Delving into the Latest Updates on Cocarboxylase with Synapse

Overview

Basic Info

Drug Type

Small molecule drug

Synonyms

Cocarboxylase (JAN/INN), Thiamine diphosphate, Thiamine pyrophosphate

+ [3]

Target-

Action-

Mechanism-

Therapeutic Areas

Endocrinology and Metabolic Disease

Active Indication

Thiamine Deficiency

Inactive Indication-

Originator Organization-

Active Organization-

Inactive Organization-

Drug Highest PhaseApproved

First Approval Date-

Regulation-

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Structure/Sequence

Molecular FormulaC12H19N4O7P2S

InChIKeyAYEKOFBPNLCAJY-UHFFFAOYSA-O

CAS Registry136-08-3

AbstractNitrogenous heterocyclic rings are present in a wide range of drugs, natural compounds, and fine chemicals and are considered privileged scaffolds in medicinal chemistry. Seeking novel anti‐protozoal drugs acting on new targets or by novel mechanisms of action, we focused on a preliminary evaluation of the potential of “linear‐shaped” diaryl pyrazines. To this purpose, a two‐enzyme chemoenzymatic synthesis of this heteroaromatic core was carried out. Specifically, starting from simple, commercially available aromatic aldehydes, the target pyrazines were obtained through a sequence of biocatalytic benzoin condensation, chemical oxidation and a transaminase‐mediated tandem process of transamination and cyclization. The profiles of the compounds as antiprotozoal agents were evaluated in vitro against parasites cultures of the Leishmania and Plasmodium genera and using the human cell line HepG2.

18 May 2024·International Journal of Ophthalmology

Lacidipine, thiamine pyrophosphate and their combination on the ocular ischemic syndrome induced by bilateral common carotid artery ligation

Article

Author: Suleyman, Bahadir ; Bulut, Seval ; Coban, Taha Abdulkadir ; Mammadov, Renad ; Altuner, Durdu ; Bal Tastan, Tugba ; Somuncu, Ahmet Mehmet ; Suleyman, Halis ; Cicek, Ibrahim

AIM: To investigate the effect of lacidipine, thiamine pyrophosphate (TPP) and the combination of lacidipine and TPP against oxidative and inflammatory eye damage induced by bilateral common carotid artery ligation in rats. METHODS: Male albino Wistar rats were categorized as those who underwent sham surgery (SG), right and left common carotid cross-clamping and unclamping procedure (CCU), lacidipine+CCU (LCCU), TPP+CCU (TCCU), and combination of lacidipine and TPP (LTC)+CCU (LTCCU). One hour before anesthesia, the LCCU (n=6) received lacidipine (4 mg/kg, orally) and the TCCU (n=6) received TPP (20 mg/kg, intraperitoneally). The SG (n=6) and CCU (n=6) received the same volume of distilled water from the same route. After anesthesia (60 mg/kg ketamine, intraperitoneally), the necks of the rats were opened in the midline. Ischemia was created for 10min by placing clips on the right and left common carotid arteries. Rats in the SG only underwent subcutaneous incision. After 10min, the clips were removed and reperfusion was achieved for six days. Then, the animals were euthanized (120 mg/kg ketamine, intraperitoneally) and the levels of oxidant, antioxidant and proinflammatory cytokines in the eye tissues were determined. The retinal tissue of the eye was also examined histopathologically. RESULTS: Lacidipine, TPP, and LTC significantly prevent the increase in malondialdehyde, tumor necrosis factor-alpha, interleukin-1β (IL-1β), and IL-6 levels, decrease in total glutathione levels, superoxide dismutase and catalase activities and histopathological retinal damage in eye tissue induced by bilateral common carotid artery ligation in rats. The impact of these drugs on protection is determined to be LTC>lacidipine>TPP. CONCLUSION: As a result of the study, it is concluded that LTC may be more effective than lacidipine and TPP alone in treating ocular ischemic syndrome.

09 May 2024·The Journal of Physical Chemistry B

Riboswitch Distribution in the Human Gut Microbiome Reveals Common Metabolite Pathways

Article

Author: Quarta, Giulio ; Schlick, Tamar

Riboswitches are widely distributed, conserved RNAs which regulate metabolite levels in bacterial cells through direct, noncovalent binding of their cognate metabolite. Various riboswitch families are highly enriched in gut bacteria, suggestive of a symbiotic relationship between the host and bacteria. Previous studies of the distribution of riboswitches have examined bacterial taxa broadly. Thus, the distribution of riboswitches associated with bacteria inhabiting the intestines of healthy individuals is not well understood. To address these questions, we survey the gut microbiome for riboswitches by including an international database of prokaryotic genomes from the gut samples. Using Infernal, a program that uses RNA-specific sequence and structural features, we survey this data set using existing riboswitch models. We identify 22 classes of riboswitches with vitamin cofactors making up the majority of riboswitch-associated pathways. Our finding is reproducible in other representative databases from the oral as well as the marine microbiomes, underscoring the importance of thiamine pyrophosphate, cobalamin, and flavin mononucleotide in gene regulation. Interestingly, riboswitches do not vary significantly across microbiome representatives from around the world despite major taxonomic differences; this suggests an underlying conservation. Further studies elucidating the role of bacterial riboswitches in the host metabolome are needed to illuminate the consequences of our finding.

100 Deals associated with Cocarboxylase

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External Link

KEGG	Wiki	ATC	Drug Bank
D01225	Cocarboxylase	A11DA	DB01987

R&D Status

10 top approved records.

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Indication	Country/Location	Organization	Date
Thiamine Deficiency	-	-	-

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Clinical Result

Indication

Phase

Evaluation

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Study	Phase	Population	Analyzed Enrollment	Group	Results	Evaluation	Publication Date


NCT03509350 (VICTAS, CTgov)	Phase 3	Sepsis	501	Vitamin C+Thiamine+Hydrocortisone (Treatment Protocol)	imdocqaomt(kvsphnpjvs) = gjtrlatnwt iwoukqpfnj (elneejtpwd, glohbulwty - oextfcrgjz) View more	-	18 Sep 2020
				Vitamin C Placebo (Control Protocol)	imdocqaomt(kvsphnpjvs) = jtyqbsdyuh iwoukqpfnj (elneejtpwd, mmuiqxcttl - sdprtxhztj) View more
NCT01985685 (TVO2_RCT, CTgov)	Phase 2	Respiratory Failure \| Critical Illness	66	Thiamine (Thiamine)	wbbmgscgel(pxmcaagfcl) = yvqjnmrphj oicrgibrjz (dykhoxwplg, vxclsnnrbl - netcbhgovz) View more	-	02 Oct 2017
				Thiamine (Placebo)	wbbmgscgel(pxmcaagfcl) = lwnjztprgi oicrgibrjz (dykhoxwplg, wxenkvqpvl - knvtsrwjua) View more