Antimalarial activities of new pyrrolo[3,2-f]quinazoline-1,3-diamine derivatives

Jian Guan, Quan Zhang, Michael O'Neil, Nicanor Obaldia, Arba L Ager, Lucia Gerena, Ai J. Lin

Research output: Contribution to journalArticle

44 Citations (Scopus)

Abstract

WR227825 is an antimalarial pyrroloquinazolinediamine derivative with a high potency but a low therapeutic index. A series of carbamate, carboxamide, succinimide, and alkylamine derivatives of WR227825 were prepared to search for compounds with an improved therapeutic index. The new acetamides and imide showed potent cell growth inhibition against four clones of Plasmodium falciparum (D-6, RCS, W-2, and TM91C235), with a 50% inhibitory concentration of ∼0.01 ng/ml, and were highly active against Plasmodium berghei, with 100% cure at doses from

Original languageEnglish (US)
Pages (from-to)4928-4933
Number of pages6
JournalAntimicrobial Agents and Chemotherapy
Volume49
Issue number12
DOIs
StatePublished - Dec 2005

Fingerprint

Quinazolines
Diamines
Antimalarials
Acetamides
Imides
Plasmodium berghei
Carbamates
Plasmodium falciparum
Inhibitory Concentration 50
Clone Cells
Therapeutics
Growth
succinimide

ASJC Scopus subject areas

  • Pharmacology (medical)

Cite this

Guan, J., Zhang, Q., O'Neil, M., Obaldia, N., Ager, A. L., Gerena, L., & Lin, A. J. (2005). Antimalarial activities of new pyrrolo[3,2-f]quinazoline-1,3-diamine derivatives. Antimicrobial Agents and Chemotherapy, 49(12), 4928-4933. https://doi.org/10.1128/AAC.49.12.4928-4933.2005

Antimalarial activities of new pyrrolo[3,2-f]quinazoline-1,3-diamine derivatives. / Guan, Jian; Zhang, Quan; O'Neil, Michael; Obaldia, Nicanor; Ager, Arba L; Gerena, Lucia; Lin, Ai J.

In: Antimicrobial Agents and Chemotherapy, Vol. 49, No. 12, 12.2005, p. 4928-4933.

Research output: Contribution to journalArticle

Guan, J, Zhang, Q, O'Neil, M, Obaldia, N, Ager, AL, Gerena, L & Lin, AJ 2005, 'Antimalarial activities of new pyrrolo[3,2-f]quinazoline-1,3-diamine derivatives', Antimicrobial Agents and Chemotherapy, vol. 49, no. 12, pp. 4928-4933. https://doi.org/10.1128/AAC.49.12.4928-4933.2005
Guan, Jian ; Zhang, Quan ; O'Neil, Michael ; Obaldia, Nicanor ; Ager, Arba L ; Gerena, Lucia ; Lin, Ai J. / Antimalarial activities of new pyrrolo[3,2-f]quinazoline-1,3-diamine derivatives. In: Antimicrobial Agents and Chemotherapy. 2005 ; Vol. 49, No. 12. pp. 4928-4933.
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