Metal-based drugs, including lanthanide complexes, have been extremely effective in clinical treatments against various diseases and raised major interest recent decades. Hence, this work, a series of lanthanum (III) cerium Schiff base ligands derived from (1

Based on the previously reported in vitro antiplasmodial activity of several xanthones from Garcinia mangostana , two xanthones, α‐mangostin and a new compound, δ‐mangostin, were isolated mangosteen husk, cytotoxic effects determined. α‐Mangostin was more active against resistant Plasmodium falciparum chloroquine‐resistant (FCR3) strain (IC 50 = 0.2 ± 0.01 μM) than δ‐mangostin 121.2 1.0 μM). Furthermore, therapeutic response according to administration route evaluated berghei malarial murine...

Background: Patients suffering from a new variant of endemic pemphigus foliaceus in El Bagre, Colombia, South America (El Bagre-EPF) produce autoantibodies (Abs) to different proteins the skin (frustre form), as well those other organs (Senear–Usher-like and systemic forms). Here, we hypothesize whether patients’ play role triggering epicardium pericardium autoimmunity pathogenicity. We based this hypothesis on knowing that these patients frequently show clinical symptoms chest heart,...

Abstract A new series of N ‐substituted pyrazoline derivatives 6a–g , 7a–g 8a–g and 9a–g was synthetized by reaction hydrazine chalcone–thiazole hybrids bearing nitrogen mustard 5a–g . The chalcones were obtained Claisen–Schmidt condensation thiazole‐2‐nitrogen 3 selected acetophenones 4a–g These compounds 6/7/8/9a–g screened for their antifungal activity against Cryptococcus neoformans with IC 50 values 3.9–7.8 µg/ml the ‐3,5‐dichlorophenyl pyrazolines 9e – g Interestingly, those show low...

Traditionally, hamsters are experimentally inoculated in the snout or footpad. However these sites an ulcer not always occurs, measurement of lesion size is a hard procedure and animals show difficulty to eat, breathe move because lesion. In order optimize hamster model for cutaneous leishmaniasis, young adult male female golden (Mesocricetus auratus) were injected intradermally at dorsal skin with 1 1.5 x l07 promastigotes Leishmania species progression subsequent lesions evaluated up 16...

Cutaneous leishmaniasis (CL) is a neglected tropical disease, which causes severe skin lesions. Due to the lack of effective vaccines, and toxicity or reduced effectiveness available drugs in addition complex prolonged treatments, there an urgent need develop alternatives for treatment CL with different mechanisms action. In our effort search new promising hits against Leishmania parasites we prepared 18 acyl hydrazone derivatives thiochroman-4-ones. Compounds were evaluated their vitro...

Abstract Chalcones are a group of natural products with many recognized biological activities, including antiparasitic activity. Although lot chalcones have been synthetized and assayed against parasites, the number structural features known to be involved in this property is small. Thus, present study, 21 were synthesized determine effect substituents A B rings on activity Leishmania braziliensis, Trypanosoma cruzi , Plasmodium falciparum . The compounds active L. braziliensis...

Toxicity and poor adherence to treatment that favors the generation of resistance in Leishmania parasites highlight need develop better alternatives. Here, we evaluated vitro effectiveness hydrazone derived from chromanes 2-(2,3-dihydro-4H-1-benzothiopyran-4-ylidene) hydrazide (TC1) 2-(2,3-dihydro-4H-1-benzopyran-4-ylidene) (TC2) mixture triterpene saponin hederagenin-3-O-(3,4-O-diacetyl-ß-D-xylopyranosyl-(1à3)-a-L- rhamnopyranosyl-(1à2)-a-L-arabinofuranoside,...

Traditionally, hamsters are experimentally inoculated in the snout or footpad. However these sites an ulcer not always occurs, measurement of lesion size is a hard procedure and animals show difficulty to eat, breathe move because lesion. In order optimize hamster model for cutaneous leishmaniasis, young adult male female golden (Mesocricetus auratus) were injected intradermally at dorsal skin with 1 1.5 x l07 promastigotes Leishmania species progression subsequent lesions evaluated up 16...

Six derivatives of the known biopesticide rotenone were prepared by several chemical transformations. Rotenone and its showed differential in vitro antiparasitic activity selective cytotoxicity. In general, compounds more active against Plasmodium falciparum than Leishmania panamensis. had an EC50 19.0 µM P. falciparum, 127.2 L. Although transformation does not improve biological profile three a significant level action within adequate range with values < 50.0 µM. This antiplasmodial was...

