Development of antitubercular compounds based on a 4-quinolylhydrazone scaffold. Further structure-activity relationship studies

S Gemma; L Savini; M Altarelli; P Tripaldi; L Chiasserini; Ss Coccone; V Kumar; C Camodeca; G Campiani; E Novellino; Sandra Clarizio; Giovanni Delogu; S. Butini

doi:10.1016/j.bmc.2009.06.051

Development of antitubercular compounds based on a 4-quinolylhydrazone scaffold. Further structure-activity relationship studies

S Gemma, L Savini, M Altarelli, P Tripaldi, L Chiasserini, Ss Coccone, V Kumar, C Camodeca, G Campiani, E Novellino, Sandra Clarizio, Giovanni Delogu, S. Butini

Research output: Contribution to journal › Article › peer-review

48 Citations (Scopus)

Abstract

A series of 4-quinolylhydrazones was synthesized and tested in vitro against Mycobacterium tuberculosis. At a concentration of 6.25microg/mL, most of the newly synthesized compounds displayed 100% inhibitory activity against M. tuberculosis in cellular assays. Further screening allowed the identification of very potent antitubercular agents. Compound 4c was also tested in a time-course experiment and against mtb clinical isolates, displaying interesting results.

Original language	English
Pages (from-to)	6063-6072
Number of pages	10
Journal	BIOORGANIC & MEDICINAL CHEMISTRY
Volume	17
DOIs	https://doi.org/10.1016/j.bmc.2009.06.051
Publication status	Published - 2009

Keywords

Animals
Antitubercular Agents
Cell Line
Cercopithecus aethiops
Hydrazones
Microbial Sensitivity Tests
Mycobacterium tuberculosis
Structure-Activity Relationship
Vero Cells

UN SDGs

This output contributes to the following UN Sustainable Development Goals (SDGs)

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10.1016/j.bmc.2009.06.051

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Gemma, S., Savini, L., Altarelli, M., Tripaldi, P., Chiasserini, L., Coccone, S., Kumar, V., Camodeca, C., Campiani, G., Novellino, E., Clarizio, S., Delogu, G., & Butini, S. (2009). Development of antitubercular compounds based on a 4-quinolylhydrazone scaffold. Further structure-activity relationship studies. BIOORGANIC & MEDICINAL CHEMISTRY, 17, 6063-6072. https://doi.org/10.1016/j.bmc.2009.06.051

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title = "Development of antitubercular compounds based on a 4-quinolylhydrazone scaffold. Further structure-activity relationship studies",

abstract = "A series of 4-quinolylhydrazones was synthesized and tested in vitro against Mycobacterium tuberculosis. At a concentration of 6.25microg/mL, most of the newly synthesized compounds displayed 100% inhibitory activity against M. tuberculosis in cellular assays. Further screening allowed the identification of very potent antitubercular agents. Compound 4c was also tested in a time-course experiment and against mtb clinical isolates, displaying interesting results.",

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author = "S Gemma and L Savini and M Altarelli and P Tripaldi and L Chiasserini and Ss Coccone and V Kumar and C Camodeca and G Campiani and E Novellino and Sandra Clarizio and Giovanni Delogu and S. Butini",

year = "2009",

doi = "10.1016/j.bmc.2009.06.051",

language = "English",

volume = "17",

pages = "6063--6072",

journal = "BIOORGANIC & MEDICINAL CHEMISTRY",

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Gemma, S, Savini, L, Altarelli, M, Tripaldi, P, Chiasserini, L, Coccone, S, Kumar, V, Camodeca, C, Campiani, G, Novellino, E, Clarizio, S, Delogu, G & Butini, S 2009, 'Development of antitubercular compounds based on a 4-quinolylhydrazone scaffold. Further structure-activity relationship studies', BIOORGANIC & MEDICINAL CHEMISTRY, vol. 17, pp. 6063-6072. https://doi.org/10.1016/j.bmc.2009.06.051

TY - JOUR

T1 - Development of antitubercular compounds based on a 4-quinolylhydrazone scaffold. Further structure-activity relationship studies

AU - Gemma, S

AU - Savini, L

AU - Altarelli, M

AU - Tripaldi, P

AU - Chiasserini, L

AU - Coccone, Ss

AU - Kumar, V

AU - Camodeca, C

AU - Campiani, G

AU - Novellino, E

AU - Clarizio, Sandra

AU - Delogu, Giovanni

AU - Butini, S.

PY - 2009

Y1 - 2009

N2 - A series of 4-quinolylhydrazones was synthesized and tested in vitro against Mycobacterium tuberculosis. At a concentration of 6.25microg/mL, most of the newly synthesized compounds displayed 100% inhibitory activity against M. tuberculosis in cellular assays. Further screening allowed the identification of very potent antitubercular agents. Compound 4c was also tested in a time-course experiment and against mtb clinical isolates, displaying interesting results.

AB - A series of 4-quinolylhydrazones was synthesized and tested in vitro against Mycobacterium tuberculosis. At a concentration of 6.25microg/mL, most of the newly synthesized compounds displayed 100% inhibitory activity against M. tuberculosis in cellular assays. Further screening allowed the identification of very potent antitubercular agents. Compound 4c was also tested in a time-course experiment and against mtb clinical isolates, displaying interesting results.

KW - Animals

KW - Antitubercular Agents

KW - Cell Line

KW - Cercopithecus aethiops

KW - Hydrazones

KW - Microbial Sensitivity Tests

KW - Mycobacterium tuberculosis

KW - Structure-Activity Relationship

KW - Vero Cells

KW - Animals

KW - Antitubercular Agents

KW - Cell Line

KW - Cercopithecus aethiops

KW - Hydrazones

KW - Microbial Sensitivity Tests

KW - Mycobacterium tuberculosis

KW - Structure-Activity Relationship

KW - Vero Cells

UR - http://hdl.handle.net/10807/6591

U2 - 10.1016/j.bmc.2009.06.051

DO - 10.1016/j.bmc.2009.06.051

M3 - Article

SN - 1464-3391

VL - 17

SP - 6063

EP - 6072

JO - BIOORGANIC & MEDICINAL CHEMISTRY

JF - BIOORGANIC & MEDICINAL CHEMISTRY

ER -

Development of antitubercular compounds based on a 4-quinolylhydrazone scaffold. Further structure-activity relationship studies

Abstract

Keywords

UN SDGs

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