Month: February 2023

Evaluation of indole-picolinamide hybrid molecules as carbonic anhydrase-II inhibitors: Biological and computational studies was written by Zaib, Sumera;Khan, Imtiaz;Anbar, Hanan S.;Zaraei, Seyed-Omar;Sbenati, Rawan M.;Maryam, Hafiza Taha;Shah, Hamid Saeed;El-Gamal, Mohammed I.. And the article was included in Journal of Molecular Structure in 2022.Category: chlorides-buliding-blocks This article mentions the following:

The present study reported the successful synthesis and evaluation of a series of indole-picolinamide hybrids I, II [Ar = Ph, 3-CF₃C₆H₄, 3,4-di-ClC₆H₃], III, IV and V as potent inhibitors of bovine carbonic anhydrase II, a promising therapeutic target for the treatment of neurol. disorders, osteoporosis, glaucoma, cancer and obesity. Various multistep synthetic approaches were utilized to access the desired structures having exclusive sites for chem. modifications and diverse spots for biol. interactions between the ligand and enzyme. Compound I was observed as a potent inhibitor of the bovine CA-II with an IC₅₀ value of 0.0440 卤 0.009渭M. The inhibition potency was about 22-fold higher than the standard drug acetazolamide (IC₅₀ = 0.9618 卤 0.180渭M). Several relevant structure-activity relationships were deduced that enlighten the crucial role of substituents as well as the key pharmacophores involved in the inhibition process. Mol. docking tools reinforced the in vitro assay results. The most active compound I was also investigated for anticancer potential using sulforhodamine B assay and results showed two-fold efficacy against HeLa cells when compared to standard drug cisplatin (IC₅₀ = 8.045 卤 3.791渭g/mL and 4.128 卤 1.473渭g/mL, resp.). These findings were also confirmed by flow cytometry and comet tests. Moreover, fluorescence microscopy with DAPI staining revealed apoptosis as a mechanism of cancer cell death. In the experiment, the researchers used many compounds, for example, 3-(Trifluoromethyl)benzene-1-sulfonyl chloride (cas: 777-44-6Category: chlorides-buliding-blocks).

3-(Trifluoromethyl)benzene-1-sulfonyl chloride (cas: 777-44-6) belongs to organic chlorides. An organic chloride is an organic compound containing at least one covalently bonded atom of chlorine. Their wide structural variety and divergent chemical properties lead to a broad range of names and applications. Aryl chlorides may be prepared by the Friedel-Crafts halogenation, using chlorine and a Lewis acid catalyst.Category: chlorides-buliding-blocks

Referemce:
Chloride – Wikipedia,
Chlorides – an overview | ScienceDirect Topics

Synthesis and biological evaluation of novel sulfonamide derivatives of tricyclic thieno[2,3-d]pyrimidin-4(3H)-ones on melanin synthesis in murine B16 cells was written by Nie, Li Fei;Bozorov, Khurshed;Niu, Chao;Huang, Guozheng;Aisa, Haji Akber. And the article was included in Research on Chemical Intermediates in 2017.COA of Formula: C7H4ClF3O2S This article mentions the following:

A series of novel sulfonamide derivatives containing tricyclic thieno[2,3-d]pyrimidinones I (R = Ph, 4-FC₆H₄, 2-F₃CC₆H₄, 3,5-Cl₂C₆H₃, etc.) was synthesized and evaluated for melanin synthesis in murine B16 cells. All new compounds were characterized by ¹H NMR, ¹³C NMR, IR and HRMS. Among them, 6 compounds demonstrated excellent activity than pos. control (8-methoxylpsoralen, 8-MOP) with more than 1.5-fold potency. Compound I (R = 3,5-Cl₂C₆H₃) was the most potent one (658.3 卤 8.7%), exhibiting 5.0-fold stronger activity than 8-MOP (130.9 卤 8.6%). The compound I (R = 3,5-F₂C₆H₃) increased melanin synthesis in murine B16 cells with a 4.35-fold potency as compared to 8-MOP. These compounds may serve as lead compounds for further drug discoveries for the treatment of vitiligo. In the experiment, the researchers used many compounds, for example, 3-(Trifluoromethyl)benzene-1-sulfonyl chloride (cas: 777-44-6COA of Formula: C7H4ClF3O2S).

