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Journal articles on the topic 'Benzamidine derivative'

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1

Eick, Sigrun, Wolfgang Pfister, Uta Stürzebecher, Sigrid Jarema, and Jörg Stürzebecher. "Inhibitors of benzamidine type influence the virulence properties of Porphyromonas gingivalis strains." Acta Biochimica Polonica 50, no. 3 (2003): 725–34. http://dx.doi.org/10.18388/abp.2003_3663.

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Synthetic inhibitors of benzamidine type have been found to have inhibiting effects on arginine specific cysteine proteinases of P. gingivalis. The purpose of our study was to assess the effects of these inhibitors on the virulence properties of two P. gingivalis strains, the reference strain ATCC 33277 and JH16-1, a clinical isolate obtained from a patient with severe periodontitis. The inhibitors tested were pentamidine, benzamidine, three bis-benzamidine derivatives with a pentamidine-related structure, one bis-benzamidine derivative with another structure, and one arginine derivative as a
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2

Sa’ad, Mohammad Auwal, Ramasamy Kavitha, Shivkanya Fuloria, Neeraj Kumar Fuloria, Manickam Ravichandran, and Pattabhiraman Lalitha. "Synthesis, Characterization and Biological Evaluation of Novel Benzamidine Derivatives: Newer Antibiotics for Periodontitis Treatment." Antibiotics 11, no. 2 (2022): 207. http://dx.doi.org/10.3390/antibiotics11020207.

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Periodontal disease (PD) is complex polymicrobial disease which destroys tooth-supporting tissue. Although various synthetic inhibitors of periodontitis-triggering pathogens have been recognized, their undesirable side effects limit their application. Hence, the present study intended to perform the synthesis, characterization, antimicrobial evaluation, and cytotoxicity analysis of novel benzamidine analogues (NBA). This study involved the synthesis of novel imino bases of benzamidine (4a–c), by reacting different aromatic aldehydes with 2-(4-carbamimidoylphenoxy) acetohydrazide (3), which was
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3

Jain, A., M. A. Sa'ad, S. Ugrappa, et al. "Synthesis, Characterization and Biological Evaluation of New Benzamidine Derivatives: Antibiotics for Periimplantitis Causing Pathogen." Asian Journal of Chemistry 35, no. 8 (2023): 1927–31. http://dx.doi.org/10.14233/ajchem.2023.28022.

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Periimplantitis (PI) is complex polymicrobial disease, which destroys implant-supporting tissue. Although facts suggest several synthetic inhibitors of periimplantitis causing bacteria (PCB), but the undesirable side effects of them limits their application. Hence, current investigation was intended to carry out the synthesis, characterization, in vitro antimicrobial evaluation and cytotoxicity (cell viability) analysis of new benzamidine derivatives (NBDs) against periimplantitis causing bacteria. Present study involved synthesis of 2-(4-((4-substituted)carbamothioyl)phenoxy)-N-(4-substituted
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4

Nishimura, Yasuhiko, Wataru Yasui, Kazuhiro Yoshida, Toshiya Matsuyama, Kiyohiko Dohi, and Eiichi Tahara. "A Serine Protease-inhibitory Benzamidine Derivative Inhibits the Growth of Human Colon Carcinoma Cells." Japanese Journal of Cancer Research 83, no. 7 (1992): 723–28. http://dx.doi.org/10.1111/j.1349-7006.1992.tb01972.x.

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5

Kantlehner, Willi, Jochen Mezger, Ralf Kreß, and Wolfgang Frey. "Orthoamide und Iminiumsalze, XCII. Synthese und Reaktionen von Orthoamiden aus ethinylierten Terpenderivatena." Zeitschrift für Naturforschung B 73, no. 7 (2018): 437–55. http://dx.doi.org/10.1515/znb-2018-0011.

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Abstract β-Ionone and camphor were ethynylated to give the alkynols 14, 16, 17 which can be transformed to the alkynolethers 5b, 5i, 5j, 5k, 5l, 5m by treatment with dimethylsulfate and chlorotrimethylsilane, respectively. From the alkynolethers 5h, 5i, 5j/5k, 5l/5m the orthoamide derivatives 4h, 4i, 4j/4k, 4l/4m can be prepared by treatment with N,N,N′,N′,N″,N″-hexamethylguanidinium chloride (8) in the presence of sodium hydride. The orthoamides 4h, 4i react with the sulfonamide 30 under condensation yielding the N-sulfonylated acrylamidines 31, 32. From the orthoamide 4h and p-nitroaniline t
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6

Salchert, Katrin, Marie-Françoise Gouzy, Maja Glorius, Anett Kühn, Mirko Nitschke, and Carsten Werner. "Immobilization of an anticoagulant benzamidine derivative: Effect of spacer arms and carrier hydrophobicity on thrombin binding." Acta Biomaterialia 1, no. 4 (2005): 441–49. http://dx.doi.org/10.1016/j.actbio.2005.04.001.

