A biologically active acid hydrolysis product of saxitoxin

1976 ◽  
Vol 68 (3) ◽  
pp. 776-780 ◽  
Author(s):  
V.E. Ghazarossian ◽  
E.J. Schantz ◽  
H.K. Schnoes ◽  
F.M. Strong
Keyword(s):  
Acid Hydrolysis ◽  
Hydrolysis Product ◽  
Biologically Active

scholarly journals 7-Bromo-[1,2,5]selenadiazolo[3,4-d]pyridazin-4(5H)-one

Molbank ◽  
10.3390/m1229 ◽  
2021 ◽  
Vol 2021 (2) ◽  
pp. M1229
Author(s):  
Timofey N. Chmovzh ◽  
Oleg A. Rakitin
Keyword(s):  
Mass Spectrometry ◽  
Heterocyclic System ◽  
High Resolution Mass Spectrometry ◽  
Uv Spectroscopy ◽  
Hydrolysis Product ◽  
Selenium Dioxide ◽  
Biologically Active ◽  
Photovoltaic Materials ◽  
Organic Photovoltaic Materials ◽  
Ir And Uv Spectroscopy

New heterocyclic systems containing 1,2,5-chalcogenadiazoles are of great interest for the creation of organic photovoltaic materials and biologically active compounds. In this communication, 3,6-dibromopyridazine-4,5-diamine was investigated in reaction with selenium dioxide in order to obtain 4,7-dibromo-[1,2,5]selenadiazolo[3,4-d]pyridazine. We found that 7-bromo-[1,2,5]selenadiazolo[3,4-d]pyridazin-4(5H)-one, the first representative of the new heterocyclic system, was isolated as a hydrolysis product of the corresponding 4,7-dibromoderivative. The structure of the newly synthesized compound was established by means of elemental analysis, high-resolution mass spectrometry, 1H, 13C NMR, IR and UV spectroscopy, and mass spectrometry.

Structure Elucidation of 2-Amino-5-phenyl-2-oxazolin-4-one (Pemoline) and X-Ray Structure of its Hydrolysis Product 5-Phenyl-oxazolidine-2,4- dione

2005 ◽  
Vol 60 (8) ◽  
pp. 853-857 ◽  
Author(s):  
Piotr Kuś ◽  
Peter G. Jones ◽  
Rafał Celiński
Keyword(s):  
Acetic Acid ◽  
Hydrogen Bonds ◽  
Acid Hydrolysis ◽  
Single Crystals ◽  
Structure Elucidation ◽  
Hydrolysis Product ◽  
Spectroscopic Properties ◽  
Aqueous Acetic Acid ◽  
X Ray ◽  
Independent Molecules

In this study we compare spectroscopic properties of pemoline (2-amino-5-phenyl-2-oxazolin- 4-one) and its acid hydrolysis product 5-phenyl-oxazolidine-2,4-dione. Crystallization of pemoline from aqueous acetic acid gave single crystals of compound 2, the structure of which was determined by X-ray studies. All four crystallographically independent molecules form dimers linked by N-H···O = C hydrogen bonds.

scholarly journals The Effects of Microwave-Assisted Pretreatment and Cofermentation on Bioethanol Production from Elephant Grass

2020 ◽  
Vol 2020 ◽  
pp. 1-11
Author(s):  
Sefrinus Maria Dolfi Kolo ◽  
Deana Wahyuningrum ◽  
Rukman Hertadi
Keyword(s):  
Acid Hydrolysis ◽  
Hydrolysis Product ◽  
Pichia Stipitis ◽  
Pennisetum Purpureum ◽  
Bioethanol Production ◽  
Elephant Grass ◽  
Microwave Assisted ◽  
Liquid Chromatographic Analysis ◽  
High Concentrations ◽  
Liquid Chromatographic

The process of acid hydrolysis using conventional methods at high concentrations results in products having lower yields, and it needs a longer time of process; therefore, it becomes less effective. In this study, we analyzed the effects of microwave-assisted pretreatment and cofermentation on bioethanol production from elephant grass (Pennisetum purpureum). We used a combination of delignification techniques and acid hydrolysis by employing a microwave-assisted pretreatment method on elephant grass (Pennisetum purpureum) as a lignocellulosic material. This was followed by cofermentation with Saccharomyces cerevisiae ITB-R89 and Pichia stipitis ITB-R58 to produce bioethanol. The optimal sugar mixtures (fructose and xylose) of the hydrolysis product were subsequently converted into bioethanol by cofermentation with S. cerevisiae ITB-R89 and P. stipitis ITB-R58, carried out with varying concentrations of inoculum for 5 days (48 h) at 30°C and pH 4.5. The high-power liquid chromatographic analysis revealed that the optimal inoculum concentration capable of converting 76.15% of the sugar mixture substrate (glucose and xylose) to 10.79 g/L (34.74% yield) of bioethanol was 10% (v/v). The optimal rate of ethanol production was 0.45 g/L/d, corresponding to a fermentation efficiency of 69.48%.

