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Journal articles on the topic 'Primary Moiety for The Synthesis of Several Antimicrobial'

Author: Grafiati

Published: 3 June 2025

Last updated: 31 July 2025

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1

Journal, Baghdad Science. "Synthesis and Evaluation of Antimicrobial activity of several new Maleimides to Benzothiazole moiety." Baghdad Science Journal 10, no. 3 (2013): 658–72. http://dx.doi.org/10.21123/bsj.10.3.658-672.

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In this work, a series of new maleimides linked to substituted benzothiazole moiety were synthesized. Synthesis of these new cyclic imides were performed via three steps, the first one involved preparation of a series of 2-aminobenzothiazole substituted with different substituents via reaction of different primary aromatic amines with ammonium thiocyanate and bromine in glacial acetic acid. The prepared 2- amino benzothiozoles were introduced in the second step in reaction with maleic anhydride producing a series of N-(substituted benzothiazole-2-yl) maleamic acids.The resulted maleamic acids

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2

Azzawi, Ahlam Marouf AL, and Suroor Abdul Rhahman Mahdi. "Synthesis and Evaluation of Antimicrobial activity of several new Maleimides to Benzothiazole moiety." Baghdad Science Journal 10, no. 3 (2013): 658–72. http://dx.doi.org/10.21123/bsj.2013.10.3.658-672.

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In this work, a series of new maleimides linked to substituted benzothiazole moiety were synthesized. Synthesis of these new cyclic imides were performed via three steps, the first one involved preparation of a series of 2-aminobenzothiazole substituted with different substituents via reaction of different primary aromatic amines with ammonium thiocyanate and bromine in glacial acetic acid. The prepared 2- amino benzothiozoles were introduced in the second step in reaction with maleic anhydride producing a series of N-(substituted benzothiazole-2-yl) maleamic acids.The resulted maleamic acids

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3

Taj, Muhammad Babar, Muneera D. F. Alkahtani, Uzma Ali, et al. "New Heteroleptic 3D Metal Complexes: Synthesis, Antimicrobial and Solubilization Parameters." Molecules 25, no. 18 (2020): 4252. http://dx.doi.org/10.3390/molecules25184252.

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The microbial resistance to current antibiotics is increasing day by day, which in turn accelerating the development of new effective drugs. Several studies have proved the high antimicrobial potential of the interaction of several organic ligands with a variety of metal ions. In the present study, a conventional method has been adopted in the synthesis of twelve new heteroleptic complexes of cobalt (II), nickel (II), copper (II) and zinc (II) using three aldimines, namely, (HL1 ((E)-2-((4-chloro-2-hydroxybenzylidene)amino)-3,4-dimethyl-5-phenylcyclopent-2-en-1-one), HL2 ((Z)-3-((4-chlorobenzy

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4

Desiatkina, Oksana, Serena K. Johns, Nicoleta Anghel, et al. "Synthesis and Antiparasitic Activity of New Conjugates—Organic Drugs Tethered to Trithiolato-Bridged Dinuclear Ruthenium(II)–Arene Complexes." Inorganics 9, no. 8 (2021): 59. http://dx.doi.org/10.3390/inorganics9080059.

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Tethering known drugs to a metalorganic moiety is an efficient approach for modulating the anticancer, antibacterial, and antiparasitic activity of organometallic complexes. This study focused on the synthesis and evaluation of new dinuclear ruthenium(II)–arene compounds linked to several antimicrobial compounds such as dapsone, sulfamethoxazole, sulfadiazine, sulfadoxine, triclosan, metronidazole, ciprofloxacin, as well as menadione (a 1,4-naphtoquinone derivative). In a primary screen, 30 compounds (17 hybrid molecules, diruthenium intermediates, and antimicrobials) were assessed for in vitr

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5

Eikemo, Vebjørn, Leiv K. Sydnes, and Magne O. Sydnes. "Photodegradable antimicrobial agents − synthesis, photodegradation, and biological evaluation." RSC Advances 11, no. 51 (2021): 32339–45. http://dx.doi.org/10.1039/d1ra06324c.

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6

Lupascu, Dan, Lenuta Profire, Maria Apotrosoaei, et al. "Synthesis and Antimicrobial Activities of Novel Rutin Derivatives Carrying Quinoline Moiety." Revista de Chimie 71, no. 6 (2020): 401–7. http://dx.doi.org/10.37358/rc.20.6.8206.

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Antimicrobial resistance constitutes a topical subject and it is one of the major threats to public health. According to statistics, the incidence of multidrug-resistant microorganisms, such as bacteria, fungi and protozoa has increased in the last decades and it continues to spread. Therefore, the development of novel antimicrobial agents to combat drug-resistant infections is very important, among other research directions in this field. Quinoline ring is a very interesting structure for researchers because of its diverse biological properties (antimicrobial, anticancer, anticonvulsant, anti

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7

Pathak, Ashutosh, P. Malairajan Arti Gautam, and Shibu Das. "Isatin: A Short Review of their Antimicrobial Activities." International Journal of Current Microbiology and Applied Sciences 11, no. 1 (2022): 61–77. http://dx.doi.org/10.20546/ijcmas.2022.1101.009.