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7

Letari, Ornella, Catherine Booth, Albino Bonazzi, et al. "Efficacy of CR3294, a new benzamidine derivative, in the prevention of 5-fluorouracil-induced gastrointestinal mucositis and diarrhea in mice." Cancer Chemotherapy and Pharmacology 66, no. 5 (2009): 819–27. http://dx.doi.org/10.1007/s00280-009-1224-1.

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8

Jaafar, Mohammed Thamer, Luma Majeed Ahmed, and Rahman Tama Haiwal. "Synthesis, Characterization, and Electrochemical Study of Novel Porphyrin Derivatives as Corrosion Inhibitors for Carbon Steel in HCl Solutions." Indonesian Journal of Chemistry 24, no. 2 (2024): 379. http://dx.doi.org/10.22146/ijc.87682.

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This study involves the synthesis of some porphyrins derivatives, these are termed as 4,4',4'',4'''-(porphyrin-5,10,15,20-tetrayl)tetrakis(N-(6-aminoacridin-3-yl)benzamide) (3a), 4,4',4'',4'''-(porphyrin-5,10,15,20-tetrayl)tetrakis(N-(5-methoxybenzo[d]thiazol-2-yl)benzamide) (3b), 4,4'-(10,20-bis(3-hydroxyphenyl)porphyrin-5,15-diyl)bis(N-(6-aminoacridin-3yl)benzamide) (5a), and 4,4'-(10,20-bis(3-hydroxyphenyl)porphyrin-5,15-diyl)bis(N-(benzo[d]thiazol-2-yl)benzamide) (5b). These derivatives were synthesized using open circuit potential (OCP) and potentiodynamic polarization (PDP) in 0.1 M HCl
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9

PLESCIA, Janet, and Dario C. ALTIERI. "Activation of Mac-1 (CD11b/CD18)-bound factor X by released cathepsin G defines an alternative pathway of leucocyte initiation of coagulation." Biochemical Journal 319, no. 3 (1996): 873–79. http://dx.doi.org/10.1042/bj3190873.

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Leucocyte initiation of coagulation preserves the haemostatic balance and may aberrantly contribute to vascular injury. In addition to the extrinsic activation mediated by tissue factor: factor VIIa, monocytes express an alternative procoagulant response after binding of the zymogen factor X to the integrin Mac-1 (CD11b/CD18). Here, factor X-activating activity was found in purified monocyte granules, and coincided with size-chromatographed fractions containing cathepsin G. In contrast, elastase-containing granule fractions did not activate factor X. In the presence of Ca2+ ions, purified cath
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10

Li, Yawen, Ming-Kuan Chyan, Donald K. Hamlin, Holly Nguyen, Eva Corey, and D. Scott Wilbur. "Oxidation of p-[125I]Iodobenzoic Acid and p-[211At]Astatobenzoic Acid Derivatives and Evaluation In Vivo." International Journal of Molecular Sciences 23, no. 18 (2022): 10655. http://dx.doi.org/10.3390/ijms231810655.

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The alpha particle-emitting radionuclide astatine-211 (211At) is of interest for targeted radiotherapy; however, low in vivo stability of many 211At-labeled cancer-targeting molecules has limited its potential. As an alternative labeling method, we evaluated whether a specific type of astatinated aryl compound that has the At atom in a higher oxidation state might be stable to in vivo deastatination. In the research effort, para-iodobenzoic acid methyl ester and dPEG4-amino acid methyl ester derivatives were prepared as HPLC standards. The corresponding para-stannylbenzoic acid derivatives wer
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11

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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12

Phutdhawong, Weerachai, Apiwat Chuenchid, Thongchai Taechowisan, Jitnapa Sirirak, and Waya S. Phutdhawong. "Synthesis and Biological Activity Evaluation of Coumarin-3-Carboxamide Derivatives." Molecules 26, no. 6 (2021): 1653. http://dx.doi.org/10.3390/molecules26061653.