Weekly dosing of the investigational oral proteasome inhibitor MLN9708 in patients (pts) with relapsed/refractory multiple myeloma (MM): A phase I study.

2012 ◽  
Vol 30 (15_suppl) ◽  
pp. 8034-8034 ◽  
Author(s):  
Shaji Kumar ◽  
William Bensinger ◽  
Craig B. Reeder ◽  
Todd M. Zimmerman ◽  
James R. Berenson ◽  
...  
Keyword(s):  
Dose Escalation ◽  
Proteasome Inhibitor ◽  
Phase 1 ◽  
Hydrolysis Product ◽  
Proteasome Inhibition ◽  
Median Number ◽  
Current Data ◽  
Biologically Active ◽  
Multiple Tumor ◽  
Grade 3

8034 Background: Phase 1 studies are evaluating IV and oral dosing of the reversible proteasome inhibitor MLN9708 in multiple tumor types. We report the safety, MTD, pharmacokinetics (PK), pharmacodynamics, and preliminary responses with weekly oral MLN9708 in pts with relapsed/refractory MM (NCT00963820). Methods: Pts aged ≥18 yrs received MLN9708 on d 1, 8, and 15 of 28-d cycles. In the dose-escalation phase, pts required ≥2 prior therapies (including bortezomib, thalidomide/lenalidomide, and corticosteroids). At the MTD, pts were to be enrolled to relapsed and refractory (RR), bortezomib-relapsed (VR), proteasome inhibitor (PI) naïve, and carfilzomib (CZ) expansion cohorts. Results: 36 pts have been enrolled to date (data cut-off: Dec 1, 2011), 32 in the dose-escalation phase (0.24–3.95 mg/m2) and 8 to expansion cohorts (2 RR, 5 VR, 1 PI naïve; RR and VR cohorts each include 2 pts from MTD dose-escalation cohort). Median age was 64.5 yrs (range 40–79), 53% were male, and median number of prior lines of therapy was 3.5 (range 1-13), including 92%, 92%, 56%, and 8% who had prior bortezomib, lenalidomide, thalidomide, and carfilzomib, respectively. Pts have received a median of 2 cycles (range 1–11); 5 pts remain on treatment. Among 24 DLT-evaluable pts, 3 DLTs were seen: 2 at 3.95 mg/m2 (1 grade 3 rash, 1 grade 3 GI AEs) and 1 at 2.97 mg/m2 (grade 3 GI AEs). The MTD was determined as 2.97 mg/m2. Overall, 69% of pts had drug-related AEs, and 28% had related grade ≥3 AEs, including thrombocytopenia (17%), diarrhea (11%), nausea, neutropenia, and fatigue (each 8%). Only 3 (8%) pts had drug-related peripheral neuropathy (PN; no grade ≥3). 2 pts discontinued due to AEs. In 18 response-evaluable pts, 1 had a VGPR at 3.95 mg/m2, 1 had a PR at 2.97 mg/m2, and 8 have achieved SD durable for up to 9.5 mos. PK analyses showed linear plasma PK (0.8–3.95 mg/m2), Tmax of 0.5-2 hr, and terminal half-life of 7 d for MLN2238 (biologically active hydrolysis product). There was a trend for a dose-dependent increase in whole blood 20S proteasome inhibition. Conclusions: Current data suggest weekly oral MLN9708 is generally well tolerated with infrequent PN, and shows early signs of antitumor activity.

scholarly journals The borohydride-reducible compounds of human aortic elastin. Demonstration of a new cyclic amino acid in alkali hydrolysate, and changes with age and in patients with annulo-aortic ectasia including one with Marfan syndrome

1985 ◽  
Vol 232 (1) ◽  
pp. 169-175 ◽  
Author(s):  
T Halme ◽  
M Jutila ◽  
T Vihersaari ◽  
P Oksman ◽  
N D Light ◽  
...  
Keyword(s):  
Acid Hydrolysis ◽  
Marfan Syndrome ◽  
Aldol Condensation ◽  
Condensation Product ◽  
Hydrolysis Product ◽  
Exchange Chromatography ◽  
Spectrometric Analysis ◽  
Cross Link ◽  
Aortic Ectasia ◽  
And Control

