Antimicrobial activities and mode of action of the selected novel thienopyrimidines derivatives 2-[2-(diphenylmethylene) hydrazino]-5-isopropyl-3-methylthieno [2, 3-d] pyrimidin-4-one

El-Batanony, Nadia H.

doi:10.18054/pb.v119i1.4393

Cited by 5 publications

(4 citation statements)

References 25 publications

(41 reference statements)

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“…Damage to cell membranes, which is often secondary to cell wall disruption, is characterized by discernable leakage of cytoplasmic constituents, especially low molecular weight constituents such as potassium ions ( Abbanat et al, 1998 ; Amarnath et al, 2003 ; Epstein, 2003 ; Johnston et al, 2003 ; Amin et al, 2015 ; El-Batanony, 2017 ). Quinine and chloroquine alone, and in combination with ampicillin did not result in appreciable amounts of potassium leakage even at the MIC of quinine ( Table 3 ).…”

Section: Discussionmentioning

confidence: 99%

Quinoline Antimalarials Increase the Antibacterial Activity of Ampicillin

et al. 2021

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Bacterial and malaria co-infections are common in malaria endemic countries and thus necessitate co-administration of antibiotics and antimalarials. There have long been anecdotal clinical reports of interactions between penicillins and antimalarial agents, but the nature and mechanisms of these interactions remain to be investigated. In this study, we employed antimicrobial interaction testing methods to study the effect of two antimalarials on the antibacterial activity of ampicillin in vitro. Paper strip diffusion, a modified disc diffusion and checkerboard methods were used to determine the nature of interactions between ampicillin and quinoline antimalarials, chloroquine and quinine, against Gram-positive and Gram-negative bacteria. The impact of antimalarials and ampicillin-antimalarial drug combinations on cell integrity of test bacteria were determined by measuring potassium release. The tested antimalarials did not show substantial antibacterial activity but quinine was bactericidal at high concentrations. Chloroquine and quinine increased ampicillin activity, with increasing concentrations extending the antibacterial’s inhibition zones by 2.7-4.4 mm and from 1.1 to over 60 mm, respectively. Observed interactions were largely additive with Fractional Inhibitory Concentration Indices of >0.5-1 for all ampicillin-antimalarial combinations. Quinine and, to a lesser extent, chloroquine increase the activity of ampicillin and potentially other β-lactams, which has implications for combined clinical use.

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Section: Discussionmentioning

confidence: 99%

Quinoline Antimalarials Increase the Antibacterial Activity of Ampicillin

et al. 2021

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“…Consequently, the enzyme β-galactosidase is dispensed into the culture, which is identified by a suitable chromogenic reagent substrate reacting with the enzyme resulting in the production of color around the test compound, which is used as a DNA-damaging induction in the colorimetric broth micro-dilution method [ 53 ]. This assay was carried out according to the method described by Hamed El-Batanony [ 54 ] with slight modifications. In short, a sterile cotton swab of E. coli suspension (10 8 CFU/mL) was evenly dispensed on agar plates and incubated at 37 °C for 48 h. The plates were spotted with 1x, 2x MIC, 10 µg/mL ciprofloxacin (positive control), and PBS (negative control), then incubated at 37 °C for 3 h. After incubation, the plates were overlaid with a methanolic solution of 6-Bromo-2-naphthyl B-D-glucopyranoside (8 mg/mL) (Sigma-Aldrich, Louis, MO, USA).…”

Section: Methodsmentioning

confidence: 99%

Antibacterial Mechanism of Action of Two Types of Honey against Escherichia coli through Interfering with Bacterial Membrane Permeability, Inhibiting Proteins, and Inducing Bacterial DNA Damage

et al. 2022

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Honey is a sweet natural food produced by bees from flower nectar or some part of plant secretions that exhibit antimicrobial activity against many microorganisms. It has been used as traditional therapy for skin infections. Antibiotics play an essential role in managing wound infection; however, some pathogenic bacteria have begun to possess resistance against them, which may cause chronic infections and severe adverse effects. This study investigates the antibacterial activities and mechanism of action of Yemeni Sidr honey (SH) and Manuka honey (MH) against Escherichia coli. The inhibitory effects of SH and MH using the disk diffusion method on bacterial growth were remarkable at 700 mg/disk. The minimum inhibitory concentration (MIC) and minimum bactericidal concentration (MBC) were similar for both kinds of honey. However, MH showed a better bactericidal effect (30%) than SH (50%). The antimicrobial mechanism of action showed that SH substantially impacted the bacterial membrane's permeability and increased the potassium and protein leakage rate. On the contrary, MH demonstrated remarkable inhibition of bacterial protein synthesis, while both kinds of honey caused bacterial DNA damage. These data reveal that SH and MH could be used as a remedy for skin infections and might be further developed as a promising dressing for bacterial wound infections.

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“…Heterocyclic pipyridinium and glucopyranose quaternary ammonium salts are new groups of Quaternary Ammonium compounds which have shown good antimicrobial activity [7]. Thienopyrimidines act on membrane potentials, membrane permeability and net surface charge of the bacterial membranes by their physicochemical characteristics leading to leakage of cellular contents and bacterial death [8]. Phenolic compounds are widely used as antibacterial agents and numerous mechanisms are understood for their bactericidal activity.…”

Section: Mechanism Of Actionmentioning

confidence: 99%

“…Antimicrobial properties of forty two adamantyl based cyclohexane diamine derivatives (as shown in Figure 1 hydrazino]-5-isopropyl-3methylthieno [2, 3-d] pyrimidin-4-one showed most strong antimicrobial properties [8]. Six new benzoxazolinone derivatives were prepared and investigated for antimicrobial properties.…”

Section: Antimicrobial Properties Of Functionally Substituted Chemicamentioning

confidence: 99%

Functionally Substituted Chemical Organic Compounds: Potential Antimicrobial Substances

Ganbar¹

2019

OAJMB

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The development of resistance to antimicrobial agents is a global health problem for humans as well as animals. Over the past decade, the rate of microbial resistance to antibiotics has alarmingly increased. Factors contributing to this ever increasing antibiotic resistance pertain to microorganism as well as excessive and unwise use of the antibiotics. Biofilm formation and use of efflux pumps are the examples of microbial factors responsible for emergence of antimicrobial resistance. To ameliorate this condition, it is dire need of time to develop new antimicrobial agents. In this regard, chemical organic compounds are best available substances with potential antimicrobial properties. This review summarizes the antimicrobial activities of some important organic compounds as well as potential of functionally substituted chemical organic compounds as probable antimicrobial agents of future. These important organic compounds include functionally substituted derivatives of cyclohexane, quaternary ammonium compounds, hydrazones, pyrazolone, triazole, thiones, isatin, indole, chalcones, quinoxaline, anthraquinones, coumarins, thiophenes, piperidine, benzoxazolinone, phthalazinone, sulfones, thiazole and volatile organic compounds.

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Antimicrobial activities and mode of action of the selected novel thienopyrimidines derivatives 2-[2-(diphenylmethylene) hydrazino]-5-isopropyl-3-methylthieno [2, 3-d] pyrimidin-4-one

Cited by 5 publications

References 25 publications

Quinoline Antimalarials Increase the Antibacterial Activity of Ampicillin

Quinoline Antimalarials Increase the Antibacterial Activity of Ampicillin

Antibacterial Mechanism of Action of Two Types of Honey against Escherichia coli through Interfering with Bacterial Membrane Permeability, Inhibiting Proteins, and Inducing Bacterial DNA Damage

Functionally Substituted Chemical Organic Compounds: Potential Antimicrobial Substances

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