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A series of novel coumarin-3-carboxamide derivatives were designed and synthesized to evaluate their biological activities. The compounds showed little to no activity against gram-positive and gram-negative bacteria but specifically showed potential to inhibit the growth of cancer cells. In particular, among the tested compounds, 4-fluoro and 2,5-difluoro benzamide derivatives (14b and 14e, respectively) were found to be the most potent derivatives against HepG2 cancer cell lines (IC50 = 2.62–4.85 μM) and HeLa cancer cell lines (IC50 = 0.39–0.75 μM). The activities of these two compounds were
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13

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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14

Baek, Heung Soo, Soo Mi Ahn, Byoung Young Woo, et al. "Whitening Effects of Adamantyl Benzamide Derivatives." Journal of the Society of Cosmetic Scientists of Korea 39, no. 2 (2013): 127–32. http://dx.doi.org/10.15230/scsk.2013.39.2.127.

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15

Kushwaha, Mr Abhay, Dr Shailesh Jain, Mr Ajay Kumar, Mr Ritesh Raj, Dr Phool Singh Yaduwanshi, and Dr Dhanraj Patidar. "An Overall Review of Different Derivatives That Activate Glucokinase Enzyme Having Multiple Actions to Treat Type 2 Diabetes." International Journal of Pharmaceutical Research and Applications 10, no. 1 (2025): 358–67. https://doi.org/10.35629/4494-1001358367.

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Different derivatives like3,6-disubstituted2- pyridine carboxamide derivatives, Phenylethyl benzamide derivatives, Carboxypyridine benzamide derivatives, Pyrazole benzamide derivatives, Quinazoline-2,4 dione analogs, Ketopiperazine analogs, Cycloalkyl-fused Nthiazol-2-yl-benzamides derivatives, 1,4- disubstituted indazoles derivatives, 2,5,6- trisubstituted indole derivatives, Azaindole derivatives andPyrimidone derivatives was designed, synthesized and evaluated the pharmacological activity in mice. Such compounds activate the glucokinase by interaction between glucokinase activators and gluc
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16

A. Abdulqader, Kany, Ahmed W. Naser, Muthanna S. Farhan та Sabah J. Salih. "Synthesis, Characterization and Cytotoxic Activity of some new 1,2,3-Triazole, Oxadiazole and Aza- β-lactam Derivatives". Oriental Journal of Chemistry 34, № 5 (2018): 2350–60. http://dx.doi.org/10.13005/ojc/340516.

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A series of 1,2,3-triazole, oxadiazole and aza-β-lactam derivatives were synthesized through consecutive reaction began from o-(N-propargyl) sulfonamido benzoic acid (1a). The reaction of (1a) with absolute ethanol in the presence of concentrated H2SO4 resulted in the formation of ester derivative (2a). The product of the previous reaction was reacted with 80% hydrazine hydrate to prepare benzohydrazide derivative (3a). 1,3,4-oxadiazole compound (4a) was obtained by condensation of compound (3a) with CS2 in presence KOH . Compound (3a) react with Phenyl isocyanates to give Carboxamide derivati
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17

Aparicio Acevedo, Deiby F., Marlyn C. Ortiz Villamizar, and Vladimir V. Kouznetsov. "Three-Step Synthesis of N-(7-chloro-4-morpholinoquinolin-2-yl)benzamide from 4,7-Dichloroquinoline." Molbank 2024, no. 1 (2024): M1796. http://dx.doi.org/10.3390/m1796.

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The quinoline derivative, N-(7-chloro-4-morpholinoquinolin-2-yl)benzamide, was synthesized in a conventional three-step procedure from 4,7-dichloroquinoline using a N-oxidation reaction/C2-amide formation reaction/C4 SNAr reaction sequence. The structure of the compound was fully characterized by FT-IR, 1H-, 13C-NMR, DEPT-135°, and ESI-MS techniques. Its physicochemical parameters (Lipinski’s descriptors) were also calculated using the online SwissADME database. Such derivatives are relevant therapeutic agents exhibiting potent anticancer, antibacterial, antifungal, and antiparasitic propertie
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18

Wu, Yan Ling, Li Wen Shen, Yan Ping Ding, Yoshimasa Tanaka, and Wen Zhang. "Inhibition of Tumor Cell Proliferation In Vitro by Benzamide Derivatives." Advanced Materials Research 997 (August 2014): 225–28. http://dx.doi.org/10.4028/www.scientific.net/amr.997.225.