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Isatin(2, 3-dioxindate), a particularly effective scaffold with a variety of pharmacological actions, has been developed due to its therapeutic significance in organic and medicinal chemistry. Many researchers have been drawn to this skeleton because of its diverse biological response profile and its multiple possibilities against a variety of activities. Sandmeyer's and Stolle processes are two typical ways for synthesizing isatin derivatives. Many researchers have taken advantage of the isatin moiety by using NH at the first position, C2 and C3 carbonyl positions for the creation of numerous

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8

López-López, Lluvia Itzel, Denisse de Loera, Ernesto Rivera-Avalos, and Aidé Sáenz-Galindo. "Green Synthesis of Hydantoins and Derivatives." Mini-Reviews in Organic Chemistry 17, no. 2 (2020): 176–84. http://dx.doi.org/10.2174/1570193x16666181206100225.

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The hydantoin moiety is found in several bioactive compounds with important pharmacological properties such as antimicrobial, antifungal, anti-androgens, anticancer and the historical action anticonvulsant. Because of these reasons, the synthesis of these compounds and their derivatives is important to review considering the philosophy of the green chemistry. In this review, we present the actual importance in the green synthesis of hydantoins and their derivatives using green methods, such as microwave and ultrasound irradiation, ionic liquids, solid-phase and solvent-free synthesis. Finally,

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9

Sultan, Mohammed Ibrahim, Ahmed M. Abdula, Rana I. Faeq, and Mahdi F. Radi. "New Pyrazoline Derivatives Containing Imine Moiety: Synthesis, Characterization and Antimicrobial Study." Al-Mustansiriyah Journal of Science 32, no. 3 (2021): 8. http://dx.doi.org/10.23851/mjs.v32i3.955.

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A new series of pyrazoline derivatives (3-10) have been synthesized and characterized on the basis of FT-IR, 1H-NMR, and Mass techniques. 1-(4-Aminophenyl)-3-(pyridin-4-yl)prop-2-en-1-one (1) as a starting material was prepared by the reaction of 4-aminoacetophenone and 4-pyridinecarboxaldehyde in ethanol, using sodium hydroxide as a catalyst. Pyrazoline derivatives 2 was obtained via the cyclization reaction of compound 1 by the action of hydrazine hydrate 80% in ethanol. The target derivatives (3-8) were obtained by the reaction of pyrazoline derivative (2) with the corresponding aldehyde in

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10

V., N. PATOLIA, K. PATEL P., and J. BAXI A. "Studies on 4-Thiazolidinones. Part-IX. Synthesis and Antimicrobial Activity of 2-(2'-Aryl-4-thiazolidinon-3'-yl)- 4-(2" -methyl-4" -hydroxy-5"-isopropylphenyl)thiazoles." Journal of Indian Chemical Society Vol. 71, Nov 1994 (1994): 683–85. https://doi.org/10.5281/zenodo.5897621.

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Department of Chemistry, Saurashtra University, Rajkot-360 005 <em>Manuscript received 25 August 1992, revised 7 September 1993, accepted 17 September 1993</em> Several new 4-thiazolidinones have been prepared bearing 2-amino-4-(2'-methyl-4'-hydroxy-5'-isopropylphenyl)thiazole moiety. Their structures have been supported by ir and mass spectral studies. The products have been screened for their antimicrobial activity.

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11

Breznica-Selmani, Pranvera, Kristina Mladenovska, Gerald Dräger, et al. "Synthesis, physicochemical characterization and antibacterial activity of novel (benzoylamino)methyl derivatives of quinolones." Macedonian Journal of Chemistry and Chemical Engineering 35, no. 2 (2016): 179. http://dx.doi.org/10.20450/mjcce.2016.919.

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Herein we report the synthesis of different derivatives of (fluoro)quinolones norfloxacin, ciprofloxacin and pipemidic acid, by incorporating (benzoylamino)methyl on the free nitrogen of the pyperazinyl moiety. The compounds were structurally characterized by 1D and 2D NMR, FTIR and high-resolution mass spectroscopy. In addition, their physicochemical properties were a matter of interest to be correlated with their structure and antimicrobial activity<em> in vitro</em>. Their antimicrobial activities were screened against Gram-positive, Gram-negative bacteria and <em>C. albic

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12

Laddha, Purushottam R., and Kailash R. Biyani. "Synthesis and Biological Evaluation of Novel Schiff Bases of Aryloxy Moiety." Journal of Drug Delivery and Therapeutics 9, no. 5-s (2019): 44–49. http://dx.doi.org/10.22270/jddt.v9i5-s.3635.

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Schiff's bases are condensation products of primary amines with carbonyl compounds. Schiff bases (imines) possess wide variety of biological activities that include antibacterial and antifungal activity. In present work, Schiff bases from 3,5- Dimethoxyphenol (aryloxy moiety) as starting material synthesized. Esterification of 3,5- Dimethoxyphenol led to formation of (3,5-Dimethoxy-phenoxy)-acetic acid ethyl ester (1). (3,5-Dimethoxy-phenoxy)-acetic acid hydrazide (2) is derived from Compound (1) by hydrazination. Compound (2) was reacted with different aromatic aldehydes to yield novel imines

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13

Shivani Kapletiya, Shivani Kapletiya, Harsh Mehta Harsh Mehta, and Sabirkhan Pathan Sabirkhan Pathan. "“Exploring Pyridine-Quinoline Hybrids: Efficient Synthesis and Their Promising Antimicrobial Properties”." International Journal of Advances in Engineering and Management 7, no. 5 (2025): 396–407. https://doi.org/10.35629/5252-0705396407.