3-(Trifluoromethyl)benzene-1-sulfonyl chloride (cas: 777-44-6) belongs to organic chlorides. An organic chloride is an organic compound containing at least one covalently bonded atom of chlorine. Their wide structural variety and divergent chemical properties lead to a broad range of names and applications. Alkyl chlorides are versatile building blocks in organic chemistry. While alkyl bromides and iodides are more reactive, alkyl chlorides tend to be less expensive and more readily available.COA of Formula: C7H4ClF3O2S

Referemce:
Chloride – Wikipedia,
Chlorides – an overview | ScienceDirect Topics

Occurrence of pharmaceutical and personal care products in Cau River, Vietnam was written by Ngo, Thanh Huy;Van, Dieu-Anh;Tran, Hoai Le;Nakada, Norihide;Tanaka, Hiroaki;Huynh, Trung Hai. And the article was included in Environmental Science and Pollution Research in 2021.Safety of 1-(4-Chlorophenyl)-3-(3,4-dichlorophenyl)urea This article mentions the following:

Abstract: This study evaluated the occurrence of PPCPs in Cau River (Vietnam). Surface water and sediment samples were collected to determine PPCP concentrations The anal. results showed the presence of 36 out of 56 investigated PPCPs in samples. The total concentration of PPCPs in water samples ranged from 8.21 to 529 ng/L and the value observed in sediment was from 17.4 to 172.8 渭g/kg. Along the Cau River, there was a trend of accumulation of PPCPs at the downstream. The highest level of PPCP was observed after the river flows through Thai Nguyen and Bac Ninh provinces. Among detected PPCPs, the ones detected with high frequency (over 70%) and high concentration were caffeine, sulfamethoxazole, and lincomycin in water and triclocarban, levofloxacin, and griseofulvin in sediment. The water-sediment partition coefficient (K_d) was estimated to explore the fate of PPCP in the river, and the observed K_d mean values for lincomycin, sulfamethoxazole, and griseofulvin were 223.0, 7.6, and 997.0 kg/L, resp. Risk assessment was initially conducted by applying a semi-quant. assessment risk quotient (RQ); the potential ecol. risk to the aquatic organism of PPCPs posed a moderate risk. In the experiment, the researchers used many compounds, for example, 1-(4-Chlorophenyl)-3-(3,4-dichlorophenyl)urea (cas: 101-20-2Safety of 1-(4-Chlorophenyl)-3-(3,4-dichlorophenyl)urea).

1-(4-Chlorophenyl)-3-(3,4-dichlorophenyl)urea (cas: 101-20-2) belongs to organic chlorides. Organochlorines stimulate the central nervous system and cause convulsions, tremor, nausea, and mental confusion. Examples are dichlorodiphenyltrichloroethane (DDT), chlordane, lindane, endosulfan, and dieldrin. Alkanes and aryl alkanes may be chlorinated under free radical conditions, with UV light. However, the extent of chlorination is difficult to control.Safety of 1-(4-Chlorophenyl)-3-(3,4-dichlorophenyl)urea

Referemce:
Chloride – Wikipedia,
Chlorides – an overview | ScienceDirect Topics

Symmetrical biaryls from diazotized amines. Scope of the reaction. Unsymmetrical biaryls was written by Atkinson, Edward R.;Morgan, C. R.;Warren, H. H.;Manning, T. J.. And the article was included in Journal of the American Chemical Society in 1945.Recommanded Product: 5344-49-0 This article mentions the following:

