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Synthetic and Medicinal Chemistry in Drug Discovery: Needs for Today

  • December 2017
Authors:
Dr Prakash Prajapat at Shri KV Parekh Science College, Mahuva
Dr Prakash Prajapat
  • Shri KV Parekh Science College, Mahuva
Hasit Vinodrai Vaghani at Mehsana Urban Institute of Sciences Ganpat university
Hasit Vinodrai Vaghani
  • Mehsana Urban Institute of Sciences Ganpat university
Shikha Gupta at Mohan Lal Sukhadia University
Shikha Gupta
GL Talesara
GL Talesara
GL Talesara
  • This person is not on ResearchGate, or hasn't claimed this research yet.
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Annals of Medicinal Chemistry and Research
Cite this article: Prajapat P, Vaghani H, Agarwal S, Talesara GL (2017) Synthetic and Medicinal Chemistry in Drug Discovery: Needs for Today. Ann Med Chem Res
3(1): 1021.
*Corresponding author
Prakash Prajapat, Department of Chemistry, Ganpat
University, Mehsana-384012, Gujarat, India, Tel:
917891554090; Email:
Submitted: 09 December 2017
Accepted: 11 December 2017
Published: 12 December 2017
ISSN: 2378-9336
Copyright
© 2017 Prajapat et al.
OPEN ACCESS
Editorial
Synthetic and Medicinal
Chemistry in Drug Discovery:
Needs for Today
Prakash Prajapat1*, Hasit Vaghani1, Shikha Agarwal2, and
GLTalesara2
1Department of Chemistry, Ganpat University, India
2Department of Chemistry, MLS University, India
EDITORIAL
Synthetic organic and medicinal chemistry (Figure 1) is
         
    
       
         
         
         
      
       
      
       
       
        


        
etc.        
viz.      
  
etc
     
        
       
etc
      
         
       
        
       
        
      
        
        
  
       
      
    
