ChemInform Abstract: Combinatorial Chemistry: A Review

Rasheed, Anas; Farhat, Rumana

doi:10.1002/chin.201429280

Cited by 7 publications

(8 citation statements)

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“…A traditional chemist can synthesise 100-200 compounds per year. A combinatorial robotic system can produce in a year thousands or millions compounds, which can be tested for potential drug candidates in a high-throughput screening process [11].…”

Section: A + B → Abmentioning

confidence: 99%

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Integrated Approach to Nature as Source of New Drug Lead

Kohli¹

2018

Molecular Insight of Drug Design

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Classically, the development and launching of a new drug is a highly time consuming, tedious and expensive process involving following fundamental steps: (1) Identification of cause of Disease and Search for target site. (2) Search and Optimisation of active compound, that is, the Drug Lead. (3) Testing of Drug in Animals (pre-clinical phase). (4) Clinical Trials. (5) Approval of New Drug by Competent authority and availability of the drug. Drug discovery and development process involves around 10-15 years of investigation period and incredibly high cost and investment. This process also involves participation of experts from various disciplines and fields. Therefore, the new approaches are obligatory to be developed not only to expedite the process but also to ensure the launch of safer and effective drug. Over this background, the importance of experimental wisdom and holistic approach is intensifying to offer good base as an attractive discovery engine. Natural product drug discovery, ethno-pharmacology, traditional and attractive medicines are re-emerging as new strategic options. In the past decade, the number of new chemical entity (NCG) in drug development channel is declining markedly might have led to the rekindling of interest in emergence of natural product as new drug leads. The novel natural products can be optimised on the basis of their biological activities using highly sophisticated combinatorial biosynthetic techniques, microbial genomes and screening process.

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Section: A + B → Abmentioning

confidence: 99%

“…Employing HTS, it is comparatively trouble-free and swift to identify active compounds. HTS is hassle free technique that collects large amount of experimental data in a relatively short time [11].…”

Section: High Throughput Screeningmentioning

confidence: 99%

Integrated Approach to Nature as Source of New Drug Lead

Kohli¹

2018

Molecular Insight of Drug Design

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“…Combinatorial chemistry has been used for both drug lead discovery and optimization [12,13,14•]. Figure 1 summarizes the various combinatorial library methods, the nature of the library compounds involved and the screening methods available to each of the technologies.…”

Section: Introductionmentioning

confidence: 99%

Combinatorial chemistry in drug discovery

Liu

Lam

2017

Current Opinion in Chemical Biology

250

131

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Several combinatorial methods have been developed to create focused or diverse chemical libraries with a wide range of linear or macrocyclic chemical molecules: peptides, non-peptide oligomers, peptidomimetics, small-molecules, and natural product-like organic molecules. Each combinatorial approach has its own unique high-throughput screening and encoding strategy. In this article, we provide a brief overview of combinatorial chemistry in drug discovery with emphasis on recently developed new technologies for design, synthesis, screening and decoding of combinatorial library. Examples of successful application of combinatorial chemistry in hit discovery and lead optimization are given. The limitations and strengths of combinatorial chemistry are also briefly discussed. We are now in a better position to truly leverage the power of combinatorial technologies for the discovery and development of next-generation drugs.

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“…One way to achieve this, is by employing the combinatorial chemistry approach that allows synthesize compounds via rapid and efficient methodologies, with a variety of substituents simple and complex as heterocyclic scaffolds of interest in medicinal chemistry [2]. Condensation of a primary amine with an aldehyde or ketone to obtain imines compounds is an example of such reactions and was first reported by Hugo Schiff in 1864.…”

Section: Introductionmentioning

confidence: 99%

“…Schiff bases are of great importance in medicinal chemistry, considered as "privileged ligands ", due their derivatives or analogues have been shown to exhibit a plethora of biological activities, including anti-cancer, antiviral, antibacterial, antifungal, antioxidant, anticonvulsant, anti-inflammatory, antitubercular, antidepressant and antimalarial properties [3][4][5]. The biological activity of these molecules is mainly due to the hydrogen bond formation between the target and the lone pair of electrons in a sp 2 hybridized orbital of nitrogen atom of the imine functional group (-C=N-) [6].…”

Section: Introductionmentioning

confidence: 99%