The reducing agent was prepared by-reducing Cu₂SO₄ in NH₄OH with NH₂OH; the exptl. conditions were those reported in C.A. 35, 2879.8. The yields of R₂ and (:NR)₂ are given (%), as well as other products isolated. PhNH₂, small, 45, ROH; o-MeC₆H₄NH₂, 0, 45, ROH, RCl; m-MeC₆H₄NH₂, 0, 27, ROH; p-MeC₆H₄NH₂, 0, 50, ROH, RCl; o-O₂NC₆H₄NH₂, 45, 3, RCl (14%); m-O₂NC₆H₄NH₂, 45, 3, RCl (13%); p-O₂NC₆H₄Me (at 30-5掳), 12, small, RCl (14%); 2,6-Me(O₂N)C₆H₃NH₂, 24, 16; 2,4-isomer, 31, -; 2,4-O₂N(MeO)C₆H₃NH₂, 64, small; p-HOC₆H₄NH₂, 0, 45; p-AcNHC₆H₄NH₂, 0, 28; o-H₂NC₆H₄CO₂H, 85-90, 0, RNHR; 4,2-Cl(H₂N)C₆H₃CO₂H, 75, 0, RX, R₂O, ROH; 5-Cl isomer, 50, 0, RX, ROH; 6-Cl isomer, 80, 0; 3,5,2-Cl₂(H₂N)C₆H₂CO₂H, 50, 0, RCl, RNH₂; 3,5,2-Br₂(H₂N)C₆H₂CO₂H, 40, 0, RCl, RNH₂; 2,4-H₂N(O₂N)C₆H₃CO₂H, 61, -; 6-NO₂ isomer, 40, -, RCl; m-H₂NC₆H₄CO₂H, 0, 31, RCl; p-isomer, 0, 35; o-H₂NC₆H₄SO₃H gives 20% of (2-C₆H₄SO₃H)₂; aminonaphthalenecarboxylic acid gives high yields of R₂. A mixture of the diazo solutions from 10 g. of 3,5,2-Cl₂(H₂N)C₆H₂CO₂H and 10 g. of o-H₂NC₆H₄CO₂H gives 2 g. of 4,4′,6,6′-tetrachlorodiphenic acid and 0.5 g. of 4,6-dichlorodiphenic acid (II), m. 216-17掳. II (0.3 g.) and 2 g. concentrated H₂SO₄, heated 10 min. at 150掳 and for 2 days at 80掳, give 2,4-dichlorofluorenone-5-carboxylic acid (III), yellow, m. 240-2掳. The formation of III is a convenient method for estimating II in a mixture of diphenic acid and its tetra-Cl derivative A mixture of the diazo solutions from o-O₂NC₆H₄NH₂ and o-H₂NC₆H₄CO₂H gives the same reduction products as are obtained from their reduction sep. In the experiment, the researchers used many compounds, for example, 2-Chloro-6-nitrobenzoic acid (cas: 5344-49-0Recommanded Product: 5344-49-0).

2-Chloro-6-nitrobenzoic acid (cas: 5344-49-0) belongs to organic chlorides. Chlorinated organic compounds are found in nearly every class of biomolecules and natural products including alkaloids, terpenes, amino acids, flavonoids, steroids, and fatty acids. Aryl chlorides may be prepared by the Friedel-Crafts halogenation, using chlorine and a Lewis acid catalyst.Recommanded Product: 5344-49-0

Referemce:
Chloride – Wikipedia,
Chlorides – an overview | ScienceDirect Topics

Discovery of novel indole derivatives that inhibit NEDDylation and MAPK pathways against gastric cancer MGC803 cells was written by Fu, Dong-Jun;Cui, Xin-Xin;Zhu, Ting;Zhang, Yan-Bing;Hu, Yang-Yang;Zhang, Li-Rong;Wang, Sheng-Hui;Zhang, Sai-Yang. And the article was included in Bioorganic Chemistry in 2021.Reference of 620-19-9 This article mentions the following:

A series of novel indole derivatives were synthesized and evaluated for their antiproliferative activity against three selected cancer cell lines (MGC803, EC-109 and PC-3). Among these analogs, 2-(5-methoxy-1H-indol-1-yl)-N-(4-methoxybenzyl)-N-(3,4,5-trimethoxyphenyl)acetamide (I) showed the best inhibitory activity against MGC803 cells with an IC₅₀ value of 1.59渭M. Cellular mechanisms elucidated that I inhibited colony formation, induced apoptosis and arrested cell cycle at G2/M phase. Importantly, indole analog I inhibited NEDDylation pathway and MAPK pathway against MGC803 cells. In the experiment, the researchers used many compounds, for example, 1-(Chloromethyl)-3-methylbenzene (cas: 620-19-9Reference of 620-19-9).

