Synthesis of Substituted Indole Derivatives as a New Class of Antimalarial Agents.

ChemInform ◽  
2005 ◽  
Vol 36 (43) ◽  
Author(s):  
Anu Agarwal ◽  
Kumkum Srivastava ◽  
S. K. Puri ◽  
Prem M. S. Chauhan
Keyword(s):  
Indole Derivatives ◽  
New Class ◽  
Antimalarial Agents

Synthesis of substituted indole derivatives as a new class of antimalarial agents

2005 ◽  
Vol 15 (12) ◽  
pp. 3133-3136 ◽  
Author(s):  
Anu Agarwal ◽  
Kumkum Srivastava ◽  
S.K. Puri ◽  
Prem M.S. Chauhan
Keyword(s):  
Indole Derivatives ◽  
New Class ◽  
Antimalarial Agents

Pyrimido[5,4-b]indole derivatives. 1. A new class of potent and selective .alpha.1 adrenoceptor ligands

1991 ◽  
Vol 34 (6) ◽  
pp. 1850-1854 ◽  
Author(s):  
Filippo Russo ◽  
Giuseppe Romeo ◽  
Salvatore Guccione ◽  
Antonio De Blasi
Keyword(s):  
Indole Derivatives ◽  
New Class

scholarly journals Synthesis and Antimalarial Activities of Cyclen 4-Aminoquinoline Analogs

2009 ◽  
Vol 53 (4) ◽  
pp. 1320-1324 ◽  
Author(s):  
M. O. Faruk Khan ◽  
Mark S. Levi ◽  
Babu L. Tekwani ◽  
Shabana I. Khan ◽  
Eiichi Kimura ◽  
...  
Keyword(s):  
Mammalian Cells ◽  
High Selectivity ◽  
Antimalarial Activity ◽  
New Class ◽  
Antimalarial Agents ◽  
Sensitive Clone ◽  
Resistant Strains ◽  
Incorporation Assay

ABSTRACT In an attempt to augment the efficacy of 7-chloro 4-aminoquinoline analogs and also to overcome resistance to antimalarial agents, we synthesized three cyclen (1,4,7,10-tetraazacyclododecane) analogs of chloroquine [a bisquinoline derivative, 7-chloro-4-(1,4,7,10-tetraaza-cyclododec-1-yl)-quinoline HBr, and a 7-chloro-4-(1,4,7,10-tetraaza-cyclododec-1-yl)-quinoline-Zn2+ complex]. The bisquinoline displays the most potent in vitro and in vivo antimalarial activities. It displays 50% inhibitory concentrations (IC50s) of 7.5 nM against the D6 (chloroquine-sensitive) clone of Plasmodium falciparum and 19.2 nM against the W2 (chloroquine-resistant) clone, which are comparable to those of artemisinin (10.6 and 5.0 nM, respectively) and lower than those of chloroquine (10.7 and 87.2 nM, respectively), without any evidence of cytotoxicity to mammalian cells, indicating a high selectivity index (>1,333 against D6 clone and >521 against W2 clone). Potent antimalarial activities of the bisquinoline against chloroquine- and mefloquine-resistant strains of P. falciparum were also confirmed by in vitro [3H]hypoxanthine incorporation assay. The in vivo antimalarial activity of the bisquinoline, as determined in P. berghei-infected mice, is comparable to that of chloroquine (50% effective dose, ≤1.1 mg/kg when given orally); no apparent toxicity has been observed up to the highest dose tested (3 × 30 mg/kg). The bisquinoline inhibits in vitro hemozoin (β-hematin) formation with an IC50 of 1.1 μM, which is about 10-fold more potent than chloroquine (IC50 9.5 μM). Overall, this article describes the discovery of a new class of cyclen 4-aminoquinoline analogs as potent antimalarial drugs.

scholarly journals Discovery of oxybisbenzoylamides as a new class of antimalarial agents

MedChemComm ◽  
2015 ◽  
Vol 6 (6) ◽  
pp. 1173-1177 ◽  
Author(s):  
A. Pancotti ◽  
S. Parapini ◽  
M. Dell'Agli ◽  
L. Gambini ◽  
C. Galli ◽  
...  
Keyword(s):  
Plasmodium Falciparum ◽  
New Class ◽  
Antimalarial Agents ◽  
Dual Inhibitors

A new antimalarial pharmacophore has been obtained starting from previously described dual inhibitors of Plasmodium falciparum.

Synthesis of 4-pyrido-6-aryl-2-substituted amino pyrimidines as a new class of antimalarial agents

2005 ◽  
Vol 13 (22) ◽  
pp. 6226-6232 ◽  
Author(s):  
Anu Agarwal ◽  
Kumkum Srivastava ◽  
S.K. Puri ◽  
Prem M.S. Chauhan
Keyword(s):  
New Class ◽  
Antimalarial Agents

ChemInform Abstract: Indole Derivatives as a New Class of Steroid 5α-Reductase Inhibitors.

ChemInform ◽  
2010 ◽  
Vol 28 (16) ◽  
pp. no-no
Author(s):  
H. TAKAMI ◽  
H. KOSHIMURA ◽  
N. KISHIBAYASHI ◽  
A. ISHII ◽  
H. NONAKA ◽  
...  
Keyword(s):  
Indole Derivatives ◽  
New Class ◽  
Reductase Inhibitors

Synthesis and bioevaluation of hybrid 4-aminoquinoline triazines as a new class of antimalarial agents

2008 ◽  
Vol 18 (24) ◽  
pp. 6530-6533 ◽  
Author(s):  
Ashok Kumar ◽  
Kumkum Srivastava ◽  
S. Raja Kumar ◽  
S.K. Puri ◽  
Prem M.S. Chauhan
Keyword(s):  
New Class ◽  
Antimalarial Agents

Glycosyl hydroperoxides: A new class of potential antimalarial agents

2015 ◽  
Vol 23 (13) ◽  
pp. 3033-3039 ◽  
Author(s):  
Barbara Szechner ◽  
Anna Jaromin ◽  
Silvia Parapini ◽  
Nicoletta Basilico ◽  
Barbara Grzeszczyk ◽  
...  
Keyword(s):  
New Class ◽  
Antimalarial Agents

Synthesis of 2-[3-(7-Chloro-quinolin-4-ylamino)-alkyl]-1-(substituted phenyl)-2,3,4,9-tetrahydro-1H-β-carbolines as a new class of antimalarial agents

2008 ◽  
Vol 18 (11) ◽  
pp. 3306-3309 ◽  
Author(s):  
Leena Gupta ◽  
Kumkum Srivastava ◽  
Shubhra Singh ◽  
S.K. Puri ◽  
Prem M.S. Chauhan
Keyword(s):  
New Class ◽  
Antimalarial Agents

ChemInform Abstract: Synthesis of 9-Anilinoacridine Triazines as New Class of Hybrid Antimalarial Agents.

ChemInform ◽  
2010 ◽  
Vol 41 (16) ◽  
Author(s):  
Ashok Kumar ◽  
Kumkum Srivastava ◽  
S. Raja Kumar ◽  
S. K. Puri ◽  
Prem M. S. Chauhan
Keyword(s):  
New Class ◽  
Antimalarial Agents
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