Antimycobacterial agents: Synthesis and biological evaluation of novel 4-(substituted-phenyl)-6-methyl-2-oxo-N-(pyridin-2-yl)-1,2,3, 4-tetrahydropyrimidine-5-carboxamide derivatives by using one-pot multicomponent method

Abdulrahman I. Almansour; Mohamed Ashraf Ali; Sadath Ali; Ang Chee Wei; Yeong Keng Yoon; Rusli Ismail; Tan Soo Choon; Suresh Pandian; Raju Suresh Kumar; Natarajan Arumugam; Hasnah Osman

doi:10.2174/157018012804586879

Antimycobacterial agents: Synthesis and biological evaluation of novel 4-(substituted-phenyl)-6-methyl-2-oxo-N-(pyridin-2-yl)-1,2,3, 4-tetrahydropyrimidine-5-carboxamide derivatives by using one-pot multicomponent method

Abdulrahman I. Almansour, Mohamed Ashraf Ali, Sadath Ali, Ang Chee Wei, Yeong Keng Yoon, Rusli Ismail, Tan Soo Choon, Suresh Pandian, Raju Suresh Kumar, Natarajan Arumugam, Hasnah Osman

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

4 Citations (Scopus)

Abstract

The aim of this work was to synthesize a series of compounds to study their antimycobacterial potential. Eight compounds were found to be most active with minimum inhibitory concentration of less than 6μM and were more active than Isoniazid (INH) against Mycobacterium tuberculosis H37Rν (MTB). Compounds with electron withdrawing group substituted on the aryl ring were showing better activity. Among the fifteen newly synthesized compounds, compound 6-methyl-4-(4-nitrophenyl)-2-oxo-N-(pyridin-2-yl)-1,2,3,4tetrahydropyrimidine-5- carboxamide (B) was found to be the most active agent against MTB and INH resistant Mycobacterium tuberculosis (INHR-MTB) with minimum inhibitory concentration of <0.35 μM.

Original language	English
Pages (from-to)	953-957
Number of pages	5
Journal	Letters in Drug Design and Discovery
Volume	9
Issue number	10
DOIs	https://doi.org/10.2174/157018012804586879
Publication status	Published - Dec 2012
Externally published	Yes

Keywords

Antimycobacterial
Biginelli
Dihydropyrimidine
One pot

UN SDGs

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

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10.2174/157018012804586879

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Almansour, A. I., Ali, M. A., Ali, S., Wei, A. C., Yoon, Y. K., Ismail, R., Choon, T. S., Pandian, S., Kumar, R. S., Arumugam, N., & Osman, H. (2012). Antimycobacterial agents: Synthesis and biological evaluation of novel 4-(substituted-phenyl)-6-methyl-2-oxo-N-(pyridin-2-yl)-1,2,3, 4-tetrahydropyrimidine-5-carboxamide derivatives by using one-pot multicomponent method. Letters in Drug Design and Discovery, 9(10), 953-957. https://doi.org/10.2174/157018012804586879

Almansour, Abdulrahman I. ; Ali, Mohamed Ashraf ; Ali, Sadath et al. / Antimycobacterial agents : Synthesis and biological evaluation of novel 4-(substituted-phenyl)-6-methyl-2-oxo-N-(pyridin-2-yl)-1,2,3, 4-tetrahydropyrimidine-5-carboxamide derivatives by using one-pot multicomponent method. In: Letters in Drug Design and Discovery. 2012 ; Vol. 9, No. 10. pp. 953-957.

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title = "Antimycobacterial agents: Synthesis and biological evaluation of novel 4-(substituted-phenyl)-6-methyl-2-oxo-N-(pyridin-2-yl)-1,2,3, 4-tetrahydropyrimidine-5-carboxamide derivatives by using one-pot multicomponent method",

abstract = "The aim of this work was to synthesize a series of compounds to study their antimycobacterial potential. Eight compounds were found to be most active with minimum inhibitory concentration of less than 6μM and were more active than Isoniazid (INH) against Mycobacterium tuberculosis H37Rν (MTB). Compounds with electron withdrawing group substituted on the aryl ring were showing better activity. Among the fifteen newly synthesized compounds, compound 6-methyl-4-(4-nitrophenyl)-2-oxo-N-(pyridin-2-yl)-1,2,3,4tetrahydropyrimidine-5- carboxamide (B) was found to be the most active agent against MTB and INH resistant Mycobacterium tuberculosis (INHR-MTB) with minimum inhibitory concentration of <0.35 μM.",

keywords = "Antimycobacterial, Biginelli, Dihydropyrimidine, One pot",

author = "Almansour, \{Abdulrahman I.\} and Ali, \{Mohamed Ashraf\} and Sadath Ali and Wei, \{Ang Chee\} and Yoon, \{Yeong Keng\} and Rusli Ismail and Choon, \{Tan Soo\} and Suresh Pandian and Kumar, \{Raju Suresh\} and Natarajan Arumugam and Hasnah Osman",

