scholarly journals Design, Synthesis, Molecular Modeling, and Biological Evaluation of Novel Thiouracil Derivatives as Potential Antithyroid Agents

Molecules ◽  
2018 ◽  
Vol 23 (11) ◽  
pp. 2913 ◽  
Author(s):  
Samir Awad ◽  
Yasser Zohny ◽  
Sahar Ali ◽  
Shahenda Mahgoub ◽  
Ahmed Said
Keyword(s):  
Thyroid Hormones ◽  
Biological Evaluation ◽  
Side Chains ◽  
Design Synthesis ◽  
Serum T3 ◽  
Serum T4 ◽  
Structural Activity Relationship ◽  
Antithyroid Agents ◽  
Thiouracil Derivatives

Hyperthyroidism is the result of uncontrolled overproduction of the thyroid hormones. One of the mostly used antithyroid agents is 6-n-propyl-2-thiouracil (PTU). The previously solved X-ray crystal structure of the PTU bound to mammalian lactoperoxidase (LPO) reveals that the LPO-PTU binding site is basically a hydrophobic channel. There are two hydrophobic side chains directed towards the oxygen atom in the C-4 position of the thiouracil ring. In the current study, the structural activity relationship (SAR) was performed on the thiouracil nucleus of PTU to target these hydrophobic side chains and gain more favorable interactions and, in return, more antithyroid activity. Most of the designed compounds show superiority over PTU in reducing the mean serum T4 levels of hyperthyroid rats by 3% to 60%. In addition, the effect of these compounds on the levels of serum T3 was found to be comparable to the effect of PTU treatment. The designed compounds in this study showed a promising activity profile in reducing levels of thyroid hormones and follow up experiments will be needed to confirm the use of the designed compounds as new potential antithyroid agents.

Design, synthesis, and biological evaluation of monopyrrolinone-based HIV-1 protease inhibitors possessing augmented P2′ side chains

2006 ◽  
Vol 16 (4) ◽  
pp. 859-863 ◽  
Author(s):  
Amos B. Smith ◽  
Adam K. Charnley ◽  
Hironori Harada ◽  
Jason J. Beiger ◽  
Louis-David Cantin ◽  
...  
Keyword(s):  
Protease Inhibitors ◽  
Biological Evaluation ◽  
Side Chains ◽  
Design Synthesis ◽  
Synthesis And Biological Evaluation ◽  
Hiv 1

scholarly journals Study on Serum Levels of Thyroid Hormones and Thyroid Stimulating Hormone in Different Trimester of Normal Pregnancy

2012 ◽  
Vol 2 (2) ◽  
pp. 19-23
Author(s):  
Zinat Begum ◽  
Rezina Akhtar Banu ◽  
TH Zahra Moon Moon
Keyword(s):  
Thyroid Hormones ◽  
Pregnant Women ◽  
Serum Levels ◽  
Normal Pregnancy ◽  
Thyroid Stimulating Hormone ◽  
Control Group ◽  
Serum T3 ◽  
Serum T4 ◽  
The Mean ◽  
And Control

Objective: The present study was conducted to study the changes in serum levels of thyroid hormones and thyroid stimulating hormone (TSH) in different trimesters of normal pregnancy. Methods: This cross-sectional study was conducted in the Department of Physiology, Rangpur Medical College Hospital over a period 1 year from July 2008 to June 2009. Apparently healthy pregnant women aged between 20 - 35 years were consecutively included in the study. Patients suffering from thyroid disorders or any other systemic diseases and lactating mothers were excluded from the study. A total of 100 subjects - 75 pregnant women (25 selected from each trimester of pregnancy) and 25 non-pregnant women were purposively selected as case and control groups respectively. Result: The mean age was almost identically distributed between the two groups (23.8 ± 3.9 vs. 24.9 ±4.6, p = 0.343). Lower class patient was predominant in case and control group (68% vs. 64%, p =0.756). The mean serum T3 level was higher in case group compared to control group. The mean serum T3 level was identically distributed in 1st and 3rd trimester (p = 0.536 and p = 0.145 respectively) but significant difference was found in 2nd trimester (p = 0.001). The mean serum T4 level of control group did not experience any change throughout the whole observation period. The serum T4 level was 210 nmol/L at 1st trimester then it began to increase almost a plateau at 2nd   trimester and then gradually dropped 232.2 nmol/L at third trimester. The mean serum TSH level was 1.1 mIU/L at 1st trimester then it began to increase sharply assumed a mean score 1.3 mIU/L at 2nd trimester. From 2nd trimester onwards it began to decrease upto the end of observation when no change in the non-pregnant women in 1st, 2nd & 3rd trimester. Conclusion: Thyroid hormones (T3, T4) increase in the 2nd trimester of pregnancy and fall again in the 3rdtrimester but TSH does not experience any significant change throughout the pregnancy. Ibrahim Cardiac Med J 2012; 2(2): 19-23

scholarly journals Effect of natural neosporosis on levels of testosterone and thyroid hormones in bulls