1-(Chloromethyl)-3-methylbenzene (cas: 620-19-9) belongs to organic chlorides. Organic chlorides can cause corrosion in pipelines, valves and condensers, and cause catalyst poisoning. The hydrocarbon processing industry (HPI) and others are affected by damage caused by these substances. Aryl chlorides may be prepared by the Friedel-Crafts halogenation, using chlorine and a Lewis acid catalyst.Reference of 620-19-9

Referemce:
Chloride – Wikipedia,
Chlorides – an overview | ScienceDirect Topics

Synthesis and central nervous system depression properties of 3-[(1′-pyrazolyl)phenyl]sydnones was written by Havanur, Shambhuling B.;Badami, Bharati V.;Puranik, Gurubasav S.. And the article was included in Archiv der Pharmazie (Weinheim, Germany) in 1981.HPLC of Formula: 7476-66-6 This article mentions the following:

Sydnones I [R = R² (R³ = H, Me); R¹ = H, Me, Ph] were prepared by the reaction of 2-RC₆H₄NH₂ and ClCHR¹CO₂Me and subsequent nitrosation and cyclization of 2-RC₆H₄NHCHR¹CO₂H. I [R = R² (R³ = H), R¹ = H] had central nervous system depressant activity and considerable toxicity. In the experiment, the researchers used many compounds, for example, Methyl 2-chloro-2-phenylacetate (cas: 7476-66-6HPLC of Formula: 7476-66-6).

Methyl 2-chloro-2-phenylacetate (cas: 7476-66-6) belongs to organic chlorides. Chlorination modifies the physical properties of hydrocarbons in several ways. These compounds are typically denser than water due to the higher atomic weight of chlorine versus hydrogen. Alkyl chlorides readily react with amines to give substituted amines. Alkyl chlorides are substituted by softer halides such as the iodide in the Finkelstein reaction.HPLC of Formula: 7476-66-6

Referemce:
Chloride – Wikipedia,
Chlorides – an overview | ScienceDirect Topics

Synthesis and properties of 2-guanidinopurines was written by Cesnek, Michal;Masojidkova, Milena;Holy, Antonin;Solinova, Veronika;Koval, Dusan;Kasicka, Vaclav. And the article was included in Collection of Czechoslovak Chemical Communications in 2006.Recommanded Product: 203436-45-7 This article mentions the following:

2-Guanidinopurines were prepared as derivatives of 2,6-diamino-9-[2-(phosphonomethoxy)ethyl]-9H-purine (PMEDAP) (I), which shows an important antiviral activity. It completes earlier described synthesis of 6-guanidinopurine derivatives The title compounds were obtained by the reaction of the corresponding 2-chloropurines with guanidine. 2- And 6-guanidinopurines were used as model compounds for determination of dissociation constants (pK_a) of their ionogenic groups by capillary zone electrophoresis. The pK_a values of ionogenic groups of the above compounds were compared with those of the corresponding aminopurines. The pK_a of guanidino group at the purine moiety varies from 7.77 to 10.32. There is no protonation of N¹-position in contrast to aminopurines. None of these compounds showed any antiviral activity. In the experiment, the researchers used many compounds, for example, 2,6-Dichloro-9-isopropyl-9H-purine (cas: 203436-45-7Recommanded Product: 203436-45-7).

2,6-Dichloro-9-isopropyl-9H-purine (cas: 203436-45-7) belongs to organic chlorides. Organochlorines are organic compounds having multiple chlorine atoms. They were the first synthetic pesticides that were used in agriculture. They are resistant to most microbial and chemical degradations. Aliphatic organochlorides are often alkylating agents as chlorine can act as a leaving group, which can result in cellular damage.Recommanded Product: 203436-45-7

Referemce:
Chloride – Wikipedia,
Chlorides – an overview | ScienceDirect Topics

Bioengineering of CuO porous (nano)particles: role of surface amination in biological, antibacterial, and photocatalytic activity was written by Bagherzadeh, Mojtaba;Safarkhani, Moein;Ghadiri, Amir Mohammad;Kiani, Mahsa;Fatahi, Yousef;Taghavimandi, Fahimeh;Daneshgar, Hossein;Abbariki, Nikzad;Makvandi, Pooyan;Varma, Rajender S.;Rabiee, Navid. And the article was included in Scientific Reports in 2022.Formula: C16H18ClN3S This article mentions the following:

Nanotechnol. is one of the most impressive sciences in the twenty-first century. Not surprisingly, nanoparticles/nanomaterials have been widely deployed given their multifunctional attributes and ease of preparation via environmentally friendly, cost-effective, and simple methods. Although there are assorted optimized preparative methods for synthesizing the nanoparticles, the main challenge is to find a comprehensive method that has multifaceted properties. The goal of this study has been to synthesize aminated (nano)particles via the Rosmarinus officinalis leaf extract-mediated copper oxide; this modification leads to the preparation of (nano)particles with promising biol. and photocatalytic applications. The synthesized NPs have been fully characterized, and biol. activity was evaluated in antibacterial assessment against Bacillus cereus as a model Gram-pos. and Pseudomonas aeruginosa as a model Gram-neg. bacterium. The bio-synthesized copper oxide (nano)particles were screened by MTT assay by applying the HEK-293 cell line. The aminated (nano)particles have shown lower cytotoxicity (鈭?21%), higher (鈭?50%) antibacterial activity, and a considerable increase in 味 potential value (鈭?+ 13.4 mV). The prepared (nano)particles also revealed considerable photocatalytic activity compared to other studies wherein the dye degradation process attained 97.4% promising efficiency in only 80 min and just 7% degradation after 80 min under dark conditions. The biosynthesized copper oxide (CuO) (nano)particle’s biomedical investigation underscores an eco-friendly synthesis of (nano)particles, their noticeable stability in the green reaction media, and impressive biol. activity. In the experiment, the researchers used many compounds, for example, 3,7-Bis(dimethylamino)phenothiazin-5-ium chloride (cas: 61-73-4Formula: C16H18ClN3S).

3,7-Bis(dimethylamino)phenothiazin-5-ium chloride (cas: 61-73-4) belongs to organic chlorides. Organic chlorides can be used in production of: PVC, pesticides, chloromethane, teflon, insulators. Alkyl chlorides readily react with amines to give substituted amines. Alkyl chlorides are substituted by softer halides such as the iodide in the Finkelstein reaction.Formula: C16H18ClN3S

Referemce:
Chloride – Wikipedia,
Chlorides – an overview | ScienceDirect Topics

Structure-Activity Relationship Studies on Diversified Salicylamide Derivatives as Potent Inhibitors of Human Adenovirus Infection was written by Xu, Jimin;Berastegui-Cabrera, Judith;Chen, Haiying;Pachon, Jeronimo;Zhou, Jia;Sanchez-Cespedes, Javier. And the article was included in Journal of Medicinal Chemistry in 2020.Application In Synthesis of 5-Chloro-2-methoxybenzoic acid This article mentions the following:

The effective treatment of adenovirus (HAdV) infections in immunocompromised patients still poses great challenges. Herein, we reported our continued efforts to optimize a series of salicylamide derivatives as potent inhibitors of HAdV infection. Of these, nine compounds (11, 13, 14, 17, 20, 58, 60, 62, and 70) showed significantly improved anti-HAdV activities with nanomolar to submicromolar IC₅₀ values and high selectivity indexes (SI > 100), indicating better safety windows, compared to those of the lead compound niclosamide. Our mechanistic assays suggest that compounds 13, 62, and 70 exert their activities in the HAdV entry pathway, while compounds 14 and 60 likely target the HAdV DNA replication, and 11, 17, 20, and 58 inhibit later steps after DNA replication. Given the broad anti-viral activity profile of niclosamide, these derivatives may also offer therapeutic potential for other viral infections. In the experiment, the researchers used many compounds, for example, 5-Chloro-2-methoxybenzoic acid (cas: 3438-16-2Application In Synthesis of 5-Chloro-2-methoxybenzoic acid).

5-Chloro-2-methoxybenzoic acid (cas: 3438-16-2) belongs to organic chlorides. Organochlorines stimulate the central nervous system and cause convulsions, tremor, nausea, and mental confusion. Examples are dichlorodiphenyltrichloroethane (DDT), chlordane, lindane, endosulfan, and dieldrin. Organochlorine compounds are lipophylic, meaning they are more soluble in fat than in water. This gives them a high tenancy to accumulate in the food chain (biomagnification).Application In Synthesis of 5-Chloro-2-methoxybenzoic acid

Referemce:
Chloride – Wikipedia,
Chlorides – an overview | ScienceDirect Topics