Antimalarial agents. 8. Ring-substituted bis(4-aminophenyl) sulfones and their precursors

Abstract

Ka of 0.01 and * of 0.10, Et and Me derivatives should have similar optimum partition coefficients.The data in this report substantiate this observation.This study demonstrates the usefulness of the extrathermodynamic approach in understanding structureactivity relationships. Thus, the antibacterial activities of leucomycins, as well as lincomycin and clindamycin analogs depend on their relative hydrophobic Popoff, el al.properties. Through use of dummy variables, steric effects could be examined in the lincomycin series. Finally, a comparison of the optimum value for one subseries with that of another subseries results in the indication of an electronic effect. In the case of the leucomycin series the electronic and steric effects could not be separated because of lack of variety in the derivatives tested.

A review of published data on acridine derivatives with different biological activities

“…These compounds ( Fig. 4) showed activity due to structural similarity with dapsone and its derivatives (POPOFF et al, 1971) or acridine derivatives (FIGGITT et al, 1992). According to SANTELLI-ROUVIER et al, activities were not dependent on the presence of para-aminobenzoic acid (PABA) and acridine ring was part of the compounds responsible for the particular antimalarial activity.…”

A facile solvent‐free synthesis of 1‐alkyl/aralkyl‐2‐(1‐arylsulfonyl alkyl) benzimidazoles using “TBAB” as surface catalyst

“…Substituted benzimidazole derivatives have applications in diverse therapeutic areas including antiulcers, antihypertensive, antiviral, antifungal, anticancer, and antihistaminics to name just a few [1–3]. Sulphones exhibit noteworthy antibacterial, antimalarial, antifungal, and antitubercular properties [4–10]. In recent years, considerable attention has been paid to the reactions done under solvent‐free conditions [11, 12].…”

Activation of Aryl Thiocyanates Followed by Aryne Insertion: Access to 1,2-Thiobenzonitriles

“…The development of novel methodologies to form carbon–sulfur bonds is crucial for the synthesis and derivatization of target molecules in pharmaceutical and material science . Important classes of sulfur-containing compounds are biaryl sulfides and their higher oxidized homologues.…”