Falcipains: biochemistry, target validation and structure-activity relationship studies of inhibitors as antimalarials

J Patra, D Rana, S Arora, M Pal, N Mahindroo - European Journal of …, 2023 - Elsevier
Malaria is a tropical disease with significant morbidity and mortality burden caused by
Plasmodium species in Africa, the Middle East, Asia, and South America. Pathogenic …

Exploring the recent pioneering developments of small molecules in antimalarial drug armamentarium: A chemistry prospective appraisal

T Bagratee, R Prawlall, T Ndlovu, S Sibisi… - Chemistry & …, 2024 - Wiley Online Library
Malaria is a very destructive and lethal parasitic disease that causes significant mortality
worldwide, resulting in the loss of millions of lives annually. It is an infectious disease …

New antileishmanial quinoline linked isatin derivatives targeting DHFR-TS and PTR1: Design, synthesis, and molecular modeling studies

A Sabt, WM Eldehna, TM Ibrahim, AA Bekhit… - European Journal of …, 2023 - Elsevier
In a search for new drug candidates for one of the neglected tropical diseases,
leishmaniasis, twenty quinoline-isatin hybrids were synthesized and tested for their in vitro …

Discovery of 4-alkoxy-2-aryl-6, 7-dimethoxyquinolines as a new class of topoisomerase I inhibitors endowed with potent in vitro anticancer activity

MM Elbadawi, WM Eldehna, W Wang… - European journal of …, 2021 - Elsevier
In our attempt to develop potential anticancer agents targeting Topoisomerase I (TOP1), two
novel series of 4-alkoxy-2-arylquinolines 14a-p and 19a-c were designed and synthesized …

Synthesis, antimicrobial, DFT, and in silico pharmacokinetic profiling of nitroaldol quinoline derivatives: A comprehensive exploration for designing potential oral …

F Guenfoud, O Khaoua, Z Cherak, L Loucif… - Journal of Molecular …, 2024 - Elsevier
This study presents a thorough exploration of the synthesis, biological activities, and
molecular properties of a novel series of β-nitroaldol quinoline derivatives (4a-4i). Structural …

Development of diphenylmethylpiperazine hybrids of chloroquinoline and triazolopyrimidine using Petasis reaction as new cysteine proteases inhibitors for malaria …

H Madhav, TS Patel, Z Rizvi, GS Reddy… - European Journal of …, 2023 - Elsevier
Malaria is a widespread infectious disease, causing nearly 247 million cases in 2021. The
absence of a broadly effective vaccine and rapidly decreasing effectiveness of most of the …

Synthesis, spectroscopic characterization, DFT, molecular docking and in vitro antibacterial potential of novel quinoline derivatives

Y Bouzian, Y Sert, K Khalid, L Van Meervelt… - Journal of Molecular …, 2021 - Elsevier
In this work, three new quinolone derivatives were prepared by alkylation of 2-oxo-1, 2-
dihydroquinoline-4-carboxylic acid with ethyl 2-bromoacetate. The synthesized compounds …

The Plasmodium falciparum ABC transporter ABCI3 confers parasite strain-dependent pleiotropic antimalarial drug resistance

JM Murithi, I Deni, CFA Pasaje, J Okombo… - Cell chemical …, 2022 - cell.com
Widespread Plasmodium falciparum resistance to first-line antimalarials underscores the
vital need to develop compounds with novel modes of action and identify new druggable …

Pd-catalyzed synthesis, characterization, and biological evaluations of pyrazole derivatives: DFT, molecular modelling and antioxidant studies

R Mehandi, C Twala, A Ali, S Ahmedi, M Rana… - Journal of …, 2024 - Elsevier
Abstract Using Pd (PPh 3) 4 as a catalyst, a new series of coupling products (5a–5l)
synthesized from pyrazole derivatives (4a-4c) and substituted boronic acids. Afterward, 1 H …

Iron-Catalyzed Oxidative Cyclization of 2-Amino Styrenes with Alcohols and Methyl Arenes for the Synthesis of Polysubstituted Quinolines

SB Lee, S Chun, SH Choi, J Hong… - The Journal of Organic …, 2023 - ACS Publications
Herein, we present the iron-catalyzed oxidative cyclization of alcohol/methyl arene with 2-
amino styrene to synthesize polysubstituted quinoline. Low-oxidation level substrates such …