Human aortic elastin reduced with [3H]borohydride was analysed by ion-exchange chromatography after alkali or acid hydrolysis. Alkali hydrolysates of elastins contained a radioactive peak that was eluted between proline and leucine. This peak was not present in foetal elastin, but its proportion increased steadily during aging. Aortic samples from patients with annulo-aortic ectasia (aneurysm of the ascending aorta), including one with classical Marfan syndrome, contained less elastin (CNBr-insoluble material) than did the age-matched controls. The proportion of radioactivity in the new peak of all these aortas was low when compared with age-matched controls. Gas-chromatographic/mass-spectrometric analysis suggested that it contained a cyclic derivative of a hydrated aldol-condensation product. The concentration of the cross-link precursors, lysine aldehyde and aldol-condensation product (estimated from the acid-hydrolysis product 6-chloronorleucine and the acid-degradation product of reduced aldol-condensation product) was high in very young aortas but remained quite stable after childhood. No differences were observed in cross-link profiles of acid hydrolysates between pathological and control aortas. A low proportion of radioactivity in the new peak may indicate the presence of young or immature elastin in the pathological aortas.

Phase I study of twice-weekly dosing of the investigational oral proteasome inhibitor MLN9708 in patients (pts) with relapsed and/or refractory multiple myeloma (MM).

2012 ◽  
Vol 30 (15_suppl) ◽  
pp. 8017-8017 ◽  
Author(s):  
Sagar Lonial ◽  
Rachid C. Baz ◽  
Michael Wang ◽  
Moshe Talpaz ◽  
Guohui Liu ◽  
...  
Keyword(s):  
Disease Control ◽  
Dose Escalation ◽  
Proteasome Inhibitor ◽  
Clinical Investigation ◽  
Hydrolysis Product ◽  
Current Data ◽  
Biologically Active ◽  
Clinical Activity ◽  
Low Grade ◽  
Grade 3

8017 Background: MLN9708 is the first oral proteasome inhibitor to enter clinical investigation in MM. This study (NCT00932698) assessed safety, MTD, and response rate with twice-weekly oral MLN9708 in pts with relapsed and/or refractory MM, and characterized plasma pharmacokinetics (PK) and blood pharmacodynamics. Methods: Pts aged ≥18 yrs with measurable MM received MLN9708 on d 1, 4, 8, and 11 of 21-d cycles. In the dose-escalation phase, pts required ≥2 prior therapies (including bortezomib, thalidomide/lenalidomide, and corticosteroids). At the MTD (2.0 mg/m2), pts were enrolled to relapsed and refractory [RR], bortezomib-relapsed [VR], proteasome-inhibitor [PI] naïve, and carfilzomib [CZ] expansion cohorts. Results: 57 pts (53% M) were enrolled, 37 to the expansion cohorts (16 RR, 14 VR, 6 PI naïve, 1 CZ). Median age was 65 yrs (range 50-86). Median number of prior lines of therapy was 4 (range 1-28); 88%, 84%, 61%, and 5% had prior bortezomib, lenalidomide, thalidomide, and carfilzomib, respectively. Pts have received a median of 3 cycles (range 1-24) to date (data cut-off Dec 1, 2011); 7 (12%) have received ≥13 cycles. Drug-related AEs were seen in 89% of pts, including fatigue (46%), thrombocytopenia (40%), and nausea (30%); 63% had drug-related grade ≥3 AEs, including thrombocytopenia (33%), neutropenia (14%), fatigue (9%), and rash (7%). Only 6 (11%) pts had drug-related peripheral neuropathy (PN; no grade ≥3). 7 pts discontinued due to AEs. 2 pts died on study, due to PD and an unrelated cardiac disorder. Of 46 response-evaluable pts, 6 have achieved ≥PR, with 1 sCR (PI naïve cohort) and 5 PRs (2 in dose-escalation, 1 in RR, 2 in VR cohorts), and 1 VR pt has achieved MR, with duration of disease control of up to 18.6 mo. PK analyses showed MLN2238 (biologically active hydrolysis product) has linear plasma PK (0.8-2.23 mg/m2), Tmax of 0.5-1.25 hr, and terminal half-life of 4-6 d. A dose-dependent increase in whole blood 20S proteasome inhibition was observed. Conclusions: Current data suggest MLN9708 has clinical activity in heavily pretreated MM pts, with durable responses/disease control, and is generally well tolerated with infrequent low-grade PN.

4-O-METHYL-D-GLUCURONIC ACID AND 4-O-METHYL-D-GLUCOSE

1957 ◽  
Vol 35 (7) ◽  
pp. 595-598 ◽  
Author(s):  
P. A. J. Gorin
Keyword(s):  
Acid Hydrolysis ◽  
Good Yield ◽  
Glucuronic Acid ◽  
Hydrolysis Product ◽  
Novel Method

A novel method for the preparation of 4-O-methyl-D-glucuronic acid is described. This sugar and 4-O-methyl-D-glucose were obtained in good yield by two different series of reactions from 2-O-(4-O-methyl-D-glucopyranuronosido)-D-xylose, an acid hydrolysis product of the hemicellulose of Populustacamahacca Mill.

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