A number of compounds were prepared using this methodology in acceptable yield. Two of these compounds showed promising antibacterial activities when tested against both Gram-positive and Gram-negative bacterial strains.

No abstract

This is a PDF file of an unedited manuscript that has been accepted for publication. As a service to our customers we are providing this early version of the manuscript. The manuscript will undergo copyediting, typesetting, and review of the resulting proof before it is published in its final form. Please note that during the production process errors may be discovered which could affect the content, and all legal disclaimers that apply to the journal pertain. 1 Novel alkynyl substituted 3,4-dihydropyrimidin-2(1H)-one derivatives as potential inhibitors of chorismate mutase ---------------------------------------------------------------------------------------------------------------------Abstract: A series of novel alkynyl substituted 3,4-dihydropyrimidin-2(1H)-one (DHPM) derivatives were designed, synthesized and evaluated in vitro as potential inhibitors of chorismate mutase (CM). All these compounds were prepared via a multi-component reaction (MCR) involving sequential I 2 -mediated Biginelli reaction followed by Cu-free Sonogashira coupling. Some of them showed promising inhibitory activities when tested at 30 µM. One compound showed dose dependent inhibition of CM with IC 50 value of 14.76 ± 0.54 µM indicating o-alkynylphenyl substituted DHPM as a new scaffold for the discovery of promising inhibitors of CM.

No abstract

A mild and operationally simple method is presented for the cyclization reactions of 2‐aminoacetophenones or enamines with phenylalkynes to form indoles and pyrroles, respectively.