Critical Examination of Synthetic Compounds and Drug Efficacy
Keywords:
synthetic compounds, drug efficacy, drug discovery, pharmacokinetics, pharmacodynamics, personalized medicine, drug repurposing, green chemistry, innovation, regulatory challengesAbstract
Synthetic compounds has revolutionized the field of pharmacology and drug development, enabling researchers to precisely create, modify, and optimize drugs that may not be attainable through natural product isolation. This paper explores the critical role of synthetic compounds in drug development and their impact on drug efficacy.
Drug discovery is a complex process aimed at identifying chemical compounds with therapeutic potential, particularly for addressing unmet medical needs in life-threatening diseases lacking effective treatments. However, this journey is fraught with challenges, including high attrition rates and significant time and financial investments. To mitigate these challenges, well-thought-out strategies are essential, especially when exploring new drug targets or therapeutic areas. A working definition of a "drug" within the context of drug discovery is presented, emphasizing chemically defined entities subjected to rigorous testing and validation, distinct from recreational or herbal substances.
The role of synthetic compounds in drug discovery is crucial, with chemists aiming to balance in vitro potency, selectivity, oral bioavailability, and safety. An example highlights the importance of addressing hERG channel inhibition while preserving other critical attributes. To enhance the drug discovery process, three key recommendations are offered. First, an integrated approach that coordinates in vitro and in vivo testing can provide a more robust foundation for lead compound selection. Second, appointing a dedicated drug champion with deep institutional knowledge can guide drug development teams effectively. Lastly, passing on the tacit knowledge of experienced chemists to the next generation is crucial for sustaining the art of successful drug discovery.
The development of synthetic compounds has played a pivotal role in modern medicine, leading to the discovery of numerous pharmaceutical drugs that have revolutionized healthcare. This research paper critically examines the relationship between synthetic compounds and drug efficacy, aiming to shed light on the complexities, challenges, and innovations in drug development. We explore the synthetic compounds' role in drug discovery, their impact on drug efficacy, the factors affecting drug efficacy, and future prospects in the field.
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References
• Ahmad, Z., Makaya, N. H., & Grosset, J. (2011). History of drug discovery: Early evaluation studies and lessons learnt from them. In Antituberculosis chemotherapy (Vol. 40, pp. 2-9). Karger Publishers.
• Coura, J. R., & De Castro, S. L. (2002). A critical review on Chagas disease chemotherapy. Memórias do Instituto Oswaldo Cruz, 97, 3-24.
• Drews, J. (2000). Drug discovery: a historical perspective. science, 287(5460), 1960-1964.
• Elinson, Michail N., Ilovaisky, Alexey I., Dorofeev, Alexander S., Merkulova, Valentina M., Stepanov, Nikita O., Miloserdov, Fedor M., Ogibin, Yuri N., Nikishin, Gennady I. ane Tetrahedron (2007). Electrocatalytic multicomponent transformation of cyclic 1,3-diketones, isatins, and malononitrile: facile and convenient way to functionalize spirocyclic (5,6,7,8-tetrahydro-4H-chromene)-4,3′-oxindole system. N. D. Zelinsky Institute of Organic Chemistry, Leninsky prospect 47, 119991 Moscow, Russia
• Li H, Qiu Y, Guo C, Han M, Zhou Y, Feng Y, Luo S, Tong Y, Zheng G, Zhu S. (2019). Pyrroloindoline cyclization in tryptophan-containing cyclodipeptides mediated by an unprecedented indole C3 methyltransferase from Streptomyces sp. HPH0547. Chem Commun (Camb). 2019 Jul 25;55(58):8390-8393. doi: 10.1039/c9cc03745d. Epub 2019 Jul 1. PMID: 31257394.
• Manouchehr Mamaghani & Roghayeh Hossein Nia (2021) A Review on the Recent Multicomponent Synthesis of Pyranopyrazoles, Polycyclic Aromatic Compounds, 41:2, 223-291, DOI: 10.1080/10406638.2019.1584576
• Newman, D. J., Cragg, G. M., & Snader, K. M. (2000). The influence of natural products upon drug discovery. Natural product reports, 17(3), 215-234.
• Pina, A. S., Hussain, A., & Roque, A. C. A. (2010). An historical overview of drug discovery. Ligand-Macromolecular Interactions in Drug Discovery: Methods and Protocols, 3-12.
• Schedler, D. J. (2006). Drug discovery: a history (sneader, walter).
• Shanthi, G., Subbulakshmi, G., & Perumal, P. T. (2007). A new InCl3-catalyzed, facile and efficient method for the synthesis of spirooxindoles under conventional and solvent-free microwave conditions. Tetrahedron, 63(9), 2057-2063.
• Sneader, W. (2005). Drug discovery: a history. John Wiley & Sons.
• Syam Kumar UK, Ila H, Junjappa H. (2001). A new route to spiropyrrolidinyl-oxindole alkaloids via iodide ion induced rearrangement of [(N-aziridinomethylthio) methylene]-2-oxindoles. Org Lett. 2001 Dec 27;3(26):4193-6. doi: 10.1021/ol016824i. PMID: 11784175.
• Vadivel V, Ganesan R, Kannaiyan V, Vellikannu E, Vijayakumar T. (2019). Synthesis of Substituted Isatins from the MBH Adduct of 1,5,6-Trisubstituted Isatins Using (2,4-Dinitrophenyl) hydrazine and K-10 Clay Explored as Protection-Deprotection Chemistry. ACS Omega. 2019 May 31;4(5):9563-9568. doi: 10.1021/acsomega.9b01002. PMID: 31460047; PMCID: PMC6648401.
• Zhao, C., Rakesh, K. P., Ravidar, L., Fang, W. Y., & Qin, H. L. (2019). Pharmaceutical and medicinal significance of sulfur (SVI)-Containing motifs for drug discovery: A critical review. European journal of medicinal chemistry, 162, 679-734.