   
Figure 1
Figure 2
         

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Bringing Excellence in Open Access
Prajapat et al. (2017)
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Ann Med Chem Res 3(1): 1021 (2017) 2/2
REFERENCES
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Prajapat P, Vaghani H, Agarwal S, Talesara GL (2017) Synthetic and Medicinal Chemistry in Drug Discovery: Needs for Today. Ann Med Chem Res 3(1): 1021.
Cite this article
... The process of drug discovery involves the identification of candidates, synthesis, characterization, screening, and assays for therapeutic efficacy. Once a compound has shown its value in these tests, it will begin the process of drug development prior to clinical trials [1][2][3][4][5][6][7]. Pharmaceutical chemistry is focused on quality aspects of medicines and aims to assure fitness for the purpose of medicinal products. ...
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Drug design is a creative act of the same magnitude as composing, sculpting, or writing. The results can touch the lives of millions and bring dollars of millions. Drug design, sometimes referred to as rational drug design or simply rational design, is the inventive process of finding new medications based on the knowledge of a biological target. Similarly, drug development is the process of bringing a new pharmaceutical drug to the market once a lead compound has been identified through the process of drug discovery. It includes pre-clinical research (microorganisms/animals) and clinical trials (on humans) and may include the step of obtaining regulatory approval to market the drug. This review helps in the development of newer molecules for future drug discovery.
... The development of new drug and pharmaceuticals is currently a critical and challenging issue to the researchers and pharmaceutical industry. A wide range of synthetic and medicinal properties shown by heterocyclic hybrids inspired organic and medicinal chemists to pursue the synthesis of newer motifs and evaluate their pharmacophoric properties [1][2][3][4][5][6]. Modifications on the benzothiazole scaffold have resulted in a huge number of compounds having diverse pharmacological activities [7,8]. ...
New Benzothiazole-Thiazolidinone hybrids containing Phthalimidoxy and Ethoxyphthalimide: Design, Synthesis and Pharmacological Assay
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... This science has found application in the production of molecules of commercial interest; in the construction of newer pharmacological active therapeutic agents derived from rational drug design, into synthesize complex natural molecules, in the finding innovative approaches to render this chemical science more efficient. 1 The role played by organic chemist in pharmaceutical industry continues to be one of the main drivers in the drug discovery process. ...
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Organic molecules perform key functions in nature, drug, and technology. It plays as the engine for understanding structure and reactivity. This science has found application in the production of molecules of commercial interest; in the construction of newer pharmacological active therapeutic agents derived from rational drug design, into synthesize complex natural molecules, in the finding innovative approaches to render this chemical science more efficient. The role played by organic chemist in pharmaceutical industry continues to be one of the main drivers in the drug discovery process.
... Drug discovery process ( Figure 2 & 3) is long, time and money intensive process [1]. This science of has found application in the production of molecules of commercial interest in the construction of newer pharmacological active therapeutic agents derived from rational drug design, into synthesize complex natural molecules, in the finding innovative approaches to render this chemical science more efficient [2,3]. The development of newer pharmaceuticals is currently a critical and challenging task to the pharmaceutical industry. ...
... Heterocyclic hybrids have enormous potential as the most promising molecules as lead structures for the design of novel drug candidates in the field of modern drug discovery ( Figure 1). The development of newer drug and pharmaceuticals is currently a critical and challenging issue to the academic researchers and pharmaceutical industry [1,2]. A wide range of synthetic and medicinal properties shown by heterocyclic hybrids inspired organic and medicinal chemists to pursue the synthesis of newer motifs and screen their pharmacophoric properties. ...
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Synthetic biology (SB) is an emerging discipline, which is slowly reorienting the field of drug discovery. For thousands of years, living organisms such as plants were the major source of human medicines. The difficulty in resynthesizing natural products, however, often turned pharmaceutical industries away from this rich source for human medicine. More recently, progress on transformation through genetic manipulation of biosynthetic units in microorganisms has opened the possibility of in-depth exploration of the large chemical space of natural products derivatives. Success of SB in drug synthesis culminated with the bioproduction of artemisinin by microorganisms, a tour de force in protein and metabolic engineering. Today, synthetic cells are not only used as biofactories but also used as cell-based screening platforms for both target-based and phenotypic-based approaches. Engineered genetic circuits in synthetic cells are also used to decipher disease mechanisms or drug mechanism of actions and to study cell-cell communication within bacteria consortia. This review presents latest developments of SB in the field of drug discovery, including some challenging issues such as drug resistance and drug toxicity.
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Small molecules remain the backbone for modern drug discovery. They are conceived and synthesized by medicinal chemists, many of whom were originally trained as organic chemists. Support from government and industry to provide training and personnel for continued development of this critical skill set has been declining for many years. This Viewpoint highlights the value of organic chemistry and organic medicinal chemists in the complex journey of drug discovery as a reminder that basic science support must be restored.
An overview of molecular hybrids in drug discovery
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Introduction: The hybridization of biologically active molecules is a powerful tool for drug discovery used to target a variety of diseases. It offers the prospect of better drugs for the treatment of a number of illnesses including cancer, malaria, tuberculosis and AIDS. Hybrid drugs can provide combination therapies in a single multi-functional agent and, by doing so, be more specific and powerful than conventional classic treatments. This research field is in great expansion and attracts many researchers worldwide. Area covered: This review covers the main research published between early 2013 to mid-2015 and takes into account several previous reviews on the subject. Its intention is to showcase the most recent advances reported towards the development of molecular hybrids in drug discovery. Particular attention is given to anticancer hybrids throughout the review. Expert opinion: Current advances show that molecular hybrids of biologically active molecules can lead to powerful therapeutics. Natural products play a key role in this field. It is also believed that toxin hybrids present a great opportunity for future progress and should be further explored. Furthermore, the synthesis of hybrid organometallics should be systematically studied as it can lead to potent drugs. The crucial requirement for growth still remains the efficacy of synthesis. Hence, the development of efficient synthetic methods allowing rapid access to diverse series of hybrids must be further investigated by researchers.
Quantitative structure–activity relationship (QSAR) studies as strategic approach in drug discovery
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Drug design is a process which is driven by technological breakthroughs implying advanced experimental and computational methods. Nowadays, the techniques or the drug design methods are of paramount importance for prediction of biological profile, identification of hits, generation of leads, and moreover to accelerate the optimization of leads into drug candidates. Quantitative structure–activity relationship (QSAR) has served as a valuable predictive tool in the design of pharmaceuticals and agrochemicals. From decades to recent research, QSAR methods have been applied in the development of relationship between properties of chemical substances and their biological activities to obtain a reliable statistical model for prediction of the activities of new chemical entities. Classical QSAR studies include ligands with their binding sites, inhibition constants, rate constants, and other biological end points, in addition molecular to properties such as lipophilicity, polarizability, electronic, and steric properties or with certain structural features. 3D-QSAR has emerged as a natural extension to the classical Hansch and Free–Wilson approaches, which exploit the three-dimensional properties of the ligands to predict their biological activities using robust chemometric techniques such as PLS, G/PLS, and ANN. This paper provides an overview of 1-6 dimension-based developed QSAR methods and their approaches. In particular, we present various dimensional QSAR approaches, such as comparative molecular field analysis (CoMFA), comparative molecular similarity analysis, Topomer CoMFA, self-organizing molecular field analysis, comparative molecule/pseudo receptor interaction analysis, comparative molecular active site analysis, and FLUFF-BALL, 4D-QSAR, and G-QSAR approaches.