Pharmaceutical agents for treatment of leishmaniasis: a patent landscape

Carvalho, Yasmim Maria Barbosa Gomes de; Saravanan, S.; Batista, Mayrton Santos; Serafini, Mairim Russo; Araújo, Adriano Antunes de Souza; Quintans‐Júnior, Lucindo José

doi:10.1080/13543776.2020.1789100

Cited by 8 publications

(8 citation statements)

References 24 publications

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“…The spots were detected under UV at 245nm and R f value was calculated. The structures assigned to the compounds were supported by the results of IR, 1 H NMR, 13 C NMR and mass spectral data.…”

Section: Chemistrymentioning

confidence: 77%

“…IR spectra were recorded on FT-IR, Agilents spectrophotometer by using KBr pellets in the range of 4000 − 400 cm − 1 . The 1 H NMR and 13 C NMR spectra of the synthesized compounds were recorded on Bruker Top spin 3.2 instrument in solvent (CDCl 3 ); chemical shift (δ) values reported in parts per million (ppm) using tetramethylsilane as internal reference. The splitting pattern of NMR spectra were abbreviated are as follows: s, singlet; bs, broad singlet; d, doublet; dd, double doublet; t, triplet; m, multiplet.…”

Section: Methodsmentioning

confidence: 99%

“…Structure of all the synthesized compounds was monitored by the FTIR, 1 HNMR, 13 CNMR, and Mass spectral analysis. Compound Kp-1 showed actual peak of OCH3, C = N, N-H(stretching), C = C, C-H(aromatic), C-H(aliphatic) is at 1258cm -1 , 1121 cm -1 , 3295 cm -1 , 1513 cm -1 .…”

Section: Chemistrymentioning

confidence: 99%

“…Thiazole and thiosemicarbazone derivatives are widely described in the literature and present a wide range of biological activities [12]. There are various reasons that make thiazole scaffolds interesting prototypes are their accessible chemical synthesis, low costs pertaining to reactivity, good yield reactions, and ability to generate a series of analogues, among others [13]. Thiazole motif has been widely explored by various researchers in the eld of medicinal chemistry to combat various illnesses.…”

Section: Introductionmentioning

confidence: 99%

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Design, Synthesis and Molecular Modeling Studies of Thiosemicarbazone & Thiazole Derivatives as Potential Anti-Malarial Agents

Kaur

Asati

2021

Preprint

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A series of novel thiosemicarbazone & thiazole derivatives (Kp1-10) have been designed, synthesized and evaluated for potential anti-malarial activity. The antimalarial activity of the synthesized thiazole derivatives (Kp1-10) was assessed against human pathogenic malarial strain viz. Plasmodium falciparum while quinine was taken as the standard drug. compound Kp-9 was found to be most promising which exhibited strongest inhibitory activity against P. falciparumwith an IC50 value of 0.29µg/mL which was higher than the reference drug quinine (1.26µg/mL). The SAR studyrevealed that thesubstitution with electron withdrawing group at phenyl increases anti-malarial activity as shown in compound Kp-9. The result of molecular docking studies showed that compounds Kp-9, Kp-1, Kp-3, Kp-4 showed good docking scores with protein (PDB code: 5TBO). The compound Kp-9 showed highest docking score (-9.519). Whereas, compounds Kp-1, Kp-3, Kp-4 and Kp-10 showed good docking scores (-8.764, -8.406, -9.062, -9.435 respectively) with critical interactions with the amino acid residues such as VAL532, ILE237, LEU531, HIE185, TYR528, ASN274, ARG265. The results of biological activity and docking study revealed that the presence of electron withdrawing group at 4th position of phenyl ring attached is crucial for better anti-malarial activity and favorable drug-like profile which can emerge as a potential drug molecule in further development.

