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.

DNA Binders: 2. Molecular Recognition of DNA by 2,3,6,7-tetrahydro-1Hpyrrolo[1,2-a]indole-1,8(5H)-dione bis(4,5-dihydro-1H-imidazol-2-ylhydrazone) as a Prototype of “Two-Armed” Intercalating Agents

A series of new benzoylquinoxaline derivatives (7-26) was synthesized and evaluated for antitumor activity against a panel of 60 human cell lines at the NCI of Bethesda. Among the compounds which have passed the preliminary screening, compound 23 exhibited the best profile and growth inhibition activity at 100 - 10 μM. The compounds were then tested towards a folate-dependent enzymes bio-library including Thymidylate synthases enzymes and human Dihydrofolate reductase at 10 μM. The most of compounds exhibited a moderate inhibitory activity towards all or some of the enzymes tested with detectable inhibition constants (Ki) values in the range of 0.6-70 μM. Compounds 21, 23, 24 showed Ki in the range of 10-38 μM against both hDHFR and hTS.

Novel 3‐Benzoyl‐2‐piperazinylquinoxaline Derivatives as Potential Antitumor Agents.

Thirty 3-(2-aryl-5R-benzimidazol-1-yl)butanoic acids were prepared in order to evaluate substitution effects on the 2 and 5 positions of the heterocyclic ring upon the previously recorded choleretic activity of 3-(2-phenylbenzimidazol-1-yl)butanoic acid. A general choleretic activity is shown by the acids tested, which in several cases it is superior to that of the model compound and sometimes also to that of dehydrocholic acid.

Synthesis and Choleretic Activity of 3-(2-Aryl-5-R-benzimidazol-1-yl)butanoic Acids.

Addition reactions of acetylenic esters upon 1-(2-thienyl)- and 1-(3-thienyl)-ethanone oximes and upon 6,7-dihydrobenzo[b]thiophen-4(5H)-one and 5,6-dihydrobenzo[b]-thiophen-7(4H)-one oximes. Formation of 2-(thienyl)-pyrroles and 4,5-dihydro-1H-thieno[g]indoles

1-Aryl-1,4-dihydropyridines combine with dimethyl acetylenedicarboxylate to form tetramethyl 1-aryl-1,3a,3b,4,6a,6b-hexahydrocyclopenta[3,4]cyclobuta[1,2-b]pyrrole-3,3a,6,6a-tetracarboxylates, the structures of which were deduced from their 1H, 13C n.m.r., and mass spectra. The mode of formation of the adducts is discussed.

Addition reactions of heterocyclic compounds. Part 71. The formation of 1,3a,3b,4,6a,6b-hexahydrocyclopenta[3,4]cyclobuta[1,2-b]pyrroles from dimethyl acetylenedicarboxylate and 1-aryl-1,4-dihydropyridines

Giuseppe Paglietti

Papers

DNA Binders: 2. Molecular Recognition of DNA by 2,3,6,7-tetrahydro-1Hpyrrolo[1,2-a]indole-1,8(5H)-dione bis(4,5-dihydro-1H-imidazol-2-ylhydrazone) as a Prototype of “Two-Armed” Intercalating Agents

Novel 3‐Benzoyl‐2‐piperazinylquinoxaline Derivatives as Potential Antitumor Agents.

Synthesis and Choleretic Activity of 3-(2-Aryl-5-R-benzimidazol-1-yl)butanoic Acids.

Addition reactions of acetylenic esters upon 1-(2-thienyl)- and 1-(3-thienyl)-ethanone oximes and upon 6,7-dihydrobenzo[b]thiophen-4(5H)-one and 5,6-dihydrobenzo[b]-thiophen-7(4H)-one oximes. Formation of 2-(thienyl)-pyrroles and 4,5-dihydro-1H-thieno[g]indoles

Addition reactions of heterocyclic compounds. Part 71. The formation of 1,3a,3b,4,6a,6b-hexahydrocyclopenta[3,4]cyclobuta[1,2-b]pyrroles from dimethyl acetylenedicarboxylate and 1-aryl-1,4-dihydropyridines