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Natural-Product-Directed Catalytic Stereoselective Synthesis of Functionalized Fused Borane Cluster–Oxazoles for the Discovery of Bactericidal Agents

Rajesh Varkhedkar, Fan Yang, Rakesh Dontha, Jianglin Zhang, Jiyong Liu, Bernhard Spingler, Stijn van der Veen, Simon Duttwyler

2022ACS Central Science45 citationsDOIOpen Access PDF

Abstract

-dodecaborate anion with natural products such as menthol and camphor as the directing groups. This method allowed the rapid construction of a library of 1,2,3-trisubstituted clusters, which were evaluated in terms of their antibacterial activity against WHO priority pathogens. Several of the synthesized dodecaborate derivatives displayed medium- to high-level bactericidal activity against Gram-positive and Gram-negative bacteria.

Topics & Concepts

Combinatorial chemistryChemistryNatural productAntimicrobialDrug discoveryRegioselectivitySteric effectsChemical spaceCatalysisOrganic chemistryBiochemistryBoron Compounds in ChemistryOrganoboron and organosilicon chemistryOrthopedic Infections and Treatments