Background: In many countries and laboratories, techniques such as direct immunofluorescence (DIF) are not available for the diagnosis of skin diseases. Thus, these laboratories limited in full diagnoses autoimmune diseases, vasculitis, rheumatologic our experience with diseases patient's biopsies, we have noted a positive correlation between periodic acid-Schiff (PAS) staining patterns; however, were just empiric observations. current study, aim to confirm observations, given concept that...

Leishmaniasis is a neglected, parasitic tropical disease caused by an intracellular protozoan from the genus Leishmania . Quinoline alkaloids, secondary metabolites found in plants Rutaceae family, have antiparasitic activity against sp. N -methyl-8-methoxyflindersin ( 1 ), isolated leaves of Raputia heptaphylla and also known as 7-methoxy-2,2-dimethyl-2H,5H,6H-pyran[3,2-c]quinolin-5-one, shows promastigotes amastigotes. This study used silico tools to identify synthetic quinoline alkaloids...

Introduction: Proteinases and proteinase inhibitors have been described to play a role in autoimmune skin blistering diseases.We studied lesional biopsies from patients affected by several diseases for proteinases inhibitors.Methods: We utilized immunohistochemistry evaluate α-1-antitrypsin, human matrix metalloproteinase 9 (MMP9), tissue inhibitor of metalloproteinases 1 (TIMP-1), metallothionein urokinase type plasminogen activator receptor (uPAR).We tested 30 endemic pemphigus, controls...

Current chemotherapeutic agents for leishmaniasis have several disadvantages interfering with the effective treatment and therefore more better antileishmanial drugs are needed. Discovery of candidates requires not only accurate precise methodologies but also well-known biological system to measure infectivity parasites activity new compounds. Significant variation in vitro vivo sensitivity established experimental Leishmania strains reported. This work reports behavior different green...

Neglected tropical diseases are a major health problem throughout the world, and there few effective safe drugs. In this study, we report design synthesis of novel series carbonates eugenol using different aliphatic alcohols N,N-carbonyldiimidazole. Spectroscopic techniques, including 1 H nuclear magnetic resonance (NMR), 13 C NMR, Fourier transform infrared, high-resolution mass spectrometry, were used to confirm structures synthesized compounds. vitro in silico studies prodrugs performed...

Cutaneous Leishmaniasis (CL) is a neglected tropical disease, which causes severe skin lesions. Due to the lack of effective vaccines, treatment can be complex and prolonged, high toxicity, side effects cost, there an urgent need develop alternatives for CL that may have different mechanisms action. In our effort search new promising hits against Leishmania parasites we prepared 18 acyl hydrazone derivatives thiochroman-4-ones. Compounds were evaluated their in vitro antileishmanial activity...

BackgroundWe identified a new variant of endemic pemphigus foliaceus in El Bagre, Colombia, South America, which we term Bagre‐EPF, and observed reactivity to arrector pili muscle (APM), thus tested for autoimmunity APM.

Abstract The synthesis, in silico studies, antiprotozoal and cytotoxic activities of eleven quinoline‐biphenyl hybrids are described herein. structure the synthesized products was elucidated by a combination spectrometric analyses. compounds were evaluated against Plasmodium falciparum, amastigotes forms both Leishmania (V) panamensis Trypanosoma cruzi . Cytotoxicity human U‐937 macrophages. 8‐phenylquinoline ( 4 ) showed similar activity than meglumine antimoniate 4‐(quinolin‐8‐yl)phenol b...

In the last decade, World Health Organization has driven development of drugs for topical use in patients with cutaneous leishmaniasis (CL), most prevalent clinical form leishmaniasis, a neglected tropical disease. The chemicals C6 I, TC1, and TC2 were reported as promising antileishmanial drugs. We aimed to develop nanoformulation that enhances advantageous effect TC2, guaranteeing higher stability bioavailability pharmacologically active components through route. Nanoemulsions prepared by...

Cutaneous leishmaniasis (CL) is a neglected tropical disease, which causes severe skin lesions. Due to the lack of effective vaccines, and toxicity or reduced effectiveness available drugs in addition complex prolonged treatments, there an urgent need develop alternatives for treatment CL with different mechanisms action. In our effort search new promising hits against Leishmania parasites we prepared 18 acyl hydrazone derivatives thiochroman-4-ones. Compounds were evaluated their vitro...