Abstract
Fourteen new hydrazones representing derivatives of pyrrole were synthesized by condensation of six carbohydrazides with ten carbonyl compounds. The new products were evaluated as potential tuberculostatics by means of two levels of high-throughput screening. The preliminary screening against <i>Mycobacterium tuberculosis</i> H37Rv (ATCC 27294) at 6.25 µg/mL in 12B medium using the Microplate Alamar Blue Assay measured the inhibitory activity within the total series in the range of 98–0%. Compound 3-i (N 4-[l-(4-acetyl-3,5-dimethyl-lH-2-pyrrolyl)-methylidene]-4-pyridinecarbohydrazide) was identified as the compound showing the highest inhibition (98%) and was subjected to level 2 screening, whereat the resulting data (IC<sub>50</sub> < 0.2 and IC<sub>90</sub> = 22.581) identified 3-i as a prospective candidate for further and more detailed evaluations. The inhibitory activity within the series was found to drop with the increase of the relevant dipole moments and all the inactive compounds distinguished themselves with a higher molecular polarity.
Sign-in/Register to access full text options 
Talk to us
Join us for a 30 min session where you can share your feedback and ask us any queries you have
Schedule a callDisclaimer: All third-party content on this website/platform is and will remain the property of their respective owners and is provided on "as is" basis without any warranties, express or implied. Use of third-party content does not indicate any affiliation, sponsorship with or endorsement by them. Any references to third-party content is to identify the corresponding services and shall be considered fair use under The CopyrightLaw.
