Journal ArticleDOI
Highly potent anti-malarial activity of benzopyrano(4,3-b)benzopyran derivatives and in silico interaction analysis with putative target Plasmodium falciparum lactate dehydrogenase.
Nishant Joshi,Rahul S. Hada,Sonal Gupta,Sonal Gupta,Juveria Khan,Jeremy C. Dobrowolski,Pawan K. Dhar,Naresh Kumar,Shailja Singh +8 more
TLDR
In this article, a rapid increase in resistance to existing drugs has posed an urgent problem for the treatment of Malaria infection caused by Plasmodium falciparum.Abstract:
Malaria infection caused by Plasmodium falciparum is majorly responsible for millions of deaths in humans every year. Moreover, a rapid increase in resistance to existing drugs has posed an urgent ...read more
Citations
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2D-quantitative structure-activity relationships model using PLS method for anti-malarial activities of anti-haemozoin compounds.
Phuong Thuy Viet Nguyen,Truong Van Dat,Shusaku Mizukami,Duy Le Hoang Nguyen,Farhana Mosaddeque,Son Ngoc Kim,Duy Hoang Bao Nguyen,Oanh Thi Đinh,Tu Linh Vo,Giang Le Tra Nguyen,Cuong Quoc Duong,Satoshi Mizuta,Dao Ngoc Hien Tam,M. Phuong Truong,Nguyen Tien Huy,Kenji Hirayama +15 more
TL;DR: In this article, the authors developed two-dimensional-quantitative structure-activity relationships (QSAR) models of a series of 21 haemozoin inhibitors to explore the useful physicochemical parameters of the active compounds for estimation of anti-malarial activities.
Journal ArticleDOI
Sustainable synthesis of benzopyranderivativescatalyzed by MgO nanoparticles: Spectral, DFT and TEM analysis
Journal ArticleDOI
Naturally Occurring 8ß,13ß-kaur-15-en-17-al and Anti-Malarial Activity from Podocarpus polystachyus Leaves
M. S. Amir Rawa,Mohammad G Al-Thiabat,Toshihiko Nogawa,Yushi Futamura,Akiko Okano,Habibah A. Wahab +5 more
TL;DR: In this article , the anti-malarial evaluation of Podocarpus polystachyus phytoconstituents was investigated for the first time, and a new natural product, 8ß,13ß-kaur-15-en-17-al (1), along with three known compounds, including α-tocopherol hydroquinone (4), were isolated via HR-ESI-MS and NMR analyses.
Journal ArticleDOI
Identification of starvation-mimetic bioactive phytocomponent from Withania somnifera using in-silico molecular modelling and flow cytometry-based analysis for the management of malaria.
Deepak Pradhan,Prativa Biswasroy,Sharvari Kulkarni,Dilip Kumar Pradhan,Rajesh Bhola,Goutam Ghosh,Goutam Rath +6 more
TL;DR: In this article , a C28 steroidal lactone Withaferin A (WS-3) isolated from Withania somnifera leave extract shows better thermodynamically stable interactions with the glucose transporters (GLUT-1 and PfHT) to standard drugs metformin and lopinavir.
References
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Journal ArticleDOI
Design, synthesis, and biological evaluation of Plasmodium falciparum lactate dehydrogenase inhibitors.
Seoung-Ryoung Choi,Anupam Pradhan,Nicholas L. Hammond,Amar G. Chittiboyina,Babu L. Tekwani,Mitchell A. Avery +5 more
TL;DR: Certain members of these oxamic acid derivatives may have dual inhibitory activities against both pfLDH and pfMDH, presumed that dual LDH/MDH inhibitors would have enhanced potential as antimalarial drugs.
Journal ArticleDOI
In vitro antimalarial activity of biflavonoids from Wikstroemia indica.
Shinyu Nunome,Aki Ishiyama,Miyuki Kobayashi,Kazuhiko Otoguro,Hiroaki Kiyohara,Haruki Yamada,Satoshi Omura +6 more
TL;DR: In this investigation of in vitro antimalarial screening of medicinal herbal extracts, the n-BuOH extract from the root of Wikstroemia indica showed a potent inhibitory effect and two biflavonoids were isolated, 1 and 2 of which were confirmed by (1)H- and (13)C-NMR.
Journal ArticleDOI
Antileishmanial, Toxicity, and Phytochemical Evaluation of Medicinal Plants Collected from Pakistan
TL;DR: All the plants extract and its derived fraction exhibited toxicity in safety range (LC50 > 100) in brine shrimp toxicity evaluation assay and antileishmanial activity was observed for J. dolomiaea methanol extract.
Journal ArticleDOI
Generation of Oxamic Acid Libraries: Antimalarials and Inhibitors of Plasmodium falciparum Lactate Dehydrogenase
Seoung-Ryoung Choi,Aaron B. Beeler,Anupam Pradhan,E. Blake Watkins,John M. Rimoldi,Babu L. Tekwani,Mitchell A. Avery +6 more
TL;DR: An effective automated synthetic strategy for the rapid synthesis of oxamic acid and ester libraries to screen for potential lead inhibitors of lactate dehydrogenase and some oxamic acids showed activities against pfLDH and mammalian LDH at the micromolar range.
Journal ArticleDOI
Dimeric Flavonoids from Arrabidaea brachypoda and Assessment of Their Anti-Trypanosoma cruzi Activity
Cláudia Quintino da Rocha,Emerson Ferreira Queiroz,Cássio Santana Meira,Diogo Rodrigo Magalhães Moreira,Milena Botelho Pereira Soares,Laurence Marcourt,Wagner Vilegas,Jean-Luc Wolfender +7 more
TL;DR: The nonpolar fraction of an aqueous ethanol extract of the roots of Arrabidaea brachypoda, a Brazilian medicinal plant, demonstrated significant in vitro activity against Trypanosoma cruzi, the parasite responsible for Chagas disease.
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