N-(5-Chloro-2-meth­oxy­phen­yl)benzene­sulfonamide

In the title compound, C13H12ClNO3S, the dihedral angle between the two aromatic rings is 73.94 (9)°. An intra­molecular C—H⋯O hydrogen bond occurs. In the crystal, inter­molecular N—H⋯O hydrogen bonds connect the mol­ecules to centrosymmetric dimers, forming an R 2 2(8) ring motif. The packing is consolidated by C—H⋯O hydrogen bonds and weak π–π inter­actions [centroid–centroid distances = 3.81 (3) and 3.81 (3) Å]

Protozoidal activities of Eucalyptus cammeldulensis, Dalbergia sissoo and Acacia arabica woods and their different parts on the entozoic flagellates of Heterotermes indicola and Coptotermes heimi

Different parts of three woods of Eucalyptus cammeldulensis, Dalbergia sissoo and Acacia arabica were analyzed for their toxicity potentials against two species of termites (Heterotermis indicola and Coptotermis heimi). Termite workers were allowed to feed on 2 g complete wood powder of plant species and their parts, including; bark, sapwood and heartwood. Samples of flagellates were collected after each 24 h from the termites’ gut and they showed a significant variation in their mortality rate as per the wood species and their parts used in the experiments. After six days, mortality rates in flagellates were 100% with all wood parts of E. cammeldulensis, whereas it was 87.2, 47.61 and 100% with bark, sapwood and heartwood of D. sissoo respectively. However, in the case of A. Arabica, only bark inflicted 44.5% mortality on the flagellates in termites on the 6th day. It is revealed from the results that different woods or their specific parts have some specific toxic compounds that inflicted varying degree of toxicity on enteric flagellates of termites. Considering the toxigenic nature of different woods and their respective parts, the three woods; E. cammeldulensis, D. sissoo and A. arabica and their parts barks, sapwoods and heartwoods were analyzed for the presence of water soluble constituents such as lignin, benzene-ethanol soluble components and alpha cellulose contents. However, it is highly recommended that such protozoicidal compounds should be isolated, purified and biochemically characterized in order to apply them as commercial products for the control of pest like termites, which cause a huge damage to woody plants, and their products.Keywords: Bark, sapwood, heartwood, Eucalyptus cammeldulensis, Dalbergia sissoo, Acacia arabica, termite flagellate

Deciphering the Potential Therapeutic Intervention Points of 2019-nCoV: A Pharmacological Perspective

The emerging and re-emergence of viral outbreaks in the history of mankind has always pose severe global intimidation to public health and economy. The debilitating effects of 2019-nCoV (2019 novel coronavirus) outbreak has swiftly spread worldwide due to its highly contagious nature with severe risk of respiratory tract infections and higher mortality rate, necessitating the urgent need for the production of effective vaccine and potential therapeutic agents. The active evolution of SARS-CoV-2 strain in different population and environment strive immense challenge against anti-viral therapeutic development based on viral pathogenicity. The potential FDA drugs are evaluated based on their known safety and efficacy with exceptional pharmacokinetic profiles for the treatment of nCoV-2019. Existing knowledge related to MERS-CoV and SARS-CoV epidemic has provided a better understanding to explore purposeful therapeutics strategies against novel coronavirus disease (COVID-19). To limited extend, the ongoing promising and hopeful treatments includes convalescent plasma therapy, remdesivir, lopinavir/ritonavir, ACE inhibitors, TMPRSS2 inhibitors, hydroxychloroquine, interferon, ribavirin, tocilizumab, and corticosteroids however clinical efficacy of some of them need to be validated in randomized clinical trials (RCTs). The global struggle to make a protected and successful Coronavirus immunization is finally proving to be fruitful. Although challenges such as strain variation resistant, possible side effects, adequate supply of vaccines to all countries and limited availability of second dose still diverting the option of possible efficacious therapeutics strategies to work alongside with vaccine development with improved efficacy and safety profile. This review is focused on the potential advancement in therapeutic approaches with possible repurposing of the available drugs and explores the current status of available vaccines with hope that these strategies found to be cogent in controlling SARS-CoV-2 outbreak.Keywords: Coronavirus disease 2019 (COVID-19); Remdesivir; Therapeutics; Plasma therapy; Hydroxychloroquine; Anti-viral; Angiotensin-converting enzyme 2; Type II transmembrane serine protease    

