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.

Reaction of 5-aminobenzotriazoles with methyl propiolate. Formation of triazolo[4,5-f]quinolines and related compounds. Unusual products in the Michael addition reaction of 2-methyl-2H-5-aminobenzotriazole

In the course of our work aimed at developing novel heterocycles of pharmaceutical interest, a
new tricycle, the tetrahydropyrrolo[1,2- a ]indole-1,8-dione, has been synthesized by an
intramolecular Friedel-Crafts acylation, as a synthon suitable to be functionalized to give novel
compounds with potential biological properties. Also, an unusual nucleophilic α-addition to
methyl propiolate by 1,5,6,7-tetrahydro-4 H -indol-4-one was observed and discussed.

/pdf/synthesis-of-pyrrol-1-2-a-indole-1-8-5h-diones-as-new-31uq1brc45.pdf

Synthesis of pyrrol-[1,2-a]indole-1,8(5H)-diones as new synthones for developing novel tryciclic compounds of pharmaceutical interest

A new series of 23 6,7-difluoro-3-methyl-2-phenylthio/phenylsulfonyl/phenylsulfinyl/benzylamino/phenylamino-quinoxaline 1,4-dioxides variously substituted in the phenyl moiety, was synthesized and submitted to in vitro evaluation for anti-mycobacterial, anti-trichomonas, anti-candida, anti-mycoplasma and antibacterial activities. In anti-mycobacterial assays, several compounds resulted active (MIC90 = 2.0-4.0 microg/ml) against Mycobacterium tuberculosis H37Rv. Anti-trichomonas screening showed a generally good activity of all compounds (MBC = 0.39-25.0 microg/ml) versus Trichomonas vaginalis, in particular the derivatives 5a,d, 7a, 9 and 11c ranged 0.39-0.78 microg/ml (metronidazole MBC = 12.5 microg/ml). Results of anti-candida assays showed that derivatives 7a, 8a,d and 9 were active against several species of Candida (C. albicans, C. krusei, C. parapsilosis and C. glabrata), having MIC50 between 3.9 and 31.25 microg/ml. The latter compounds were also submitted to anti-mycoplasma assay against Mycoplasma hominis, the results obtained showed that 7a, 8a,d and 9 inhibited the growth of the mycoplasma at the concentration of 0.1 mg/ml. In antibacterial tests only a few compounds showed an MIC50 lower than 62.5 microg/ml against representative strains of Gram-positive and Gram-negative bacteria (Escherichia coli, Klebsiella pneumoniae, Staphylococcus aureus, Vibrio alginolyticus and Pseudomonas aeruginosa).

Synthesis, anti‐Mycobacterial, anti‐Trichomonas and anti‐Candida in vitro Activities of 2‐Substituted‐6,7‐difluoro‐3‐methylquinoxaline 1,4‐Dioxides.

Thermal rearrangement of 6,7-dihydrobenzo[ b ]furan-4(5 H )-one and 4,5,6,7-tetrahydroindol-4-one 4(7)- O -( E )-(1,2-
dimethoxycarbonylvinyl)ketoximes gave 4,5-dihydrofuro[2,3g]- and 4,5-dihydropyrrolo[2,3 g ]- and [3,2- g ] indoles,
three novel tricyclic systems

Addition reactions of acetylenic esters to 6,7-dihydrobenzo[b]furan-4(5H)-one, 6,7-dihydroindol-4(5H)-one, 5,6-dihydrobenzo[b]furan-7(6H)-one and 5,6-dihydroindol-7(6H)-one ketoximes. Formation of reduced furo[g]- and pyrrolo[g]-indoles

Thirty compounds possessing quinoxaline structure bearing either substituted arylmethylmercapto-, arylmethylsulfinyl group or a piperazinyl moiety in position 2 were prepared in order to evaluate an antiulcer and gastroprotective activity in rat pylorus ligature, in comparison with omeprazole and ranitidine at the dose of 100 mg/kg after oral administration. Among the compounds of the first group one third showed a moderate activity being about half potent as omeprazole whereas in the second group compound 5b exibited an activity superior to that of ranitidine accompanied with the lowest incidence of lesions and mortality and another compound (5i) was equiactive as ranitidine.

Quinoxaline Chemistry. Part 6. Synthesis and Evaluation of Antiulcer and Gastroprotective Activity of 2‐(Arylmethylmercapto‐, Arylmethylsulfinyl‐, Piperazinyl‐3‐R‐substituted) Quinoxalines.

Giuseppe Paglietti

Papers

Reaction of 5-aminobenzotriazoles with methyl propiolate. Formation of triazolo[4,5-f]quinolines and related compounds. Unusual products in the Michael addition reaction of 2-methyl-2H-5-aminobenzotriazole

Synthesis of pyrrol-[1,2-a]indole-1,8(5H)-diones as new synthones for developing novel tryciclic compounds of pharmaceutical interest

Synthesis, anti‐Mycobacterial, anti‐Trichomonas and anti‐Candida in vitro Activities of 2‐Substituted‐6,7‐difluoro‐3‐methylquinoxaline 1,4‐Dioxides.

Addition reactions of acetylenic esters to 6,7-dihydrobenzo[b]furan-4(5H)-one, 6,7-dihydroindol-4(5H)-one, 5,6-dihydrobenzo[b]furan-7(6H)-one and 5,6-dihydroindol-7(6H)-one ketoximes. Formation of reduced furo[g]- and pyrrolo[g]-indoles

Quinoxaline Chemistry. Part 6. Synthesis and Evaluation of Antiulcer and Gastroprotective Activity of 2‐(Arylmethylmercapto‐, Arylmethylsulfinyl‐, Piperazinyl‐3‐R‐substituted) Quinoxalines.