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Benzamide derivatives have been shown to have antitumor activity in various tumor cell lines in vitro as well as in vivo. In this study, we examined the anti-proliferative effect of four benzamide derivativeson Hela, H7402, and SK-RC-42 tumor cell lines in vitro by means of Real-Time cell assay (RTCA), and found that four benzamide derivatives suppressed proliferation of tumor cells in a time-and dose-dependent manner. The anti-proliferative activity of benzamide derivatives demonstrated that theycould be promising lead compounds for developing therapeutic agents for malignant tumors.
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19

Jiao, Min-Ru, Bo Han, Xiu Gu, Hao Zhang, Ai-Ping Wang, and Qing-Wei Zhang. "Design, Synthesis, and Evaluation of Benzoheterocyclic-Containing Derivatives as Novel HDAC1 Inhibitors." Pharmaceutical Fronts 04, no. 01 (2022): e22-e29. http://dx.doi.org/10.1055/s-0042-1743487.

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In this study, the synthesis and biological evaluation of a variety of benzoheterocyclic-containing benzamide derivatives were described. Some of these compounds were proved to inhibiting the activity of histone deacetylase 1 (HDAC1) with IC50 values below the micromolar range, retarding proliferation of several human cancer cells, and surprisingly, not possessing toxicity to human normal cells and hERG K+ ion channels. Among those compounds, 3c was the most potent and efficacious derivative. Compound 3c was orally active and displayed excellent in vivo antitumor activity in a HCT-116 xenograf
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20

Al-Soud, Yaseen A., Najim A. Al-Masoudi, Hossam H. Al-Suod, and Christophe Pannecouque. "Nitroimidazoles Part 8. Synthesis and Anti-HIV Activity of New 4-Nitroimidazole Derivatives Using the Suzuki Cross-Coupling Reaction." Zeitschrift für Naturforschung B 67, no. 9 (2012): 925–34. http://dx.doi.org/10.5560/znb.2012-0185.

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The development of new HIV non-nucleoside reverse transcriptase inhibitors (NNRTIs) offers the possibility of generating structures of increased potency. To this end, a series of 1-(1-benzyl-2-ethyl- 4-nitro-1H-imidazol-5-yl)-4-(1,1'-biaryl)-4-yl-piperazine derivatives (6a-l) was synthesized via the Suzuki coupling reaction. Analogously, coupling of the acid derivative 5, prepared from 4, with various amino acid methyl esters in the presence of HOBt/DCC reagents afforded the benzamide derivatives 8-11. The newly synthesized compounds were assayed against HIV-1 and HIV-2 in MT- 4 cells. All com
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21

Ergezinger, Christina, Frank Weller, and Kurt Dehnicke. "Die Kristallstruktur von N,N,N'-tris(trimethylsilyl)benzamidin sowie die Synthese und Kristallstruktur von DichIorantimon-N,N'-bis(trimethylsilyl)benzamidinat." Zeitschrift für Naturforschung B 43, no. 9 (1988): 1119–24. http://dx.doi.org/10.1515/znb-1988-0906.

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Abstract N,N,N'-Tris(trimethylsilyl)benzamidine, [C6H5-C(NSiMe3)N(SiMe3)2], reacts with antimony trichloride in CH2Cl2 solution to form monomeric dichloroantimony-N,N'-bis(trimethylsilyl)- benzamidine, [SbCl2(NSiMe3)2C-C6H5]. Both benzamidine derivatives have been character­ized by crystal structure determinations. [C6H5-C(NSiMe3)N(SiMe3)2]: space group P21/c, Z = 4, 2278 observed independent refle­xions, R = 0,038. Lattice dimensions (19 °C): a = 1521,0(1); b = 656.7(1); c = 2163,0(1) β = 94,21(1)°. The compound forms monomeric molecules with CN distances of 126,6 pm, and 141,0 pm, respective
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22

Xuesong Wang and Xiaorong Tang, Xuesong Wang and Xiaorong Tang. "Design, Synthesis and Evaluate In Vitro Antifungal Activity of Novel Benzamide Derivatives." Journal of the chemical society of pakistan 41, no. 3 (2019): 549. http://dx.doi.org/10.52568/000763/jcsp/41.03.2019.

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A series of novel benzamide derivatives according to fluopicolide were designed and synthesized following the rule of combination carboxylic acid amides and amines derivatives together. The antifungal activity of the 15 new compounds were evaluated in vitro against five pathogenic fungi, including Sclerotinia sclerotiorum, Gibberella zeae, Rhizoctonia solani, Helminthosporium maydis and Botrytis cinerea. Almost all the structure have not been reported, except compounds 3, 5 and 6. A surprising finding is that all the five tested fungi breed faster than negative controls when supplementary with
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23

Vadiraj, Kurdekar, N. Dighe Satish, and R. Jadhav Hemant. "Study of arginine mimetic benzamidine urea derivatives as PAD4 inhibitors." Journal of Indian Chemical Society Vol. 97, Aug 2020 (2020): 1273–78. https://doi.org/10.5281/zenodo.5656697.

