HIV infection and ART use are associated with altered plasma clot characteristics in Black South Africans.

Background: Human immunodeficiency virus (HIV) and antiretroviral treatment (ART) are both associated with hypercoagulability. Altered clot properties could be a potential mechanism thereof. We aimed to investigate the association of HIV and ART, with fibrinogen and plasma clot properties in a group of Black South Africans.

Synthesis,Antidiabetic and Antitubercular Evaluation of Quinoline-pyrazolopyrimidine hybrids and Quinoline-4-Arylamines.

Two libraries of quinoline-based hybrids 1-(7-chloroquinolin-4-yl)-1H-pyrazolo[3,4-d]pyrimidin-4-amine and 7-chloro-N-phenylquinolin-4-amine were synthesized and evaluated for their α-glucosidase inhibitory and antioxidant properties. Compounds with 4-methylpiperidine and para-trifluoromethoxy groups, respectively, showed the most promising α-glucosidase inhibition activity with IC=46.70 and 40.

Ecotoxicology of Trace Elements in European Oyster (Ostrea edulis), Seawater, and Sedimentsacross Boston Harbor, Massachusetts,USA.

European oyster (Ostrea edulis) can be used for biological monitoring of water and sediment quality and serve as a conduit of trace elements to humans via consumption. Trace element concentrations in seawater, sediment, O. edulis edible tissues and shells from Boston Harbor were studied and found to be elevated relative to comparative studies in native ecosystems in the Adriatic Sea and Bay of Biscay.

New azaaurone derivatives as potential multitarget agents in HIV-TB coinfection.

Tuberculosis (TB) disease, caused by Mycobacterium tuberculosis (Mtb) is the leading cause of death among people with human immunodeficiency virus (HIV) infection. No dual-target drug is currently being used to simultaneously treat both infections. This work aimed to obtain new multitarget HIV-TB agents, with the goal of optimizing treatments and preventing this coinfection.

Structural Optimization of Antimycobacterial Azaaurones Towards Improved Solubility and Metabolic Stability.

While N-acetyl azaaurones have already been disclosed for their potential against tuberculosis (TB), their low metabolic stability remains an unaddressed liability. We now report a study designed to improve the metabolic stability and solubility of the azaaurone scaffold and to identify the structural requirements for antimycobacterial activity. Replacing the N-acetyl moiety for a N-carbamoyl group led to analogues with sub- and nanomolar potencies against M.

Change in body size in a rapidly warming marine ecosystem: Consequences of tropicalization.

Climate change is profoundly affecting the physical environment and biota of the Northeast U.S. Continental Shelf ecosystem.

Quinolone analogues of benzothiazinone: Synthesis, antitubercular structure-activity relationship and ADME profiling.

Mycobacterium tuberculosis (Mtb) has an impermeable cell wall which gives it an inherent ability to resist many antibiotics. DprE1, an essential enzyme in Mtb cell wall synthesis, has been validated as a target for several TB drug candidates. The most potent and developmentally advanced DprE1 inhibitor, PBTZ169, is still undergoing clinical development.

Discovery and biological evaluation of an adamantyl-amide derivative with likely MmpL3 inhibitory activity.

A series of molecules containing bulky lipophilic scaffolds was screened for activity against Mycobacterium tuberculosis and a number of compounds with antimycobacterial activity were identified. The most active compound, (2E)-N-(adamantan-1-yl)-3-phenylprop-2-enamide (C1), has a low micromolar minimum inhibitory concentration, low cytotoxicity (therapeutic index = 32.26), low mutation frequency and is active against intracellular Mycobacterium tuberculosis.

Quinolone-3-amidoalkanol: A New Class of Potent and Broad-Spectrum Antimicrobial Agent.

Herein, we describe 39 novel quinolone compounds bearing a hydrophilic amine chain and varied substituted benzyloxy units. These compounds demonstrate broad-spectrum activities against acid-fast bacterium, Gram-positive and -negative bacteria, fungi, and leishmania parasite. Compound maintained antitubercular activity against moxifloxacin-, isoniazid-, and rifampicin-resistant , while exhibited low micromolar activities (<1 μg/mL) against World Health Organization (WHO) critical pathogens: , , and .

Diversification of the African legless skinks in the subfamily Acontinae (Family Scincidae).

Cladogenic diversification is often explained by referring to climatic oscillations and geomorphic shifts that cause allopatric speciation. In this regard, southern Africa retains a high level of landscape heterogeneity in vegetation, geology, and rainfall patterns. The legless skink subfamily Acontinae occurs broadly across the southern African subcontinent and therefore provides an ideal model group for investigating biogeographic patterns associated with the region.

Hydrazone-Tethered 5-(Pyridin-4-yl)-4H-1,2,4-triazole-3-thiol Hybrids: Synthesis, Characterisation, in silico ADME Studies, and in vitro Antimycobacterial Evaluation and Cytotoxicity.

Compounds containing arylpyrrole-, 1,2,4-triazole- and hydrazone structural frameworks have been widely studied and demonstrated to exhibit a wide range of pharmacological properties. Herein, an exploratory series of new 1,2,4-triazole derivatives designed by amalgamation of arylpyrrole and 1,2,4-triazole structural units via a hydrazone linkage is reported. The synthesised compounds were tested in vitro for their potential activity against Mycobacterium tuberculosis (MTB) H Rv strain.

Arylnitro monocarbonyl curcumin analogues: Synthesis and in vitro antitubercular evaluation.

Curcumin is a natural product that has been reported to exhibit myriad pharmacological properties, one of which is antitubercular activity. It demonstrates antitubercular activity by directly inhibiting Mycobacterium tuberculosis (M.tb) and also enhances immune responses that ultimately lead to the elimination of M.

