A method for treating a microbial infection, including an infection from a protozoan pathogen, such as Trypanosoma brucei rhodesiense and Plasmodium falciparum, in a subject in need thereof by administering to the subject an effective amount of a dicationic imidazopyridine compound or a dicationic tetrahydro-imidazopyridine compound. Processes for synthesizing dicationic imidazopyridines and dicationic tetrahydro-imidazopyridines and the novel dicationic imidazopyridine and dicationic tetrahydro-imidazopyridine compounds themselves.

NOVEL DICATIONIC IMIDAZO[1,2-a]PYRIDINES AND 5,6,7,8-TETRAHYDRO-IMIDAZO[1,2a]PYRIDINES AS ANTIPROTOZOAL AGENTS

Chemical and physical properties of bicyclic 5-6 systems with one bridgehead N and one extra heteroatom (1:0) as well as their reactivity and syntheses are reported Systems described in this chapter include the following: imidazo[1,2- a ]pyridine, imidazo[1,5- a ]pyridine, isothiazolo[2,3- a ]pyridine, isoxazolo[2,3- a ]pyridine, oxazolo[3,2- a ]pyridine, oxazolo[3,4- a ]pyridine, pyrazolo[1,5- a ]pyridine, thiazolo[3,2- a ]pyridine, thiazolo[3,4- a ]pyridine, and systems containing a less common heteroatom Emphasis was put on the partially or fully saturated ring systems which were covered in less detail compared to their fully conjugated analogues in CHEC(1984) and CHEC-II(1996), and which also correspond to a growing number of publications reporting on the synthesis, reactivity, and use of these saturated compounds Whenever appropriate, diastereo- and enantioselective transformations were covered in detail Finally, important compounds of each family are reported, together with the applications they have found in organic synthesis or medicinal chemistry

Bicyclic 5-6 Systems with One Bridgehead (Ring Junction) Nitrogen Atom: One Extra Heteroatom 1:0

Novel diphenylalkyl piperazine derivatives with dual calcium antagonistic and antioxidative activities.

This study reports a series of 14 new iodinated and fluorinated compounds offering both early imaging ((123)I, (124)I, (18)F) and systemic treatment ((131)I) of melanoma potentialities. The biodistribution of each (125)I-labeled tracer was evaluated in a model of melanoma B16F0-bearing mice, using in vivo serial γ scintigraphic imaging. Among this series, [(125)I]56 emerged as the most promising compound in terms of specific tumoral uptake and in vivo kinetic profile. To validate our multimodality concept, the radiosynthesis of [(18)F]56 was then optimized and this radiotracer has been successfully investigated for in vivo PET imaging of melanoma in B16F0- and B16F10-bearing mouse model. The therapeutic efficacy of [(131)I]56 was then evaluated in mice bearing subcutaneous B16F0 melanoma, and a significant slow down in tumoral growth was demonstrated. These data support further development of 56 for PET imaging ((18)F, (124)I) and targeted radionuclide therapy ((131)I) of melanoma using a single chemical structure.

Single photon emission computed tomography/positron emission tomography imaging and targeted radionuclide therapy of melanoma: new multimodal fluorinated and iodinated radiotracers.

Synthesis, structure investigations, and antimicrobial activity of selected s-trans-6-aryl-4-isopropyl-2-[2-[(E)-1-phenylalkylidene]-(E)-hydrazino]-1,4-dihydropyrimidine hydrochlorides.

A series of guanylhydrazone, amidine, and hydrazone derivatives of 2-phenylimidazo[1,2-a]pyridine have been prepared and evaluated for macrofilarial activity against Acanthocheilonema viteae and Brugia pahangi in jirds. Compounds with 4‘,6-bis-substitution by cyclic guanylhydrazone groups show activity. 4‘,6-Bis-amidines show some activity but are more toxic; 4‘- or 6-monosubstituted compounds are inactive. 2,6-Bis-substituted compounds lacking the phenyl ring are inactive. 4‘,6-Bis-substituted compounds having additional double bonds inserted between the heterocyclic ring and the phenyl ring or between the substituent and the ring system show reduced activity.

Bis-cationic heteroaromatics as macrofilaricides: synthesis of bis-amidine and bis-guanylhydrazone derivatives of substituted imidazo[1,2-a]pyridines.

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Bis-cationic heteroaromatics as macrofilaricides: synthesis of bis-amidine and bis-guanylhydrazone derivatives of substituted imidazo[1,2-a]pyridines.