Category: 30165-97-0

Bodor, Nicholas published the artcileImproved delivery through biological membranes. 26. Design, synthesis, and pharmacological activity of a novel chemical delivery system for β-adrenergic blocking agents, Application In Synthesis of 30165-97-0, the publication is Journal of Medicinal Chemistry (1988), 31(1), 100-6, database is CAplus and MEDLINE.

Novel ketoxime analogs, e.g., I and II, of known β-blockers (propranolol, timolol, carteolol) were synthesized and tested as potential site-specific chem. delivery systems. It was assumed that a hydrolysis-reduction sequence could produce the active β-blockers in the iris-ciliary body. Some of these bioprecursors are remarkably active in reducing intraocular pressure in rabbits. I is more effective and a much less irritant than its parent β-blocker. While the ketoximes also displayed activity on isoprenaline-induced tachycardia after i.v. administration, they were void of activity when given orally. Propranolol was found for a prolonged time and in significant concentrations in the rabbit’s eye following topical administration of I; however, the inactive ketoximes apparently were not converted to the corresponding β-blockers in the eye. A correlation was found between the physicochem. properties of the ketoximes and their conversion to the amino alc. and thus their subsequent activity. The results suggest that at least some of the ketoxime precursors could have a use as antiglaucoma agents without systemic side effects.

Journal of Medicinal Chemistry published new progress about 30165-97-0. 30165-97-0 belongs to alcohols-buliding-blocks, auxiliary class Morpholine,Thiadiazole,Alcohol, name is 4-Morpholino-1,2,5-thiadiazol-3-ol, and the molecular formula is C6H9N3O2S, Application In Synthesis of 30165-97-0.

Referemce:
https://en.wikipedia.org/wiki/Alcohol,
Alcohols – Chemistry LibreTexts

Lacroix, Pauline M. published the artcileHPLC and NMR methods for the quantitation of the (R)-enantiomer in (-)-(S)-timolol maleate drug raw materials, Recommanded Product: 4-Morpholino-1,2,5-thiadiazol-3-ol, the publication is Chirality (1994), 6(6), 484-91, database is CAplus.

HPLC and ¹N-NMR methods for the quantitation of the (R)-enantiomer in (-)-(S)-timolol maleate were developed and validated. The HPLC method requires a 25 cm × 4.6 nm 5 μm Chiracel OD-H (cellulose tris-3,5-dimethylphenylcarbamate) column, a mobile phase of 0.2% (volume/volume) diethylamine and 4% (volume/volume) isopropanol in hexane at a flow rate of 1 mL/min and UV detection at 297 nm. A system suitability test was devised to verify the separation of the (R)- and (S)-enantiomers of timolol from other drug-related impurities. The NMR method requires the use of a high-field NMR spectrometer (> 360 MHz) and a chiral solvating agent, (-)-(R)-2,2,2-trifluoro-1-(9-anthrylethanol)(R-TFAE). The limits of quantitation were 0.5% and 0.2% (m/m) for HPLC and NMR, resp. The methods were applied to the determination of the (R)-enantiomer in eight lots of raw material. The results for the two methods were in very good agreement, with results ranging from 0.1 to 4.1% (m/m) by HPLC and none detected to 4.3% (m/m) by NMR. The USP method for sp. rotation was found to be unsuitable for detecting the presence of low levels of the (R)-enantiomer in (-)-(S)-timolol maleate.

Chirality published new progress about 30165-97-0. 30165-97-0 belongs to alcohols-buliding-blocks, auxiliary class Morpholine,Thiadiazole,Alcohol, name is 4-Morpholino-1,2,5-thiadiazol-3-ol, and the molecular formula is C6H9N3O2S, Recommanded Product: 4-Morpholino-1,2,5-thiadiazol-3-ol.

Referemce:
https://en.wikipedia.org/wiki/Alcohol,
Alcohols – Chemistry LibreTexts

Rosenbaum, Anton I. published the artcileThiadiazole Carbamates: Potent Inhibitors of Lysosomal Acid Lipase and Potential Niemann-Pick Type C Disease Therapeutics, HPLC of Formula: 30165-97-0, the publication is Journal of Medicinal Chemistry (2010), 53(14), 5281-5289, database is CAplus and MEDLINE.

Niemann-Pick type C (NPC) disease is a lysosomal storage disorder characterized at the cellular level by abnormal accumulation of cholesterol and other lipids in lysosomal storage organelles. Lysosomal acid lipase (LAL) has been recently identified as a potential therapeutic target for NPC. LAL can be specifically inhibited by a variety of 3,4-disubstituted thiadiazole carbamates. An efficient synthesis of the C(3) oxygenated/C(4) aminated analogs has been developed that furnishes the products in high yields and high degrees of purity. Common intermediates can also be used for the synthesis of the C(3) carbon substituted derivatives Herein we tested various thiadiazole carbamates, amides, esters, and ketones for inhibition of LAL. In addition, we tested a diverse selection of com. available non-thiadiazole carbamates. Our studies show that, among the compounds examined herein, only thiadiazole carbamates are effective inhibitors of LAL. We present a mechanism for LAL inhibition by these compounds whereby LAL transiently carbamoylates the enzyme similarly to previously described inhibition of acetylcholinesterase by rivastigmine and other carbamates as well as acylation of various lipases by orlistat.

