Cellulose Ester-Based Aerogel: Lightweight and Highly Water-Absorbent.

Cellulose was extracted from waste generated by pruning tea stem wastes. The interaction between pure cellulose and homophthalic acid produced a light (0.22 g·cm-3) and eco-friendly hybrid aerogel product that is highly absorbent (85 g of water per 1 g of aerogel). The product has a Brunauer-Emmett-Teller surface area of 221 m2·g-1. In addition, the product was analyzed for its structural and functional properties using scanning electron microscopy, Fourier transform infrared, and X-ray diffraction. The methodology employed in this study is uncomplicated, utilizing easily accessible and sustainable biowaste at a low cost. As a result, the current process is well-adapted for industrial-scale production, with the potential for significant advancements in the field of green materials.

Inhibition Profiles of Some Symmetric Sulfamides Derived from Phenethylamines on Human Carbonic Anhydrase I, and II Isoenzymes.

In this work, the inhibitory effect of some symmetric sulfamides derived from phenethylamines were determined against human carbonic anhydrase (hCA) I, and II isoenzymes, and compared with standard compound acetazolamide. IC50 values were obtained from the Enzyme activity (%)-[Symmetric sulfamides] graphs. Also, Ki values were calculated from the Lineweaver-Burk graphs. Some symmetric sulfamides compounds (11-18) demonstrated excellent inhibition effects against hCA I, and II isoenzymes. These compounds demonstrated effective inhibitory profiles with IC50 values in ranging from 21.66-28.88 nM against hCA I, 14.44-30.13 nM against hCA II. Among these compounds, the best Ki value for hCA I (Ki : 8.34±1.60 nM) and hCA II (Ki : 16.40±1.00 nM) is compound number 11. Besides, the IC50 value of acetazolamide used as a standard was determined as hCA I, hCA II 57.75 nM, 49.50 nM, respectively. Moreover, in silico ADME-Tox study showed that all synthesized compounds (11-18) had good oral bioavailability in light of Jorgensen's rule of three, and of Lipinski's rule of five.

Concise syntheses and some biological activities of dl-2,5-di-O-methyl-chiro-inositol, dl-1,4-di-O-methyl-scyllo-inositol, and dl-1,6-dibromo-1,6-dideoxy-2,5-di-O-methyl-chiro-inositol.

The regio- and stereospecific synthesis of O-methyl-chiro-inositols and O-methyl-scyllo-inositol was achieved, starting from p-benzoquinone. After preparing dimethoxy conduritol-B as a key compound, regiospecific bromination of the alkene moiety of dimethoxy conduritol-B and acid-catalyzed ring opening of dimethoxydiacetate conduritol-B epoxide with Ac2 O afforded the desired new chiro-inositol derivatives and scyllo-inositol derivative, respectively. Spectroscopic methods were employed for the characterization of all synthesized compounds. The novel inositols (11-17) had effective inhibition profiles against human carbonic anhydrase isoenzymes I and II (hCA I and II) and acetylcholinesterase (AChE). The novel inositols 11-17 were found to be effective inhibitors against AChE, hCA I, and hCA II enzymes. Ki values were calculated in the range of 87.59 ± 7.011 to 237.95 ± 17.75 µM for hCA I, 65.08 ± 12.39 to 538.98 ± 61.26 µM for hCA II, and 193.28 ± 43.13 to 765.08 ± 209.77 µM for AChE, respectively. Also, due to the inhibitory effects of the novel inositols 11-17 against the tested enzymes, these novel inositols are potential drug candidates to treat some diseases such as glaucoma, epilepsy, leukemia, and Alzheimer's disease.

Synthesis of novel sulfamides incorporating phenethylamines and determination of their inhibition profiles against some metabolic enzymes.

A series of sulfamides were synthesized and evaluated for their acetylcholinesterase (AChE), butyrylcholinesterase (BChE), and carbonic anhydrase inhibition properties. The synthesis of sulfamides was achieved by the reactions of phenethylamines with N,N-dimethylsulfamoyl chloride in the presence of Et3 N. The methoxylated sulfamides were converted into their phenolic derivatives with BBr3 for structure-activity relationships. The synthesized sulfamide/phenolic sulfamide derivatives were investigated as cholinesterase inhibitors and their relative role in AChE versus BChE inhibition was defined. Sulfamide/phenolic sulfamide derivatives are known as important carbonic anhydrase inhibitors; therefore, the synthesized compounds were investigated for inhibitory effects on both carbonic anhydrase isoenzymes. Additionally, we evaluated four different enzymes, which were inhibited in the low nanomolar range by these compounds. According to the present studies, for AChE, BChE, and carbonic anhydrase I and II, the ranges of results are recorded as 0.027-0.076 nM, 0.075-0.327 nM, 0.123-0.678 nM, and 0.024-0.688 nM, respectively.

Cancer Frequency in Retrosternal Goiter.

