The aim of the present study was to investigate and compare specific in vitro pharmacological actions of human α- and β-CGRP applied as single concentrations to prostaglandin F2α precontracted segments of guinea pig basilar artery. To support the suggestion of a possible link between the phar...

In this study we have analysed, by in situ hybridization, the expression of the genes for both α-CGRP and β-CGRP in hypoglossal motor nuclei following transection of the left hypoglossal nerve. Our results show that the gene for α-CGRP displays a peculiar sequence of regulation (a successive ...

Along with acetylcholine, motoneurons express several neuromodulatory peptides. The most extensively studied of these peptides is calcitonin gene-related peptide (CGRP). CGRP modulates the biochemical, physiological and metabolic properties of skeletal muscle primarily through activation of memb...

The effects of the recently described human α-calcitonin gene-related peptide (CGRP), human β-CGRP and rat α-CGRP have been compared with those of the vasodilator sodium nitroprusside, on the rat and rabbit isolated heart. Hearts were perfused at constant flow and [Arg8]-vasopressin was used ...

Calcitonin gene-related peptide (CGRP)-α is expressed in heart ventricles in sensory nerves and cardiomyocytes. It modifies inotropism and induces ischaemic preconditioning. This study investigates the effect of CGRP-α on the contractile responsiveness of isolated adult ventricular rat cardiom...

In an attempt to discover new potent inhibitors for Mycobacterium tuberculosis (Mtb), a series of 2-(2-hydrazinyl)thiazole derivatives with a wide range of substitutions at 2-, 4- and 5-positions were designed by considering Lipinski rule. The designed compounds were synthesized, characterized a...

PI3Kδ, which is mainly expressed in leukocytes, plays a critical role in B-cell receptor mediated signaling pathway and has been extensively studied as a drug discovery target for B cell malignances such as AML, CLL etc. In this manuscript, we report the discovery, SAR optimization and pharmaco...

A simple and efficient method has been developed for the synthesis of 2-aminothiazoles and N-allylthioureas from commercially available materials in one pot by using a supported reagents system, KSCN/SiO2–RNH3OAc/Al2O3, in which α-halo ketone reacts first KSCN/SiO2 and the product, α-thiocyan...

Tuberculosis (TB) is one of the deadliest infectious diseases of all times, and its recent resurgence is a supreme matter of concern. Co-infection with HIV and, in particular, the continuous isolation of new resistant strains, makes the discovery of novel anti-TB agents a strategic priority. The...

The synthesis and study of the structure–activity relationships of cytotoxic compounds based on N-pyridinyl or N-aryl-2-(1-benzylindol-3-yl)glyoxamide skeleton, represented by the lead structures D-24241 and D-24851, are described. The presence of N-(pyridin-4-yl) moiety was crucial for activit...

The chiral ester ethyl (2R)-hydroxy-2-(1′,2′,3′,4′-tetrahydro-1′,1′,4′,4′-tetramethyl-6′-naphthalenyl) acetate 2 and the corresponding acid 4 were prepared as intermediates in the synthesis of the retinoic acid receptor gamma-specific agonist (R)-3-fluoro-4-[[hydroxy(5,6,7,8-tetrahydro-...

Aromatic retinoids having a meta-substituted aromatic ring bridge, such as 4-[3-(5,6,7,8-tetrahydro-5,5,8,8-tetramethyl-2-naphthalenyl)phenyl]benzoic acid and its 3,5-diaryl-substituted 4,5-dihydroisoxazole analogue, function as retinoid receptor panagonists by activating both retinoic acid and ...

A series of truncated naphthoic acid retinoids have been prepared using the Heck reaction. These retinoids were evaluated in the RAR transactivation assay in vitro and in the utriculi reduction assay in vivo. It has been found that the naphthalene ring of the retinoids is crucial for their retin...

Synthesis and structure–activity relationships (SAR) of RARα-selective agonists are discussed. 4-[5-(5,8-Dimethyl-2H-3-chromenyl)-1H-2-pyrrolyl]benzoic acid (12a), which possesses a flat structural moiety and an oxygen atom at the hydrophobic part, showed highly selective transactivation activ...

Deprotection of various substituted alkyl and phenolic TBDMS ethers were carried out using prepared silver exchanged silicotungstic acid (AgSTA) salt as heterogeneous catalyst in methanol at room temperature. The Brönsted acidic protons of silicotungstic acid were substituted by Lewis acidic sil...

Chitosan (CS) based edible coatings has been widely applied in postharvest preservation in fruit and vegetables. In this work, the incorporation of chlorogenic acid onto chitosan was conducted using free radical mediated grafting procedure. The effects of chitosan grafted with chlorogenic acid (...

The co-existence of dyes, Cr(VI) and high concentration of salt in dyeing wastewater causes serious and complex environmental problems. In this study, a salt-tolerant strain Bacillus circulans BWL1061 was reported to simultaneously remove 50 mg/L methyl orange and 50 mg/L Cr(VI) under the anaero...

Lately, an “all-in-one” strategy via direct pyrolysis of protic salt has attracted great attention in the preparation of hetero-doped porous carbons due to its distinctive simplicity. However, protic salt derived carbons usually process large grain sizes thus hamper their applications. Herein,...

Interleukin-2 (IL-2) is a multifunctional cytokine in immune regulation. It is essential for the differentiation, expansion and stability of CD25+Foxp3+ regulatory T (Treg) cells, which is an important factor in immune suppression and self-tolerance. Meanwhile, IL-2 also stimulate effector T (Te...

Newcastle disease virus (NDV) have shown oncolytic therapeutic efficacy in preclinical study and are currently approved for clinical trials. NDV Anhinga strain which is a mesogenic strain should be classified as lytic strain and has a therapeutic efficacy in hepatocellular cancer. In this study,...