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The main focus of the current research is on the substituted aldehydes that are produced from the reaction of 4-ethoxy acetanilide, DMF, and POCl3. To synthesize a range of substituted quinolinechalcone conjugates, 2-chloro-6-ethoxyquinoline3-carbaldehyde reacts with substituted acetophenone(i-iv), and their nucleolytic activity is evaluated. Afterward, substituted chalcone interacts with glacial acetic acid containing ammonium acetate in the presence of malononitrile and Ethylcyanoacetate. Pyridine is a crucial pharmacophore in drug studies, and a preferred scaffold and an exceptional heteroc

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14

Chavan, Uma, Kratika Daniel, and Neetesh Kumar Jain. "To Synthesize Naphthalene Derivatives Having Isoxazole Central Core as Anti- Microbial Agents." International Journal of Medical Sciences and Pharma Research 8, no. 2 (2022): 60–64. http://dx.doi.org/10.22270/ijmspr.v8i2.40.

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The presence of heterocycles such as pyrrole, thiazole, oxazole, furane, imidazole, and isoxazole and pyrimidine nucleus as central scaffold is a common feature in the chemical structure of several antimicrobial agents. So the aim has been designed to synthesize the molecule having Naphthalene ring in one of diaryl having isoxazole as pharmacophoric heterocyclic moiety for synthesis of safer anti-microbial agents. Keywords: Naphthalene, isoxazole, anti-microbial agents.

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15

Mishra, Brijeshkunvar, and Richa Mishra. "Triazine: A Scaffold with Never Ending Pharmacological Potential." International Journal of Advanced Pharmaceutical Sciences and Research 4, no. 3 (2024): 20–34. https://doi.org/10.54105/ijapsr.e4084.04030424.

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Background: The triazine moiety occupies a unique position in medicinal chemistry due to its extensive biological and pharmacological potential. Over the decades, the moiety has been investigated for developing molecules that may be used to treat a plethora of pathological conditions, including inflammation, cancer, and infections. Several lead molecules have been developed from the triazine moiety. The fusion of triazine with other heterocyclic rings, such as imidazoles and pyrroles, has produced several bicyclic compounds with biological activity. The broad spectrum of activities displayed b

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16

Kasabe, Amit, Vijay Mohite, Jayesh Ghodake, and Jaydeep Vidhate. "Synthesis, Characterization and Primary Antimicrobial, Antifungal Activity Evaluation of Schiff bases of 4-Chloro-(3-substituted-phenylimino) - methyl-[2H] - chromene-2-one." E-Journal of Chemistry 7, no. 2 (2010): 377–82. http://dx.doi.org/10.1155/2007/237645.

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Coumarins show promising antimicrobial and antifungal activity, this prompted to us to synthesize new derivatives of coumarins. 4-Chloro-2-oxo-2H-chromene-3-carbaldehyde was reacted with substituted aniline and rectified spirit to obtain a new series of Schiff bases of 4-chloro-(3-substituted-phenylimino) -methyl- [2H]-chromene-2-one (3a-i). Their structures were confirmed by IR,1H NMR spectral data. The synthesized compounds were investigated for antimicrobial and antifungal activities. The data reported showed that the effect of variation in chemical structure was rather unpredictable. Seldo

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17

LINA, MEHTA, and PAREKH HANSA. "Studies on 4-Thiazolidinones. Part-V. Synthesis and Antimicrobial Activity of 2-Aryl-3(2',4'-diphenylamino-s- triazin-6'-yl)-5-H/ methy / carboxymethyl-4-thiazolidinones." Journal of Indian Chemical Society Vol. 65, Sep 1988 (1988): 648–50. https://doi.org/10.5281/zenodo.6043069.

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Department of Chemistry, Saurashtra University, Rajkot-360 005 <em>Manuscript received 18 January 1988, revised 5 May 1988, accepted 6 July 1988</em> Several new 4-thiazolidinone derivatives were prepared bearing 2,4- diphenylamino-6-amino-<em>s</em>-triazine moiety. Their structures were supported by ir and mass spectral study. The products were screened for antimicrobial activity.

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18

Journal, Baghdad Science. "Synthesis, Characterization and Antimicrobial Screening of New Schiff Bases Linked to Phthalimidyl Phenyl Sulfonate Moiety." Baghdad Science Journal 11, no. 2 (2014): 438–46. http://dx.doi.org/10.21123/bsj.11.2.438-446.

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A series of Schiff bases linked to phthalimidyl phenyl sulfonate moiety have been synthesized via multistep synthesis. The first step involved reaction of phthalic anhydride with aniline producing N-phenyl phthalamic acid which was subsequently dehydrated to the corresponding N-phenyl phthalimide via treatment with acetic anhydride and anhydrous sodium acetate. The synthesized imide was treated with chlorosulfonic acid in the third step producing 4-(N-phthalimidyl) phenyl sulfonyl chloride which was introduced in reaction with 4-hydroxy acetophenone in the fourth step producing 4-[4-(N-phthali

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19

Al-Azzawi, Ahlam M., and Marwa S. Abd Al-Razzak. "Synthesis, Characterization and Antimicrobial Screening of New Schiff Bases Linked to Phthalimidyl Phenyl Sulfonate Moiety." Baghdad Science Journal 11, no. 2 (2014): 438–46. http://dx.doi.org/10.21123/bsj.2014.11.2.438-446.

