Sulfur-containing pyrroles (1-3), tris(2-pyridyl)phosphine(selenide) sulfide (4-5) and 4-benzyl-6-(thiophen-2-yl)pyrimidin-2-amine (6) were synthesized and characterized by elemental analysis, IR and NMR spectra. In this study, the synthesized compounds of nitrogen, phosphorus, selenium and sulfur-containing heterocyclic compounds (1-6) were evaluated against the human erythrocyte carbonic anhydrase I, and II isoenzymes, acetylcholinesterase (AChE), butyrylcholinesterase (BChE), and α-glycosidase enzymes. The synthesized heterocyclic compounds showed IC values in range of 33.32-60.79 nM against hCA I, and 37.05-66.64 nM against hCA II closely associated with various physiological and pathological processes. On the other hand, IC values were found in range of 13.13-22.21 nM against AChE, 0.54-31.22 nM against BChE, and 13.51-26.55 nM against α-glycosidase as a hydrolytic enzyme. As a result, nitrogen, phosphorus, selenium and sulfur-containing heterocyclic compounds (1-6) demonstrated potent inhibition profiles against indicated metabolic enzymes. Therefore, we believe that these results may contribute to the development of new drugs particularly in the treatment of some global disorders including glaucoma, Alzheimer's disease and diabetes.

Download full-text PDF

Source
http://dx.doi.org/10.1016/j.bioorg.2020.104171DOI Listing

Publication Analysis

Top Keywords

heterocyclic compounds
16
nitrogen phosphorus
12
phosphorus selenium
12
selenium sulfur-containing
12
sulfur-containing heterocyclic
12
carbonic anhydrase
8
compounds 1-6
8
values range
8
compounds
5
synthesis nitrogen
4

Similar Publications

Objectives: Vomiting is frequently observed in cats after dexmedetomidine administration. This study aimed to compare the efficacy of different antiemetics in preventing vomiting in cats after dexmedetomidine administration.

Methods: Sixty-four cats were randomly allocated to receive saline solution (0.

View Article and Find Full Text PDF

Purpose: Sulfur mustard gas (SM) exposure to eyes causes multiple corneal injuries including stromal cell loss in vivo. However, mechanisms mediating stromal cell loss/death remains elusive. This study sought to test the novel hypothesis that SM-induced toxicity to human corneal stromal fibroblasts involves ferroptosis mechanism via p38 MAPK signaling.

View Article and Find Full Text PDF

Background: Chemotherapy drugs may lead to hepatic injury, which is considered one of the limitations of these drugs.

Objectives: The aim of this study was to evaluate the effect of quercetin (QUE) on M1/M2 macrophage polarization and hepatoprotective effect in cyclophosphamide (CTX)-induced liver toxicity.

Methods: Twenty-four mice were divided into four groups (Control, QUE, CTX, CTX + QUE).

View Article and Find Full Text PDF

This study aimed to compare the inhibitory effect of flunixin meglumine and meloxicam on the smooth muscles of the gastrointestinal tract in male cattle. Tissue samples, including the abomasum, ileum, proximal loop and centripetal gyri of the ascending colon, were collected from routinely slaughtered male cattle. These samples were sectioned into strips and mounted in an isolated tissue bath system.

View Article and Find Full Text PDF

Background: In African populations, estimated glomerular filtration rate by cystatin C (eGFRcys) is better aligned with gold-standard GFR measurements than eGFR by creatinine (eGFRcr). Moreover, eGFRcys is unaffected by the effects of antiretroviral therapy (ART) on tubular secretion and may thus provide better estimates of GFR in people with HIV on ART.

Setting: Observational cohort study of people of African ancestry living with suppressed HIV RNA on ART in London, United Kingdom.

View Article and Find Full Text PDF

Want AI Summaries of new PubMed Abstracts delivered to your In-box?

Enter search terms and have AI summaries delivered each week - change queries or unsubscribe any time!