year = "2012",

month = dec,

doi = "10.2174/157018012804586879",

language = "English",

volume = "9",

pages = "953--957",

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Almansour, AI, Ali, MA, Ali, S, Wei, AC , Yoon, YK, Ismail, R, Choon, TS, Pandian, S, Kumar, RS, Arumugam, N & Osman, H 2012, 'Antimycobacterial agents: Synthesis and biological evaluation of novel 4-(substituted-phenyl)-6-methyl-2-oxo-N-(pyridin-2-yl)-1,2,3, 4-tetrahydropyrimidine-5-carboxamide derivatives by using one-pot multicomponent method', Letters in Drug Design and Discovery, vol. 9, no. 10, pp. 953-957. https://doi.org/10.2174/157018012804586879

Antimycobacterial agents: Synthesis and biological evaluation of novel 4-(substituted-phenyl)-6-methyl-2-oxo-N-(pyridin-2-yl)-1,2,3, 4-tetrahydropyrimidine-5-carboxamide derivatives by using one-pot multicomponent method. / Almansour, Abdulrahman I.; Ali, Mohamed Ashraf; Ali, Sadath et al.
In: Letters in Drug Design and Discovery, Vol. 9, No. 10, 12.2012, p. 953-957.

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

TY - JOUR

T1 - Antimycobacterial agents

T2 - Synthesis and biological evaluation of novel 4-(substituted-phenyl)-6-methyl-2-oxo-N-(pyridin-2-yl)-1,2,3, 4-tetrahydropyrimidine-5-carboxamide derivatives by using one-pot multicomponent method

AU - Almansour, Abdulrahman I.

AU - Ali, Mohamed Ashraf

AU - Ali, Sadath

AU - Wei, Ang Chee

AU - Yoon, Yeong Keng

AU - Ismail, Rusli

AU - Choon, Tan Soo

AU - Pandian, Suresh

AU - Kumar, Raju Suresh

AU - Arumugam, Natarajan

AU - Osman, Hasnah

PY - 2012/12

Y1 - 2012/12

N2 - The aim of this work was to synthesize a series of compounds to study their antimycobacterial potential. Eight compounds were found to be most active with minimum inhibitory concentration of less than 6μM and were more active than Isoniazid (INH) against Mycobacterium tuberculosis H37Rν (MTB). Compounds with electron withdrawing group substituted on the aryl ring were showing better activity. Among the fifteen newly synthesized compounds, compound 6-methyl-4-(4-nitrophenyl)-2-oxo-N-(pyridin-2-yl)-1,2,3,4tetrahydropyrimidine-5- carboxamide (B) was found to be the most active agent against MTB and INH resistant Mycobacterium tuberculosis (INHR-MTB) with minimum inhibitory concentration of <0.35 μM.

AB - The aim of this work was to synthesize a series of compounds to study their antimycobacterial potential. Eight compounds were found to be most active with minimum inhibitory concentration of less than 6μM and were more active than Isoniazid (INH) against Mycobacterium tuberculosis H37Rν (MTB). Compounds with electron withdrawing group substituted on the aryl ring were showing better activity. Among the fifteen newly synthesized compounds, compound 6-methyl-4-(4-nitrophenyl)-2-oxo-N-(pyridin-2-yl)-1,2,3,4tetrahydropyrimidine-5- carboxamide (B) was found to be the most active agent against MTB and INH resistant Mycobacterium tuberculosis (INHR-MTB) with minimum inhibitory concentration of <0.35 μM.

KW - Antimycobacterial

KW - Biginelli

KW - Dihydropyrimidine

KW - One pot

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U2 - 10.2174/157018012804586879

DO - 10.2174/157018012804586879

M3 - Article

AN - SCOPUS:84870423326

SN - 1570-1808

VL - 9

SP - 953

EP - 957

JO - Letters in Drug Design and Discovery

JF - Letters in Drug Design and Discovery

IS - 10

ER -

Almansour AI, Ali MA, Ali S, Wei AC , Yoon YK, Ismail R et al. Antimycobacterial agents: Synthesis and biological evaluation of novel 4-(substituted-phenyl)-6-methyl-2-oxo-N-(pyridin-2-yl)-1,2,3, 4-tetrahydropyrimidine-5-carboxamide derivatives by using one-pot multicomponent method. Letters in Drug Design and Discovery. 2012 Dec;9(10):953-957. doi: 10.2174/157018012804586879

Antimycobacterial agents: Synthesis and biological evaluation of novel 4-(substituted-phenyl)-6-methyl-2-oxo-N-(pyridin-2-yl)-1,2,3, 4-tetrahydropyrimidine-5-carboxamide derivatives by using one-pot multicomponent method

Abstract

Keywords

UN SDGs

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