다중혈관 관상동맥 환자에서 y-문합을 이용하여 양쪽 내흉동맥만을 사용한 우회술의 조기 성적

The increasing use of recombinantly expressed therapeutic proteins in the pharmaceutical industry has highlighted issues such as their stability during long-term storage and means of efficacious delivery that avoid adverse immunogenic side effects. Controlled chemical modifications, such as substitutions, acylation and PEGylation, have fulfilled some but not all of their promises, while hydrogels and lipid-based formulations could well be developed into generic delivery systems. Strategies to curb the aggregation and misfolding of proteins during storage are likely to benefit from the recent surge of interest in protein fibrillation. This might in turn lead to generally accepted guidelines and tests to avoid unforeseen adverse effects in drug delivery.

Protein drug stability: a formulation challenge

The therapeutic journey of benzimidazoles: a review.

Tyrosinase is a multi-copper enzyme which is widely distributed in different organisms and plays an important role in the melanogenesis and enzymatic browning. Therefore, its inhibitors can be attractive in cosmetics and medicinal industries as depigmentation agents and also in food and agriculture industries as antibrowning compounds. For this purpose, many natural, semi-synthetic and synthetic inhibitors have been developed by different screening methods to date. This review has focused on the tyrosinase inhibitors discovered from all sources and biochemically characterised in the last four decades.

https://northumbria-test.eprints-hosting.org/id/document/268389

A comprehensive review on tyrosinase inhibitors.

Antituberculosis drugs: ten years of research.

With the aim to improve the biological activities discovered for compounds containing the triazolo[4,5-g]quinoline nucleus, we describe the chemical behaviour of 4-chlorotriazolo[4,5-g]quinolines (la,b) and some its triazolo-N 1 -oxide derivatives (1c-e and II) with electrophilic reagents in order to optimize the synthetic pathways for obtaining both mixtures of N 1,2,3 -alkyl isomers and selectively N 1 -O-alkyl derivatives.

REACTIONS OF ALKYLATION OF BIOLOGICALLY INTERESTING TRIAZOLO[4,5-g]QUINOLINES AND TRIAZOLO[4,5-g]QUINOLINE-1-OXIDES WITH ELECTROPHILIC REAGENTS

New Synthesis of Aminopropylbensenes and 1,2,3,4-Tetrahydroazocines from N-Substituted Tetrahydronicotinamides with Acetylenic Esters

Thirty quinoxalines bearing a substituted phenoxy or hydroxybenzoylglutamate group on position 2, a carboethoxy or carboxy group on position 3 and a trifluoromethyl group on position 6 or 7 of the heterocycle were prepared in order to evaluate the in vitro anticancer activity. Screening over 21 compounds selected at the National Cancer Institute (Bethesda, MD) showed that only few derivatives exhibited a moderate growth inhibition activity on various tumor panel cell lines at 10 −4 molar concentration. The acid derivatives showed no growth inhibition activity. The results obtained in this series seem to indicate that in general carboxy or carboethoxy groups close to O-link with phenyl or benzoyl glutamates on position 2 are detrimental for anticancer activity.

Quinoxaline Chemistry. Part 12. 3‐Carboxy‐2[phenoxy]‐6(7) Substituted Quinoxalines and N‐[4‐(6(7) Substituted‐3‐carboxyquinoxalin‐2‐yl)hydroxy] Benzoylglutamates. Synthesis and Evaluation of in vitro Anticancer Activity.

Twenty compounds possessing benzimidazole, imidazo[4,5-b]pyridine and quinoxaline structure bearing either a substituted arylmethylmercapto- or an arylmethylsulfinyl group in position 2 were prepared in order to evaluate an antiulcer and gastroprotective activity in rat pylorus ligature, in comparison with omeprazole at the dose of 50 mg/kg after i.m. administration. One third of these compounds showed a moderate activity, being about half potent as omeprazole.

Synthesis and Evaluation of Gastroprotective Activity of Omeprazole Related Benzimidazole, Imidazo(4,5-b)pyridine and Quinoxaline 2- Substituted Derivatives.

Sixteen 2-(4'R')phenyl-5R-benzimidazoles and two 2-(4'-pyridinyl)-5R-benzimidazoles were prepared and tested, together with 2-phenylbenzimidazole, for their activity on the acquisition of a conditioned avoidance response in rats and for analgesic activity in mice, and compared with chlorpromazine and acetylsalicylic acid. Several compounds inhibit strongly the acquisition of a C.A.R., with 2-(4'-alkoxy)phenylbenzimidazoles (XVI) and (XVII) clearly exceeding chlorpromazine. Analgesic activity is also generally present in the examined compounds; those bearing in the position 5 a trifluoromethyl or an acetyl group exhibit an activity higher than that of acetylsalicylic acid. Deconditioning and analgesic activities are not correlated with each other.

Preparation and Pharmacological Activity of 2-(4′R′-Phenyl)-5R-benzimidazoles and 2-(4′-Pyridinyl)-5R-benzimidazoles. Analgesic Activity and Effect on Conditioned Avoidance Response.

Giuseppe Paglietti

Papers

REACTIONS OF ALKYLATION OF BIOLOGICALLY INTERESTING TRIAZOLO[4,5-g]QUINOLINES AND TRIAZOLO[4,5-g]QUINOLINE-1-OXIDES WITH ELECTROPHILIC REAGENTS

New Synthesis of Aminopropylbensenes and 1,2,3,4-Tetrahydroazocines from N-Substituted Tetrahydronicotinamides with Acetylenic Esters

Quinoxaline Chemistry. Part 12. 3‐Carboxy‐2[phenoxy]‐6(7) Substituted Quinoxalines and N‐[4‐(6(7) Substituted‐3‐carboxyquinoxalin‐2‐yl)hydroxy] Benzoylglutamates. Synthesis and Evaluation of in vitro Anticancer Activity.

Synthesis and Evaluation of Gastroprotective Activity of Omeprazole Related Benzimidazole, Imidazo(4,5-b)pyridine and Quinoxaline 2- Substituted Derivatives.

Preparation and Pharmacological Activity of 2-(4′R′-Phenyl)-5R-benzimidazoles and 2-(4′-Pyridinyl)-5R-benzimidazoles. Analgesic Activity and Effect on Conditioned Avoidance Response.