Retrosternal goiter prevalence is 5 to 40 per cent according to classifications in goiter series. Goiters with mediastinal extension were reported to be related with higher cancer rates. In our study, we aimed to investigate whether cancer incidence increased in retrosternal goiters compared with the cervical ones. Three hundred and ninety consecutive patients, who had surgery because of retrosternal goiter in Istanbul University Medical Faculty Department of General Surgery between 2005 and 2015 were included in the study (Group 1). Control group included 880 patients who had surgery because of nontoxic multinodular goiter in the same period (Group 2). Preoperative ultrasonography (USG) was performed to each patient. Fine-needle aspiration biopsy was performed in suspicious nodules and results were recorded. Carcinomas in histopathological examination were classified as intrathorasic and extrathorasic. Diagnostic rates of USG results were compared with histopathologic cancer results. Papillary carcinoma was diagnosed in 76 patients with retrosternal goiter (19%) and in 200 patients in the control group (22%). No statistically significant difference was detected between groups regarding the tumor rates (P > 0.05). One hundred and forty-four tumoral foci were detected in 76 patients with papillary carcinoma in retrosternal goiter patients. Three hundred and seventy tumoral foci were detected in 200 patients with papillary carcinoma in the control group. In the retrosternal goiter group, 104 carcinoma lesions of 144 papillary carcinomas were intrathorasic (72%). No statistically significant difference was detected between intrathorasic (2.1 ± 1 cm) and extrathorasic regiones (1.9 ± 0.8 cm) regarding the tumor size P > 0.05. When patients with and without cancer in the retrosternal goiter group were compared regarding familial thyroid cancer history, radiation to the neck, and cervical adenopathy, no statistically significant difference was detected. Cancer incidence of retrosternal goiters was not higher than that of the cervical ones. Yet, cancer foci of retrosternal goiters were commonly located in the intrathorasic area and were not detected with USG. Depending on these findings, we suggest that all retrosternal goiters should be surgically treated.

Antioxidant Activity, Acetylcholinesterase, and Carbonic Anhydrase Inhibitory Properties of Novel Ureas Derived from Phenethylamines.

A series of ureas derived from phenethylamines were synthesized and evaluated for human carbonic anhydrase (hCA) I and II, acetylcholinesterase (AChE), and butyrylcholinesterase (BChE) enzyme inhibitory activities and antioxidant properties. The ureas were synthesized from the reactions of substituted phenethylamines with N,N-dimethylcarbamoyl chloride; then, the synthesized compounds were converted to their corresponding phenolic derivatives via O-demethylation. hCA I and II were effectively inhibited by the newly synthesized compounds, with Ki values in the range of 0.307-0.432 nM for hCA I and 0.149-0.278 nM for hCA II. On the other hand, the Ki parameters of these compounds for AChE and BChE were determined in the range of 0.129-0.434 and 0.095-0.207 nM, respectively. Phenolic ureas also showed good antioxidant activities.

Acetylcholinesterase inhibitory and antioxidant activities of novel symmetric sulfamides derived from phenethylamines.

The antioxidant and acetylcholinesterase inhibitory properties of novel symmetric sulfamides derived from phenethylamines were evaluated. Phenethylamines 8-11 were reacted with SO2Cl2 in the presence of Et3N to afford sulfamides in good yields. The synthesized sulfamides were converted to their phenolic derivatives with BBr3. We elucidated the antioxidant activity of novel symmetric sulfamides by using different bioanalytical assays. For this purpose, the radical scavenging activities of the novel symmetric sulfamides were assessed by DPPH(•), ABTS(•+), DMPD(•+), and O2(•-) radical scavenging tests. In addition, the reducing abilities of the novel symmetric sulfamides were evaluated by Fe(3+)-Fe(2+) reducing, Cu(2+)-Cu(+) reducing, and [Fe(3+)-(TPTZ)2](3+)-[Fe(2+)-(TPTZ)2](2+) reducing activity tests. Also, the Fe(2+) chelating activity by the pipyrdyl reagent and the acetylcholinesterase inhibitory activities of the novel symmetric sulfamides were studied. Especially, the novel phenolic and symmetric sulfamides 16-19 showed high antioxidant and acetylcholinesterase inhibitory properties. On the other hand, IC50 values were calculated for the DPPH(•), ABTS(•+), DMPD(•+), and O2(•-) scavenging, the metal chelating, and the acetylcholinesterase inhibition effects of the novel symmetric sulfamides.

Synthesis and carbonic anhydrase inhibitory properties of sulfamides structurally related to dopamine.

A series of novel sulfamides incorporating the dopamine scaffold were synthesized. Reaction of amines and tert-butyl-alcohol/benzyl alcohol in the presence of chlorosulfonyl isocyanate (CSI) afforded sulfamoyl carbamates, which were converted to the title compounds by treatment with trifluoroacetic acid or by palladium-catalyzed hydrogenolysis. Inhibition of six α-carbonic anhydrases (CAs, EC 4.2.1.1), that is, CA I, CA II, CA VA, CA IX, CA XII and CA XIV, and two ß-CAs from Candida glabrata (CgCA) and Mycobacterium tuberculosis (Rv3588) with these sulfamides was investigated. All CA isozymes were inhibited in the low micromolar to nanomolar range by the dopamine sulfamide analogues. K(i)s were in the range of 0.061-1.822 µM for CA I, 1.47-2.94 nM for CA II, 2.25-3.34 µM for CA VA, 0.041-0.37 µM for CA IX, 0.021-1.52 µM for CA XII, 0.007-0.219 µM for CA XIV, 0.35-5.31 µM for CgCA and 0.465-4.29 µM for Rv3588. The synthesized sulfamides may lead to inhibitors targeting medicinally relevant CA isoforms with potential applications as antiepileptic, antiobesity antitumor agents or anti-infective.