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Department of Pharmacy, Birla Institute of Technology and Sciences Pilani, Pilani Campus, Pilani-333 031, Rajasthan, India <em>E-mail</em>: hemantrj@pilani.bits-pilani.ac.in <em>Manuscript received online 01 July 2020, accepted 30 July 2020</em> Rheumatoid Arthritis (RA) is an autoimmune inflammatory disease, where antibodies are generated against citrullinated proteins. Citrullinated proteins are catalytic products of the Peptidyl Arginine Deiminase 4 (PAD4) enzyme. Since PAD4 acts on peptidyl arginine, a series of arginine mimetic compounds having 4-benzamidine urea scaffold were synthesized
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24

Lauro, Figueroa-Valverde, Diaz-Cedillo Francisco, García-Cervera Elodia, et al. "Facile Synthesis of Two Benzamidine-steroid Derivatives." Letters in Organic Chemistry 11, no. 10 (2014): 725–30. http://dx.doi.org/10.2174/1570178611666140813210013.

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25

Fröhlich, E., T. Kantyka, K. Plaza, et al. "Benzamidine derivatives inhibit the virulence ofPorphyromonas gingivalis." Molecular Oral Microbiology 28, no. 3 (2012): 192–203. http://dx.doi.org/10.1111/omi.12015.

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26

Qasim, Zahraa S., and Kareem S. Abbas. "BENZAMINE DERIVATIVES: SYNTHESIS, CHARACTERIZATION AND BIOLOGICAL ACTIVITY STUDY." Chemical Problems 22, no. 4 (2024): 411–35. http://dx.doi.org/10.32737/2221-8688-2024-4-411-435.

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: Our study is included the synthesis of a number of benzamide drivatives through two chemical processes. The first is the benzoylation of some aromatic amines containing a pyrimidine or a pyrazoline ring in their structures (A-G) using benzoyl chloride or p-chloronbenzoyl chloride in the presence of 1,4- dioxan as solvent productive (N1-N6, N13-N16) derivatives. The second is the tosylation of (N2-N6, N15) by p-toluene sulfonyl chloride in the presence of pyridine as catalyst and base at room temperature to produce (B1-B6 ) derivatives . The products have been characterized by IR, 1H-NMR ,13
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27

Kavitha, Ramasamy, Mohammad Auwal Sa’ad, Shivkanya Fuloria, Neeraj Kumar Fuloria, Manickam Ravichandran, and Pattabhiraman Lalitha. "Synthesis, Characterization, Cytotoxicity Analysis and Evaluation of Novel Heterocyclic Derivatives of Benzamidine against Periodontal Disease Triggering Bacteria." Antibiotics 12, no. 2 (2023): 306. http://dx.doi.org/10.3390/antibiotics12020306.

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Periodontal disease (PD) is multifactorial oral disease that damages tooth-supporting tissue. PD treatment includes proper oral hygiene, deep cleaning, antibiotics therapy, and surgery. Despite the availability of basic treatments, some of these are rendered undesirable in PD treatment due to side effects and expense. Therefore, the aim of the present study is to develop novel molecules to combat the PD triggering pathogens. The study involved the synthesis of 4-((5-(substituted-phenyl)-1,3,4-oxadiazol-2-yl)methoxy)benzamidine (5a-e), by condensation of 2-(4-carbamimidoylphenoxy)acetohydrazide
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28

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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29

Purgatorio, Rosa, Nicola Gambacorta, Francesco Samarelli, et al. "Assessing the Role of a Malonamide Linker in the Design of Potent Dual Inhibitors of Factor Xa and Cholinesterases." Molecules 27, no. 13 (2022): 4269. http://dx.doi.org/10.3390/molecules27134269.

