ABSTRACT
In the pursuit of novel antimicrobial solutions, this project explores the synthetic modification of the widely used drug metformin through the incorporation of aromatic aldehydes; vanillin (4-hydroxy-3-methoxybenzaldehyde) and benzaldehyde through the conventional method of forming Schiff base compounds with a percentage yield of 66% and 56% respectively. The synthetic procedures involve the reaction of metformin with vanillin and benzaldehyde using a reflux under suitable conditions, followed by the purification and characterization of the resulting Schiff base derivatives using standard analytical techniques, including Fourier Transform Infrared Spectroscopy (FT-IR) and UV-visible spectroscopy. The FT-IR spectrums of the two compounds showed C=N absorption bands at 1662.4 cm-1 and 1625.1 cm-1 and maximum wavelength of absorption at 230 nm and 236 nm respectively. The antimicrobial potential of the synthesized Schiff base compounds will be evaluated against a panel of clinically relevant bacterial and fungal strains; staphylococcus aureus, pseudomonas aeruginosa, aspergillus fumigatus and aspergillus flavus through standard microbiological assay, disk diffusion method. The anticipated outcome of this research was the development of novel Schiff base derivatives of metformin, incorporating vanillin and benzaldehyde moieties, exhibiting potent antimicrobial properties against a spectrum of pathogenic microorganisms. This work has the potential to provide valuable insights into the utilization of conventional synthetic strategies for the repurposing of existing drugs, thereby contributing to the advancement of novel antimicrobial therapies in the face of the growing challenge of antimicrobial resistance.
Table of contents
Title Page………………………………………………………………………....i
Declaration ii
Certification iii
Dedication iv
Acknowledgment v
Abstract vi
Table Of Content vii
List Of Tables x
CHAPTER ONE
1.0 INTORODUCTION
1.1 Background of the Study 1
1.2 Statement of Problem 3
1.3 Justification of the Study 3
1.4 Aim and Objectives of Study 4
CHAPTER TWO
2.0 LITERATURE REVIEW
2.1 Introduction 5
2.2 Drug Repurposing 6
2.3 Metformin 6
2.4 Chemistry of Metformin 8
2.5 Antimicrobial Activities of Vanillin 8
2.6 Chemistry of Vanillin 9
2.7 Benzaldehyde 9
2.8 Schiff Base 10
CHAPTER THREE
3.0 METHODOLOGY
3.1 Introduction 12
3.2 Material 12
3.3 Instrument 12
3.4 Apparatus 12
3.5 Methods 13
3.5.1 Procedure for the synthesis of compound I 13
3.5.2 Procedure for the synthesis of compound II 13
3.6 Characterization 14
3.6.1 Melting Point 14
3.6.2 Thin layer chromatography 14
3.6.3 FT-IR 14
3.6.4 Antimicrobial Screening 14
3.6.5 Serial Dilution – 2 fold dilution 14
3.6.6 Preparation of bacterial and fungi media 15
3.6.7 Inoculation of the Media 15
CHAPTER FOUR
4.0 RESULTS AND DISCUSSION
4.1 Introduction 16
4.2 Results 16
4.2.1 Chemical data of compound 16
4.2.2 Spectroscopic data of compounds 17
4.2.3 Antimicrobial screening 19
4.3 Discussion 20
4.3.1 Synthesis and characterization 20
4.3.2 Antibacterial Activity 21
CHAPTER FIVE
5.0 SUMMARY, CONCLUSION AND RECOMMENDATION
5.1 Summary 22
5.2 Conclusion 22
5.3 Recommendation 23
APPENDICES 24
REFERENCES 30
LIST OF TABLES
Table 4.1: Physical and chemical data of synthesized compounds 16
Table 4.2: Spectroscopic data of synthesized compounds 17
Table 4.3: Antimicrobial effect of compound I in (mm) on some microbes 19
Table 4.4: Antimicrobial effect of compound II in (mm) on some microbes. 20
CHAPTER ONE
1.0 INTORODUCTION
1.1 Background of the Study
Drug resistance is the reduction in effectiveness of a medication or a drug such as an antimicrobial or an antineoplastic in treating a disease, illness or condition (Alfarouk et al., 2015). Antimicrobial Resistance (AMR) occurs when bacteria, viruses, fungi and parasites change over time and no longer respond to medicines making infections harder to treat and increasing the risk of disease spread, severe illness and death (W.H.O, 2021).
The emergence of multidrug resistant (MDR) pathogens is a global threat and has created problems in providing adequate treatment of many diseases. The way infections have been treated over time has changed drastically, especially over the past decades with the advent of modern antibacterial drugs (W.H.O, 2021). (Gill et al., 2014) describes antibiotics as drugs that either directly kill bacteria or inhibit the growth of bacteria. They are also known as bactericidal agents and bacteriostatic agents respectively.
