Synthesis, antimalarial, antileishmanial, antimicrobial, cytotoxicity, and methemoglobin (MetHB) formation activities of new 8-quinolinamines.

Synthesis, antimalarial, antileishmanial, antimicrobial, cytotoxicity, and methemoglobin (MetHB) formation activities of new 8-quinolinamines. Research Abstract Details 

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Synthesis, antimalarial, antileishmanial, antimicrobial, cytotoxicity, and methemoglobin (MetHB) formation activities of new 8-quinolinamines. Abstract Text:

Kirandeep Kaur,Sanjay R Patel,Premanand Patil,Meenakshi Jain,Shabana I Khan,Melissa R Jacob,Shobana Ganesan,Babu L Tekwani,Rahul Jain,

We report the synthesis, in vitro antiprotozoal (against Plasmodium and Leishmania), antimicrobial, cytotoxicity (Vero and MetHb-producing properties), and in vivo antimalarial activities of two series of 8-quinolinamines. N1-{4-[2-(tert-Butyl)-6-methoxy-8-quinolylamino]pentyl}-(2S/2R)-2-aminosubstitutedamides (21-33) and N1-[4-(4-ethyl-6-methoxy-5-pentyloxy-8-quinolylamino)pentyl]-(2S/2R)-2-aminosubstitutedamides (51-63) were synthesized in six steps from 6-methoxy-8-nitroquinoline and 4-methoxy-2-nitro-5-pentyloxyaniline, respectively. Several analogs displayed promising antimalarial activity in vitro against Plasmodium falciparum D6 (chloroquine-sensitive) and W2 (chloroquine-resistant) clones with high selectivity indices versus mammalian cells. The most promising analogs (21-24) also displayed potent antimalarial activity in vivo in a Plasmodium berghei-infected mouse model. Most interestingly, many analogs exhibited promising in vitro antileishmanial activity against Leishmania donovani promastigotes, and antimicrobial activities against a panel of pathogenic bacteria and fungi. Several analogs, notably 21-24, 26-32, and 60, showed less MetHb formation compared to primaquine indicating the potential of these compounds in 8-quinolinamine-based antimalarial drug development.

Synthesis, antimalarial, antileishmanial, antimicrobial, cytotoxicity, and methemoglobin (MetHB) formation activities of new 8-quinolinamines. Publishing Authors By Initials

K Kaur,SR Patel,P Patil,M Jain,SI Khan,MR Jacob,S Ganesan,BL Tekwani,R Jain,

For similar cells: cells, cultured: cell line: vero cells research abstracts see: cells: cells, cultured: cell line: vero cells research

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Synthesis, antimalarial, antileishmanial, antimicrobial, cytotoxicity, and methemoglobin (MetHB) formation activities of new 8-quinolinamines. Journal Published:

PUBLICATION TYPE: Research Support, U.S. Gov't,

Journal: Bioorganic & medicinal chemistry

VOLUME: 15

Page Numbers: 915-30

Journal Abbreviation: Bioorg. Med. Chem.

ISSN: 0968-0896

DAY: 20

MONTH: 10

YEAR: 2006

Synthesis, antimalarial, antileishmanial, antimicrobial, cytotoxicity, and methemoglobin (MetHB) formation activities of new 8-quinolinamines. Information

Number of References:

LANGUAGE: eng

NlmUniqueID: 9413298

Synthesis, antimalarial, antileishmanial, antimicrobial, cytotoxicity, and methemoglobin (MetHB) formation activities of new 8-quinolinamines. Keywords Mesh Terms:

KEYWORDS: Vero Cells

MESH TERMS: drug effects

Chemical & Substance for Abstract: Synthesis, antimalarial, antileishmanial, antimicrobial, cytotoxicity, and methemoglobin (MetHB) formation activities of new 8-quinolinamines. Information

Substance Name: L-Lactate Dehydrogenase

Registry Number: EC 1.1.1.27

Grant and Affiliation Information for Synthesis, antimalarial, antileishmanial, antimicrobial, cytotoxicity, and methemoglobin (MetHB) formation activities of new 8-quinolinamines.

AFFILIATION: Department of Medicinal Chemistry, National Institute of Pharmaceutical Education and Research, Sector 67, S.A.S. Nagar, Punjab 160 062, India.

Country: England

AGENCY: United States NIAID

GRANT: AI 27094

ACRONYM: AI

MEDLINETA: Bioorg Med Chem

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