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Chemistry underpins everything in the modern and sustainable development of science and the importance of organic chemistry has been recognised at the centre stage of drug discovery program. However, often the importance of chemistry is underestimated in the medicinal chemistry research! The present discussion will be in the context of the recent emphasis on the Sustainable Practices in Medicinal Chemistry urging for the necessity of use green chemistry tools such as the use of: water and ionic liquids (ILs) as alternative reaction media, catalytic procedures to construct new C-C bonds through C-X/H bond activation. Examples will be drawn on the exploration of new chemistries such as ensembling cooperative effect of heterobimetallic nano-clusters for new C-C bond formation via C-Br/O bond activation, transition metal-based C-H bond activation, and metal-free (organo-catalytic) C-H/dioxygen activation to generate therapeutic leads for inflammatory disorders and TB. |