927-92-4

Upstream product

• 629-06-1 1-Chloroheptane 
• 142-82-5 n-heptane 
• 7782-50-5 chlorine 
• 22767-50-6 sodium heptanesulfonate 
• 60586-80-3 heptane-1-sulfonic acid 
• 10026-13-8 phosphorus pentachloride 
• 629-04-9 1-Bromoheptane 
• 1639-09-4 heptanethiol 

Downstream Products

• 57603-96-0 heptane-1-sulfonamide 
• 335-71-7 perfluoroheptane sulfonylfluoride 
• 100337-54-0 Aethyl-4-heptansulfonamidobenzoat 
• 88413-12-1 N-<3-(methylamino)-4-nitrophenyl>heptanesulfonamide 
• 88412-83-3 Heptane-1-sulfonic acid [4-(acridin-9-ylamino)-3-methylamino-phenyl]-amide 
• 97213-15-5 (4-Heptansulfonamidobenzoyl)hydrazin 

Relevant academic research and scientific papers

Efficient Synthesis of Benzothiazinone Analogues with Activity against Intracellular Mycobacterium tuberculosis

8-Nitrobenzothiazinones (BTZs) are a promising class of antimycobacterial agents currently under investigation in clinical trials. Starting from thiourea derivatives, a new synthetic pathway to BTZs was established. It allows the formation of the thiazinone ring system in one synthetic step and is applicable for preparation of a wide variety of BTZ analogues. The synthetic procedure furthermore facilitates the replacement of the sulphur atom in the thiazinone ring system by oxygen or nitrogen to afford the analogous benzoxazinone and quinazolinone systems. 36 BTZ analogues were prepared and tested in luminescence-based assays for in vitro activity against Mycobacterium tuberculosis (Mtb) using the microdilution broth method and a high-throughput macrophage infection assay.

Beyond Basicity: Discovery of Nonbasic DENV-2 Protease Inhibitors with Potent Activity in Cell Culture

The viral serine protease NS2B-NS3 is one of the promising targets for drug discovery against dengue virus and other flaviviruses. The molecular recognition preferences of the protease favor basic, positively charged moieties as substrates and inhibitors, which leads to pharmacokinetic liabilities and off-target interactions with host proteases such as thrombin. We here present the results of efforts that were aimed specifically at the discovery and development of noncharged, small-molecular inhibitors of the flaviviral proteases. A key factor in the discovery of these compounds was a cellular reporter gene assay for the dengue protease, the DENV2proHeLa system. Extensive structure-activity relationship explorations resulted in novel benzamide derivatives with submicromolar activities in viral replication assays (EC50 0.24 μM), selectivity against off-target proteases, and negligible cytotoxicity. This structural class has increased drug-likeness compared to most of the previously published active-site-directed flaviviral protease inhibitors and includes promising candidates for further preclinical development.

Sulfonyl halide synthesis by thiol oxyhalogenation using NBS/NCS – iPrOH

A rapid and facile method provides a general route to sulfonyl bromides/chlorides by the oxidation of thiols using NXS – ROH (X?=?Br,Cl, R?=?iPr) as an oxyhalogenation reagent. Control experiments suggest that the alcohol component is the source of oxygen. The proposed method enable the access to structurally diverse sulfonyl bromides and chlorides including challenging examples, inaccessible by other synthetic methods.

Synthesis and evaluation of 5-substituted 2′-deoxyuridine monophosphate analogues as inhibitors of flavin-dependent thymidylate synthase in mycobacterium tuberculosis

A series of 5-substituted 2′-deoxyuridine monophosphate analogues has been synthesized and evaluated as potential inhibitors of mycobacterial ThyX, a novel flavin-dependent thymidylate synthase in Mycobacterium tuberculosis. A systematic SAR study led to the identification of compound 5a, displaying an IC50 value against mycobacterial ThyX of 0.91 μM. This derivative lacks activity against the classical mycobacterial thymidylate synthase ThyA (IC50 > 50 μM) and represents the first example of a selective mycobacterial FDTS inhibitor.

N-Sulfonyl homoserine lactones as antagonists of bacterial quorum sensing

A series of 11 N-sulfonyl homoserine lactones has been synthesised. Some of them were found to competitively inhibit the action of 3-oxohexanoyl-L- homoserine lactone, the natural inducer of bioluminescence in the bacterium Vibrio fischeri. Molecular modeling suggests a possible explanation based on the prevention of structural rearrangements necessary for the formation of the active dimer of LuxR.

Novel 4-phenylpiperidines for the treatment of pruritic dermatoses

Novel compounds having general formula (I), and pharmaceutically and veterinarily acceptable salts thereof wherein R 1, R 2, R 3, W, Y 1, Y 2, X, n and y are as defined above and processes for their preparation and intermediate compounds prepared therein. The novel compounds are useful for having utility in the treatment. of pruritic dermatoses including allergic dermatitis and atopy in animals and humans

COMPOUNDS AND METHODS FOR CONTROLLING BACTERIAL VIRULENCE

Novel sulfonated homoserine lactones formula I have been found to act ac quorum sensing inhibitors. As such, they may be useful in the treatment of bacterial infections.

THE PHOTOCHEMICAL CHLOROSULFONATION OF HEPTANE BY SULFURYL CHLORIDE. THE ROLE OF SOLVENT AND CATALYST. A REINVESTIGATION.

Sulfuryl chloride has been tested as a chlorosulfonation reagent of n-heptane under various conditions.Pyridine was confirmed as the best catalyst for the reaction and the sulfochlorination yield was found to be enhanced by the use of benzene as solvent.The distribution of all the isomeric chlorinated and sulfochlorinated products has been measured.This information is used in order to understand the mechanism of this rather complex reaction.The catalyzed photoinitiation leads to the in situ formation of a low concentration of molecular chlorine.The observed selectivity is the result of a delicate balance between the photoinitiation leading the chlorine atoms and the rather short chain propagations leading to the formation of the chlorosulfonyl radical.

Cobalt(II)-Porphyrin Catalyzed Selective Functionalization of Alkanes with sulfurylchloride: A Remarkable Substituent Effect

Cobalt(II)-porphyrin complex 1 and 2 catalyses the chlorination and sulfochlorination respectively of n-alkanes and cycloalkanes with sulfuryl chloride in benzene.The p-substituent of the benzene ring in the porphyrin complex 1 and 2 shows a remarkable chemoselectivity in these reactions.