Journal of Medicinal Chemistry published new progress about 30165-97-0. 30165-97-0 belongs to alcohols-buliding-blocks, auxiliary class Morpholine,Thiadiazole,Alcohol, name is 4-Morpholino-1,2,5-thiadiazol-3-ol, and the molecular formula is C6H9N3O2S, HPLC of Formula: 30165-97-0.

Referemce:
https://en.wikipedia.org/wiki/Alcohol,
Alcohols – Chemistry LibreTexts

Shehaj, Livia published the artcileSmall-Molecule Inhibitors of Haemophilus influenzae IgA1 Protease, SDS of cas: 30165-97-0, the publication is ACS Infectious Diseases (2019), 5(7), 1129-1138, database is CAplus and MEDLINE.

Newly identified, nontypable Haemophilus influenzae (H. influenza) strains represent a serious threat to global health. Due to the increasing prevalence of antibiotic resistance, virulence factors have emerged as potential therapeutic targets that would be less likely to promote resistance. IgA1 proteases are secreted virulence factors of many Gram-neg. human pathogens. These enzymes play important roles in tissue invasion as well as evasion of the immune response, yet there has been limited work on pharmacol. inhibitors. Here, we report the discovery of the first small mol., nonpeptidic inhibitors of H. influenzae IgA1 proteases. We screened over 47 000 compounds in a biochem. assay using recombinant protease and identified a hit compound with micromolar potency. Preliminary structure-activity relationships produced addnl. inhibitors, two of which showed improved inhibition and selectivity for IgA protease over other serine proteases. We further showed dose-dependent inhibition against four different IgA1 protease variants collected from clin. isolates. These data support further development of IgA protease inhibitors as potential therapeutics for antibiotic-resistant H. influenza strains. The newly discovered inhibitors also represent valuable probes for exploring the roles of these proteases in bacterial colonization, invasion, and infection of mucosal tissues.

ACS Infectious Diseases published new progress about 30165-97-0. 30165-97-0 belongs to alcohols-buliding-blocks, auxiliary class Morpholine,Thiadiazole,Alcohol, name is 4-Morpholino-1,2,5-thiadiazol-3-ol, and the molecular formula is C17H19N3O6, SDS of cas: 30165-97-0.

Referemce:
https://en.wikipedia.org/wiki/Alcohol,
Alcohols – Chemistry LibreTexts

Strunskaya, E. I. published the artcileSynthesis of aryloxy-substituted 1,2,5-thiadiazoles by the Ullmann reaction, Formula: C6H9N3O2S, the publication is Russian Journal of Organic Chemistry (Translation of Zhurnal Organicheskoi Khimii) (2001), 37(9), 1330-1334, database is CAplus.

3-Aryloxy-1,2,5-thiadiazoles were synthesized by the Ullmann reaction either from 3-chloro-1,2,5-thiadiazoles and phenols having donor substituents or from 3-hydroxy-1,2,5-thiadiazoles and chlorobenzenes containing acceptor substituents.

Russian Journal of Organic Chemistry (Translation of Zhurnal Organicheskoi Khimii) published new progress about 30165-97-0. 30165-97-0 belongs to alcohols-buliding-blocks, auxiliary class Morpholine,Thiadiazole,Alcohol, name is 4-Morpholino-1,2,5-thiadiazol-3-ol, and the molecular formula is C10H14N2O, Formula: C6H9N3O2S.

Referemce:
https://en.wikipedia.org/wiki/Alcohol,
Alcohols – Chemistry LibreTexts

Azam, Syed Sikander published the artcileInvestigation of novel chemical inhibitors of human lysosomal acid lipase: virtual screening and molecular docking studies, Safety of 4-Morpholino-1,2,5-thiadiazol-3-ol, the publication is Combinatorial Chemistry & High Throughput Screening (2014), 17(5), 473-482, database is CAplus and MEDLINE.

In the current study, identification of new potent small inhibitors of human lysosomal acid lipase using structure-based methods has been reported. Virtual Screening (VS), compounds from literature and mol. docking studies were employed to find the suitable inhibitors against lysosomal acid lipase (LAL). Specifically for this study a homol. model of LipA enzyme was generated based on the structure of dog gastric lipase. As a result of structure-based virtual screening 28 inhibitors were identified from ZINC database. Rest of the inhibitors were selected from literature. Among the studied 65 inhibitors, compound having zinc ID ZINC15707335 exhibiting min. binding affinity and hydrogen bond and hydrophobic interactions with specific amino acid residues was selected as lead compound

Combinatorial Chemistry & High Throughput Screening published new progress about 30165-97-0. 30165-97-0 belongs to alcohols-buliding-blocks, auxiliary class Morpholine,Thiadiazole,Alcohol, name is 4-Morpholino-1,2,5-thiadiazol-3-ol, and the molecular formula is C6H9N3O2S, Safety of 4-Morpholino-1,2,5-thiadiazol-3-ol.

Referemce:
https://en.wikipedia.org/wiki/Alcohol,
Alcohols – Chemistry LibreTexts