BackgroundThere is no direct correlation between acne severity and lesion numbers and patients with moderate acne may present with varying lesion counts. The fixed-dose adapalene 0.1%-benzoyl peroxide (BPO) 2.5% combination gel is an efficacious and safe acne treatment.

BackgroundAcne vulgaris is a disorder of the pilosebaceous unit of the skin, and the underlying mechanism is still obscure. Kyoto rhino (krh/krh) rats were made by ethylnitrosourea (ENU) mutagenesis and harbor S413X nonsense mutation of the rat hairless (Hr) gene. Krh/krh rats develop comedones ...

ABSTRACTThe aim of this study was to develop a microemulsion formulation of adapalene for transfollicular delivery. A pseudoternary phase diagram was developed for microemulsion consisting of oleic acid as oil phase, tween 20 as surfactant, Transcutol® as cosurfactant, and deionized water. Diffe...

Hair follicles are a promising target for the administration of drugs to treat diseases associated with the pilosebaceous unit, such as acne. For solid lipid microparticle dispersions a successful and selective delivery of adapalene via targeted erosion of the particles in sebum has been shown. ...

The aim of present study was to design and optimize 0.1% adapalene loaded nano-emulsion to improve the drug efficacy and increase its user compliance. Effect of type and concentration of surfactants was studied on size of 0.1% adapalene loaded nano-emulsion. Optimized formulation was then evalua...

The purpose of this study is to develop a new formulation of adapalene for the topical treatment of acne. We investigated applicability of polymeric nanocarriers based on tyrosine-derived nanospheres (TyroSpheres) for adapalene delivery. TyroSpheres effectively encapsulated adapalene and substan...

Malignant melanoma was the leading cause of mortality among the skin-associated cancer owing to its highly metastatic feature, increasing incidence and drug resistance requirement. Retinoids played important roles in the treatment of cancer via the activation of retinoid acid receptor (RAR) or r...

Small molecule retinoids are potential therapeutics for a variety of neurological diseases. However, most retinoids are poorly water soluble and difficult to deliver in vivo, which prevents further study of their utility to treat disease. Here, we focus on adapalene, an FDA approved drug that is...

This paper reports the synthesis of a series of methylpyruvate thiosemicarbazone derivatives containing, on the terminal nitrogen, substituents of different nature and size and namely, ethyl, phenyl and methylphenyl. These ligands were reacted with bis(triphenylphosphine)copper(I) nitrate and ac...

The physico-chemical properties of tris(triphenylphosphane)copper(I) nitrate dimer (1) have been investigated. 1 exists as dimer in which one nitrate group acts as a bridge between two Cu(I) centers to complete the tetrahedral coordination about the metal while another nitrate is present as an a...

This paper reports the synthesis and characterization of six compounds of copper(I), stabilized in its reduced state by two triphenylphosphines, in which 4-fluorobenzaldehyde thiosemicarbazone and N-methylthiosemicarbazone act as chelating through their sulfur and imino nitrogen. The three oxoan...

The syntheses of four compounds, obtained by the reaction of methylpyruvate thiosemicarbazone (Hmpt) and its methyl (Me-Hmpt) and allyl (Allyl-Hmpt) derivatives with bis(triphenylphosphine)copper(I) acetate, are reported. The compounds [Cu(PPh3)2(ptc)(Hptc)]·H2O (1), [Cu(PPh3)2(Me-ptc)] (2), [C...

Previously, ω-guanidino- and ω-aminoalkanamides, structurally derived from arpromidine-like histamine H2 receptor agonists, were reported as novel neuropeptide Y Y1 antagonists. Regardless of the backbone, they resemble BIBP 3226, an argininamide with high NPY Y1 receptor affinity and selectiv...

Arpromidine analogs in which the guanidino group was replaced or substituted were investigated in functional studies for NPY Y1 and histamine H1 antagonism as well as for H2 agonism (HEL cells, guinea pig ileum and atrium). A basic guanidine or amidine system proved to be important for both Y1 a...

Analogues of the potent histamine H2 agonist arpromidine, characterized by non-heterocyclic groups (phenyl, cyclohexyl, alkyl) instead of the pheniramine-like portion, were prepared and tested for their H2 agonistic and H1 antagonistic activity in the isolated guinea pig right atrium and ileum, ...

Structure-activity relationships for a series of 65 H2-agonists of the impromidine (phenyl analogues) and arpromidine type were investigated by Free-Wilson analysis. These compounds have in common an imidazolylpropylguanidine moiety which is connected to 1 or 2 aromatic rings through a flexible ...

Herein we report for the first time an efficient synthetic procedure for the preparation of N-aryl-N’-ureido-O-sulfamates (AUSs) as a new class of Carbonic Anhydrase Inhibitors (CAIs). The compounds were tested for the inhibition of several human (h) Carbonic Anhydrase (CA; EC 4.2.1.1) isoforms...

A series of twenty novel ureido benzenesulfonamides incorporating 1,3,5-triazine moieties substituted on one side with aromatic amines and on the other side with dimethylamine, morpholine and piperidine is reported. The compounds were synthesized from the 4-(3-(4,6-dichloro-1,3,5-triazin-2-yl)ur...

5,5-Diphenyl-2,4-thiazolidinedithione (3a), when refluxed with anhydrous AlCl3 in toluene, is desulfurated and rearranged to 4,5-diphenyl-4-thiazoline-2-thione (4). Neither 2,2-diphenyl-1,4,2H- benzothiazine-3(4H)-thione (5b) nor its S-Me derivative (6 are changed on similar treatment.

The geometries of 15 conformations of the model tripeptide N-formyl l-alanyl l-alanine amide (Ala-Ala) were determined by ab initio gradient geometry refinements at the HF/4-21G level. The results can be compared with previous HF/4-21G calculations on the single residue, N-formyl alanine amide (...