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. Author manuscript; available in PMC: 2017 Dec 6.
Published in final edited form as: J Org Chem. 2017 Oct 13;82(23):11961–11980. doi: 10.1021/acs.joc.7b02088

Figure 15.

Figure 15

Representative OL-135 analogs containing iterative single heavy atom changes or exchanges in the activating heterocycle. Reduction in the steric size of the heterocycle position 4 heavy atom (potency: N > O > CH) contributes to increased inhibitor potency.