Results 1 to 10 of about 4,514 (173)

Synthesis of New 4-Aminoquinolines and Evaluation of Their In Vitro Activity against Chloroquine-Sensitive and Chloroquine-Resistant Plasmodium falciparum. [PDF]

PLoS ONE, 2015
The efficacy of chloroquine, once the drug of choice in the fight against Plasmodium falciparum, is now severely limited due to widespread resistance.
Chandima S K Rajapakse, Maryna Lisai, Christiane Deregnaucourt, Véronique Sinou, Christine Latour, Dipankar Roy, Joseph Schrével, Roberto A Sánchez-Delgado   +7 more
doaj   +10 more sources

4-Aminoquinoline: a comprehensive review of synthetic strategies [PDF]

Frontiers in Chemistry
4-Aminoquinoline is an important scaffold due to its variety of applications in medicinal, synthetic organic, and industrial chemistry. It has gained great relevance for the development of selective and potent leishmanicidal agents targeting parasite ...
Francisco Delgado, Francisco Delgado, Andrés Benítez, Lourdes Gotopo, Angel H. Romero   +4 more
doaj   +4 more sources

Synthesis and Antimycobacterial Evaluation of N-(4-(Benzyloxy)benzyl)-4-aminoquinolines [PDF]

Molecules, 2022
Tuberculosis remains a global health problem that affects millions of people around the world. Despite recent efforts in drug development, new alternatives are required.
Estevão Silveira Grams, Alessandro Silva Ramos, Mauro Neves Muniz, Raoní S. Rambo, Marcia Alberton Perelló, Nathalia Sperotto, Laura Calle González, Lovaine Silva Duarte, Luiza Galina, Adilio Silva Dadda, Guilherme Arraché Gonçalves, Cristiano Valim Bizarro, Luiz Augusto Basso, Pablo Machado   +13 more
doaj   +2 more sources

Homology modeling, docking, and ADMET studies of benzoheterocyclic 4-aminoquinolines analogs as inhibitors of Plasmodium falciparum [PDF]

Journal of Taibah University Medical Sciences, 2023
الملخص: أهداف البحث: يتم ضمان الكفاح المستمر ضد الأمراض المستوطنة من خلال مقاومة طفيل الملاريا المتزايدة للأدوية المتاحة على نطاق واسع. وهكذا، فإن البحث عن الأدوية المضادة للملاريا ذات الفعالية المحسنة يتحول إلى بحث دائم.
Zakari Y. Ibrahim, MSc, Adamu Uzairu, PhD, Gideon A. Shallangwa, PhD, Stephen E. Abechi, PhD, Sulaiman Isyaku, PhD   +4 more
doaj   +2 more sources

QSAR and molecular docking studies of 1,3-dioxoisoindoline-4-aminoquinolines as potent antiplasmodium hybrid compounds [PDF]

Heliyon, 2020
Quantitative structure–activity relationships (QSAR) provides a model that link biological activities of compounds to thier chemical stuctures and molecular docking study reveals the interaction between drug and its target enzyme.
Aliyu Wappah Mahmud, Gideon Adamu Shallangwa, Adamu Uzairu   +2 more
doaj   +2 more sources

Structural Insight into the Mechanism of 4-Aminoquinolines Selectivity for the alpha2A-Adrenoceptor [PDF]

Drug Design, Development and Therapy, 2020
Zaibing Li,1,2,* Jingyu Li,1,* Liyan Liu,1 Wenyi Deng,3 Qingrong Liu,4 Ruofan Liu,4 Wen Zhang,3 Zaiqing He,5 Lei Fan,6 Yingzhuo Yang,7 Yun Duan,7 Huifang Hou,1 Xinyuan Wang,1 Zhimei Yang,1 Xiaoying Wang,1 Shanze Chen,1 Yi Wang,1 Ning Huang,1 Junli Chen1 ...
Li Z, Li J, Liu L, Deng W, Liu Q, Liu R, Zhang W, He Z, Fan L, Yang Y, Duan Y, Hou H, Wang X, Yang Z, Wang X, Chen S, Wang Y, Huang N, Chen J   +18 more
doaj   +2 more sources

4-Aminoquinolines block heme iron reactivity and interfere with artemisinin action [PDF]

eLife
Artemisinin-based combination therapies (ACTs) remain the mainstay of treatment for Plasmodium falciparum malaria, despite reports of ACT treatment failure. ACTs consist of an artemisinin and a longer-lived partner drug, which is often a quinoline. Given
Melissa Rosenthal, Daniel E Goldberg
doaj   +2 more sources

Antimalarial activity and mechanisms of action of two novel 4-aminoquinolines against chloroquine-resistant parasites. [PDF]

PLoS ONE, 2012
Chloroquine (CQ) is a cost effective antimalarial drug with a relatively good safety profile (or therapeutic index). However, CQ is no longer used alone to treat patients with Plasmodium falciparum due to the emergence and spread of CQ-resistant strains,
Anna Caroline Campos Aguiar, Raquel de Meneses Santos, Flávio Júnior Barbosa Figueiredo, Wilian Augusto Cortopassi, André Silva Pimentel, Tanos Celmar Costa França, Mario Roberto Meneghetti, Antoniana Ursine Krettli   +7 more
doaj   +2 more sources

Long-chain 4-aminoquinolines inhibit filamentation and increase efficacy of nystatin against Candida albicans infections in vivo [PDF]

npj Biofilms and Microbiomes
In exploring a growing demand for innovative approaches to tackle emerging and life threatening fungal diseases, we identified long-chain 4-aminoquinoline (4-AQ) derivatives as a new class of anti-virulence agents.
Aleksandar Pavic, Natasa Radakovic, Ivana Moric, Nada Stankovic, Dejan Opsenica, Lidija Senerovic   +5 more
doaj   +2 more sources

Anti-Mycobacterial Evaluation of 7-Chloro-4-Aminoquinolines and Hologram Quantitative Structure–Activity Relationship (HQSAR) Modeling of Amino–Imino Tautomers [PDF]

Pharmaceuticals, 2017
In an ongoing research program for the development of new anti-tuberculosis drugs, we synthesized three series (A, B, and C) of 7-chloro-4-aminoquinolines, which were evaluated in vitro against Mycobacterium tuberculosis (MTB).
Marcelle L. F. Bispo, Camilo H. S. Lima, Laura N. F. Cardoso, André L. P. Candéa, Flávio A. F. M. Bezerra, Maria C. S. Lourenço, Maria G. M. O. Henriques, Ricardo B. Alencastro, Carlos R. Kaiser, Marcus V. N. Souza, Magaly G. Albuquerque   +10 more
doaj   +2 more sources