Current approaches to treating PCOS often address specific symptoms, highlighting the demand for innovative therapeutic agents that can tackle its multifaceted nature. The present study endeavors to investigate the potential of new chromen‐2‐one derivatives in the management of PCOS. A total of 30 derivatives have been synthesized and evaluated for their in vitro inhibitory effects on 5‐α reductase and antioxid

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