Resistant pathogens occur due to the excessive use of antimicrobial agents. Antimicrobial drug resistance in pathogens is typically a permanent trait, but it can also be acquired and passed from one bacterial species to another (Gibbons et al., 2003). In 2021, W.H.O stated that antimicrobials are not just restricted to those who are ill; they are now used to prevent the onset of infections, they are present in consumer goods such as hand soap and toothpaste and fed to livestock to increase growth rates. Unfortunately, this widespread use has increased antibiotic resistance in both human and animal and in the environment, even among bacteria that were not targets of the drugs. This ensures that pathogens have a vast and readily available pool of resistance genes and pressure from antibiotic usage provides positive selection for the spread of these resistance genes and mutations (Baquero et al., 2021).
As a result of drug resistance, antibiotics and other antimicrobial medicines become ineffective and infections become increasingly difficult or impossible to treat (W.H.O, 2021).
Antimicrobial medications have demonstrated remarkable efficiency in the management of bacterial infections ever since their discovery. In the last few years, the number of drug resistant diseases have increased in hospitals and communities. This is due to excessive use of antimicrobial agents, mutation of pathogens leading to resistant to these drugs (Mancuso et al., 2021). Other contributing factors for the decreased effectiveness of antimicrobial agents are the increasing number of immune-compromised individuals, aging and stress. For example, about 90–95% of Staphylococcus aureus strains are resistant to penicillin, whereas 70–80% are resistant to methicillin (Mun et al., 2014).
Alvan et al (2011) stated drug repurposing as one of the effective strategies for combating resistance; it is the addition of some compounds that are rich in antimicrobial agents that will neutralize the resistance mechanism, enabling the drug to still be effective against resistant microbes. A large amount of herbal extracts, essential oils and isolated pure compounds have been reported to act synergistically with existing antibiotics, antifungals and chemotherapeutics and augment the activity of these drugs. (Ayaz et al., 2019). Although the conventional antimicrobial agents are quite effective against several pathogens, yet there is a need for more effective antimicrobial agents against MDR pathogens. The emergence of drug-resistant pathogens and the limited availability of effective antimicrobial agents pose significant challenges in the treatment of microbial infections.
Metformin, a widely prescribed antidiabetic drug, has shown potential antimicrobial activity against various pathogens (Youssef et al., 2021). However, its efficiency against pathogens is limited. Metformin can be repurposed using vanillin, a natural compound found in vanilla beans with known antimicrobial properties to increase its antimicrobial activity of metformin and address the current limitations of Metformin (Salau et al., 2021).
1.2 Statement of Problem
The emergence and spread of drug resistant pathogens that have acquired new resistant mechanisms leading to antimicrobial resistance continues to threaten the ability to treat common infections. Especially alarming is the rapid increase in multi and pan resistant bacteria that cause infections that are not treatable with existing antimicrobial medicines such as antibiotics.
Lack of access to quality antimicrobials remain a major issue. Antibiotics shortages are affecting countries of all levels of development and especially in health care systems.
Antimicrobials are becoming increasingly ineffective as drug resistance spreads globally leading to difficulty in treatment thereby leading to death.
Metformin, a well-known medication for diabetes exhibits potential antimicrobial activity. However, its effectiveness against pathogens are limited. Hence, the need to investigate synthetic modifications of Metformin using Vanillin and benzaldehyde as a drug repurpose to increase its antimicrobial efficiency.
1.3 Justification of the Study
Antimicrobial resistance has become a major global concern, making many existing antibiotics ineffective. Developing new antimicrobial agents is necessary to help fight this threat. Repurposing existing drugs such as metformin that is used to treat type 2 diabetes which has shown not only antidiabetic tendencies but also recently shown antimicrobial effect with vanillin.
Drug repurposing is a cost effective and time efficient strategy for drug development. The time, funds and manpower needed in producing new drugs will be cut significantly short during drug repurposing because the properties of these drugs are already known, making them easier to work with.
Vanillin is a natural compound potentially offering an eco-friendly alternative to synthetic antibiotics.
If vanillin and metformin can be successfully modified as an antimicrobial agent, it will be a good addition to the limited arsenal of antibiotics.
1.4 Aim and Objectives of Study
This research aims to design, synthesize and evaluate Metformin- vanillin, Metformin- benzaldehyde hybrid compounds ( a Schiff base) as antimicrobial agents, explaining their potential in combating microbial infections, drug resistant pathogens and contributing to the development of effective therapeutic alternatives through the following objectives to:
i. synthesize novel Schiff bases using Metformin with Vanillin and benzaldehyde.
ii. characterize the compounds using UV-visible and FT-IR spectroscopic techniques.
iii. evaluate the antimicrobial activity of the synthesized compounds on selected bacteria and fungi.
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