8-Quinolinamines and Their pro prodrug conjugates as potent blood-Schizontocidal antimalarial agents

Vangapandu, Suryanarayana; Sachdeva, Sandeep; Jain, M.; Singh, Surinder; Singh, Prati Pal; Kaul, C. L.; Jain, Rahul

doi:10.1016/j.bmc.2003.07.003

Cited by 32 publications

(40 citation statements)

References 26 publications

Supporting

Mentioning

Contrasting

Order By: Relevance

“…This produced almost 200 PQ derivatives (Tables 2-4) bearing diverse groups in one or more given positions of the ring [6,46,[161][162][163][164][165][166][167][168][169][170][171][172][173][174][175][176][177][178][179]. Globally, the most favourable substituent insertions towards anti-malarial activity where those of methyl groups at positions 4 and 2, tert-butyl at position 2, simultaneous insertion of ethyl substituents at positions 2 and 4 and pentyloxy at position 5, as well as insertion at position 5 of alkoxy, fluoro, and 3-or 4-substituted phenoxy groups [51,163].…”

Section: Modifications At the Quinoline Ringmentioning

confidence: 99%

Primaquine revisited six decades after its discovery

Vale¹,

Moreira²,

Gomes³

2009

European Journal of Medicinal Chemistry

322

308

View full text Add to dashboard Cite

Section: Modifications At the Quinoline Ringmentioning

confidence: 99%

Primaquine revisited six decades after its discovery

Vale¹,

Moreira²,

Gomes³

2009

European Journal of Medicinal Chemistry

322

308

View full text Add to dashboard Cite

“…Jain et al 150 synthesized several N 8 -(4-amino-1-methylbutyl)-5-alkoxy-4-ethyl-6-methoxy-8-quinolinamines and their pro prodrug analogs 59 (R ¼ OC 3 H 7 to OC 8 H 17 , R 1 ¼ C 2 H 5 , R 2 ¼ linker) prepared by covalently linking redox-sensitive and esterase-sensitive linkers through the amide linkage. The most effective 8-quinolinamines of the series have exhibited in vitro and in vivo biological efficacy superior to that of the standard drug chloroquine against both drug-sensitive and drug-resistant malaria strains.…”

Section: -Aminoquinolinesmentioning

confidence: 99%

Recent advances in antimalarial drug development

Vangapandu

Jain

Kaur

et al. 2006

Medicinal Research Reviews

Self Cite

View full text Add to dashboard Cite

Malaria caused by protozoa of the genus Plasmodium, because of its prevalence, virulence, and drug resistance, is the most serious and widespread parasitic disease encountered by mankind. The inadequate armory of drugs in widespread use for the treatment of malaria, development of strains resistant to commonly used drugs such as chloroquine, and the lack of affordable new drugs are the limiting factors in the fight against malaria. These factors underscore the continuing need of research for new classes of antimalarial agents, and a re-examination of the existing antimalarial drugs that may be effective against resistant strains. This review provides an in-depth look at the most significant progress made during the past 10 years in antimalarial drug development.

show abstract

“…PQ, an 8-aminoquinoline, has serious side effects and is known to induce hemolysis, especially in glucose-6-phosphate dehydrogenase (G6PD)-deficient individuals. However, Vangapandu and coworkers (34) demonstrated that 8-quinoline amine conjugates as well as the corresponding "double prodrugs" had promising in vivo activity in mice. If these compounds, in which the basic pharmacophore is primaquine phosphate, were modified to improve their blood schizonticide activity, they would have the capability to be employed as broad-spectrum (tissue and blood schizonticides) antimalarial agents.…”

Section: Advantages Of Hybridsmentioning

confidence: 99%

Are Antimalarial Hybrid Molecules a Close Reality or a Distant Dream?

Agarwal

Gupta

Awasthi

2017

Antimicrob Agents Chemother

View full text Add to dashboard Cite

Emergence of drug-resistant Plasmodium falciparum strains has led to a situation of haste in the scientific and pharmaceutical communities. Hence, all their efforts are redirected toward finding alternative chemotherapeutic agents that are capable of combating multidrug-resistant parasite strains. In light of this situation, scientists have come up with the concept of hybridization of two or more active pharmacophores into a single chemical entity, resulting in "antimalarial hybrids." The approach has been applied widely for generation of lead compounds against deadly diseases such as cancer and AIDS, with a proven potential for use as novel drugs, but is comparatively new in the sphere of antimalarial drug discovery. A sudden surge has been evidenced in the number of studies on the design and synthesis of hybrids for treating malaria and may be regarded as proof of their potential advantages over artemisinin-based combination therapy (ACT). However, it is evident from recent studies that most of the potential advantages of antimalarial hybrids, such as lower toxicity, better pharmacokinetics, and easier formulation, have yet to be realized. A number of questions left unaddressed at present need to be answered before this approach can progress to the late stages of clinical development and prove their worth in the clinic. To the best of our knowledge, this compilation is the first attempt to shed light on the shortcomings that are surfacing as more and more studies on molecular hybridization of the active pharmacophores of known antimalarials are being published.

show abstract

8-Quinolinamines and Their pro prodrug conjugates as potent blood-Schizontocidal antimalarial agents

Cited by 32 publications

References 26 publications

Primaquine revisited six decades after its discovery

Primaquine revisited six decades after its discovery

Recent advances in antimalarial drug development

Are Antimalarial Hybrid Molecules a Close Reality or a Distant Dream?

Contact Info

Product

Resources

About