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AIM To efficiently synthesize inhibitors using high throughput screening against suitable drug targets NMT (N-myrsityltransferase Inhibitors) of Leishmania donovani (Ld).
NMT (N-myrsityltransferase Inhibitors) is an essential protein involved in the life cycle of Leishmania donovani (Ld) and Trypanosoma cruezei stages genus, signifying that NMT enzyme could be an appropriate drug target for the progress of anti-parasitic inhibitors. The study involved the high throughput screening of a collection of compounds from the Pfizer corporate. An approach has been made to synthesis and validate the hits against Ld and Leishmania major (Lm) NMT and also against Human isoforms (HsNMT1) and (Hs NMT2). It was observed that in spite of poor uptake due to lack of cell activity, the binding modes of the designed inhibitors could be key points for the designing of potent LdNMT inhibitors with improved properties....
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