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The rational discovery of new peptidomimetic inhibitors of the coagulation factor Xa (fXa) could help set more effective therapeutic options (to prevent atrial fibrillation). In this respect, we explored the conformational impact on the enzyme inhibition potency of the malonamide bridge, compared to the glycinamide one, as a linker connecting the P1 benzamidine anchoring moiety to the P4 aryl group of novel selective fXa inhibitors. We carried out structure–activity relationship (SAR) studies aimed at investigating para- or meta-benzamidine as the P1 basic group as well as diversely decorated
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Mohammadi-Farani, Ahmad, Farzaneh Moradi, Amin Hosseini, and Alireza Aliabadi. "Synthesis, docking, pharmacokinetic prediction, and acetylcholinesterase inhibitory evaluation of N-(2-(piperidine-1-yl)ethyl)benzamide derivatives as potential anti-Alzheimer agents." Research in Pharmaceutical Sciences 19, no. 6 (2024): 698–711. https://doi.org/10.4103/rps.rps_257_23.

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Background and purpose: Alzheimer’s disease is the most common form of dementia and the sixth most common cause of death in the US according to the Alzheimer’s Association. As regards, to date, no effective treatments are available because of the multifactorial nature of the disease, therefore, a large body of recent research has been allocated to the design and development of multi-target-directed ligands that can become effective drug candidates. Experimental approach: A novel series of benzamide derivatives (5a-5l) containing piperidine core were synthesized in the current work. After ident
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31

Cvejn, Daniel, Věra Klimešová та Filip Bureš. "α-Amino acid-derived 2-phenylimidazoles with potential antimycobacterial activity". Open Chemistry 10, № 5 (2012): 1681–87. http://dx.doi.org/10.2478/s11532-012-0087-1.

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Abstractα-Amino acid-derived 2-phenylimidazole derivatives were designed, synthesized, and further investigated as potential antimycobacterial agents. The synthesis of target imidazole derivatives involved the transformation of Cbz-protected α-amino acids (Ala, Val, Phe, Leu, iLe, and Pro) into α-diazoketones and α-bromoketones, respectively. Subsequent treatment of α-bromoketones with (4-nitro)benzamidine afforded imidazole derivatives bearing α-amino acid residue appended to the imidazole C4 and (4-nitro)phenyl ring in the position C2. Antimycobacterial activities of both series of compounds
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32

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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33

Rivard, Georges E., Brummel Kathleen, Fan Li, Hofer Angelique, Cohen Eli, and Mann G. Kenneth. "Evaluation of the Profile of Thrombin Generation during the Process of Whole Blood Clotting as Assessed by Thromboelastography." Blood 104, no. 11 (2004): 2981. http://dx.doi.org/10.1182/blood.v104.11.2981.2981.

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Abstract The evaluation of thrombin generation during blood coagulation has become the preferred clinically relevant approach to assess the global integrity of this complex process. In order to give the full picture of the physiology of this multifactorial reaction, all cellular and soluble plasma participants to this reaction have to be present in their natural whole blood environment. Whole blood thrombin generation tests are best suited for this purpose but are somewhat cumbersome for use in real time clinical practice. Thrombelastography has long been recognized as a clinically useful tech
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34

Ajmer Singh Grewal, Kapil Sharma, Sukhbir Singh, Vikramjeet Singh, Deepti Pandita, and Viney Lather. "Design, Synthesis and Antidiabetic Activity of Novel Sulfamoyl Benzamide Derivatives as Glucokinase Activators." Journal of Pharmaceutical Technology, Research and Management 6, no. 2 (2018): 115–24. http://dx.doi.org/10.15415/jptrm.2018.62008.

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The present work has been planned to design, synthesize and evaluate the antidiabetic potential of a series of sulfamoyl benzamide derivatives as potential glucokinase (GK) activators. A new series of sulfamoyl benzamide derivatives was synthesized starting from 3-nitrobenzoic acid and characterized. In silico docking studies were performed to determine the binding interactions for the best fit conformations in the allosteric site of GK enzyme. Based on the results of in silico studies, the selected molecules were tested for their antidiabetic activity in animal studies (alloxan induced diabet
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35

Shang, Zhenhua, Dechen Jiao, Haoran Cheng, and Daowei Huang. "Direct Synthesis of 2-(4-Hydroxyphenoxy)benzamide Derivatives from 2-Aryloxybenzamide via PhIO-Mediated Oxidation Reaction." Molecules 29, no. 24 (2024): 6048. https://doi.org/10.3390/molecules29246048.

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The 2-(4-hydroxyphenoxy)benzamide scaffold is frequently found in a variety of bioactive compounds, displaying a broad spectrum of properties, such as antibacterial and antitumor effects. In this study, we developed a new method for synthesizing 2-(4-hydroxyphenoxy)benzamide derivatives from 2-aryloxybenzamide via a PhIO-mediated oxidation reaction. The optimal reaction conditions were established as follows: TFA was used as the solvent, PhIO served as the oxidant with a substrate-to-oxidant ratio of 1:2, and the reaction was conducted at room temperature. This method, characterized by mild re
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36

Furuya, T., S. Iwanami, A. Takenaka, and Y. Sasada. "Structure of a benzamide derivative." Acta Crystallographica Section C Crystal Structure Communications 41, no. 10 (1985): 1507–9. http://dx.doi.org/10.1107/s0108270185008344.