Phytochemical screening, free radical scavenging, antioxidant activity and phenolic content of Dodonaea viscosa

The purpose of this study was to evaluate the antioxidant potential of Dodonaea viscosa Jacq. Methanolic extract of the plant was dissolved in distilled water and partitioned with n-hexane, chloroform, ethyl acetate and nbutanol sequentially. Phytochemical screening showed presence of phenolics, flavonoides and cardiac glycosides in large amount in chloroform, ethyl acetate and n-butanol fraction. The antioxidant potential of all these fractions and remaining aqueous fraction was evaluated by four methods: 1,1-Diphenyl-2-picrylhydrazyl (DPPH) free radical scavenging activity, total antioxidant activity, Ferric Reducing Antioxidant Power (FRAP) assay and ferric thiocyanate assay along with determination of their total phenolics. The results revealed that ethyl acetate soluble fraction exhibited highest percent inhibition of DPPH radical as compared to other fractions. It showed 81.14 ± 1.38% inhibition of DPPH radical at a concentration of 60 μg/ml. The IC50 of this fraction was found to be 33.95 ± 0.58 μg/ml, relative to butylated hydroxytoluene (BHT), having IC50 of 12.54 ± 0.89 μg/mL. It also showed highest FRAP value (380.53 ± 0.74 μM of trolox equivalents) as well as highest total phenolic contents (208.58 ± 1.83 GAE μg/g) and highest value of inhibition of lipid peroxidation (58.11 ± 1.49% at concentration of 500 μg/ml) as compared to the other studied fractions. The chloroform fraction showed highest total antioxidant activity i.e.1.078 ± 0.59 (eq. to BHT)

N-Benzyl-N-(2-meth­oxy­phen­yl)benzene­sulfonamide

In the title mol­ecule, C20H19NO3S, the dihedral angle between the phenyl rings is 48.93 (18)°, and they make dihedral angles of 38.37 (17) and 86.50 (19)° with the benzene ring. A weak intra­molecular C—H⋯O inter­action might stabilize the mol­ecular conformation. In the crystal, weak π–π stacking inter­actions between the benzene rings [centroid–centroid distance = 3.774 (2) Å] may help to establish the packing

Preliminary structure-activity relationship studies on some novel s-substituted aliphatic analogues of 5-{1-[(4- chlorophenyl) sulfonyl]-3-piperidinyl}-1, 3, 4-oxadiazol-2-yl sulfide

Purpose: To study the structure-activity relationships of synthetic multifunctional sulfides through evaluation of lipoxygenase and anti-bacterial activities.Methods: S-substituted derivatives of the parent compound 5-(1-(4- chlorophenylsulfonyl) piperidin-3- yl)-1, 3, 4-oxadiazole-2-thiol were synthesized through reaction with different saturated and unsaturated alkyl halides in DMF medium, with NaH catalyst. Spectral characterization of each derivative was carried out with respect to IR, 1H - NMR, 13C - NMR and EI - MS. The lipoxygenase inhibitory and antibacterial activities of the derivatives were determined using standard procedures.Results: Compound 5e exhibited higher lipoxygenase inhibitory potential than the standard (Baicalein®), with % inhibition of 94.71 ± 0.45 and IC50 of 20.72 ± 0.34 μmoles/L. Compound 5b showed significant antibacterial potential against all the bacterial strains with % inhibition ranging from 62.04 ± 2.78, 69.49 ± 0.41, 63.38 ± 1.97 and 59.70 ± 3.70 to 78.32 ± 0.41, while MIC ranged from 8.18 ± 2.00, 10.60 ± 1.83, 10.84 ± 3.00, 9.81 ± 1.86 and 11.73 ± 5.00 μmoles/L for S. typhi, E. coli, P. aeruginosa, B. subtilis and S. aureus, respectively. Compounds 5d, 5e and 5g showed good antibacterial activity against S. typhi and B. subtilis bacterial strains.Conclusion: The results suggest that compound 5e bearing n-pentyl group is a potent lipoxygenase inhibitor, while compound 5b with n-propyl substitution is a strong antibacterial agent. In addition, compounds 5d, 5e and 5g bearing n-butyl, n-pentyl and n-octyl groups, respectively, are good antibacterial agents against S. typhi and B. subtilis.Keywords: Sulfides, Antibacterial activity, Lipoxygenase activity, Spectral analysi

