The cyclothiazomycins are reported to have multiple inhibitory effects ranging from decreasing blood pressure to interfering with RNA transcription; they also exhibit some antibiotic activity.

[5] A third analogue, cyclothiazomycin C, was discovered in 2014 with the aid of genome mining, nucleophilic 1,4-addition labeling reactions, high resolution mass spectrometry, and NMR spectroscopy.

Cyclothiazomycin A contains a dehydroalanine and two dehydrohomoalanine residues within a bicyclic, macrocyclic scaffold composed of thiazolines, thiazoles, and a trisubstituted pyridine.

[6] Cyclothiazomycin is part of a class of natural products that are ribosomally synthesized and post-translationally modified peptides (RiPPs).

A series of chemical steps by biosynthetic enzymes transform the original peptide into the final (mature) natural product.

[citation needed] The gene encoding for cyclothiazomycin begins with a short open reading frame (ORF) ctmA (cltA).

CtmE and ctmF (ctlE and cltF) each encode a split lanthipeptide dehydratase which dehydrates serine and threonine to dehydroalanine and dehydrobutyrine.

[1][3] Cyclothiazomycin B shows inhibitory activity against RNA polymerase, and it is believed to act by reducing ribosome dependent GTPase.