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Section: Chemistrymentioning

confidence: 77%

Section: Methodsmentioning

confidence: 99%

Section: Chemistrymentioning

confidence: 99%

Section: Introductionmentioning

confidence: 99%

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Design, Synthesis and Molecular Modeling Studies of Thiosemicarbazone & Thiazole Derivatives as Potential Anti-Malarial Agents

Kaur

Asati

2021

Preprint

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“…This approach is based on the complexity of the pathologies and considers that single-target drugs are insufficient to achieve the desired therapeutic effects [5]. Recently, the multitarget drug strategy was reported as a tool to accelerate the discovery of safer, more active, and patient-compliant drugs for the treatment of leishmaniasis [6].…”

Section: Of 23mentioning

confidence: 99%

Flavonoid Derivatives as New Potent Inhibitors of Cysteine Proteases: An Important Step toward the Design of New Compounds for the Treatment of Leishmaniasis

Lourenço¹,

Iório²,

Silva³

et al. 2022

Preprint

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Leishmaniasis is a neglected tropical disease and affects more than 350 million people worldwide. However, there are no vaccines for humans, and current treatment is hampered due to its high cost, numerous side effects, and painful administration routes. Ending its epidemics by 2030 has become a United Nations goal, and the multitarget drug strategy emerges as a promising alternative. Flavonoids are an example of multitarget compounds and organic synthesis represents a tool to obtain high yields of these molecules. In our study, we synthesized 17 flavonoid analogs using a scalable, easy-to-reproduce, and inexpensive method. All compounds demonstrated an impressive inhibition capacity against rCPB2.8, rCPB3, and rH84Y, which are highly expressed in the amastigote stage, the target form of the parasite. Compounds 3c, f12a, and f12b stood out as effective against all isoforms and intermolecular interactions were investigated through a molecular modeling study. The compounds were highly potent against the parasite and demonstrated low cytotoxic action against mammalian cells. The results were pioneering, representing an advance in the investigation of the mechanisms behind the antileishmanial action of flavonoid derivatives. Furthermore, compounds have shown to be promising leads for the design of other cysteine protease inhibitors for the treatment of leishmaniasis diseases.

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Multi-target withaferin-A analogues as promising anti-kinetoplastid agents through the programmed cell death

Nicolás-Hernández

Hernández-Álvarez

Bethencourt-Estrella

et al. 2023

Biomedicine & Pharmacotherapy

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Pharmaceutical agents for treatment of leishmaniasis: a patent landscape

Cited by 8 publications

References 24 publications

Design, Synthesis and Molecular Modeling Studies of Thiosemicarbazone & Thiazole Derivatives as Potential Anti-Malarial Agents

Design, Synthesis and Molecular Modeling Studies of Thiosemicarbazone & Thiazole Derivatives as Potential Anti-Malarial Agents

Flavonoid Derivatives as New Potent Inhibitors of Cysteine Proteases: An Important Step toward the Design of New Compounds for the Treatment of Leishmaniasis

Multi-target withaferin-A analogues as promising anti-kinetoplastid agents through the programmed cell death

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Pharmaceutical agents for treatment of leishmaniasis: a patent landscape

Cited by 8 publications

References 24 publications

Design, Synthesis and Molecular Modeling Studies of Thiosemicarbazone &amp; Thiazole Derivatives as Potential Anti-Malarial Agents

Design, Synthesis and Molecular Modeling Studies of Thiosemicarbazone &amp; Thiazole Derivatives as Potential Anti-Malarial Agents

Flavonoid Derivatives as New Potent Inhibitors of Cysteine Proteases: An Important Step toward the Design of New Compounds for the Treatment of Leishmaniasis

Multi-target withaferin-A analogues as promising anti-kinetoplastid agents through the programmed cell death

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Product

Resources

About

Design, Synthesis and Molecular Modeling Studies of Thiosemicarbazone & Thiazole Derivatives as Potential Anti-Malarial Agents

Design, Synthesis and Molecular Modeling Studies of Thiosemicarbazone & Thiazole Derivatives as Potential Anti-Malarial Agents