Synthesis and Biological Evaluation of Novel Thiazole Hydrazines as Antimicrobial and Antimalarial Agents

Vishnu A. Gore; Sunil U. Tekale; Someshwar P. Bhale; Dhanaji P. Rajani; Abraham J. Domb; Rajendra P. Pawar

doi:10.33263/LIANBS101.18461855

Synthesis and Biological Evaluation of Novel Thiazole Hydrazines as Antimicrobial and Antimalarial Agents

Vishnu A. Gore, Sunil U. Tekale, Someshwar P. Bhale, Dhanaji P. Rajani, Abraham J. Domb, Rajendra P. Pawar^*

^*Corresponding author for this work

School of Pharmacy

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

13 Scopus citations

Abstract

Synthesis of some novel thiazole hydrazine derivatives from thiosemicarbazones of salicylaldehyde and 5-chlorosalicylaldehyde with phenacyl bromide in ethanol under reflux condition is reported. The synthesized compounds were characterized by spectral analysis and further screened against-S. aureus, E. coli, P. aeruginosa, S. pyogenus bacteria, and against C. albicans, A. clavatus, and A. niger fungal strains. Most of the compounds were active against E. coli and C. albicans. Antimalarial screening against Plasmodium falciparum showed moderate to the good activity of the synthesized compounds but less than the standard quinine. One of the synthesized compounds (4c) exhibited promising antimalarial activity against Plasmodium falciparum with IC₅₀ close to the standard quinine.

Original language	English
Pages (from-to)	1846-1855
Number of pages	10
Journal	Letters in Applied NanoBioScience
Volume	10
Issue number	1
DOIs	https://doi.org/10.33263/LIANBS101.18461855
State	Published - 30 Mar 2021

Bibliographical note

Publisher Copyright:
© 2020 by the authors.

Keywords

antimalarial
antimicrobial
thiazole hydrazines

UN SDGs

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

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10.33263/LIANBS101.18461855

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title = "Synthesis and Biological Evaluation of Novel Thiazole Hydrazines as Antimicrobial and Antimalarial Agents",

abstract = "Synthesis of some novel thiazole hydrazine derivatives from thiosemicarbazones of salicylaldehyde and 5-chlorosalicylaldehyde with phenacyl bromide in ethanol under reflux condition is reported. The synthesized compounds were characterized by spectral analysis and further screened against-S. aureus, E. coli, P. aeruginosa, S. pyogenus bacteria, and against C. albicans, A. clavatus, and A. niger fungal strains. Most of the compounds were active against E. coli and C. albicans. Antimalarial screening against Plasmodium falciparum showed moderate to the good activity of the synthesized compounds but less than the standard quinine. One of the synthesized compounds (4c) exhibited promising antimalarial activity against Plasmodium falciparum with IC50 close to the standard quinine.",

keywords = "antimalarial, antimicrobial, thiazole hydrazines",

author = "Gore, {Vishnu A.} and Tekale, {Sunil U.} and Bhale, {Someshwar P.} and Rajani, {Dhanaji P.} and Domb, {Abraham J.} and Pawar, {Rajendra P.}",

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doi = "10.33263/LIANBS101.18461855",

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AU - Gore, Vishnu A.

AU - Tekale, Sunil U.

AU - Bhale, Someshwar P.

AU - Rajani, Dhanaji P.

AU - Domb, Abraham J.

AU - Pawar, Rajendra P.

PY - 2021/3/30

Y1 - 2021/3/30

N2 - Synthesis of some novel thiazole hydrazine derivatives from thiosemicarbazones of salicylaldehyde and 5-chlorosalicylaldehyde with phenacyl bromide in ethanol under reflux condition is reported. The synthesized compounds were characterized by spectral analysis and further screened against-S. aureus, E. coli, P. aeruginosa, S. pyogenus bacteria, and against C. albicans, A. clavatus, and A. niger fungal strains. Most of the compounds were active against E. coli and C. albicans. Antimalarial screening against Plasmodium falciparum showed moderate to the good activity of the synthesized compounds but less than the standard quinine. One of the synthesized compounds (4c) exhibited promising antimalarial activity against Plasmodium falciparum with IC50 close to the standard quinine.

AB - Synthesis of some novel thiazole hydrazine derivatives from thiosemicarbazones of salicylaldehyde and 5-chlorosalicylaldehyde with phenacyl bromide in ethanol under reflux condition is reported. The synthesized compounds were characterized by spectral analysis and further screened against-S. aureus, E. coli, P. aeruginosa, S. pyogenus bacteria, and against C. albicans, A. clavatus, and A. niger fungal strains. Most of the compounds were active against E. coli and C. albicans. Antimalarial screening against Plasmodium falciparum showed moderate to the good activity of the synthesized compounds but less than the standard quinine. One of the synthesized compounds (4c) exhibited promising antimalarial activity against Plasmodium falciparum with IC50 close to the standard quinine.

KW - antimalarial

KW - antimicrobial

KW - thiazole hydrazines

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Synthesis and Biological Evaluation of Novel Thiazole Hydrazines as Antimicrobial and Antimalarial Agents

Abstract

Bibliographical note

Keywords

UN SDGs

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