Novel and potent oxazolidinone antibacterials featuring 3-indolylglyoxamide substituents

Mohamed Takhi; Gurpreet Singh; C. Murugan; Nirvesh Thaplyyal; Soma Maitra; K. M. Bhaskarreddy; P. V.S. Amarnath; Arundhuti Mallik; T. Harisudan; Ravi Kumar Trivedi; K. Sreenivas; N. Selvakumar; Javed Iqbal

doi:10.1016/j.bmcl.2008.03.043

Novel and potent oxazolidinone antibacterials featuring 3-indolylglyoxamide substituents

Mohamed Takhi, Gurpreet Singh, C. Murugan, Nirvesh Thaplyyal, Soma Maitra, K. M. Bhaskarreddy, P. V.S. Amarnath, Arundhuti Mallik, T. Harisudan, Ravi Kumar Trivedi, K. Sreenivas, N. Selvakumar, Javed Iqbal

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Abstract

Novel oxazolidinone antibacterials bearing a variety of 3-indolylglyoxamide substituents have been explored in an effort to improve the spectrum and potency of this class of agents. A subclass of this series was also made with the diversity at C-5 terminus. These derivatives have been screened against a panel of clinically relevant Gram-positive pathogens and fastidious Gram-negative organisms. Several analogs in this series were identified with in vitro activity superior to linezolid (MIC = 0.25-2 μg/mL). Compounds 10a, 10c, 10e and 10f displayed activity against linezolid resistant Gram-positive organisms (MIC = 2-4 μg/mL). Selected oxazolidinones were evaluated for in vivo efficacy against a mouse systemic infection model.

Original language	English (US)
Pages (from-to)	5150-5155
Number of pages	6
Journal	Bioorganic and Medicinal Chemistry Letters
Volume	18
Issue number	18
DOIs	https://doi.org/10.1016/j.bmcl.2008.03.043
State	Published - Sep 15 2008
Externally published	Yes

Keywords

Antibacterials
Indole
Linezolid
Oxazolidinones

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10.1016/j.bmcl.2008.03.043

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Takhi, M., Singh, G., Murugan, C., Thaplyyal, N., Maitra, S., Bhaskarreddy, K. M., Amarnath, P. V. S., Mallik, A., Harisudan, T., Trivedi, R. K., Sreenivas, K., Selvakumar, N., & Iqbal, J. (2008). Novel and potent oxazolidinone antibacterials featuring 3-indolylglyoxamide substituents. Bioorganic and Medicinal Chemistry Letters, 18(18), 5150-5155. https://doi.org/10.1016/j.bmcl.2008.03.043

Takhi, M, Singh, G, Murugan, C, Thaplyyal, N, Maitra, S, Bhaskarreddy, KM, Amarnath, PVS, Mallik, A, Harisudan, T, Trivedi, RK, Sreenivas, K, Selvakumar, N & Iqbal, J 2008, 'Novel and potent oxazolidinone antibacterials featuring 3-indolylglyoxamide substituents', Bioorganic and Medicinal Chemistry Letters, vol. 18, no. 18, pp. 5150-5155. https://doi.org/10.1016/j.bmcl.2008.03.043

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abstract = "Novel oxazolidinone antibacterials bearing a variety of 3-indolylglyoxamide substituents have been explored in an effort to improve the spectrum and potency of this class of agents. A subclass of this series was also made with the diversity at C-5 terminus. These derivatives have been screened against a panel of clinically relevant Gram-positive pathogens and fastidious Gram-negative organisms. Several analogs in this series were identified with in vitro activity superior to linezolid (MIC = 0.25-2 μg/mL). Compounds 10a, 10c, 10e and 10f displayed activity against linezolid resistant Gram-positive organisms (MIC = 2-4 μg/mL). Selected oxazolidinones were evaluated for in vivo efficacy against a mouse systemic infection model.",

keywords = "Antibacterials, Indole, Linezolid, Oxazolidinones",

author = "Mohamed Takhi and Gurpreet Singh and C. Murugan and Nirvesh Thaplyyal and Soma Maitra and Bhaskarreddy, {K. M.} and Amarnath, {P. V.S.} and Arundhuti Mallik and T. Harisudan and Trivedi, {Ravi Kumar} and K. Sreenivas and N. Selvakumar and Javed Iqbal",

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doi = "10.1016/j.bmcl.2008.03.043",

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AU - Takhi, Mohamed

AU - Singh, Gurpreet

AU - Murugan, C.

AU - Thaplyyal, Nirvesh

AU - Maitra, Soma

AU - Bhaskarreddy, K. M.

AU - Amarnath, P. V.S.

AU - Mallik, Arundhuti

AU - Harisudan, T.

AU - Trivedi, Ravi Kumar

AU - Sreenivas, K.

AU - Selvakumar, N.

AU - Iqbal, Javed

PY - 2008/9/15

Y1 - 2008/9/15

N2 - Novel oxazolidinone antibacterials bearing a variety of 3-indolylglyoxamide substituents have been explored in an effort to improve the spectrum and potency of this class of agents. A subclass of this series was also made with the diversity at C-5 terminus. These derivatives have been screened against a panel of clinically relevant Gram-positive pathogens and fastidious Gram-negative organisms. Several analogs in this series were identified with in vitro activity superior to linezolid (MIC = 0.25-2 μg/mL). Compounds 10a, 10c, 10e and 10f displayed activity against linezolid resistant Gram-positive organisms (MIC = 2-4 μg/mL). Selected oxazolidinones were evaluated for in vivo efficacy against a mouse systemic infection model.

AB - Novel oxazolidinone antibacterials bearing a variety of 3-indolylglyoxamide substituents have been explored in an effort to improve the spectrum and potency of this class of agents. A subclass of this series was also made with the diversity at C-5 terminus. These derivatives have been screened against a panel of clinically relevant Gram-positive pathogens and fastidious Gram-negative organisms. Several analogs in this series were identified with in vitro activity superior to linezolid (MIC = 0.25-2 μg/mL). Compounds 10a, 10c, 10e and 10f displayed activity against linezolid resistant Gram-positive organisms (MIC = 2-4 μg/mL). Selected oxazolidinones were evaluated for in vivo efficacy against a mouse systemic infection model.

KW - Antibacterials

KW - Indole

KW - Linezolid

KW - Oxazolidinones

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ER -

Novel and potent oxazolidinone antibacterials featuring 3-indolylglyoxamide substituents

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Keywords

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