N-(2-Hy­droxy-1,1-dimethyl­eth­yl)­benzene­sulfonamide

In the title mol­ecule, C10H15NO3S, the S atom is bonded in a distorted tetra­hedral geometry. In the crystal structure, inter­molecular N—H⋯O, O—H⋯O and weak C—H⋯O hydrogen bonds connect the mol­ecules to form a two-dimensional network parallel to (100). The 2-methyl­propan-1-ol group is disordered over two orientations with occupancies of 0.570 (3) and 0.430 (3)

N-(2-Hy­droxy-1,1-dimethyl­eth­yl)-4-methyl­benzene­sulfonamide

In the title mol­ecule, C11H17NO3S, the S atom has a distorted tetra­hedral geometry [maximum deviation: O—S—O = 119.08 (9)°]. In the crystal, mol­ecules are connected by inter­molecular N—H⋯O, O—H⋯O and C—H⋯O hydrogen bonds, forming layers of mol­ecules aligned parallel to (110). The 2-methyl­propan-1-ol group of the mol­ecule is disordered over two positions with an 0.592 (4):0.408 (4) occupancy ratio

Synthesis, spectral analysis and pharmacological study of N'- substituted-2-(5-((2,4-dimethylphenoxy)methyl)-1,3,4-oxadiazol-2-ylthio)acetohydrazides

A series of molecules bearing multiple functional groups were synthesized to study their antibiotic effect against Gram-positive and Gram-negative bacteria and lipoxygenase activity as well. 2,4-Dimethylcarbolic acid (1) was refluxed with ethyl 2-bromoacetate to synthesize ethyl 2-(2,4-dimethylphenoxy)acetate (2). Compound 2 was converted to the corresponding hydrazide 3, again on refluxing with hydrazine. The compound 5-((2,4-dimethylphenoxy)methyl)-1,3,4-oxadiazol-2-thiol (4) was synthesized by the reaction of 3 and CS2 in the presence of KOH. Compound 4 was further converted to the corresponding ester 5 and then 2-(5-((2,4-dimethylphenoxy)methyl)-1,3,4-oxadiazol-2-ylthio)acetohydrazide (6). The final molecules N'-substituted-2-(5-((2,4-dimethylphenoxy)methyl)-1,3,4-oxadiazol-2-ylthio)acetohydrazide, 8a-m, bearing ether, 1,3,4-oxadiazole, thioether, hydrazone and azomethine functional groups were synthesized by stirring the aryl carboxaldehydes 7a-m with 6 in methanol at room temperature. The depicted structures of all synthesized molecules were corroborated by IR, 1H-NMR and EIMS spectral data analysis. 8m and 8i showed substantial antibacterial activity and lipoxygenase inhibitory activity, respectively

Synthesis, Structural Analysis and Screening of Some Novel 5-Substituted Aryl/Aralkyl-1,3,4-Oxadiazol-2-Yl 4-(Morpholin-4-Ylsulfonyl)Benzyl Sulfides as Potential Antibacterial Agents

A series of new 5-substituted aryl/aralkyl-1,3,4-oxadiazol-2-yl 4-(morpholin-4-ylsulfonyl)benzyl sulfides 6a-k were synthesized by converting multifarious aryl/aralkyl organic acids 1a-k successively into corresponding esters 2a-k, hydrazides 3a-k and 5-substituted aryl/aralkyl-1,3,4-oxadiazole-2-thiols 4a-k. Finally, the target compounds, 6a-k were prepared by stirring 5-substituted-1,3,4-oxadiazole-2-thiols with 4-(4-(bromomethyl)phenylsulfonyl) morpholine (5) in the presence of N,N-dimethylformamide (DMF) and sodium hydride (NaH). The structures of the newly synthesized compounds were elucidated by spectroscopic techniques. In addition, the anti-bacterial activity of all the synthesized compounds was investigated in vitro against Gram-positive and Gram-negative bacteria by using ciprofloxacin as reference standard drug and the results showed that some of the tested compounds possessed good anti-bacterial activity