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A series of Schiff bases linked to phthalimidyl phenyl sulfonate moiety have been synthesized via multistep synthesis. The first step involved reaction of phthalic anhydride with aniline producing N-phenyl phthalamic acid which was subsequently dehydrated to the corresponding N-phenyl phthalimide via treatment with acetic anhydride and anhydrous sodium acetate. The synthesized imide was treated with chlorosulfonic acid in the third step producing 4-(N-phthalimidyl) phenyl sulfonyl chloride which was introduced in reaction with 4-hydroxy acetophenone in the fourth step producing 4-[4-(N-phthali

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20

Navin, Patel, Patel Sarvil, Purohit Amit, et al. "Synthesis and biological evaluation of newer 1,3,4-oxadiazoles incorporated with benzothiazepine and benzodiazepine moieties." Zeitschrift für Naturforschung C 72, no. 3-4 (2017): 133–46. http://dx.doi.org/10.1515/znc-2016-0129.

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Abstract A series of thiazepines and diazepines having 1,3,4-oxadiazole moiety were synthesized, and they were analyzed for their in vitro antimicrobial activity against several bacteria (Staphylococcus aureus, Staphylococcus pyogenes, Escherichia coli, and Pseudomonas aeruginosa) and fungi (Candida albicans, Aspergillus niger, and Aspergillus Clavatus) and protozoa (Entamoeba histolytica, Giardia lamblia, Trypanosoma cruzi and Leishmania mexicana). Few of the selected compounds were tested for their antitubercular activity. However, it was noticed that the potency of final analogs against eac

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21

Rogala, Patrycja, Agnieszka Jabłońska-Wawrzycka, Grzegorz Czerwonka, et al. "Synthesis, Characterization and Biological Investigations of Half-Sandwich Ruthenium(II) Complexes Containing Benzimidazole Moiety." Molecules 28, no. 1 (2022): 40. http://dx.doi.org/10.3390/molecules28010040.

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Half-sandwich Ru(II) complexes belong to group of biologically active metallo-compounds with promising antimicrobial and anticancer activity. Herein, we report the synthesis and characterization of arene ruthenium complexes containing benzimidazole moiety, namely, [(η6-p-cymene)RuCl(bimCOO)] (1) and [(η6-p-cymene)RuCl2(bim)] (2) (where bimCOO = benzimidazole-2-carboxylate and bim = 1-H-benzimidazole). The compounds were characterized by 1H NMR, 13C NMR, IR, UV–vis and CV. Molecular structures of the complexes were determined by SC-XRD analysis, and the results indicated the presence of a pseud

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22

Sharma, Shobhana, Poonam Yadav, Seema, Suman Kumari, and Mamta Ranka. "ANTIMICROBIAL STUDY AND SYNTHESIS OF MIXED LIGAND COMPLEX OF Ni(II) ION DERIVED FROM ISATIN SCHIFF BASE AND HISTIDINE." RASAYAN Journal of Chemistry 15, no. 02 (2022): 836–41. http://dx.doi.org/10.31788/rjc.2022.1526584.

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Recently, heterocyclic compounds and amino acids are of great interest to researchers owing to their various biological activities like; antimicrobial, anticancer, antiviral, anti-inflammatory, etc. Isatin is also a vital moiety containing N and O donor heteroatoms, and its Schiff base is used for complexation with metal ions which may alter their activities. The new metal complex of Ni has been synthesized using two ligands, 3-(2-phenylhydrazono) indolin-2-one (PHI) (L1) and amino acid Histidine (L2). The newly prepared ligand and the complex are further characterized by determination of mole

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23

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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24

Bamou, Fatima Zahra, Tam Minh Le, Bettina Volford, András Szekeres, and Zsolt Szakonyi. "Synthesis and Application of 1,2-Aminoalcohols with Neoisopulegol-Based Octahydrobenzofuran Core." Molecules 25, no. 1 (2019): 21. http://dx.doi.org/10.3390/molecules25010021.

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A library of 1,2-aminoalcohol derivatives with a neoisopulegol-based octahydrobenzofuran core was developed and applied as chiral catalysts in the addition of diethylzinc to benzaldehyde. The allylic chlorination of (+)-neoisopulegol, derived from natural (–)-isopulegol followed by cyclization, gave the key methyleneoctahydrobenzofuran intermediate. The stereoselective epoxidation of the key intermediate and subsequent oxirane ring opening with primary amines afforded the required 1,2-aminoalcohols. The ring closure of the secondary amine analogues with formaldehyde provided spiro-oxazolidine

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25

R., M. Kedar S. A. Deshmukh. "SYNTHESIS AND ANTIMICROBIAL ACTIVITY OF 1-(4-CHLOROPHENYL)-2-(3-SULPHOXYPHENYL-4-(4-SUBSTITUTED BENZYLIDENE)-5-IMIDAZOLONES." INDO AMERICAN JOURNAL OF PHARMACEUTICAL RESEARCH 07, no. 01 (2017): 7526–31. https://doi.org/10.5281/zenodo.1007273.

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Imidazolones are believed to be associated with several pharmacological activities. Their significance lies in the fact that they show diverse biological activities. Which include anticancer, anticonvulsant, antiparkinsonian, CNS depressant, antimicrobial, antihelmintic, anti HIV, anti-inflammatory etc.However no work is reported on imidazolone from substituted benzoyl glycine.Therefore it was thought interesting to attempt synthesis of imidazolones containing new substituent and study there antimicrobial activity In the proposed work, we have reported eight newly synthesized sulphoxy substitu

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26

Szwaczko, Katarzyna. "Coumarins Synthesis and Transformation via C–H Bond Activation—A Review." Inorganics 10, no. 2 (2022): 23. http://dx.doi.org/10.3390/inorganics10020023.