2018 ◽  
Vol 69 (2) ◽  
pp. 984 ◽  
Author(s):  
S. BAHRAMI ◽  
A. REZA ALBORZI ◽  
S. GOORANINEJAD ◽  
O. BAKRAYI
Keyword(s):  
Thyroid Hormones ◽  
Adaptive Response ◽  
Neospora Caninum ◽  
Agglutination Test ◽  
Future Research ◽  
Hormonal Changes ◽  
Serum T3 ◽  
Serum T4 ◽  
The Difference ◽  
Pituitary Adrenal Axis

Present study was aimed to investigate the effect of Neospora caninum seropositivity on testosterone and thyroid hormones levels of Iranian bulls. Two groups containing bulls with neosporosis and bulls without neosporosis were considered. To achieve bulls with neosporosis, N. caninum agglutination test (NAT) and ELISA was performed. Testosterone, thyroxin (T4) and tri-iodothyronine (T3) levels were measured and compared between infected and non-infected bulls. Testosterone of bulls with neosporosis was decreased but the difference was not significant. Serum T4 of bulls with neosporosis was decreased significantly but changes of serum T3 was not significant. The hypothalamic–pituitary–adrenal axis (HPA axis) impairment, direct effect of N. caninum and its antigens on testis function, interrelationships between thyroid dysfunction and hypogonadism, adaptive response of infected animals to N. caninum and occurrence of oxidative stress in testis due to the presence of Neospora may be the reasons of hormonal changes. The effect of N. caninum on hormonal changes remains incomplete at present and is an area for future research so as to better characterize the effects and mechanisms.

scholarly journals Design, Synthesis, Molecular Docking and Biological Evaluation of Novel 2-[(2-{[5-(Pyridin-4-yl)-1, 3, 4-Oxadiazol-2-yl]Sulfanyl}Ethyl)Sulfanyl]-1,3-Benzoxazole

2021 ◽  
pp. 472-484
Author(s):  
Anees Fathima ◽  
H. M. Vagdevi ◽  
N. D. Jayanna ◽  
R. Mohammed Shafeeulla ◽  
. Subbaraju
Keyword(s):  
Amino Acids ◽  
Molecular Docking ◽  
Heterocyclic Ring ◽  
Docking Studies ◽  
Biological Evaluation ◽  
Present Communication ◽  
Design Synthesis ◽  
Analysis Technique ◽  
Wide Range ◽  
Structural Activity Relationship

In the present communication, a simple and facile method was adopted to synthesize  a series of novel 2-[(2-{[5-(pyridin-4-yl)-1,3,4-oxadiazol-2-yl]sulfanyl}ethyl)sulfanyl]-1,3-benzoxazole by fusing 5-(pyridin-4-yl)-1,3,4-oxadiazole-2-thiol with substituted 2-[(2-bromoethyl)sulfanyl]-1,3-benzoxazole and 2-[(2-chloroethyl)sulfanyl]-1,3-benzoxazole to obtain heterocyclic ring systems of 1,3,4 oxadiazole linked benzoxazole  moiety. The synthesized compounds were characterized by the aid of LCMS, IR, 1H NMR, 13CNMR, and C, H, N analysis technique. All the newly synthesized compounds were assessed for antimicrobial, antioxidant and antitubercular activities against standard strains. Microbiological results showed that the compounds showcased a wide range of activities and further the results of antimicrobial, antioxidant and molecular docking studies revealed that the compounds 6c, 6d and 6e are more potent and displays excellent docking scores with various amino acids interaction like alkyl-alkyl, pi-alkyl and hydrogen bonding of antitubercular receptor H37R with benzoxazole moieties and displayed encouraging antitubercular results to 6c, 6d and 6e molecules. The structural activity relationship studies illuminated the obtained results.

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