Nitrothiazole-Thiazolidinone Hybrids: Synthesis and in Vitro Antimicrobial Evaluation.

Herein we report the synthesis of novel compounds inspired by the antimicrobial activities of nitroazole and thiazolidin-4-one based compounds reported in the literature. Target compounds were investigated in vitro for antitubercular, antibacterial, antifungal, and overt cell toxicity properties. All compounds exhibited potent antitubercular activity.

Investigation of quinolone-tethered aminoguanidine as novel antibacterial agents.

A recent study identified quinolone-based thiosemicarbazone with an MIC value of 2 µM against Mycobacterium tuberculosis (Mtb). Herein, we report further optimization of the previous hit, which led to the discovery of quinolone-tethered aminoguanidine molecules with generally good antitubercular activity. Compounds 7f and 8e emerged as the hits of the series with submicromolar antitubercular activity, exhibiting MIC values of 0.

Decadal-scale phenology and seasonal climate drivers of migratory baleen whales in a rapidly warming marine ecosystem.

Species' response to rapid climate change can be measured through shifts in timing of recurring biological events, known as phenology. The Gulf of Maine is one of the most rapidly warming regions of the ocean, and thus an ideal system to study phenological and biological responses to climate change. A better understanding of climate-induced changes in phenology is needed to effectively and adaptively manage human-wildlife conflicts.

Exploration of 4-aminopyrrolo[2,3-d]pyrimidine as antitubercular agents.

Tuberculosis (TB) is one of the leading causes of death worldwide. Developing new anti-TB compounds using cost-effective processes is critical to reduce TB incidence and accomplish the End TB Strategy milestone. Herein, we describe the synthesis and structure-activity relationships of a library of thirty 7H-Pyrrolo[2,3-d]pyrimidine derivatives providing insights into the contributions of different aromatic, aryl and alkyl substitution at the C-4 position of the 7-deazapurine ring.

Antiplasmodial and antimycobacterial activities of crude and lead-like enhanced extracts from Namibian medicinal plants.

Ethnopharmacological Relevance: Eight indigenous medicinal plants which are used traditionally for the treatment of tuberculosis (TB), malaria, and associated symptoms, were selected for this study.

Aim Of Study: The aim of this study was to evaluate the antiplasmodial and antimycobacterial activities of the organic and aqueous crude extracts of different plant parts, by comparing the activities of subfractions (lead-like enhanced [LLE] extracts and methanol fractions) prepared from the bioactive crude extracts.

Materials & Methods: Crude aqueous and organic extracts were prepared for 25 different plant parts obtained from eight plant species.

Identification of supraoptimal temperatures in juvenile blueback herring () using survival, growth rate and scaled energy reserves.

For young fishes, growth of somatic tissues and energy reserves are critical steps for survival and progressing to subsequent life stages. When thermal regimes become supraoptimal, routine metabolic rates increase and leave less energy for young fish to maintain fitness-based activities and, in the case of anadromous fishes, less energy to prepare for emigration to coastal habitats. Thus, understanding how energy allocation strategies are affected by thermal regimes in young anadromous fish will help to inform climate-ready management of vulnerable species and their habitat.

Anthropogenic Sources Dominate Foliar Chromium Dust Deposition in a Mining-Based Urban Region of South Africa.

Dust pollution can be severe in urban centers near mines and smelters. Identification of dust sources and assessing dust capturing plant morphological traits may help address the problem. A chromium (Cr) mining and ferrochrome smelting region in Sekhukhuneland, South Africa, was investigated to identify the sources of Cr in soil and plant leaf surfaces and to evaluate the association between Cr sources and plant morphology.

Drought risk for agricultural systems in South Africa: Drivers, spatial patterns, and implications for drought risk management.

The regular drought episodes in South Africa highlight the need to reduce drought risk by both policy and local community actions. Environmental and socioeconomic factors in South Africa's agricultural system have been affected by drought in the past, creating cascading pressures on the nation's agro-economic and water supply systems. Therefore, understanding the key drivers of all risk components through a comprehensive risk assessment must be undertaken in order to inform proactive drought risk management.

Antimycobacterial Activity, Synergism, and Mechanism of Action Evaluation of Novel Polycyclic Amines against .

has developed extensive resistance to numerous antimycobacterial agents used in the treatment of tuberculosis. Insufficient intracellular accumulation of active moieties allows for selective survival of mycobacteria with drug resistance mutations and accordingly promotes the development of microbial drug resistance. Discovery of compounds with new mechanisms of action and physicochemical properties that promote intracellular accumulation, or compounds that act synergistically with other antimycobacterial drugs, has the potential to reduce and prevent further drug resistance.

Synthesis and comparison of in vitro dual anti-infective activities of novel naphthoquinone hybrids and atovaquone.

A principal factor that contributes towards the failure to eradicate leishmaniasis and tuberculosis infections is the reduced efficacy of existing chemotherapies, owing to a continuous increase in multidrug-resistant strains of the causative pathogens. This accentuates the dire need to develop new and effective drugs against both plights. A series of naphthoquinone-triazole hybrids was synthesized and evaluated in vitro against Leishmania (L.

Direct and size-mediated effects of temperature and ration-dependent growth rates on energy reserves in juvenile anadromous alewives (Alosa pseudoharengus).

Growth rate and energy reserves are important determinants of fitness and are governed by endogenous and exogenous factors. Thus, examining the influence of individual and multiple stressors on growth and energy reserves can help estimate population health under current and future conditions. In young anadromous fishes, freshwater habitat quality determines physiological state and fitness of juveniles emigrating to marine habitats.