“…Whereas 5-substituted tetrazoles are well-known bioisosteres of carboxylic acid function, 1,5-disubstituted derivatives can be used to mimic the cis configuration of the amide bond, , which is higher in energy to the commonly found trans configuration (Figure A). Recently, the 1-alkyl-5-(alkylamino)tetrazole motif was envisioned as a potential replacement of the alkyl urea moiety, which is present in the structures of dozens therapeutics. , 1,5-Disubstituted tetrazoles are represented by a series of approved cephalosporin antibiotics (e.g., cefmetazole, , ceforanide , ) and antiplatelet therapeutic cilostazol , (Figure B). Therefore, access to the diverse library based on an N-substituted 1-alkyl-5-aminotetrazole scaffold 1 became the prime objective of the current work.…”