Synthesis of Biologically Active Molecules through Multicomponent Reactions

Molecules, Journal Year: 2020, Volume and Issue: 25(3), P. 505 - 505

Published: Jan. 24, 2020

Focusing on the literature progress since 2002, present review explores highly significant role that multicomponent reactions (MCRs) have played as a very important tool for expedite synthesis of vast number organic molecules, but also, highlights fact many such molecules are biologically active or at least been submitted to any biological screen. The selected papers covered in this must meet two mandatory requirements: (1) reported products should be obtained via reaction; (2) actives tested property. Given diversity synthetic approaches utilized MCRs, diverse nature activities evaluated synthesized compounds, and considering their huge structural variability, much data organized into concise schemes tables facilitate comparison, underscore key points review.

Language: Английский

---

Natural product based leads to fight against leishmaniasis

Bioorganic & Medicinal Chemistry, Journal Year: 2013, Volume and Issue: 22(1), P. 18 - 45

Published: Dec. 5, 2013

Language: Английский

---

Mucosal Leishmaniasis: An Underestimated Presentation of a Neglected Disease

BioMed Research International, Journal Year: 2013, Volume and Issue: 2013, P. 1 - 7

Published: Jan. 1, 2013

We present a review of current knowledge about mucosal leishmaniasis (ML). Although involvement mucous membranes is classically admitted in New World leishmaniasis, particularly occurring infection by Leishmania (L.) braziliensis species complex, ML also possible presentation Old either L. donovani or major complex infections. Thus, has to be considered not only as Latin American disease but an and disease. describe epidemiology, pathogenesis, clinics, diagnosis, therapy. Considering both its highly disfiguring lesions lethal outcome, should underestimated physicians. Moreover, expected increase burden many countries sandfly vector distribution widespreading towards non-endemic areas. Finally, the lack clear understanding pathogenesis absence effective human vaccines strongly claim for more research.

Language: Английский

---

Searching for drugs for Chagas disease, leishmaniasis and schistosomiasis: a review

International Journal of Antimicrobial Agents, Journal Year: 2020, Volume and Issue: 55(4), P. 105906 - 105906

Published: Jan. 25, 2020

Language: Английский

---

mRNA Technology in Modern Medicine: Review and Future Prospects

Deleted Journal, Journal Year: 2025, Volume and Issue: 2, P. 1 - 1

Published: Jan. 17, 2025

Messenger RNA (mRNA) technology has revolutionized modern medicine, particularly in developing vaccines and gene therapies. While its prominence soared during the COVID-19 pandemic, foundation was built on decades of meticulous research. This review explores historical evolution mRNA technology, stabilization delivery breakthroughs, applications combating infectious diseases, cancer, genetic disorders. The study utilized a systematic search peer-reviewed articles from leading databases such as PubMed Scopus, focusing advancements clinical applications. Future potential treating chronic enhancing immunotherapy, addressing public health emergencies is also discussed, emphasizing need for sustained research innovation to harness transformative capabilities fully.

Language: Английский

---

Targeting Cysteine Protease B to Discover Antileishmanial Drugs: Directions and Advances

European Journal of Medicinal Chemistry, Journal Year: 2025, Volume and Issue: 289, P. 117500 - 117500

Published: March 11, 2025

Language: Английский

---

Experimental Validation of Multi-Epitope Peptides Including Promising MHC Class I- and II-Restricted Epitopes of Four Known Leishmania infantum Proteins

Frontiers in Immunology, Journal Year: 2014, Volume and Issue: 5

Published: June 10, 2014

Leishmaniasis is a significant worldwide health problem for which no vaccine exists. Activation of CD4+ and CD8+ T cells crucial the generation protective immunity against parasite. Recent trend in design has been shifted to epitope-based vaccines that are more specific, safe, easy produce. In present study, four known antigenic Leishmania (L.) infantum proteins, CPA, histone H1, KMP-11 LeIF were analysed prediction binding epitopes H2d MHC class I II molecules, using online available algorithms. Based on silico analysis, eight peptides including highly scored I- II-restricted synthesized. Peptide immunogenicity was validated compatible BALB/c mice immunized with each synthetic peptide emulsified CFA/IFA. CPA_p2, CPA_p3, H1_p1 LeIF_p6 induced strong spleen cell proliferation upon vitro re-stimulation. addition, majority peptides, except LeIF_p1 KMP-11_p1, IFN-γ secretion, while KMP-11_p1 indicated suppressive effect IL-10 production. LeIF_p3 IFN-γ-producing indicating TH1 type response. CPA_p3 also induction cells. The peptide-specific IgG designated existence B sequences. Combining immunoinformatic tools experimental validation, we demonstrated H1_p1, H1_p3, likely include potential cytotoxic and/or TH1-type immune responses supporting feasibility peptide-based development leishmaniasis.

Language: Английский

---

Electrospray Encapsulation of Toll-Like Receptor Agonist Resiquimod in Polymer Microparticles for the Treatment of Visceral Leishmaniasis

Molecular Pharmaceutics, Journal Year: 2013, Volume and Issue: 10(3), P. 1045 - 1055

Published: Jan. 15, 2013

Leishmaniasis is a disease caused by the intracellular protozoan, Leishmania. A current treatment for cutaneous leishmaniasis involves delivery of imidazoquinolines via topical cream. However, there are no parenteral formulations most deadly version disease, visceral leishmaniasis. This work investigates use electrospray to encapsulate imidazoquinoline adjuvant resiquimod in acid sensitive microparticles composed acetalated dextran (Ac-DEX) or Ac-DEX/Tween blends. The particles were characterized and tested both vitro vivo. Solutions Ac-DEX ethanol electrosprayed generate approximately 2 μm containing with an encapsulation efficiency 85%. To prevent particle aggregation, blends Tween 20 80 investigated. was then blended at ∼10% (w/w) total polymer formed efficiencies between 40% 60%. In release profiles from exhibited acid-sensitive nature Ac-DEX, 100% drug after 8 h pH 5 (phagosomal pH) 48 7.4 (physiological pH). Treatment elicited significantly greater immune response RAW macrophages over free drug. When injected intravenously into mice inoculated Leishmania, parasite load reduced bone marrow compared blank phosphate-buffered saline controls. Overall, appears offer elegant, scalable way vehicle treating

Language: Английский

---

Promising nanotherapy in treating leishmaniasis

International Journal of Pharmaceutics, Journal Year: 2018, Volume and Issue: 547(1-2), P. 421 - 431

Published: June 8, 2018

Language: Английский

---

Squalene Synthase As a Target for Chagas Disease Therapeutics

PLoS Pathogens, Journal Year: 2014, Volume and Issue: 10(5), P. e1004114 - e1004114

Published: May 1, 2014

Trypanosomatid parasites are the causative agents of many neglected tropical diseases and there is currently considerable interest in targeting endogenous sterol biosynthesis these organisms as a route to development novel anti-infective drugs. Here, we report first x-ray crystallographic structures enzyme squalene synthase (SQS) from trypanosomatid parasite, Trypanosoma cruzi, agent Chagas disease. We obtained five T. cruzi SQS eight human with four classes inhibitors: substrate-analog S-thiolo-farnesyl diphosphate, quinuclidines E5700 ER119884, several lipophilic bisphosphonates, thiocyanate WC-9, two very potent suggesting strategies for selective inhibitor development. also show that bisphosphonates have low nM activity against inhibit acts synergistically azole drug, posaconazole. The determination enzymes diverse set inhibitors active cells provides insights into inhibition, context drugs

Language: Английский

---