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For several decades, coumarins have attracted considerable attention due to the fact of their application in diverse fields such as medical science and biomedical research as well as several industrial branches. Recently, many compounds containing the coumarin moiety have been intensively studied, mainly due to the fact of their biological activities such as antitumor, antioxidative, anti-HIV, vasorelaxant, antimicrobial, and anticancer. They are also widely used as fluorescent dyes and probes because of their great structural flexibility and large fluorescent quantum yields. For this reason,

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27

Mohammad, Asif. "Anti-neuropathic and anticonvulsant activities of various substituted triazoles analogues." Chemistry International 1, no. 4 (2015): 174–83. https://doi.org/10.5281/zenodo.1470200.

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Various heterocyclic compounds along their derivatives were evaluated for their biological activities as antiviral, antitumor, anticonvulsant, antibacterial, antifungal, antituberculosis, analgesic, anti-inflammatory, antidiabetic, antihistamine and other biological activities. The triazole moiety seems to be very small, but in the biological profile has attracted the attention of many researchers to explore this skeleton to its multiple potential against several activities. The triazole derivatives possess a great importance in medicinal chemistry and can be used for the synthesis of numerous

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28

Koshti, S. "Synthesis, Antimicrobial, Anthelmintic Activity, Enzymatic Degradation and Molecular Docking Studies of Some Azo Compounds containing Carvacrol Moiety." Asian Journal of Chemistry 34, no. 12 (2022): 3206–14. http://dx.doi.org/10.14233/ajchem.2022.23949.

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In present work, the carvacrol was derivatized as azo compound by coupling method with eight different diazonium salts. The newly synthesized azo derivatives of carvacrol screened against four bacterial species and four fungal species and expressed in terms of zone of inhibition in mm and compared with standard. Furthermore, enzymatic degradation studies also been done by inoculating these newly synthesized azo derivatives with Pseudomonas aeruginosa bacterium species, which secretes the azoreductase enzyme as responsible for reduction of –N=N– linkage into two different primary aromatic amine

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29

Bakhale, Sunil C., and Pushpendra Tiwari. "Synthesis, Characterization and Antimicrobial Evaluation of Aromatic Aldehyde Derivatives of 4-Hydrazinyl-7H-pyrrolo[2,3-d]pyrimidine." Asian Journal of Chemistry 37, no. 2 (2025): 355–60. https://doi.org/10.14233/ajchem.2025.33044.

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A novel series of pyrrolo[2,3-d]pyrimidine derivatives (2a-j), incorporating a biologically active hydrazone moiety, was synthesized and subjected to antibacterial evaluation. Structural elucidation of the synthesized compounds was achieved using various spectroscopic methods, including IR, 1H and 13C NMR and mass spectrometry. The compounds demonstrated antibacterial and antifungal activities, with MIC values ranging between 50 and 250 µg/mL. The most resistant strains tested were Escherichia coli (MCC 2412), Staphylococcus aureus (MCC 2408), Bacillus subtilis (MCC 2010), Pseudomonas aerugino

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30

A. Phor, Mamta, Subhash, J. S. Phor, R. Kumar, and A. Chaudhary. "DESIGN, SYNTHESIS, SPECTRAL ANALYSIS, ANTIMICROBIAL EVALUATION AND TOXICOLOGICAL ASPECTS OF BIVALENT TIN COMPLEXES WITH MACROCYCLIC MOIETY." RASAYAN Journal of Chemistry 17, no. 01 (2024): 78–86. http://dx.doi.org/10.31788/rjc.2024.1718631.

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The novel complexes Sn(II), were synthesized of macrocyclic ligands derived from various diamine and dicarboxylic acids in the ratio of 2:2 and characterized by elemental analysis, molar conductance measurements, mass, NMR, FT-IR, and electronic spectra. The interactions of macrocyclic ligands (MLn) with SnCl2 in a 1:1 molar ratio in methanol produced the ensuing physiologically active [Sn(MLn)Cl2] type complexes, where n = 1 or 2. The complexes were initially identified using conductivity tests, molecular weight calculations, and elemental investigations. The bonding mode was determined using

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31

Kaur, Harmeet, Sapna D. Desai, Jasbir Singh, and Balasubramanian Narasimhan. "Morpholine Based Diazenyl Chalcones: Synthesis, Antimicrobial Screening and Cytotoxicity Study." Anti-Cancer Agents in Medicinal Chemistry 18, no. 15 (2019): 2193–205. http://dx.doi.org/10.2174/1871520618666180830152701.

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Background: Microbial infections have been the major cause of morbidity and mortality for the centuries and continue to present the formidable challenge to the human health. Several studies have been performed to explore the antimicrobial potential of various synthesized chalcone derivatives. The morpholine derivatives are also gaining considerable importance due to diverse biological activities. Hybridization of morpholine and chalcone moiety together can be the useful approach for the development of new effective antimicrobial agents. Methods: A new series of morpholine based heterocyclic di

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32

Freitas, Emanuelle Dantas, Celso Fidelis Moura Jr., Jonas Kerwald, and Marisa Masumi Beppu. "An Overview of Current Knowledge on the Properties, Synthesis and Applications of Quaternary Chitosan Derivatives." Polymers 12, no. 12 (2020): 2878. http://dx.doi.org/10.3390/polym12122878.

