 Apparatus for processing flushing liquor from coke ovens |
| The present invention processes flushing liquor by a construction and arrangement of an apparatus ... |
|
| Coal suspensions in organic liquids |
| OF THE INVENTION In the former aforementioned U.S. Patent, coal dust suspensions in water provide ... |
|
| Propagation of microbial cells on single carbon products |
| It is an object of the present invention is to provide an anaerobic process for propagation of ... |
|
| Fermentation process for improved oxygen utilization |
| OF THE INVENTION My fermentation apparatus comprises a fermentation section 1 with an upper ... |
|
| Method of conditioning flue gas |
| OF THE PREFERRED EMBODIMENTS The conditioners useful in the present invention are finely divided ... |
|
| Enzyme granules |
| What is claimed is: 1. An enzyme granule comprising a granule core of solid material carrying an ... |
|
| Process for producing yeast cells |
| What we claim is: 1. A process for producing yeast cells which comprises culturing aerobically a ... |
|
| Interestification of fats |
| In accordance with the present invention, there is used a customary animal fat, vegetable oil or ... |
|
| Process for the preparation of cholesterol esterase |
| What is claimed is: 1. Process for obtaining cholesterol esterase from micro-organisms, which ... |
|
|
N-substituted cyclopeptide derivatives and preparation thereof
| Details |
Inventors: Failli, Amedeo; Immer, Hans U.; Gotz, Manfred K.;
Assignee: American Home Products Corporation (New York, NY)
Primary Examiner: Ore; Dale R.
Assistant Examiner:
Attorney, Agent or Firm: Wilfond; Arthur E.
The N-substituted cyclopeptide derivatives of formula I ##STR1## in which R.sup.1 is lower alkyl, R.sup.2 is lower alkyl or cyclo(lower)alkyl, R.sup.3 is a neutral amino acid side chain and Y is a peptide residue having three to nine amino acid residues and a method for the preparation of the compounds of formula I are disclosed. The compounds of formula I are useful antibacterial and antifungal agents. Pharmaceutical compositions also are disclosed. |
|
DETAILED DESCRIPTION We claim: 1.
A process for preparing a compound of formula I ##STR4## in which R.
sup.
1 is lower alkyl, R.
sup.
2 is lower alkyl or cyclo(lower)alkyl, R.
sup.
3 is an amino acid side chain selected from hydrogen and lower alkyl and Y is a peptide residue of the formula NHCH(R.
sup.
4)CH--NHCH(R.
sup.
5)CO--NHCH(R.
sup.
6)CO--NHCH(R.
sup.
7)CO--NHCH(R .
sup.
8)CO wherein R.
sup.
4 is hydrogen, lower alkyl or benzyl; R.
sup.
5, R.
sup.
6, and R.
sup.
7 each independently is hydrogen or lower alkyl and R.
sup.
8 is hydrogen, lower alkyl or 2-(methylthio)ethyl, which comprises: condensing together an aldehyde of formula R.
sup.
1 CHO in which R.
sup.
1 is as defined herein, an isonitrile of formula R.
sup.
2 NC in which R.
sup.
2 is as defined herein and a peptide of formula H.
sub.
2 N-CH(R.
sup.
3)--CO--Y--OH in which R.
sup.
3 and Y are as defined herein.
2.
The process as claimed in claim 1 wherein R.
sup.
2 is cyclo(lower)alkyl.
Description:
BACKGROUND OF THE INVENTION (a) Field of Invention The present invention relates to N-substituted cyclopeptide derivatives with antibacterial and antifungal activity and to a process for their preparation.
(B) Description of the Prior Art A number of cyclic peptides have been either isolated from natural sources or prepared by classical synthetic methods, for example, see the review by E.
Schroder and K .
L.
Lubke, "The Peptides"; Vol II; Academic Press, New York, 1966, pp424-478.
The present invention discloses novel cyclopeptide derivatives in which a nitrogen atom of the peptide back bone is substituted.
These compounds have been found to have the desirable attributes of useful microbial activity coupled with a low order of toxicity.
In addition, a novel process for preparing N-substituted cyclopeptides is disclosed.
SUMMARY OF THE INVENTION The N-substituted cyclopeptide derivatives of this invention are represented by the compounds of formula I ##STR2## in which R.
sup.
1 is lower alkyl, R.
sup.
2 is lower alkyl or cyclo(lower)alkyl, R.
sup.
3 is a neutral amino acid side chain and Y is a peptide residue having three to nine neutral amino acid residues
|
|
Molecular Biology 
