WO2019155266A1

WO2019155266A1 - Flavocillin: a new novel antibitoic that the bacteria will never develop

Info

Publication number: WO2019155266A1
Application number: PCT/IB2018/050851
Authority: WO
Inventors: Mustafa Pehlivan
Original assignee: Mustafa Pehlivan
Priority date: 2018-02-12
Filing date: 2018-02-12
Publication date: 2019-08-15
Also published as: EP3752509A1; WO2019155266A8

Abstract

This invention is about the discovery of a new novel compound as an antibiotic to stop this potential resistance problem completely. With Organic Chemistry studies and methods and other modified antibiotics, adding a flavonoid group to varibale side R instead which will result in flavocilin formation will be the most effective and revolutionary antibiotic that the bacteria will never be able to resist. Evidentful pathways have been conculded stating that the Flavocilin use in Medicine for heavy infectious conditions or where no other antibiotic works will outweigh all its risks.

Description

Flavocillin: A new novel antibitoic that the bacteria will never develop resistance

Resistance to antibiotics is a complicated growing problem of the centruy. Presently, this problem has been so much getting the attention of Medical Research Institutions and health organizations that there is a huge alert in preventing antibiotic resistance. There are reports estimating that many people will die in 2050’s due to antibiotics not working anymore as a result of this resistance. The simplest evidence that Flavocillin will be an effective antibiotic is that many stronger antibiotics were obtained by modifying the variable group (R) in Penicilin Chemical structure.

For obtaining Flavocilin, the R group must be replaced with a basic flavonoid and there may be more ways than what is being described at the claims part of this invention. Fortunately, obtaining Flavocilin is a simple Chemical process as a conclusion drawn from its theoretical studies.

Flavonoids are very useful antimicrobial compounds of herbal origin found naturally in certain teas and Propolis, a solution available to be used in Medicine which is what the honey bee uses to prevent his honey comb from microbes while producing honey. Propolis alone, readily available from Holland and Barret Stores, is full of flavonoids and as such it is effective in treating certain respiratory tract infections and also persistent flue, as a natural remedy.

In drug discovery and development process, adding effective Bioactive compounds to R groups of already active Chemical compounds as drug molecules is important to obtain much stronger effects than that of those drug molecules being used alone in treatment.

Possible advantages and disadvantages of Flavocilin as a new drug

development

Advantages:

Due to dual destructive mechanism effects (Cell wall inhibition and microbial destruction by bioactive flavonoid group as R (variable) group of Penicillin), the bacteria will never have the ability to resist to Flavocilin and therefore it will be the most powerful antibiotic via this defined dual strength of bioactivity.

As suggested in Chemical synthesis route part of claims, Flavocilin can easily be obtained with simple reactions.

Non-competitive advantage for the developer industry or for the drug company as a company holding the license rights of production during 20 years of patent protection. Flavocilin can always be used as a final choice of antibiotic where patient responds to no other antibiotic treatment, and it is impossible not to respond to Flavocilin due to dual mechanism of action stated previously.

Flavocilin will be the solution for the problem of the century, antibiotic resistance, even after centuries due to penicilin-flavonoid dual strength effects.

Flavocilin needs to be tested against virus effectiveness also. Due to its flavonoid group and Penicilin group, it can have a wider range of Pharmacological use and tests can determine if it will cancel, prevent, treat or minimise viral resistance, and if so, to what levels? The likelihood of finding out that it is very powerful against virus also will add benefit to its revolutionary importance and non-competitive unique advantages.

Disadvantages:

Stronger effects may bring further side effects (but as flavonids are naturally found in tea and little or moderate tea consumption is known to have no noticable toxic effects, this risk is not likely).

Clinical testing to fully determine Pharmacological effects have not yet been determined.

Easy making of flavocilin can result in easy illegal flavocilin production (This is a probability but yet it is not very likely as per strict regulationbs and restrictions of patent law and also because a laboratory is still needed for its production although the method is not quite complicated.

References:

1. Nature volume 179, pages 892-893 (04 May 1957) doi: 10.1038/179892a0

2. J. Am. Chem. Soc. , 1957, 79 (5), pp 1262-1263. DOI:

10.1021/ja01562a063

3. Protein Sci. 2009 Mar; 18(3): 595-605. doi: 10.1002/pro.67 PMCID:

PMC2760365

Claims

1. This invention is about the discovery of a new novel antibiotic of maximum effectiveness that can ever be obtained by simpler than usual Chemical synthesis and modification methods, namely“Flavocilin”.

2. Flavocilin will overcome all the possible and potential antibiotic resistance problems and mechanisms as per stated mechnaisms of action and its unqiue and basic structure will be the strongest antibiotic ever used in Medicine, according to claim 1.

3. Flavocilin will consist of a flavonoid as R group attached to basic penicilin structure, according to claim 2.

4. Flavocilin can simply be obtained/synthesized in a Chemistry laboratory as following moderate detail synthesis methods (Other synthetic methods can also be developed besides this and grams and scales yet need to be determined by expert Organic/synthetic Chemists in field): Any basic flavonoid or a flavone solution is firstly extracted from a herbal tea by using any one of dichloromethane, diethyl ether, chloroform or ethyl acetate as a solvent. There are more than one way of extraction and many of these methods are available from many different public resources. The flavonoid extract is then isolated from the rest of the tea and H₂S0₄ is added to the isolated flavonoid solution to produce lone paired Oxygens (as Flavonoids contain Oxygen around Cyclic carbons). The solution is then reacted with a readily available penicilin powder so that the formed lone pairs around Oxygen(s) in flavonoid attack the carbon attached to NH, O and R groups of Penicilin. This will result in double bond brokage and newly formed bond with the flavonoid due to an SN reaction. Since Penicilin contains Sulphur atom and methyls, an acid or other acidic compounds such as Sulphuric acid is likely to be resulted from this reaction, but such formed acids can easily be removed with the addition of a base to the solution resulting in salt formation that can be extracted and isolated later on so that it is gotten rid as it is unwanted. Finally, identification methods such as High Performance Liquid Chromatography (HPLC) and Carbon NMR must be used to analyze the solution to ensure the finally obtained sample contains Flavocilin and to ensure its structure represents the Flavocilin structure as identified in figure 2 of drwaings part of the invention. Once this is ensured, the very final step of the process is to purify the sample with purification methods to obtain 99% Flavocilin. Alternative synthetic routes or pathways at any stage is also possible.