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37

Isakhanyan, A. U., Z. A. Ovasyan, G. S. Grigoryan, et al. "Pyrazolines and pyrimidines based on (<i>E</i>)-1-(4-pentyloxyphenyl)-3-arylprop-2-en-1-ones. Synthesis, docking study and luminescent properties." Žurnal obŝej himii 94, no. 5 (2024): 569–82. http://dx.doi.org/10.31857/s0044460x24050048.

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(E)-1-(4-Pentyloxyphenyl)-3-(aryl)prop-2-en-1-ones were obtained by condensation of 1-(4-pentyloxyphenyl)ethanone with aromatic aldehydes in an aqueous ethanol solution in the presence of NaOH. The corresponding pyrazoline derivatives were prepared by cyclization of substituted chalcones with phenylhydrazine in an acidic medium, while 2,4,6-triaryl-substituted pyrimidines were produced in the case of benzamidine hydrochloride in the KOH–ethanol. It was found that all synthesized pyrazoline derivatives exhibit pronounced luminescent properties. A docking study of the compounds was carried out a
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38

Hasana, Ani Riani, Siswandono Siswandono, and Marcellino Rudyanto. "Synthesis and characterization of 2-Benzamido-NBenzylbenzamide Derivative." JURNAL ILMU KEFARMASIAN INDONESIA 20, no. 2 (2022): 281. http://dx.doi.org/10.35814/jifi.v20i2.1135.

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Anthranilamide derivatives exhibit anti-inflammatory, antipyretic, antibacterial, antiangiogenic, and anticoagulant properties. With an early in silico examination of its analgesic capabilities, this study aimed to generate a novel anthranilamide molecule by altering 2-Benzamido-N-Benzylbenzamide. Modification of anthranilamide with 1/2/3-chloro benzoyl chloride by acylation resulted in the design, synthesis, characterization, and research of the analgesic effects of 2-benzamido-N-benzoylbenzamide derivatives. 2-(2-chlorobenzamido)-N-(2-chlorobenzoyl)benzamide, 2-(3-chlorobenzamido)-N-(3-chlor
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39

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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40

Stürzebecher, J., D. Prasa, and O. Taby. "Inhibition of activated protein C by benzamidine derivatives." Thrombosis Research 69, no. 6 (1993): 533–39. http://dx.doi.org/10.1016/0049-3848(93)90057-u.

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41

J. Prathyusha and C. Asha Deepti. "SYNTHESIS, ANTIMICROBIAL, AND ANTITUBERCULAR ACTIVITIES OF NOVEL N-PYRAZOLYLBENZAMIDE DERIVATIVES." RASAYAN Journal of Chemistry 15, no. 04 (2022): 2407–16. http://dx.doi.org/10.31788/rjc.2022.1547092.

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The current study investigated the antimicrobial and antitubercular activities of novel N-Pyrazolyl Benzamide derivatives. The study includes the synthesis, characterization, and ligand-based molecular docking of the designed molecules. Synthesis of N-Pyrazolyl Benzamide derivatives involves a two-step process in which 5-amino pyrazole (3) intermediate is produced by the condensation reaction of aryl hydrazine (1) and β-keto nitrile (2) in acidic conditions. The final N-Pyrazolyl Benzamide derivatives (5a-n) were synthesized by the reaction involving amide coupling between 5-amino pyrazole (3)
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42

Younes, Eyad A., Nour Hussein, Majed Shtaiwi, Farshid Shahrokhi, Kayed A. Abu Safieh, and Yuming Zhao. "N-(Cyano(naphthalen-1-yl)methyl)benzamides: synthesis, crystal structures, and colorimetric sensing of fluoride anions." New Journal of Chemistry 44, no. 38 (2020): 16546–56. http://dx.doi.org/10.1039/d0nj03105d.

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43

Wisnu, Elok Dea Orens Ubung, Indah Purnama Sary, and Dwi Koko Pratoko. "Sintesis dan Uji Aktivitas Antibakteri Senyawa N-fenil-4-klorobenzamida." Pustaka Kesehatan 6, no. 2 (2018): 212. http://dx.doi.org/10.19184/pk.v6i2.7569.

