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A hybrid molecule is a compound obtained by combination of two (or more) pharmacophores by covalent bond that is either designed to interact with multiple targets, improve the biological properties or enhance the efficacy of the compound. [1] The synthesis of hybrid molecules is an essential approach in the seeking of novel biologically active compounds for therapeutics. [2] This approach has found extensive applications in pharmacological field to overcome obstacles in pharmacokinetic, toxicity, side effects on current conventional drugs, and reduce the risk of developing resistance in cancer cells. [3]
The hybrid molecules could be a combination of two natural products or natural product pharmacophore incorporated with synthetized group molecules. [4] In general, the structures of hybrid molecule is consist of two (or more) compounds or drugs that connected covalently by either functional group, or linker which could classified as followed: [5]
The biological properties of hybrid molecules particularly described exhibiting anti- cancer, anti-microbial, and anti- malarial activities. [8] The podophyllotoxin- artesunate hybrid showed a significant inhibition against HepG2 ( liver cancer cell), A549 ( lung cancer cell), HeLa ( cervix cancer cell), and K562 ( leukemia cell) and the activities is comparable to that etoposide which it already used as cancer chemotherapy. [9] [10] Neomycin B- ciprofloxacin hybrids with an aromatic triazole linker and aliphatic triazole linker exhibited more potent activity than (free) neomycin B which has a potential as antibacterial agent. [11] Another example of hybrids of cinnamic acid and chalcones showed promising antimalarial activity against Plasmodium falciparum were found to be more potent than standard drug chloroquine. [12]
Despite the advantages and the escalating impact of hybrid molecules in medicinal area, this strategy also has potential limitations. The major problem of hybrid molecules is the large of its molecular weight (i.e. >500 Da) especially if the compound connected by a linker which possibility has a poor bioavailability and lower solubility. [13] Another challenge in research of hybrid molecules is the favored covalent bonding between two molecules is apart from the pharmacophores region in order to maintain it bioactivity. While modification any groups in pharmacophoric area could adversely affect the biological properties also possibility to have unexpected new binding target. [14]
Submission declined on 3 July 2024 by
Graeme Bartlett (
talk). Thank you for your submission, but the subject of this article already exists in Wikipedia. You can find it and improve it at
Hybrid molecule instead.
Where to get help
How to improve a draft
You can also browse Wikipedia:Featured articles and Wikipedia:Good articles to find examples of Wikipedia's best writing on topics similar to your proposed article. Improving your odds of a speedy review To improve your odds of a faster review, tag your draft with relevant WikiProject tags using the button below. This will let reviewers know a new draft has been submitted in their area of interest. For instance, if you wrote about a female astronomer, you would want to add the Biography, Astronomy, and Women scientists tags. Editor resources
|
A hybrid molecule is a compound obtained by combination of two (or more) pharmacophores by covalent bond that is either designed to interact with multiple targets, improve the biological properties or enhance the efficacy of the compound. [1] The synthesis of hybrid molecules is an essential approach in the seeking of novel biologically active compounds for therapeutics. [2] This approach has found extensive applications in pharmacological field to overcome obstacles in pharmacokinetic, toxicity, side effects on current conventional drugs, and reduce the risk of developing resistance in cancer cells. [3]
The hybrid molecules could be a combination of two natural products or natural product pharmacophore incorporated with synthetized group molecules. [4] In general, the structures of hybrid molecule is consist of two (or more) compounds or drugs that connected covalently by either functional group, or linker which could classified as followed: [5]
The biological properties of hybrid molecules particularly described exhibiting anti- cancer, anti-microbial, and anti- malarial activities. [8] The podophyllotoxin- artesunate hybrid showed a significant inhibition against HepG2 ( liver cancer cell), A549 ( lung cancer cell), HeLa ( cervix cancer cell), and K562 ( leukemia cell) and the activities is comparable to that etoposide which it already used as cancer chemotherapy. [9] [10] Neomycin B- ciprofloxacin hybrids with an aromatic triazole linker and aliphatic triazole linker exhibited more potent activity than (free) neomycin B which has a potential as antibacterial agent. [11] Another example of hybrids of cinnamic acid and chalcones showed promising antimalarial activity against Plasmodium falciparum were found to be more potent than standard drug chloroquine. [12]
Despite the advantages and the escalating impact of hybrid molecules in medicinal area, this strategy also has potential limitations. The major problem of hybrid molecules is the large of its molecular weight (i.e. >500 Da) especially if the compound connected by a linker which possibility has a poor bioavailability and lower solubility. [13] Another challenge in research of hybrid molecules is the favored covalent bonding between two molecules is apart from the pharmacophores region in order to maintain it bioactivity. While modification any groups in pharmacophoric area could adversely affect the biological properties also possibility to have unexpected new binding target. [14]