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Chitosan, a chitin-derivative polysaccharide, known for its non-toxicity, biocompatibility and biodegradability, presents limited applications due to its low solubility in neutral or basic pH medium. Quaternization stands out as an alternative to modify this natural polymer, aiming to improve its solubility over a wide pH range and, consequently, expand its range of applications. Quaternization occurs by introducing a quaternary ammonium moiety onto or outside the chitosan backbone, via chemical reactions with primary amino and hydroxyl groups, under vast experimental conditions. The oldest an

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33

Kerner, Lukáš, та Paul Kosma. "Synthesis of C-glycosyl phosphonate derivatives of 4-amino-4-deoxy-α-ʟ-arabinose". Beilstein Journal of Organic Chemistry 16 (2 січня 2020): 9–14. http://dx.doi.org/10.3762/bjoc.16.2.

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The incorporation of basic substituents into the structurally conserved domains of cell wall lipopolysaccharides has been identified as a major mechanism contributing to antimicrobial resistance of Gram-negative pathogenic bacteria. Inhibition of the corresponding enzymatic steps, specifically the transfer of 4-amino-4-deoxy-ʟ-arabinose, would thus restore the activity of cationic antimicrobial peptides and several antimicrobial drugs. C-glycosidically-linked phospholipid derivatives of 4-amino-4-deoxy-ʟ-arabinose have been prepared as hydrolytically stable and chain-shortened analogues of the

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Jeremic, Marko, Jelena Dinic, Milica Pesic, et al. "Alkylamino and aralkylamino derivatives of avarone and its mimetic as selective agents against non-small cell lung cancer cells, their antibacterial and antifungal potential." Journal of the Serbian Chemical Society 83, no. 11 (2018): 1193–207. http://dx.doi.org/10.2298/jsc180627062j.

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In this paper, the synthesis of fourteen alkylamino and arylamino derivatives of sesquiterpene quinone avarone and its model compound tert-butylquinone is described. Branched, cyclic, allylic and benzylic alkylamino/arylamino groups were introduced into the quinone moiety. For all the obtained derivatives, their biological activity and redox properties were studied. The cytotoxic activity of the synthesized derivatives towards multidrug resistant (MDR) human non-small cell lung carcinoma NCI-H460/R cells, their sensitive counterpart NCI-H460 and human normal keratinocytes (HaCaT) was investiga

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Grymel, Mirosława, Anna Lalik, Alicja Kazek-Kęsik, Marietta Szewczyk, Patrycja Grabiec, and Karol Erfurt. "Design, Synthesis and Preliminary Evaluation of the Cytotoxicity and Antibacterial Activity of Novel Triphenylphosphonium Derivatives of Betulin." Molecules 27, no. 16 (2022): 5156. http://dx.doi.org/10.3390/molecules27165156.

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For several decades, natural products have been widely researched and their native scaffolds are the basis for the design and synthesis of new potential therapeutic agents. Betulin is an interesting biologically attractive natural parent molecule with a high safety profile and can easily undergo a variety of structural modifications. Herein, we describe the synthesis of new molecular hybrids of betulin via covalent linkage with an alkyltriphenylphosphonium moiety. The proposed strategy enables the preparation of semi-synthetic derivatives (28-TPP⊕ BN and 3,28-bisTPP⊕ BN) from betulin through s

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M. Ahmed, Sarbast, Hewa Omer Ahmed, Faiq H. S. Hussain, Hayman Sardar Abdulrahman, and Hemn A. Qader. "Synthesis and Antimicrobial Activity of some Ester Functionalized Isoxazoles incorporating Anthracene Moieties via Nucleophilic Substitution Reaction." Zanco Journal of Medical Sciences 27, no. 2 (2023): 213–26. http://dx.doi.org/10.15218/zjms.2023.024.

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Background and objective: Five-membered heterocycle compounds having single oxygen and nitrogen atom at adjacent positions are known as isoxazoles. Isoxazole compounds have a broad range of biological activities and therapeutic value. In view of a strategic design of antimicrobial compounds, several new ester-functionalized isoxazoles were synthesized and characterized. Methods: A regioselective isoxazole incorporating an anthracene moiety was adducted via an effective 1,3-dipolar cycloaddition between anthracene nitrile oxide and propargyl bromide as a dipolarophile. Results: Synthesized isox

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Hong, Song, Sachin B. Baravkar, Yan Lu, Abdul-Razak Masoud, Qi Zhao, and Weilie Zhou. "Molecular Modification of Queen Bee Acid and 10-Hydroxydecanoic Acid with Specific Tripeptides: Rational Design, Organic Synthesis, and Assessment for Prohealing and Antimicrobial Hydrogel Properties." Molecules 30, no. 3 (2025): 615. https://doi.org/10.3390/molecules30030615.

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Royal jelly and medical grade honey are traditionally used in treating wounds and infections, although their effectiveness is often variable and insufficient. To overcome their limitations, we created novel amphiphiles by modifying the main reparative and antimicrobial components, queen bee acid (hda) and 10-hydroxyl-decanoic acid (hdaa), through peptide bonding with specific tripeptides. Our molecular design incorporated amphiphile targets as being biocompatible in wound healing, biodegradable, non-toxic, hydrogelable, prohealing, and antimicrobial. The amphiphilic molecules were designed in

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Bechi, Beatrice, David Amantini, Cristina Tintori, Maurizio Botta, and Romano di Fabio. "Stereocontrolled synthesis of 5-azaspiro[2.3]hexane derivatives as conformationally “frozen” analogues of L-glutamic acid." Beilstein Journal of Organic Chemistry 10 (May 14, 2014): 1114–20. http://dx.doi.org/10.3762/bjoc.10.110.