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N-phenylbenzamide is benzamide derivatives, which is potential as an antibacterial agent. N-phenyl-4-chlorobenzamide is N-phenylbenzamide derivative that substitued by chloro to the para position and it was expected to enhance the antibacterial activity. N-phenyl-4-chlorobenzamide was synthesized by reacting 1,3-diphenyilthiourea and 4-chlorobenzoil chloride. This compound has been purified and provided 53% of product with crystal shape, white color, and melting point of 195-197 oC. The purification of this compound was confirmed by TLC and the structure was identified by 1H-NMR, 13C-NMR, and
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44

USUDA, SHINJI. "Anti-dopaminergic Activity of Pyrrolidinyl-benzamide Derivatives." YAKUGAKU ZASSHI 107, no. 9 (1987): 711–19. http://dx.doi.org/10.1248/yakushi1947.107.9_711.

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45

Liu, Pei, Na Hao, Dong Yang, et al. "Iron-catalyzed para-selective C–H silylation of benzamide derivatives with chlorosilanes." Organic Chemistry Frontiers 8, no. 11 (2021): 2442–48. http://dx.doi.org/10.1039/d1qo00243k.

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46

Tang, Jinghua, Pei Liu, and Xiaoming Zeng. "N-Heterocyclic carbene–chromium-catalyzed alkylative cross-coupling of benzamide derivatives with aliphatic bromides." Chemical Communications 54, no. 67 (2018): 9325–28. http://dx.doi.org/10.1039/c8cc05026k.

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47

Manin, Alex N., Ksenia V. Drozd, Andrei V. Churakov, and German L. Perlovich. "Design of 4-aminobenzoic acid two-component molecular crystals: prediction and experiments." CrystEngComm 21, no. 13 (2019): 2119–29. http://dx.doi.org/10.1039/c8ce01857j.

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48

Loeuillet, Corinne, Bastien Touquet, Jean François Guichou, Gilles Labesse, and Denis Sereno. "A Tiny Change Makes a Big Difference in the Anti-Parasitic Activities of an HDAC Inhibitor." International Journal of Molecular Sciences 20, no. 12 (2019): 2973. http://dx.doi.org/10.3390/ijms20122973.

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We previously synthesized an hydroxamate derivative (N-hydroxy-4-[2-(3- methoxyphenyl)acetamido]benzamide) named 363 with potent anti-Toxoplasma gondii activity and histone deacetylase inhibitor (HDACi) effects. Here we show that 1-N-hydroxy-4-N- [(2-methoxyphenyl)methyl]benzene-1,4-dicarboxamide, a 363 isomer, does not have antiparasitic potency and has a 13-fold decrease in HDACi activity. The in silico modeling of T. gondii HDACs of the type II strain discloses identity varying from 25% to 62% on more than 250 residues for S8EP32_TOXG and A0A125YPH4_TOXGM. We observed a high conservation de
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49

Bhandary, Subhrajyoti, Amy J. Thompson, John C. McMurtrie, et al. "The mechanism of bending in a plastically flexible crystal." Chemical Communications 56, no. 84 (2020): 12841–44. http://dx.doi.org/10.1039/d0cc05904h.

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The mechanism of plastic deformation in crystals of a trifluoromethylated benzamide derivative has been determined with micro-focused X-ray diffraction. Fuorine–fluorine interactions are propose to mediated the observed mechanical behaviour.
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50

MAKULA, Dr AJITHA, and SANA TABASSUM. "SYNTHESIS OF NOVEL 4,6-DIPHENYLPYRIMIDINE SUBSTITUTED BENZAMIDE DERIVATIVES ITS CHARACTERIZATION AND EVALUATION FOR ANTI-OXIDANT AND ANTI-MICROBIAL ACTIVITIES." Journal of Advanced Scientific Research 14, no. 04 (2023): 13–25. http://dx.doi.org/10.55218/jasr.202314404.

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The research work involves the estimation and evaluation of pharmacological activity of designed 4, 6-diphenylpyrimidine substituted benzamide derivatives that act as HDAC inhibitors. The Histone deacetylases inhibitors are a new class of cytostatic agents that exhibits promising results cancer treatment. The four HDAC inhibitors approved by FDA for cancer chemotherapy is SAHA (Vorinostat), Belinostat (PXD-101), Panobinostat (LBH-589), and Romidepsin (FK-228). The six novel 4, 6-diphenylpyrimidine substituted benzamide derivatives were synthesized, characterized and evaluated for anti-microbia
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