Results 1 to 10 of about 4,370 (170)

Design, Synthesis, and Repurposing of Rosmarinic Acid-β-Amino-α-Ketoamide Hybrids as Antileishmanial Agents [PDF]

Pharmaceuticals, 2023
A series of rosmarinic acid-β-amino-α-ketoamide hybrids were synthesized and rationally repurposed towards the identification of new antileishmanial hit compounds.
Ahmed H.E. Hassan, Waleed A. Bayoumi, Selwan M. El-Sayed, Trong-Nhat Phan, Taegeun Oh, Gyeongpyo Ham, Kazem Mahmoud, Joo Hwan No, Yong Sup Lee   +8 more
doaj   +4 more sources

Natural-Product-Inspired Microwave-Assisted Synthesis of Novel Spirooxindoles as Antileishmanial Agents: Synthesis, Stereochemical Assignment, Bioevaluation, SAR, and Molecular Docking Studies [PDF]

Molecules, 2023
Leishmaniasis is a neglected tropical disease, and there is an emerging need for the development of effective drugs to treat it. To identify novel compounds with antileishmanial properties, a novel series of functionalized spiro[indoline-3,2′-pyrrolidin]-
Nawal Kishore Sahu, Ritu Sharma, Kshirsagar Prasad Suhas, Jyoti Joshi, Kunal Prakash, Richa Sharma, Ramendra Pratap, Xiwen Hu, Sukhbir Kaur, Mukesh Jain, Carmine Coluccini, Paolo Coghi, Sandeep Chaudhary   +12 more
doaj   +2 more sources

Pyrazole derivatives as antileishmanial agents: Biological evaluation, molecular docking study, DFT analysis and ADME prediction [PDF]

Heliyon
Leishmaniasis is a parasitic disease that is commonly found in tropical and sub-tropical regions. Currently, there is no protective antileishmanial vaccine, and the available clinical drugs have serious side effects.
Razieh Sabet, Gholamreza Hatam, Leila Emami, Elaheh Ataollahi, Fateme Zare, Leila Zamani, Behnaz Kazemi, Masood Mohabati Jahromi, Sara Sadeghian, Soghra Khabnadideh   +9 more
doaj   +2 more sources

4-Phenyl-1,3-thiazole-2-amines as scaffolds for new antileishmanial agents [PDF]

Journal of Venomous Animals and Toxins including Tropical Diseases, 2018
Background There is still a need for new alternatives in pharmacological therapy for neglected diseases, as the drugs available show high toxicity and parenteral administration.
Carina Agostinho Rodrigues, Paloma Freire dos Santos, Marcela Oliveira Legramanti da Costa, Thais Fernanda Amorim Pavani, Patrícia Xander, Mariana Marques Geraldo, Ana Mengarda, Josué de Moraes, Daniela Gonçales Galasse Rando   +8 more
doaj   +2 more sources

Discovery of 3,3′-diindolylmethanes as potent antileishmanial agents [PDF]

European Journal of Medicinal Chemistry, 2013
An efficient protocol for synthesis of 3,3'-diindolylmethanes using recyclable Fe-pillared interlayered clay (Fe-PILC) catalyst under aqueous medium has been developed. All synthesized 3,3'-diindolylmethanes showed promising antileishmanial activity against Leishmania donovani promastigotes as well as axenic amastigotes. Structure-activity relationship
Sandip B Bharate, Jaideep B Bharate, Ramesh Mudududdla   +2 more
exaly   +3 more sources

Synthesis and Activity of a New Series of Antileishmanial Agents. [PDF]

ACS Med Chem Lett, 2017
We have determined that tetrahydroindazoles such as 1 show potent activity against Leishmania donovani, the causative agent of leishmaniasis. While the Hsp90 activity and anticancer properties of 1 have previously been explored, we present here our efforts to optimize their activity against L.
Kanwar A, Eduful BJ, Barbeto L, Carletti Bonomo P, Lemus A, Vesely BA, Mutka TS, Azhari A, Kyle DE, Leahy JW.   +9 more
europepmc   +5 more sources

Discovery of triazine mimetics as potent antileishmanial agents. [PDF]

ACS Med Chem Lett, 2013
The World Health Organization has classified the leishmaniasis as a major tropical disease. The discovery of new compounds for leishmaniasis is therefore a pressing concern for the anti-infective research program. We have synthesized 19 compounds of triazine dimers as novel antileishmanial agents.
Chauhan K, Sharma M, Shivahare R, Debnath U, Gupta S, Prabhakar YS, Chauhan PM.   +6 more
europepmc   +4 more sources

Novel Thiazolylimidazole Hybrids as Promising Antileishmanial Agents: Rational Design and Biological Evaluation [PDF]

Pathogens
Leishmaniasis remains a major neglected tropical disease with limited therapeutic options, challenged by drug toxicity and emerging resistance to current treatments like miltefosine.
Cristoper Ramírez-Sandoval, María Elena Campos-Aldrete, María Estela Meléndez-Camargo   +2 more
doaj   +2 more sources

Synthesis and pharmacological evaluation of mono-arylimidamides as antileishmanial agents. [PDF]

Bioorg Med Chem Lett, 2016
Arylimidamide (AIA) compounds containing two pyridylimidamide terminal groups (bis-AIAs) possess outstanding in vitro antileishmanial activity, and the frontrunner bis-AIA DB766 (2,5-bis[2-(2-isopropoxy)-4-(2-pyridylimino)aminophenyl]furan) is active in visceral leishmaniasis models when given orally.
Zhu X, Farahat AA, Mattamana M, Joice A, Pandharkar T, Holt E, Banerjee M, Gragg JL, Hu L, Kumar A, Yang S, Wang MZ, Boykin DW, Werbovetz KA.   +13 more
europepmc   +3 more sources

Novel Heteroaryl Selenocyanates and Diselenides as Potent Antileishmanial Agents. [PDF]

Antimicrob Agents Chemother, 2016
ABSTRACT A series of new selenocyanates and diselenides bearing interesting bioactive scaffolds (quinoline, quinoxaline, acridine, chromene, furane, isosazole, etc.) was synthesized, and their in vitro leishmanicidal activities against Leishmania infantum amastigotes along with ...
Baquedano Y, Alcolea V, Toro MÁ, Gutiérrez KJ, Nguewa P, Font M, Moreno E, Espuelas S, Jiménez-Ruiz A, Palop JA, Plano D, Sanmartín C.   +11 more
europepmc   +4 more sources