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Several strategies aimed to “freeze” natural amino acids into more constrained analogues have been developed with the aim of enhancing in vitro potency/selectivity and, more in general, drugability properties. The case of L-glutamic acid (L-Glu, 1) is of particular importance since it is the primary excitatory neurotransmitter in the mammalian central nervous system (CNS) and plays a critical role in a wide range of disorders like schizophrenia, depression, neurodegenerative diseases such as Parkinson’s and Alzheimer’s and in the identification of new potent and selective ligands of ionotropic

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Kacsir, István, Adrienn Sipos, Evelin Major, et al. "Half-Sandwich Type Platinum-Group Metal Complexes of C-Glucosaminyl Azines: Synthesis and Antineoplastic and Antimicrobial Activities." Molecules 28, no. 7 (2023): 3058. http://dx.doi.org/10.3390/molecules28073058.

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While platinum-based compounds such as cisplatin form the backbone of chemotherapy, the use of these compounds is limited by resistance and toxicity, driving the development of novel complexes with cytostatic properties. In this study, we synthesized a set of half-sandwich complexes of platinum-group metal ions (Ru(II), Os(II), Ir(III) and Rh(III)) with an N,N-bidentate ligand comprising a C-glucosaminyl group and a heterocycle, such as pyridine, pyridazine, pyrimidine, pyrazine or quinoline. The sugar-containing ligands themselves are unknown compounds and were obtained by nucleophilic additi

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Sekularac, Gavrilo, Jasmina Nikolic, Predrag Petrovic, Branko Bugarski, Boban Djurovic, and Sasa Drmanic. "Synthesis, antimicrobial and antioxidative activity of some new isatin derivatives." Journal of the Serbian Chemical Society 79, no. 11 (2014): 1347–54. http://dx.doi.org/10.2298/jsc140709084s.

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The isatin derivatives, Schiff bases, were synthesized by the reaction of isatin and various substituted primary amines and characterized by several spectroscopic methods. Investigation of the antimicrobial activity of the synthesized compounds was performed by the agar dilution method, against different strains of bacteria and one fungi. The antioxidative activity of the synthesized compounds was also determined. Some of the compounds have shown the significant activity against the selected strains of microorganisms and the antioxidative activity.

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Apostol, Theodora-Venera, Luminita Gabriela Marutescu, Constantin Draghici та ін. "Synthesis and Biological Evaluation of New N-Acyl-α-amino Ketones and 1,3-Oxazoles Derivatives". Molecules 26, № 16 (2021): 5019. http://dx.doi.org/10.3390/molecules26165019.

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In order to develop novel bioactive substances with potent activities, some new valine-derived compounds incorporating a 4-(phenylsulfonyl)phenyl fragment, namely, acyclic precursors from N-acyl-α-amino acids and N-acyl-α-amino ketones classes, and heterocycles from the large family of 1,3-oxazole-based compounds, were synthesized. The structures of the new compounds were established using elemental analysis and spectral (UV-Vis, FT-IR, MS, NMR) data, and their purity was checked by reversed-phase HPLC. The newly synthesized compounds were evaluated for their antimicrobial and antibiofilm acti

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Senthil Kumar, Raju, Sundhararajan Naveena, Sekar Praveen, and Nagalingam Yogadharshini. "Therapeutic aspects of biologically potent vanillin derivatives: A critical review." Journal of Drug Delivery and Therapeutics 13, no. 7 (2023): 177–89. http://dx.doi.org/10.22270/jddt.v13i7.6159.

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4-hydroxy 3-methoxy benzaldehyde (Vanillin) is an aromatic phenolic aldehyde with unique chemical properties and pharmacological impact. Because of its potent nature, it acts as a lead for drug discovery and development techniques. Heterocyclic compounds with vanillin moiety were efficacious and thrive against many emerging infectious diseases, which can also lead to develop numerous fused heterocyclic vanillin derivatives and various heterocyclic compounds such as pyrimidines, quinoxalines, imidazoles or thiazoles. Greener-mediated synthesis is a sustained chemical reaction used to synthesize

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Barbarossa, Alexia, Jessica Ceramella, Alessia Carocci, et al. "Benzothiazole-Phthalimide Hybrids as Anti-Breast Cancer and Antimicrobial Agents." Antibiotics 12, no. 12 (2023): 1651. http://dx.doi.org/10.3390/antibiotics12121651.

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The benzothiazole nucleus is a major heterocyclic scaffold whose therapeutic potential has been thoroughly explored due to its structural simplicity and ease of synthesis. In fact, several benzothiazole derivatives have been synthesized over time, demonstrating numerous pharmacological properties such as anticancer, antimicrobial, anti-inflammatory, and antioxidant activities. Herein, we propose a new series of benzothiazole-phthalimide hybrids obtained by linking the phthalimide moiety to differently substituted benzothiazole nuclei through the N atom. These compounds have been screened for t

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Zúñiga-Miranda, Johana, Julio Guerra, Alexander Mueller, et al. "Iron Oxide Nanoparticles: Green Synthesis and Their Antimicrobial Activity." Nanomaterials 13, no. 22 (2023): 2919. http://dx.doi.org/10.3390/nano13222919.

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The rise of antimicrobial resistance caused by inappropriate use of these agents in various settings has become a global health threat. Nanotechnology offers the potential for the synthesis of nanoparticles (NPs) with antimicrobial activity, such as iron oxide nanoparticles (IONPs). The use of IONPs is a promising way to overcome antimicrobial resistance or pathogenicity because of their ability to interact with several biological molecules and to inhibit microbial growth. In this review, we outline the pivotal findings over the past decade concerning methods for the green synthesis of IONPs u

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Almalki, Ahmad J., Tarek S. Ibrahim, Ehab S. Taher, et al. "Synthesis, Antimicrobial, Anti-Virulence and Anticancer Evaluation of New 5(4H)-Oxazolone-Based Sulfonamides." Molecules 27, no. 3 (2022): 671. http://dx.doi.org/10.3390/molecules27030671.

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Since the synthesis of prontosil the first prodrug shares their chemical moiety, sulfonamides exhibit diverse modes of actions to serve as antimicrobials, diuretics, antidiabetics, and other clinical applications. This inspiring chemical nucleus has promoted several research groups to investigate the synthesis of new members exploring new clinical applications. In this study, a novel series of 5(4H)-oxazolone-based-sulfonamides (OBS) 9a–k were synthesized, and their antibacterial and antifungal activities were evaluated against a wide range of Gram-positive and -negative bacteria and fungi. Mo

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Saadeh, Haythem A., Kamal A. Sweidan, and Mohammad S. Mubarak. "Recent Advances in the Synthesis and Biological Activity of 8-Hydroxyquinolines." Molecules 25, no. 18 (2020): 4321. http://dx.doi.org/10.3390/molecules25184321.

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Compounds containing the 8-hydroxyquinoline (8-HQ) 1 nucleus exhibit a wide range of biological activities, including antimicrobial, anticancer, and antifungal effects. The chemistry and biology of this group have attracted the attention of chemists, medicinal chemists, and professionals in health sciences. A number of prescribed drugs incorporate this group, and numerous 8-HQ- based molecules can be used to develop potent lead compounds with good efficacy and low toxicity. This review focusses on the recent advances in the synthesis of 8-HQ derivatives with different pharmacological propertie

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Khan, Tahmeena, Saima Zehra, Almas Alvi, Umama Fatima, and Alfred J. Lawrence. "Medicinal Utility of Some Schiff Bases and their Complexes with First Transition Series Metals: A Review." Oriental Journal Of Chemistry 37, no. 5 (2021): 1051–61. http://dx.doi.org/10.13005/ojc/370506.

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Schiff based ligands and their complexes have emerged as potential drug candidates. Owing to their excellent chelating tendency, they easily coordinate with transition metals which have vacant orbitals. Transition metal complexes have several advantages because of their better acceptability and low toxicity in biological systems. These metals also serve as micronutrients and as co-factors of various metallo-enzymes which justifies the need of their designing and synthesis. Many modifications have been suggested in the ligand moiety for the purpose of activity enhancement and some of them have

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Ramesh, Pulabala, Vankadari Srinivasa Rao, Puchakayala Muralidhar Reddy, Katragadda Suresh Babu, and Mutheneni Srinivasa Rao. "Synthesis, Biological Evaluation and Molecular Modeling Studies of Novel C (7) Modified Analogues of Chrysin." Letters in Drug Design & Discovery 17, no. 7 (2020): 873–83. http://dx.doi.org/10.2174/1570180816666190913183623.

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Background:: Most of the currently available pharmaceutical drugs are either natural products or analogues of natural products. Flavonoids are plant based natural polyphenolic compounds which exhibit a wide range of biological activities. Chrysin, a natural flavone, exhibits several biological activities like antiallergic, anti-inflammatory and anticancer. Many efforts were made to enhance the biological activity of chrysin. In continuation of our work on synthetic modifications of chrysin, amino-alcohol containing heterocyclic moiety is linked to chrysin at C (7) position to enhance its biolo

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Zakharova, Pashirova, Doktorovova, et al. "Cationic Surfactants: Self-Assembly, Structure-Activity Correlation and Their Biological Applications." International Journal of Molecular Sciences 20, no. 22 (2019): 5534. http://dx.doi.org/10.3390/ijms20225534.

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The development of biotechnological protocols based on cationic surfactants is a modern trend focusing on the fabrication of antimicrobial and bioimaging agents, supramolecular catalysts, stabilizers of nanoparticles, and especially drug and gene nanocarriers. The main emphasis given to the design of novel ecologically friendly and biocompatible cationic surfactants makes it possible to avoid the drawbacks of nanoformulations preventing their entry to clinical trials. To solve the problem of toxicity various ways are proposed, including the use of mixed composition with nontoxic nonionic surfa

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Depp, Dima, Noémi Regina Sebők, András Szekeres, and Zsolt Szakonyi. "Stereoselective Synthesis and Antimicrobial Studies of Allo-Gibberic Acid-Based 2,4-Diaminopyrimidine Chimeras." Pharmaceuticals 18, no. 2 (2025): 168. https://doi.org/10.3390/ph18020168.

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Background: Gibberellins (GAs) are a family of tetracyclic ent-kaurenoid diterpenes found widely in several commonly used plants. Besides agricultural applications, gibberellins play an important role in the synthesis of bioactive compounds, especially those with antiproliferative and antibacterial activity. Methods: A series of gibberellic acid-based 2,4-diaminopyrimidines was designed and synthesized from commercially available gibberellic acid. The antimicrobial activity of the prepared compounds was also explored in B. subtilis, S. aureus, E. coli, and P. aeruginosa bacteria, as well as in

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